Marine sponge-derived anticancer compounds and their effects.
\r\n\tThe study of populations and plant communities in their different aspects; ecological, structural, functional and dynamic, it is essential to establish a posteriori models of forest and agricultural management.
\r\n\r\n\tFor this, the methodological approaches on the type of sampling are considered essential, since there are differences between the purely ecological and the phytosociological methods, despite the fact that both pursue the same objective.
\r\n\tAlthough the ecological method for the knowledge of the vegetation is widely extended, the phytosociological one is no less so, since in the European Union it has been developed as a consequence of policies on sustainability, through which regulations have been issued, such as the habitats directive.
\r\n\tOn the other hand, research on plant dynamics and knowledge of the landscape in an integral way, have multiplied in the last 30 years, which has favored a deep knowledge of the floristic and phytocenotic wealth, which is fundamental for agricultural management, livestock and forestry.
",isbn:"978-1-83969-386-1",printIsbn:"978-1-83969-385-4",pdfIsbn:"978-1-83969-387-8",doi:null,price:0,priceEur:0,priceUsd:0,slug:null,numberOfPages:0,isOpenForSubmission:!0,hash:"0abf2a59ee63fc1ba4fb64d77c9b1be7",bookSignature:"Dr. Eusebio Cano Carmona, Dr. Ricardo Quinto Canas, Dr. Ana Cano Ortiz and Dr. Carmelo Maria Musarella",publishedDate:null,coverURL:"https://cdn.intechopen.com/books/images_new/9662.jpg",keywords:"Climatic Factors, Bioclimate, Thermotype, Flora, Conservation, Phytocenosis, Plant Dynamics, Landscape, Cartography, Vegetation Series, Crops, Reforestation",numberOfDownloads:null,numberOfWosCitations:0,numberOfCrossrefCitations:null,numberOfDimensionsCitations:null,numberOfTotalCitations:null,isAvailableForWebshopOrdering:!0,dateEndFirstStepPublish:"November 23rd 2020",dateEndSecondStepPublish:"January 25th 2021",dateEndThirdStepPublish:"March 26th 2021",dateEndFourthStepPublish:"June 14th 2021",dateEndFifthStepPublish:"August 13th 2021",remainingDaysToSecondStep:"a month",secondStepPassed:!0,currentStepOfPublishingProcess:3,editedByType:null,kuFlag:!1,biosketch:"Dr. Cano Carmona and colleagues have directed 12 doctoral theses and more than 200 publications among articles, books, and book chapters. He has participated in national and international congresses with about 250 papers. He has held a number of different academic positions, including Dean of the Faculty of Experimental Sciences at the University of Jaen, Spain, and founder and director of the International Seminar on Management and Conservation of Biodiversity.",coeditorOneBiosketch:"Ricardo Jorge Quinto Canas is currently an Invited Assistant Professor in the Faculty of Sciences and Technology at the University of Algarve – Portugal, and a member of the Centre of Marine Sciences (CCMAR), University of Algarve. His current research projects focus on Botany, Vegetation Science (Geobotany), Biogeography, Plant Ecology, and Biology Conservation, aiming to support Nature Conservation.",coeditorTwoBiosketch:"Ana Cano Ortiz's fundamental line of research is related to botanical bioindicators. She has worked in Spain, Italy, Portugal, and Central America. It presents more than one hundred works published in various national and international journals, as well as books and book chapters; and has presented a hundred papers to national and international congresses.",coeditorThreeBiosketch:"Carmelo Maria Musarella is a biologist, specialized in Plant Biology. He is a member of the permanent scientific committee of the International Seminar on “Biodiversity Conservation and Management” guested by several European universities. He has participated in several international and national congresses, seminars, and workshops and presented oral communications and posters.",coeditorFourBiosketch:null,coeditorFiveBiosketch:null,editors:[{id:"87846",title:"Dr.",name:"Eusebio",middleName:null,surname:"Cano Carmona",slug:"eusebio-cano-carmona",fullName:"Eusebio Cano Carmona",profilePictureURL:"https://mts.intechopen.com/storage/users/87846/images/system/87846.png",biography:"Eusebio Cano Carmona obtained a PhD in Sciences from the\nUniversity of Granada, Spain. He is Professor of Botany at the\nUniversity of Jaén, Spain. His focus is flora and vegetation and he\nhas conducted research in Spain, Italy, Portugal, Palestine, the\nCaribbean islands and Mexico. As a result of these investigations,\nDr. Cano Carmona and colleagues have directed 12 doctoral theses\nand more than 200 publications among articles, books and book\nchapters. He has participated in national and international congresses with about\n250 papers/communications. He has held a number of different academic positions,\nincluding Dean of the Faculty of Experimental Sciences at the University of Jaen,\nSpain and founder and director of the International Seminar on Management and\nConservation of Biodiversity, a position he has held for 13 years. He is also a member of the Spanish, Portuguese and Italian societies of Geobotany.",institutionString:"University of Jaén",position:null,outsideEditionCount:0,totalCites:0,totalAuthoredChapters:"5",totalChapterViews:"0",totalEditedBooks:"1",institution:{name:"University of Jaén",institutionURL:null,country:{name:"Spain"}}}],coeditorOne:{id:"216982",title:"Dr.",name:"Ricardo Quinto",middleName:null,surname:"Canas",slug:"ricardo-quinto-canas",fullName:"Ricardo Quinto Canas",profilePictureURL:"https://mts.intechopen.com/storage/users/216982/images/system/216982.JPG",biography:"Ricardo Quinto Canas, Phd in Analysis and Management of Ecosystems, is currently an Invited Assistant Professor in the Faculty\nof Sciences and Technology at the University of Algarve, Portugal, and member of the Centre of Marine Sciences (CCMAR),\nUniversity of Algarve. He is also the Head of Division of Environmental Impact Assessment - Algarve Regional Coordination\nand Development Commission (CCDR - Algarve). His current\nresearch projects focus on Botany, Vegetation Science (Geobotany), Biogeography,\nPlant Ecology and Biology Conservation, aiming to support Nature Conservation.\nDr. Quinto Canas has co-authored many cited journal publication, conference articles and book chapters in above-mentioned topics.",institutionString:"University of Algarve",position:null,outsideEditionCount:0,totalCites:0,totalAuthoredChapters:"3",totalChapterViews:"0",totalEditedBooks:"0",institution:null},coeditorTwo:{id:"203697",title:"Dr.",name:"Ana",middleName:null,surname:"Cano Ortiz",slug:"ana-cano-ortiz",fullName:"Ana Cano Ortiz",profilePictureURL:"https://mts.intechopen.com/storage/users/203697/images/system/203697.png",biography:"Ana Cano Ortiz holds a PhD in Botany from the University of\nJaén, Spain. She has worked in private enterprise, in university\nand in secondary education. She is co-director of four doctoral\ntheses. Her research focus is related to botanical bioindicators.\nDr. Ortiz has worked in Spain, Italy, Portugal and Central America. She has published more than 100 works in various national\nand international journals, as well as books and book chapters.\nShe has also presented a great number of papers/communications to national and\ninternational congresses.",institutionString:"University of Jaén",position:null,outsideEditionCount:0,totalCites:0,totalAuthoredChapters:"6",totalChapterViews:"0",totalEditedBooks:"0",institution:{name:"University of Jaén",institutionURL:null,country:{name:"Spain"}}},coeditorThree:{id:"276295",title:"Dr.",name:"Carmelo Maria",middleName:null,surname:"Musarella",slug:"carmelo-maria-musarella",fullName:"Carmelo Maria Musarella",profilePictureURL:"https://mts.intechopen.com/storage/users/276295/images/system/276295.jpg",biography:"Carmelo Maria Musarella, PhD (Reggio Calabria, Italy –\n23/01/1975) is a biologist, specializing in plant biology. He\nstudied and worked in several European Universities: Messina,\nCatania, Reggio Calabria, Rome (Italy), Valencia, Jaén, Almeria\n(Spain), and Evora (Portugal). He was the Adjunct Professor\nof Plant Biology at the “Mediterranea” University of Reggio\nCalabria (Italy). His research topics are: floristic, vegetation,\nhabitat, biogeography, taxonomy, ethnobotany, endemisms, alien species, and\nbiodiversity conservation. He has authored many research articles published in\nindexed journals and books. He has been the guest editor for Plant Biosystems and a\nreferee for this same journal and others. He is a member of the permanent scientific\ncommittee of International Seminar on “Biodiversity Conservation and Management”, which includes several European universities. He has participated in several\ninternational and national congresses, seminars, workshops, and presentations of\noral communications and posters.",institutionString:'"Mediterranea" University of Reggio Calabria',position:null,outsideEditionCount:0,totalCites:0,totalAuthoredChapters:"6",totalChapterViews:"0",totalEditedBooks:"1",institution:null},coeditorFour:null,coeditorFive:null,topics:[{id:"5",title:"Agricultural and Biological Sciences",slug:"agricultural-and-biological-sciences"}],chapters:null,productType:{id:"1",title:"Edited Volume",chapterContentType:"chapter",authoredCaption:"Edited by"},personalPublishingAssistant:{id:"247865",firstName:"Jasna",lastName:"Bozic",middleName:null,title:"Ms.",imageUrl:"https://mts.intechopen.com/storage/users/247865/images/7225_n.jpg",email:"jasna.b@intechopen.com",biography:"As an Author Service Manager, my responsibilities include monitoring and facilitating all publishing activities for authors and editors. From chapter submission and review to approval and revision, copyediting and design, until final publication, I work closely with authors and editors to ensure a simple and easy publishing process. I maintain constant and effective communication with authors, editors and reviewers, which allows for a level of personal support that enables contributors to fully commit and concentrate on the chapters they are writing, editing, or reviewing. I assist authors in the preparation of their full chapter submissions and track important deadlines and ensure they are met. I help to coordinate internal processes such as linguistic review, and monitor the technical aspects of the process. As an ASM I am also involved in the acquisition of editors. Whether that be identifying an exceptional author and proposing an editorship collaboration, or contacting researchers who would like the opportunity to work with IntechOpen, I establish and help manage author and editor acquisition and contact."}},relatedBooks:[{type:"book",id:"6893",title:"Endemic Species",subtitle:null,isOpenForSubmission:!1,hash:"3290be83fff5bc015f5bd3d78ae9c6c7",slug:"endemic-species",bookSignature:"Eusebio Cano Carmona, Carmelo Maria Musarella and Ana Cano Ortiz",coverURL:"https://cdn.intechopen.com/books/images_new/6893.jpg",editedByType:"Edited by",editors:[{id:"87846",title:"Dr.",name:"Eusebio",surname:"Cano Carmona",slug:"eusebio-cano-carmona",fullName:"Eusebio Cano Carmona"}],productType:{id:"1",chapterContentType:"chapter",authoredCaption:"Edited by"}},{type:"book",id:"6418",title:"Hyperspectral Imaging in Agriculture, Food and Environment",subtitle:null,isOpenForSubmission:!1,hash:"9005c36534a5dc065577a011aea13d4d",slug:"hyperspectral-imaging-in-agriculture-food-and-environment",bookSignature:"Alejandro Isabel Luna Maldonado, Humberto Rodríguez Fuentes and Juan Antonio Vidales Contreras",coverURL:"https://cdn.intechopen.com/books/images_new/6418.jpg",editedByType:"Edited by",editors:[{id:"105774",title:"Prof.",name:"Alejandro Isabel",surname:"Luna Maldonado",slug:"alejandro-isabel-luna-maldonado",fullName:"Alejandro Isabel Luna Maldonado"}],productType:{id:"1",chapterContentType:"chapter",authoredCaption:"Edited by"}},{type:"book",id:"1591",title:"Infrared Spectroscopy",subtitle:"Materials Science, Engineering and Technology",isOpenForSubmission:!1,hash:"99b4b7b71a8caeb693ed762b40b017f4",slug:"infrared-spectroscopy-materials-science-engineering-and-technology",bookSignature:"Theophile Theophanides",coverURL:"https://cdn.intechopen.com/books/images_new/1591.jpg",editedByType:"Edited by",editors:[{id:"37194",title:"Dr.",name:"Theophanides",surname:"Theophile",slug:"theophanides-theophile",fullName:"Theophanides Theophile"}],productType:{id:"1",chapterContentType:"chapter",authoredCaption:"Edited by"}},{type:"book",id:"3092",title:"Anopheles mosquitoes",subtitle:"New insights into malaria vectors",isOpenForSubmission:!1,hash:"c9e622485316d5e296288bf24d2b0d64",slug:"anopheles-mosquitoes-new-insights-into-malaria-vectors",bookSignature:"Sylvie Manguin",coverURL:"https://cdn.intechopen.com/books/images_new/3092.jpg",editedByType:"Edited by",editors:[{id:"50017",title:"Prof.",name:"Sylvie",surname:"Manguin",slug:"sylvie-manguin",fullName:"Sylvie Manguin"}],productType:{id:"1",chapterContentType:"chapter",authoredCaption:"Edited by"}},{type:"book",id:"3161",title:"Frontiers in Guided Wave Optics and Optoelectronics",subtitle:null,isOpenForSubmission:!1,hash:"deb44e9c99f82bbce1083abea743146c",slug:"frontiers-in-guided-wave-optics-and-optoelectronics",bookSignature:"Bishnu Pal",coverURL:"https://cdn.intechopen.com/books/images_new/3161.jpg",editedByType:"Edited by",editors:[{id:"4782",title:"Prof.",name:"Bishnu",surname:"Pal",slug:"bishnu-pal",fullName:"Bishnu Pal"}],productType:{id:"1",chapterContentType:"chapter",authoredCaption:"Edited by"}},{type:"book",id:"72",title:"Ionic Liquids",subtitle:"Theory, Properties, New Approaches",isOpenForSubmission:!1,hash:"d94ffa3cfa10505e3b1d676d46fcd3f5",slug:"ionic-liquids-theory-properties-new-approaches",bookSignature:"Alexander Kokorin",coverURL:"https://cdn.intechopen.com/books/images_new/72.jpg",editedByType:"Edited by",editors:[{id:"19816",title:"Prof.",name:"Alexander",surname:"Kokorin",slug:"alexander-kokorin",fullName:"Alexander Kokorin"}],productType:{id:"1",chapterContentType:"chapter",authoredCaption:"Edited by"}},{type:"book",id:"1373",title:"Ionic Liquids",subtitle:"Applications and Perspectives",isOpenForSubmission:!1,hash:"5e9ae5ae9167cde4b344e499a792c41c",slug:"ionic-liquids-applications-and-perspectives",bookSignature:"Alexander Kokorin",coverURL:"https://cdn.intechopen.com/books/images_new/1373.jpg",editedByType:"Edited by",editors:[{id:"19816",title:"Prof.",name:"Alexander",surname:"Kokorin",slug:"alexander-kokorin",fullName:"Alexander Kokorin"}],productType:{id:"1",chapterContentType:"chapter",authoredCaption:"Edited by"}},{type:"book",id:"57",title:"Physics and Applications of Graphene",subtitle:"Experiments",isOpenForSubmission:!1,hash:"0e6622a71cf4f02f45bfdd5691e1189a",slug:"physics-and-applications-of-graphene-experiments",bookSignature:"Sergey Mikhailov",coverURL:"https://cdn.intechopen.com/books/images_new/57.jpg",editedByType:"Edited by",editors:[{id:"16042",title:"Dr.",name:"Sergey",surname:"Mikhailov",slug:"sergey-mikhailov",fullName:"Sergey Mikhailov"}],productType:{id:"1",chapterContentType:"chapter",authoredCaption:"Edited by"}},{type:"book",id:"371",title:"Abiotic Stress in Plants",subtitle:"Mechanisms and Adaptations",isOpenForSubmission:!1,hash:"588466f487e307619849d72389178a74",slug:"abiotic-stress-in-plants-mechanisms-and-adaptations",bookSignature:"Arun Shanker and B. Venkateswarlu",coverURL:"https://cdn.intechopen.com/books/images_new/371.jpg",editedByType:"Edited by",editors:[{id:"58592",title:"Dr.",name:"Arun",surname:"Shanker",slug:"arun-shanker",fullName:"Arun Shanker"}],productType:{id:"1",chapterContentType:"chapter",authoredCaption:"Edited by"}},{type:"book",id:"878",title:"Phytochemicals",subtitle:"A Global Perspective of Their Role in Nutrition and Health",isOpenForSubmission:!1,hash:"ec77671f63975ef2d16192897deb6835",slug:"phytochemicals-a-global-perspective-of-their-role-in-nutrition-and-health",bookSignature:"Venketeshwer Rao",coverURL:"https://cdn.intechopen.com/books/images_new/878.jpg",editedByType:"Edited by",editors:[{id:"82663",title:"Dr.",name:"Venketeshwer",surname:"Rao",slug:"venketeshwer-rao",fullName:"Venketeshwer Rao"}],productType:{id:"1",chapterContentType:"chapter",authoredCaption:"Edited by"}}]},chapter:{item:{type:"chapter",id:"60368",title:"Biological and Medicinal Importance of Sponge",doi:"10.5772/intechopen.73529",slug:"biological-and-medicinal-importance-of-sponge",body:'Sponges are the ancient, efficient designed multicellular parazoan organisms and show relatively little differentiation and tissue coordination. A sponge is a sessile, sedentary, filter-feeding primitive aquatic invertebrate animal which attaches itself to solid surfaces from intertidal zone to depths of 29,000 ft (85000m) or more, where they can get sufficient food to grow [1, 2]. Sponges feed on microscopic organisms (protozoa, bacteria and other small organisms in water) and organic particles [3]. There are about 10,000 known species inhabit a wide variety of marine and fresh water habitats and are found throughout deep ocean depths to rock pools, warm tropical seas to frozen arctic seas, rivers and streams [3, 4]. They are very diverse and occur in various colors, sizes and shapes such as tubular (tube-like), globular (ball-shaped), caliculate (cup-shaped), arboresecent (plant-shaped), flabellate (fan-shaped) and amorphous (shapeless). The scientific term for sponges is Porifera meaning “pore-bearing” and has bodies full of pores and channels allowing water to circulate through them, consisting of jelly-like mesohyl sandwiched between two layers of cells [5]. The shapes of their bodies are adapted for maximal efficiency of water flow through the central cavity, where it deposits the nutrients, and leaves through a hole called the osculum. Several sponges have spicules of silicon dioxide or calcium carbonate and a mesh of proteins called spongin as an internal skeleton. One of the remarkable properties of sponges is their ability to suffer damage and regenerative capacity [6, 7, 8]. Marine sponges have attracted growing attention as a source of overwhelming structurally diverse secondary metabolites with potential biological activities and were placed at the top with respect to discovery of biologically active chemical constituents [9, 10]. Although thousands of chemical compounds have been reported in the literature from these sponges, only few of them are clinically described. Many studies revealed that sponge-derived metabolites are used directly in therapy or as a prototype of bioactive leads to develop more active and less toxic analogs [11, 12]. Sponges are most primitive type of aquatic animals in existence which are dominating many benthic habitats, featuring a cell-based organization where different cells conduct all forms of bodily function, but do not form tissues [13]. They consume food and excrete waste products within cells without a body cavity [14]. Several ecological studies reported that high quantity of bioactive constituents produced by sponges often serve defensive against environmental threats such as predation, microbial infection, competition for space or overgrowth by fouling organisms [15, 16]. For this reason marine sponges are the subject of attraction for chemists due to the sheer number of metabolites produced, the novelty of structure encountered, and the therapeutic potential of these compounds in the treatment of human diseases. Scientists working in the field of natural product chemistry and research suggest that these sponges have promising potential to provide future drugs which can serve various diseases. In this chapter, we describe main isolated chemical entities from sponges and their pharmacological application.
In the recent years, marine natural products bioprospecting has yielded a considerable number of drug candidates, most still being in preclinical or early clinical development, with only a limited number already in the market [17]. A typical example of marine anticancer drugs is eribulinmesylate, a derivative of halichondrin B isolated from the marine sponge. Halichondria okadai has achieved success in phase III clinical trials. Literature studies have shown sponge-derived discodermolides antitumor compounds can play remarkable role in future to treat cancer. Plethora of secondary metabolites is produced by marine sponges and their symbionts. The spongothymidine and spongouridine nucleosides were the first successful sponge-derived pharmaceutical drugs isolated from Tectitethya crypta [18]. Ara-C (cytarabineor1-beta-D-Arabinofuranosylcytosine) recently used for the cure of leukemia [19, 20] and its combination with Daunoribicin and other anticancer drugs, is screened in clinical trials for the treatment of acute myeloid neoplasms [21] During the last few years several marine derived natural compounds are in the pipeline for evaluation in Phase I–III clinical trials for various cancers treatment [22]. A review in 2003 listed the most important anticancer candidate from marine natural compounds undergoing preclinical and clinical (I, II, III) trials and following compounds were from sponge origin: Isohomohalichondrin B, Halichondrin B, Laulimalide/Fijianolide,5-methoxyamphimedine(alkaloid)Discodermolide, Hemiasterlins A and B, Fascaphysins (alkaloid), modified halichondrin B, KRN-70000, Alipkinidine (alkaloid), and Variolin (alkaloid) [23]. Moreover marine sponges are the important source for vital diverse bioactive constituents including alkaloids, terpenoids, sterols and macrolides. Renieramycins, members of tetrahydroiso-quinoline family were isolated from marine sponges from genus Reniera with promising anticancer potential. The preclinical results reported that Renieramycin M, a natural constituent from sponge induced lung cancer cells apoptosis through p53-dependent pathway and may inhibit progression and metastasis of lung cancer cells [24]. A novel polycyclic guanidine alkaloid monanchocidin isolated from Monanchora pulchra marine sponge reported to induce cell death in human cervical cancer (HeLa),human monocytic leukemia (THP-1)and mouse epidermal (JB6 Cl41) cells [25]. In the early 1987, as esquiterpene aminoquinone, Smenospongine extracted from Smenospongia sp. reported to induces cytotoxic, antiproliferetive, antiangiogenic, and antimicrobial activities [26]. Spongistatin a macrocyclic lactone polyether isolated from Spongia sp. marine sponge in 1993 was shown to inhibit microtubule assembly, mitosis, and the binding of tubulin to vinblastine thereby inducing cytotoxic cell death in numerous cancer cell lines [27, 28]. Recently a very important compound named lectin has been isolated from Cinachyrella apion marine sponge was evaluated for antiproliferative, hemolytic, and cytotoxic properties, besides the ability to induce cell death in tumor cells. Results showed that the lectin induces cell death by apoptosis activation by pro-apoptotic protein Bax, promoting permeabilization of mitochondrial membrane, S phase cell cycle arrest and acting as both dependent and/or independent of caspases pathway. These results indicate the potential of lectin for treating cancer [29]. Another marine sponge component, heteronemin a sesterterpene isolated from Hyrtios sp. has attracted the interest of researchers as an antimour agent especially for its pharmacological effects on chronic myelogenous leukemia cells. Results revealed that heteronemin affected the various cellular processes such as cell cycle, nitrogen-activated protein kinases pathways, apoptosis, and nuclear factor kappa B signaling cascade. Thus the compound has shown anti-inflammatory as well as anticancer agent [30]. A collaborative program between experimental therapeutics laboratory of Henry Ford Hospital in Detroit and University of California Santa Cruz initiated in 1990 focused on the development and discovery of anticancer drugs from sponge extracts. About 2036 extracts from 683 individual sponges were examined by using novel in vitro assay led to the identification pure bioactive compounds from many sponges for treating solid tumors. The collaborative efforts and analogs led to the isolation of number of constituents with of anticancer potential [31].
Thus the possibility of development of new anticancer drugs for curing or reducing cancer is promising. Until now, in vitro antitumor activity studies of sponge-derived compounds were tested. Thus, the detailed pharmaceutical studies to investigate the mechanism of action and clinical trials are needed. Moreover, the extensive ongoing research on sponges and development of new advanced techniques have made it possible to access deep sea, new anticancer marine isolates with unprecedented carbon skeleton and inhibitory activities of human cancer cell continued to be discovered and developed, which will offer in future the new candidate for cancer therapy. The chemical constituents so far reported for anticancer activity include (Table 1).
Categories | Species | Active agents | Antitumor tested | References |
---|---|---|---|---|
Alkaloids | Papua | Hyrtiocarboline | H522-T1, MDA-MB- 435, U937 tumor cell lines | [31] |
Penares sp. | HL-60, HeLa | [32] | ||
Aaptos suberitoides | Aaptamine | L5178Y | [33] | |
Monanchora arbuscula | Norbatzelladine | |||
Dinorbatzelladine | MDA-MB-231 breast cancer | [34] | ||
Dinordehy-drobatzelladine | ||||
Dinorbatzelladine | ||||
Dihomodehy-drobatzelladine | MDA-MB-231 breast cancer | [34] | ||
Clathria calla | Norbatzelladine | |||
Clathriadic acid | ||||
Xestospongia sp. | Renieramycin T | HCT116, QC56, AsPC1 | [35] | |
T47D tumor cell lines | ||||
Smenospongia sp. | 6′-Iodoaureol | MOLT-3, HepG2 cells | [36] | |
Hyrtios sp. | Hyrtimomine A | Human epidermoid carcinoma KB, murine leukemia L1210 | [37] | |
Pseudoceratina verrucosa | Aplysamine | HeLa, NFF cells | [38] | |
Amphimedon sp. | Pyrinodemin G | P388 murine leukemia cells | ||
Pyrinodemin H | [39] | |||
Oceanapia sp. | Sagitol C | PC12, L5178Y, HeLa cells | [40] | |
Monanchora pulchra | Monanchocidins B | |||
Monanchocidins C | HL-60 human leukemia cells | [41] | ||
Monanchocidins D | ||||
Monanchocidins E | ||||
Agelas sp. | Hexazosceptrin | |||
Agelestes A-B | U937, PC9 human | |||
(9S, 10R, 90S, 100R)-nakamuric acid | Cancer cell lines | [42] | ||
Sterols | Ianthella sp. | Petrosterol-3,6-dione | A549 (lung), HT-29 (colon), | |
5α,6α-epoxy-petrosterol | SK-OV-3 (ovary), MCF-7 (breast) HL-60 and U937 | [43] | ||
Lissodendryx fibrosa | Manadosterol A-B | Ubc13–Uev1A complex | [44] | |
Terpenoids | Carteriospongia sp. | Homoscalarane sesterterpenes | A2780, H522-T1, A2058 | [45] |
Monanchora sp. | 9Sesterterpenoids | A498, ACHN (renal cancer) | [46] | |
MIA-paca, and PANC-1 (pancreatic cancer) | [47] | |||
Psammocinia sp. | Scalarane sesterterpenes | A498, ACHN MIA-paca,PANC-1 | [48] | |
Pseudoaxinella flava | Diterpene isonitrile | PC3(prostate cancer cell line) | [49] | |
Agelas axifera | Three axistatins (pyrimidine diterpenes) | P338, BXPC-3 MCF-7, SF-268 NCI-H460, KML20L2, and DU-145 cell lines growth | [50] | |
Thorectare ticulate | Metachromins U Metachromins V | SF-268, H460,MCF-7, HT-29, and CHOK1 (mammalian cell line) | [51] | |
Dactylospongia elegans | Nakijinol B and CHO-K1 | SF-268, H460, MCF-7, HT-29 | [51] | |
Coscinoderma sp. | Sesterterpenes coscinolactams C | K562 and A549 (human cancer cells) | [52] | |
Coscinolactams D, | ||||
Coscinolactams E | ||||
Coscinolactams F | ||||
Coscinolactams G | [53] | |||
Macrolide | Cinachyrella enigmatica | Enigmazole A | NCI 60 human tumor cells | [54] |
Jaspis splendans | Jaspamide M | MCF-7and HT-29 | [55] | |
Jaspamide N | (antimicrofilament) | |||
Jaspamide O | ||||
Jaspamide P | ||||
Mycale hentscheli | Peloruside A | P388 HL-60 cells | [56] | |
Peloruside B | ||||
Pipestela candelabra | Pipestelide A | KB cell lines | [57] | |
Pipestelide B | ||||
Polyketone | Plakortis simplex | Simplextone C | HeLa, K562, A-549 cell lines | |
Plakortoxide A | [58] | |||
Plakortis halichondrioides | Epiplakinidioic acid | DU-145, A2058 | [59] | |
Plakortoxide A | tumor cell lines | |||
Lithoplocamialithistoides | Polyketides PM050489 | HT-29, A549, MDA-MB-231 | ||
Polyketides PM060184 | Human tumor cell lines | [60] | ||
Peptides | Homophymia sp. | Homophymines B | KB, MCF7, MCF7R, HCT116 | |
Homophymines E | HCT15, HT29, OVCAR 8, OV3, | |||
Homophymines A1-E1 | PC3, Vero, MRC5, HL60, HL60R, K562, PaCa, SF268, A549, MDA231, MDA435, HepG2, and EPC human tumor cells | [61] | ||
Neamphius huxleyi | Neamphamide B | A549,HeLa, LNCaP, | ||
Neamphamide C | PC3, NFF human tumor | |||
Neamphamide D | cell lines | [62] | ||
Eurypon laughlini | Rolloamide A | LNCap, PC3MM2, PC3, DU145 (Prostrate), MDA361, MCF7, MDA231 (breast), OVCAR3, SKOV3, U87MG (Glioma), (ovarian), A498 (renal) | [63] | |
Stylissa caribica | Stylissamide H | HCT-116. | [64] | |
Homophymia lamellose | Pipecolidepsin A | A549, HT-29 MDA-MB-231 | ||
Pipecolidepsin B | Human tumor cells | [65] | ||
Glycosides | Pandaros acanthifolium | Acanthifoliosides A–E | L6 cell lines | [66] |
Rhabdastrella globostellata | Rhabdastin E-G | HL-60 | [67] | |
Quinones | Dysidea avara | Dysidavarone A | HeLa, A549, MDA231, QGY7703 | |
Dysidavarone D | HeLa tumor cells | [68] | ||
Dactylospongia metachromia | 5 Sesquiterpene aminoquinones | L5178Y mouse cancer cell lines | [69] | |
Dactylospongia avara | 3 Dysideanones A–C | HeLa HepG2 cancer cell lines | [70] | |
Miscellaneous | Petrosia sp. | 3(−) Petrosynoic acids A–D | A2058, H522-T1, | |
H460 human tumor cell line | ||||
IMR-90 human fibroblast cells | [71] | |||
Subereamollis | Subereaphenol D | HeLa cell lines | [72] | |
Mixture of Smenospongia aurea | (E)-10-benzyl-5,7-dimethylun-1 deca,5,10-trien-4-ol | HL-60 human leukemia | ||
Smenospongia cerebriformis | ||||
Verongula rigida | [73] | |||
Myrmekioderma dendyi | Myrmekioside E-2 | NSCLC-N6 and A549 tumor cell lines | [74] | |
Genus Suberea. | Four novel Psammaplysin analogs | Cytotoxicity | [75] |
Marine sponge-derived anticancer compounds and their effects.
Marine sponges are among the richest sources of interesting chemicals produced by marine organisms. Exploitation of bioactive metabolites by natural product chemist from marine sources by using antimicrobial or cytotoxic assays started back in 1970s. Later, various reputed pharmaceutical companies joined hands for this effort using more advance assay systems, including enzyme inhibition assays. As a result several new promising bioactive candidates have been discovered from marine sponges [76]. Bioactive constituents are claimed for potent in vivo or in vitro activity against infectious and parasitic diseases, such as bacterial, fungal, viral and protozoan infections. Studies revealed that the crude extracts of marine sponge have shown high incidences of antibacterial activity against terrestrial pathogenic bacteria, but very low incidences of antibacterial activity against marine bacteria [77, 78]. Very few cases of sponge infection by exogenous microorganisms are known, presumably due to the accumulation/or product by the marine sponges of substances which have antimicrobial activity [1]. A number of new metabolites with antibiotic applications are discovered every year, but in marine sponges their ubiquity is remarkable. Antibacterial screening of marine sponges led to identification and characterization of wide range of active chemical constituents, including some with promising therapeutic leads [79, 80]. Around 850 antibiotic constituents are reported from marine sponges [81]. Various antibacterial substances were identified from marine sponges by continuous efforts of marine natural product community. Despite of discovery of huge number of natural product from marine sponges, none of them has yet led to antibacterial product, but currently several are under investigation. Examples of some isolated substances from marine sponges with antibacterial activity are shown in Table 2. The first discovered antibiotic from a marine sponge was manoalide, a seterterpenoid isolated from Luffariella variabilis [82]. The most promising constituents with antibacterial properties reported from marine sponges include: agelasine D, cribrostatin 3 and 6, petrosamine B, psammaplin A and alkylpyridines (haliclonacyclamine E, arenosclerins) and among these constituents, manzamine A and psammaplin A are in preclinical trials. Many of these have excellent potential for drug development, but no commercial medication has been originated from them so far.
Categories | Species | Active agents | Antibacterial tested | References |
---|---|---|---|---|
Alkaloids | Axinella sp. | Axinellamines B-D | H. pylori Gram-(-ve) | [83] |
Acanthostrongylophora sp. | 12,34-Oxamanzamine E, | M. tuberculosis | [84] | |
8-Hydroxymanzamine J | ||||
6-Hydroxymanzamine E | ||||
Arenosclera brasiliensis | Haliclonacyclamine E, | S. aureus, P. aeruginosa | ||
Arenosclerins A-C | [85] | |||
Spongosorites sp. | Deoxytopsentin, bromotopsentin | S. aureus (MRSA strain) | ||
4,5-Dihydro-6”-deoxybromotopsentin, bis(indole) | [86] | |||
Cribrochalina sp. | Cribrostatin 3 | N. gonorrheae | [87] | |
Cribrochalina sp. | Cribrostatin 6 | S. pneumonia | [88] | |
Spongosorites sp. | Hamacanthin A | S. aureus (MRSA strain) | [86] | |
Oceanapia sp. | Petrosamine B | H. pylori | [89] | |
Latrunculia sp. | Discorhabdin R | S. aureus, M. luteus S. marcescens, E. coli | [90] | |
Hamacantha sp. | Hamacanthin A 1 | C. albicans | ||
Hamacanthin B 2 | C. neoformans | [91] | ||
Nitrogenous | Pachychalina sp. | Cyclostellettamines A-I, | S. aureus (MRSA strain), | [92] |
Cyclostel K-L | P. aeruginosa (antibiotic-resistant strain), M. tuberculosis | [93] | ||
Pachychalina sp. | Ingenamine G | S. aureus (MRSA strain) | ||
E. coli, M. tuberculosis | [92] | |||
M. sarassinorum | Melophlin C | B. subtilis, S. aureus | [47] | |
Agelas sp. | Agelasine D | M. tuberculosis Gram (+ve, -ve) | [94] | |
Terpenoids | Cacospongia sp. | Isojaspic acid, cacospongin D, jaspaquinol | S. epidermidis | [95] |
Myrmekiodermastyx | (S)-(+)-curcuphenol | M. tuberculosis | [96] | |
Miscellaneous | Oceanapia sp. | C14 acetylenic acid | E. coli, P. aeruginosa, B. subtilis, S. aureus | [97] |
C. sphaeroconia | Caminosides A-D | E. coli | [98] | |
A. coralliphaga | Corallidictyals A-D | S. aureus | [99] | |
C. varians | CvL | B. subtilis, S. aureus | [100] | |
N. magnifica | Latrunculins | S. aureus and B. cereus | [101] | |
Discodermia sp. | Polydiscamide A | B. subtilis | [93] | |
Psammaplysilla | Psammaplin A | S. aureus (MRSA strain) | [102] |
Marine sponge-derived antibacterial compounds and their effects.
The search for new antiviral substances from marine sources led to the isolation of several promising therapeutic leads which are presented in Table 3. The literature presents a good number of reports about different biological activities of marine sponges. Several papers reports the screening results of marine organisms for antiviral activity, and a diverse range of active constituents have been isolated and characterized from them [80, 103, 104]. For some of these isolated substances important antiviral activities were reported. Perhaps the most important antiviral lead of marine origin reported thus far is the nucleoside ara-A (vidarabine) isolated from the sponge Cryptotethya crypta. Ara-A is a semisynthetic compound, based on the arabinosyl nucleosides, that inhibits viral DNA synthesis [105]. Once it was realized that biological systems would recognize the nucleoside base after modifications of the sugar moiety, chemists began to substitute the typical pentoses with acyclic entities or with substituted sugars, leading to the drug azidothymidine (zidovudine). Ara-A, ara-C (1-β-Darabinosyl cytosine, cytarabine), acyclovir, and azidothymidine are in clinical use and are all examples of products of semisynthetic modifications of the arabinosyl nucleosides [106]. Several of these substances have a great potential for drug development. Ara-A has been used for the treatment of herpes virus infections, but it is less efficient and more toxic than acyclovir [107, 108]. However, ara-A is capable of inhibiting a cyclovir-resistant HSV and VZV (varicella-zoster virus) [109]. The most promising antiviral substances from sponges appear to be 4-methylaaptamine, avarol, manzamines, mycalamide A and B. Among these substances, preclinical assessments were started for avarol and manzamine A. In general, antiviral molecules from sponges do not give protection against viruses, but they may result in drugs to treat already infected individuals. In addition, broad-based antiviral agents such as 2-5A and α-glucosidase inhibitors may be useful in cases of sudden outbreaks of (less familiar) viruses such as SARS and Ebola [80].
Categories | Species | Active agents | Antiviral tests | References |
---|---|---|---|---|
Alkaloid | Aaptosa aptos | 4-Methylaaptamine | HSV-1 | [110] |
Halicortex sp. | Dragmacidin F | HSV-1 | [111] | |
Indo-Pacific | Manzamine A, 8-hydroxymanzamine A, 6-deoxymanzamine X neokauluamine | HIV-1 | [112] | |
Nucleosides | Mycale sp. | Mycalamide A-B | A59 coronavirus, HSV-1 | [113] |
Hamacantha sp. | Coscinamides 60-62, | |||
Chondriamides 63-65 | Anti-HIV | [91] | ||
Cyclic depsipeptides | Theonella sp. | Papuamides A-D | HIV-1 | [114] |
S. microspinosa | Microspinosamide | HIV-1 | [115] | |
Sterols | Haplosclerid sponges | Haplosamates A | HV-1 | |
Haplosamates B | [116] | |||
Terpenoids | D. avara | Avarol 6′-hydroxy avarol, 3′-hydroxy avarone | HV-1 | [117] |
Nucleoside | Cryptotethya crypta | Ara-A | HSV-1, HSV-2, VZV | [105] |
Mycale sp. | Mycalamide A-B | A59 coronavirus, HSV-1 | [118] | |
Miscellaneous | Dysidea avara | Callyspongymic acid | HIV, hepatitis B virus | [119] |
2′-5′ Oligoadenylates | Viral replication | [120] | ||
H. tarangaensis | Hamigeran B | Herpes, polio viruses | [121] | |
Petrosia weinbergi | Weinbersterols A-B | Leukemia virus, mouse influenza virus, mouse corona virus | [122] |
Antiviral compounds from marine sponges and their effects.
Marine sponges have been considered a gold mine for the discovery of marine natural products during the past 50 years. The need of new antifungals in clinical medicine due to various kinds of mycoses, in particular invasive mycoses have become serious health problems as their incidences has increased dramatically during last few years in relation to AIDS, transplant recipients, hematological malignancies, transplant recipients and other immunosuppressed individuals. One of the major causes of death in patients suffering from malignant disease is fungal infections and emerging resistance is also an important problem. Immunocompromised patients are mainly infected by Aspergillus, Cryptococcus, Candida, and other opportunistic fungi. Candida albicans is most often associated with serious invasive fungal infections, but other Candida species and yeast-like organisms (Blastoschizomyces, Trichosporon and Malassezia) have emerged as etiological agents of severe mycoses problem [123, 124, 125, 126]. Fungicides which are presently being used are less diverse than antimicrobials, and the usage of many of them is restricted because of their toxic effects to animals, plants and humans. Moreover the progress in this area is slow as comparison to antibacterial agents [126]. Antifungal compounds isolated from marine sponges are listed in Table 4.
Categories | species | Active agents | Antifungal tests | References |
---|---|---|---|---|
Alkaloids | A. brasiliensis | Arenosclerins A-C | C. albicans | |
Haliclonacyclamine E | [127] | |||
Acanthostrongylophora sp. | Manzamine A | C. neoformans | [112] | |
Leucetta cf. | Naamine D | Chagosensis C. neoformans | [128] | |
Pseudoceratina sp. | Ceratinadins A-C | C. albicans | [129] | |
A. citrina | (−)-Agelasidine F, | C. albicans | ||
(−)-Agelasidine C | [130] | |||
M. arbuscular | Batzelladine L | A. flavus | [131] | |
Terpenoids | L. variabilis | Secomanoalide | C. glabrata, C. krusei | |
C. albicans | [132] | |||
M. herdmani | Microsclerodermins A-B | A. fumigatus | [133] | |
Hyrtios sp. | Puupehenonol | C. neoformans, C. krusei | [134] | |
Sterols | Euryspongia sp. | Eurysterols A-B | C. albicans | [135] |
Topsentia sp | Geodisterol-3-O-sulfite, 29-demethylgeodisterol-3-OCl-sulfite | S. cerevisiae, C. albicans | ||
C. albicans | [136] | |||
Peptides | Discodermia sp. | Discobahamin A-B | C. albicans | [137] |
Jaspis sp. | Jasplakinolide or jaspamide | C. albicans | [138] | |
Latrunculia sp. | Callipeltins F-I | C. albicans | [139] | |
Latrunculia sp. | Callipeltin J-K | C. albicans | [42] | |
T. swinhoei | Theonellamide G | C. albicans | [140] | |
Theonella sp. | Theonellamide TNM-F | Candida spp, Trichophyton spp, Aspergillus sp. | [141] | |
Purine derivatives | Agelas sp. | Agelasines, agelasimines | C. krusei | [142] |
Miscellaneous | P. reticulate | Crambescin A2 392 | C. albicans | |
Crambescin A2 406 | C. neoformans var. gattii, | |||
Crambescin A2 420 | C. glabrata, C. krusei | |||
Sch 575948 | [143] | |||
Sponge | Theonellamides | Antifungal | [144] | |
Melophlus sp. | Aurantoside K | C. albicans (wild-type) | [145] | |
P. halichondrioides | Plakortide F | C. albicans, C. neoformans, A. fumigatus | [146] | |
H. viscosa | Haliscosamine | C. neoformans, C. albicans | [147] | |
D. herbacea | 3,5-Dibromo-2-(3,5-dibromo-2-methoxyphenoxy) phenol | Aspergillus | [148] | |
P. onkodes | Two α and β1,2-dioxolane peroxide acids | C. albicans | [149] | |
T. laevispirulifer | Nematocide, onnamide F | S. cerevisiae | [150] | |
T. swinhoei | Swinhoeiamide A | C. albicans, A. fumigates | [151] | |
Family Neopeltidae | Neopeltolide | C. albicans | [152] | |
Plakinastrella | Epiplakinic acid F | C. albicans | [153] | |
H. communis | (−)-Untenospongin B | C. albicans, C. tropicalis, F. oxysporum | [154] | |
H. lachne | Hippolachnin A | C. neoformans, T. rubrum, M. gypseum | [155] |
Antifungal compounds from marine sponges and their effects.
Marine organisms and microorganisms have provided a large proportion of the anti-inflammatory and natural antioxidants products over the last years. Reports suggest that marine invertebrates represent new marine resources for the isolation of novel agents which are active on inflammatory conditions have also been found in the literature. Herencia and coworkers [156] studied the effects of dichloromethane and methanol extracts from some Mediterranean marine invertebrates on carrageenan-induced paw edema in mice. Extracts partially decreased elastase activity and PGE2 levels measured in homogenates from inflamed paws, without affecting the levels of this prostanoid present in stomach homogenates. Within the framework of the European MAST III Project, extracts of different polarity from sponges, ascidians and cnidarians have been screened for immunomodulating activities [157]. It was demonstrated that endotoxin-free samples of marine origin possess effects on certain components of the immune system. As a result of all these investigations, bioassay-directed separation of active extracts identified many structurally diverse compounds as future leads. Anti-inflammatory compounds found in the marine environment include terpenes and steroids, alkaloids, peptides and proteins, polysaccharides and others. Examples of anti-inflammatory compounds marine sponge origin are presented in Table 5. Also includes diterpenes of (8E, 13Z, 20Z)-strobilinin and (7E, 13Z, 20Z)-felixinin from a marine sponge Psammocinia sp. [158], and novel anti-inflammatory spongian diterpenes from the New Zealand marine sponge Chelonaplysill aviolacea [159].
Categories | species | Active agents | Anti-inflammatory tests | References |
---|---|---|---|---|
Terpenoids | F. cavernosa | Cavernolide | TNF-α, NO and PGE2 production | [160] |
Axinella spp. | 6-Cycloamphilectenes | NO, PGE2 and TNF-α production | [161] | |
2-Cycloamphilectenes | Inhibit NF-КB pathway | [161] | ||
Psammocinia spp. | Chromarols A-E | Inhibition of 15-LOX | [162] | |
Psammocinia spp. | (8E, 13Z, 20Z)-strobilinin | Anti-inflammatory | ||
(7E, 13Z, 20Z)-felixinin | Anti-inflammatory | [158] | ||
C. violacea | Spongian | Anti-inflammatory | [163] | |
D. avara | Avarol, avarone, | Inhibition of eicosanoid release | [164] | |
Spongiaquinone, ilimaquinone | and depression of superoxide generation | [165] | ||
Dysidea spp. | Dysidotronic acid | Inhibited production of TNF-α, IL-1 PGE2, and LTB4 | [166] | |
Plakortis spp. | Plakolide A | Inhibit iNOS | [167] | |
D. elegans | Cymopol | DNA binding of NF-КB | [168] | |
L. variabilis | Manoalide, scalaradial | Inhibited IL-1 and TNF-α | [169] | |
F. cavernosa | Cacospongiolide B | Inhibited PLA2 | [170] | |
Dysidea spp | Dysidenones A-B | Inhibited human synovial PLA2 | [171] | |
L. variabilis | Cladocorans A-B | Inhibition of secretory PLA2 | [172] | |
P. nigra | Petrosa spongiolides | Inhibitor of PLA2 | [173] | |
P. nigra | Petrosa spongiolide M | Inhibited LTB4 levels | [174] | |
Cacospongia spp. | Scalaradial | Inactivate the enzyme PLA2 | [175] | |
G. sedna | Homoscalarane | Moderate activity to inhibit mammalian PLA2 | [176] | |
Hyrtios sp. | Puupehenone, hyrtenone | A high potency against 12-human, 15-human and 15-soybean LOX | [177] | |
C. linteiformis | Cyclolinteinone | iNOS and COX-2 protein expression in LPS-stimulated J774 macrophages | [178] | |
Callyspongia spp. | Akaterpin | Inhibitor of phosphatidylinositol-specific Phospholipase C | [179] | |
Steroids | C. lissosdera | Clathriol | In vitro anti-inflammatory activity against human neutrophil and rat mast cells | [180] |
Euryspongia spp. | Petrosterol, 3β-hydroxy-26-nor-campest-5-en-25 oic acid | Against 6-keto-PGF1α release in a human keratinocyte cell line HaCaT | [181] | |
Alkaloids | X. testudinaria | Hymenialdisine | Inhibitor of NF-КB and ILs production | [182] |
Agelas spp. | Nagelamides A-H | NF-КB in inflammatory diseases | [183] | |
S. flabellate | Stylissadines A-B | Antiinflammatory activity | [184] |
Anti-inflammatory compounds from marine sponges and their effects.
Derivatives of halenaquinone and xestoquinone showed various enzyme inhibitory activities besides the phosphatidylinositol 3-kinase and topoisomerase I and II inhibitory activities mentioned above. Compound xestoquinone inhibited both Ca2+ and K+-ATPase of skeletal muscle myosin [185]. SAR Investigations showed that halenaquinone and three synthetic analogs with a quinone structure significantly inhibited Ca2+ ATPase activity. In contrast, four xestoquinone analogs in which the quinine structure was converted to quinol dimethyl ether did not inhibit the Ca2+ ATPase activity [186]. The protein tyrosine kinase (PTK) inhibitory activities of halenaquinone, halenaquinol, and 14-methoxyhalenaquinone were the most remarkable with IC50 values <10 mm. The other analogs was either less potent or inactive, and a rationalization for this SAR pattern was also reported [187]. Xestoquinone also showed significant protein kinase inhibitory activity toward Pfnek-1, a serine/threonine malarial kinase, with an IC50 value of ca. 1 mm, and moderate activity toward PfPK5, a member of the cyclin-dependent kinase (CDK) family [188]. Adociaquinone B and 3-ketoadociaquinone B were the most potent inhibitors of the Cdc25 B phosphatase inhibitory activities, and the dihydro-benzothiazine dioxide in compounds Adociaquinone A, Adociaquinone B, 3-Ketoadociaquinone A, and 3-Ketoadociaquinone B appeared to be an important structural feature for this enhanced activity. Four cyclostellettamines, cyclostellettamine A, cyclostellettamine G, dehydrocyclostellettamine D and dehydrocyclostellettamine E inhibited histone deacetylase derived from K562 human leukemia cells with IC50 values ranging from 17 to 80 mm [189]. Xestospongic acid ethyl ester (207) was found to inhibit the Na+/K+ ATPase [190]. Compounds are listed in Table 6.
Categories | Species | Active agents | Enzyme-inhibitory | References |
---|---|---|---|---|
Quinones | X. exigua | Halenaquinone | Ca2+ ATPase activity | [191] |
X. exigua | Xestoquinone | Ca2+ and K+-ATPase activity | [192] | |
X. sapra | Halenaquinol | Protein tyrosine kinase activity | [193] | |
X. cf. carbonaria | 14-Methoxyhalenaquinone | Protein tyrosine kinase activity | [187] | |
Xestospongia sp. | Adociaquinone B | Protein tyrosine kinase activity | [194] | |
Xestospongia sp. | 3-Ketoadociaquinone B | Cdc25B phosphatase activity | [195] | |
Xestospongia sp. | Adociaquinone A | Cdc25B phosphatase | [194] | |
Xestospongia sp. | 3-Ketoadociaquinone | Cdc25B phosphatase | [195] | |
Cyclostellettamines | Xestospongia sp. | Cyclostellettamine | A histone deacetylase derived inhibition | |
Cyclostellettamine G | ||||
Dehydrocyclostellettamine D | ||||
Dehydrocyclostellettamine E | [189] | |||
Fatty acids | X. testudinaria | Xestospongic acid ethyl ester | inhibit the Na+/K+ ATPase | [190] |
Marine sponge-derived compounds showing enzyme-inhibitory activities.
Recently natural constituents isolated from marine sponges were tested for immunosuppressive activities and in the end of 1980s, deep water marine sponges resulted in isolation of pure compounds with immunosuppressive properties. Two important compounds: 4a-merhyl-5a-cholest-8-en-3~-ol and 4,5-dibromo-2-pyrrolic acid discovered by American scientist from deep water sponge Agelasfla bellrform is showed significant immunosuppressive activity. Both compounds were found significantly active in suppression of the response of murine splenocytes in the two-way mixed lymphocyte reaction (MLR) with little to no demonstrable cytotoxicity at low doses ([196]. Constituents isolated from the Aurora globostellata marine sponge showed immunomodulatory potential. The immunomodulatory potential was evaluated by oral administration of ethyl acetate extract of marine sponge (200 mg/kg) to Wistar rats and the results obtained showed that extracts exhibited immunosuppressant activity and can further be studied [197]. A recent investigation on an Indian marine sponge aimed to isolate and characterize bacteria with immunomodulatory and antimicrobial activity. Callyspongia difusa (Gulf of Mannar province) a marine sponge resulted in isolation of 10 marine bacterial strains which exhibited remarkable antagonistic activity against clinical bacterial pathogens. These findings suggested that the sponge associated bacterial strain Virgibacillus sp. can contribute the search for novel antibiotics to overcome infections and also for the production of potential immunomodulators [109].
In the last decade studies reported that marine sponges could have been a source of hypocholesterolemic compounds. For example, lysophosphatidylcholines and lyso-PAF analogs derived from Spirastrella abata are reported as successful inhibitors of cholesterol biosynthesis in vitro study [198, 199]. Zhao et al. [200] extracted novel lysophosphatidylcholines from marine sponges with hypocholesterolemic properties and thereby aroused an interest of compounds from marine sponge due to short lifespan of conventional lysophosphatidylcholines in vivo.
Also, over the years marine sponges are considered as a rich source of natural products and metabolites for antibiotics possessing strong inhibitory against bacteria, fungi and microbes. Several studies revealed that many natural bioactive components isolated from various marine sponges can be useful for the production of new antibiotics and antimicrobial drugs. In the recent years many scientific studies provided evidences for marine sponge metabolites with efficient antibiotic, antibacterials and antimicrobial properties. Purpuroines A-J, halogenated alkaloids isolated from Lotrochota purpurea marine sponge showed promising inhibitory activities against bacteria and fungi related diseases [201]. Haliclona sp. sponge from Korea resulted in isolation of novel cyclic bis-1,3-dialkylpyridiniums and cyclostellettamines, which showed moderate cytotoxic and antibacterial activities against A549 cell-line and Gram-positive strains, respectively [202]. A number of new alkaloids were isolated from the marine sponge Agelas mauritiana: (+)-2-oxo-agela-sidine C, (−)-8′-oxo-agelasine D,4-bromo-N-(butoxymethyl)-1H-pyrrole-2-carboxamide, ageloxime B, and (−)-ageloxime D and some of these isolated components exhibited antifungal activity against Cryptococcus neoformans, antileishmanial activity in vitro and antibacterial activity against S. aureus and methicillin-resistant S. aureus in vitro [203]. Extracts prepared from the sponge’s species Petromica citrina, Haliclona sp. and Cinachyrella sp. exhibited antibacterial activity against 61% of the coagulase-negative staphylococci (CNS) strains, including strains resistant to conventional antibiotics. P. citrina extracts showed the largest spectrum of inhibitory activity. This current study according scientist shows potential of marine sponges to become new sources of antibiotics and disinfectants for the control of CNS involved in bovine mastitis in future [204]. Isolation of isonitriles ditepene from Cymbastela hooperi, tropical marine sponge and the axisonitrile-3 sesquiterpene isolated Acanthella kletra, from the tropical marine sponge were tested for series of bioassays antibacterial, antiphotosynthetic, antifouling, antialgal, antifouling, antialgal, antiphotosynthetic, antifungal, and antitubercular. The results showed majority of the tested compounds were active against at least two of the applied test systems [152]. Recently, sponge-derived actinomycetes and sediments isolated from marine sponge were tested for bioactive constituents with antifungal and antimicrobial activity. Out of 15 prepared active extract nine were found active against Enterococcus fascism (vancomycin-resistant) and Candida albicans multidrug-resistant [132], including strains resistant to conventional antibiotics. Thus the bacterial actinomycetes from marine sponges and other marine organisms have been proved prolific producers of pharmacologically active compounds. Literature studies revealed that 70% of naturally derived antibiotics which are currently in clinical use have been derived from actinomycetes. In the recent study, Streptomyces sp. strains from Mediterranean sponges and secondary metabolite namely, cyclic depsipeptide valinomycin, indolocarbazole alkaloid staurosporine and butenolide, were screened for anti-infective activities. All the isolated compounds along with Streptomyces sp. exhibited antiparasitic activities. Researchers also claim the anti-infective potential of marine actinomycetes is very promising.
Bacterial biofilms are surface-attached microorganism’s communities that are protected by an extracellular matrix of biomolecules. Continuous use of chemical antifoulants resulted in increased tributyltin concentration and created extensive pollution problems in marine organisms. Natural antifouling molecules from marine have been recently reviewed and researches hope that will provide more specific and less toxic antifouling activity in future. Antifouling compounds derived from sponges were found to be very effective, environmentally friendly biocides and less toxic [205]. In the last few years several studies were directed to find the most promising alternative technologies to antifouling in marine organisms, especially from sponges. In a recent study structurally different compounds containing 3-alkylpyridine moiety were evaluated for antifouling potential. The compounds, namely haminols, saraine and 3-alkylpyridinium salts extracted from Reniera sarai, Haliclona sp. and the mollusk Haminoea fusar is obtained by synthesis, showed very good antifouling potential larvae of the barnacle Amphibalanus amphitrite. Bromopyrrole or diterpene alkaloids derivatives isolated from Agelas linnaei and Ageles nakamurai Indonesian marine sponges exhibited cytotoxic activity. Moreover, agelasine derivatives inhibited settling of larvae of Balanus improvisus in an antifouling bioassay as well as the growth of planktonic forms of biofilm forming bacteria S. epidermidis [206].
Marine invertebrates (Porifera, Cnidaria, Mollusca, Arthropoda, Echinodermata, etc.) are considered as one of the major groups of biological organisms which gave huge number of natural products and secondary metabolites with interesting pharmacological properties and led in the formation of novel drugs. Among marine invertebrates, marine sponges (phylum: Porifera) is the most dominant responsible group for discovering significant number of natural components, which has been used as template to develop therapeutic drugs. These natural products possesses vast range of therapeutic application, including antimicrobial, antihypertensive, antioxidant, anticancer, anticoagulant, anti-inflammatory, immune modulator, and wound healing and other medicinal effects. Therefore, marine sponges are considered a rich source of chemical diversity and health benefits for developing drug candidates, nutritional supplements, cosmetics, and molecular probes that can be supported to increase the healthy life span of humans. In this chapter we included the most important and biologically active marine sponge-derived compounds and presented selected studies of most important bioactive and promising natural products and secondary metabolites from marine sponges.
The authors declare that they have no conflict of interest.
The instability problem of the tunnel face has occurred during the construction of several tunnels in the world (STEFANO Tunnel 1984, TASSO Tunnel 1988, VASTO Tunnel 1991, recognition gallery of St Martin-de-La Porte 2001). This problem has been reported many times in Algeria (Algiers Metro Tunnel 2000, Djebel El Kantour Tunnel in Skikda 2010 and Djebel El Ouhach Tunnel in Constantine 2011). Several studies have been conducted in this regard: [1, 2, 3], and various stabilization techniques of tunnels face were used:
Fiberglass method of FIT (injection tube) was applied for the first time in 1988 HST Link Roma – Fiorenze(Italy);
The technique of shotcrete.
The tunnel face is located at kilometer point (KP 230 + 586.5), which is located inside the tunnel of «Djebel El Kantour”. The main problem in this tunnel is the instability of the face which was reported since the beginning of the project, especially in northern the tunnel because of two key factors: the quality of the ground (Marly sandstone clay) and low coverage. In this research finite element simulation were conducted using the software ANSYSE in order take into account the staged construction technique for better estimation the vertical and longitudinal deformations, as well as the failure mechanisms to the front of the tunnel face.
\nTo solve this problem, many techniques have been used to stabilize the face, but the technique did not yield the expected results. Therefore, the prime contractor applied a new technique called the Fiberglass Technique (FIT). However, it proved inadequate in this case, due to its high cost and the limited effectiveness. This is mainly due to the poor mastery of the excavation method, which in turn, was not suitable to this type of rocks. In this study, we try to demonstrate, via a numerical modeling tool, the relationship between the attack section and the deformation field on the Tunnel face.
\nT4 tunnel is located in the north-east of the department of Constantine. It crosses Djebel El Kantour from south to north with a total length of 2500 m. Its cover is higher than 15 m, and reaches 224 m in maximum points (Figure 1).
\nPosition of the tunnel T4.
The section of the tunnel was chosen according to the geometric characteristics, the geological and geotechnical data tests performed on the ground in question as well as the height of the cover. To take into account the natural conditions of the surrounding terrain, an arched profile has been adopted to ensure the stability of the structure and the service conditions during the constructions process.
\nThe design of the tunnel was performed on the basis of a geological and geomechanical survey conducted from recent geotechnical survey includes the following investigations:
Geological surveys conducted by geologists’ experts;
A recognition campaign by core drilling, in situ and laboratory tests.
It noted that any study must lead to the acquisition of the following information with the maximum possible degree of reliability, considering the wide range of technical resources currently available in the geological survey field:
Structural geological and hydrogeological conditions and the natural stress state of the ground to be tunneled;
The physical characteristics, the strength and deformability of the geological bodies affected by the excavation:
The hydrogeological conditions in the rock mass.
Geology of the area crossed by the tunnel is essentially of Cretaceous age (Telliennes Tablecloths) and consists of marl and limestone in the form of strongly folded and sheared blocks (Figure 2). These are covered by Quaternary deposits consisting of clays, silts and conglomerates.
\nPlan and geological section of the T4 tunnel and the collapse point.
The design of the tunnel was carried out on the basis of geological and geotechnical studies. The results of RMR classification are presented in Table 1.
\nN | \nParameters | \nCoefficients | \nRating | \n
---|---|---|---|
1 | \nResistance to uniaxial compression | \nR0 \n | \n0 | \n
2 | \nRock Quality Designation (RQD) | \n(115–3.3Jv) 0–25 very poor | \n3 | \n
3 | \nSpacing of discontinuities | \n\n\n | \n5 | \n
4 | \nConditions of discontinuities | \nSlickensided surfaces; 3–10; 10–20; 0.1–5 \n | \n6.5 | \n
5 | \nGroundwater | \nDamp | \n10 | \n
6 | \nRating adjustment for discontinuity orientations | \nDigging against the dip | \n−12 | \n
Total rating | \n12.5 | \n
Results according to the RMR classification system in the PK 230 + 586.5.
The table below (Table 2) shows the value of the rock classification (Rock Mass ratings) determined after application of the Total rating.
\nTotal rating | \n<21 | \n
---|---|
Class | \nV | \n
Average stand up time | \n30 min for 1 m span | \n
C « KPa » | \n<100 | \n
\n\n | \n<15 | \n
Description | \nVery poor rock | \n
Total-rating results.
In our case, the rocks are of marl-clay-sandstone type (Table 3).
\nγ (kN/m3) | \n20 | \n
---|---|
E (MPa) | \n200 | \n
C (kPa) | \n50–160 | \n
\n\n | \n25 | \n
Geotechnical parameters.
This tunnel consists of two tubes spaced 22 m. The problem of collapse occurred on the southern side of the tunnel in the right tube. The RMR classification results obtained on the Southern side during the day that preceded the crisis was similar to the classification results of the opposite side of the tunnel, which also suffers from the same problem of instability, but with a technique linked to the soil stabilization.
\nAs we dig in the initially stable soil, the preexisting stress state has changed. Indeed, the stress on the excavation contour vanishes: the decompression phenomenon. This change in the stress state appears only in an area surrounding the Tunnel face: the influence area of the face. It extends over a length towards the front edge which is of the same order of magnitude as the diameter of the tunnel according to the measurements performed on several displacement starts [4, 5].
\nThe usual methods for calculating the tunnel’s, Tunnel face stability are resulting from experimental studies [6], extrusion testing in laboratory [7] Semi-empirical and theoretical which mainly the approach of calculating the rupture [8, 9].
\nIn our case, the experiment shows that the ruptures of the Tunnel face can mobilize important volumes of ground.
\nThe first systematic studies on the face instability of the tunnels dag in the soft soil carried out by [10] were used to characterize the stability conditions starting from a stability parameter coefficient (Figure 3).
\nFormation of three characteristic zones during the digging of a tunnel (Lunardi 1993) [11].
The stability coefficient N is defined in [10].
\nWhere;
\nγ: density of the rock.
\nQ u: Shearing resistance (Figure 4).
\nTunnel face schematization.
The Figure 5 gives an indication of the relation between the amount of real stability and awaited deformations.
\nRelation between the stability coefficient and the face supporting according to [12].
In our case, the parameters required for the calculation of the stability coefficient N are the following:
The surface load; \n
The cover C = 25 m;
The tunnel radius R = 5 m. γ\n
The obtained result for the stability coefficient is N = 6.45, which means that the tunnel face is unstable.
\nIn our case, the Tunnel face is unstable; therefore, we try to find the value of the pressure of supporting σ_T suitable to be applied in order to decrease this state towards an Elastoplastic deformation.
\nThe interval of σ_T is calculated starting according to the following formula:
\n\n\n
The required \n
In this case, the pressure to be exerted on the Tunnel face will lie between the two following values:
\nThe state of stress in the ground is considerably greater than the strength properties of the material even in the zone around the face. For this consideration based for the results of the diagnosis phase, the techniques to be applied for the application of the supporting pressure on the Tunnel faces are as follows:
Shotcrete;
Fiber glass bolting.
Both methods assure the rigidity of the core of ground ahead of the face, and therefore the conditions of stability in that ground, have a decisive effect on that deformation response and determine how an arch effect is triggered and consequently the tone of the stress–strain response in the whole tunnel.
\nOn the other hand, they are difficult to apply this theoretical approach in the domains of soft rocks, flysch and soils, give insufficient consideration to the effects of natural stress states and the dimensions and geometry of an excavation on the deformation behavior of a tunnel and fail to take account of new constructions systems [13].
\nHowever, it does not give adequate consideration to the construction stages and therefore it does not constitute a fully integrated method of design and construction. To do this, our analysis of the deformation response continued using the numerical modeling which is able to consider stress states in the ground that are not of the hydrostatic type, which take due account of gravitational loads and which also calculate the effects which the various construction stages have on the statics of a tunnel by simulating the real geometry of lining structures and the sequence and the distance.
\nIn engineering practice, different design methods tend to be used; in this study, advanced numerical modeling was used due to its ability to predict vertical and longitudinal deformations; as well as the failure mechanisms at the front of the tunnel face [14, 15]. It can indeed be used to simultaneously take into account constraints and anisotropic materials, tunnel advance stages and any pre-containment and cavity containment intervention. In this work, the use of a calculation code through finite element method according to the execution situation [16, 17, 18]. The numerical parameter used in the simulation as already mentioned in the Table 3 resulting from the geotechnical investigation of the zone in question, where the behavior criteria used in the simulation is Drucker-Prager criterion, which as a generalization of the Mohr–Coulomb criterion for soils. The criterion is based on the assumption that the octahedral shear stress at failure, it depends linearly on the octahedral normal stress through material constants. The results indicate that the action of the surrounding terrain on the tunnel based on the attack section R. The main input parameters are the mesh network of elements which determines the domain to which the analysis applies, the geomechanical properties of each element, the surrounding conditions and the loads acting (Figure 6).
\nModel and meshing.
Numerical simulations allowed obtaining practical results of the radial and longitudinal displacements in the figure and table below:
\nThe following diagram shows the extrusion of different attack section based on the distance in front of the face (Figure 7).
\nUz displacement curves based on the attack section R.
The vertical and longitudinal deformations and changes of the critical zone that occur in the tunnel are linked to attack section R. When the maximum value of the attack section “R” is equal to 5 m, the corresponding Maximum Vertical Displacement (Ux) is equal to 0.53 m, and Longitudinal Deformation in front of the Tunnel face can reach a maximum of 65 m.
\nIn the case where the radius R = 3.5 m attack, the maximum vertical displacement (Ux) is 0.2 m. So, it is 3 times less than the previous case, and similarly for Longitudinal Deformation in front of the Tunnel face which does not exceed 50 m. it is shown that simulation results are consistent with the observed extent and those obtained in literature. (Figure 8).
\nUx vertical displacement curves based on the attack section R.
We studied the horizontal displacement of the solid rock in vertical section for all cases of attack sections.
\nThe (Figure 9) shows the horizontal displacements along a vertical section for various attack sections R.
\nUh horizontal displacement curves based on the attack section R.
The maximum horizontal displacement Uh is the edge of the excavation to tend towards zero displacement at a considerable distance from the tunnel. With a difference between the displacements, values of every driving section R compared to another.
\nTo ensure the stability of the Tunnel face and minimize its stress concentrations and deformations; the exploitation of this study’s results with the inclusion of geometric and geological conditions traversed by the tunnel, we recommend the following points:
The change in the advancement method in divided sections when terrain features are insufficient to ensure the necessary stability to the face. This method is adopted when the excavation cannot be performed in full section.
The chart below (Figure 10) shows the progress detailed in the proposed divided section.
Staged construction with divided section.
Applying pressure on the supporting σ_T on the Tunnel face to reduce its deformation, of which values interval should be:
\n\n\n
It is suggested that the technique proposed maybe used for construction considerations under complication geological condition which satisfactory effect in engineering practice.
\nIntechOpen celebrates Open Access academic research of women scientists: Call Opens on February 11, 2018 and closes on March 8th, 2018.
",metaTitle:'Call for Applications: "IntechOpen Women in Science 2018" Book Collection',metaDescription:"IntechOpen celebrates Open Access academic research of women scientists: Call Opens on February 11, 2018 and closes on March 8th, 2018.",metaKeywords:null,canonicalURL:"/page/women-in-science-book-collection-2018/",contentRaw:'[{"type":"htmlEditorComponent","content":"On February 9th, 2018, which marks the official celebration of UNESCO’s International Day of Women and Girls in Science, we have announced we are seeking contributors for the upcoming “IntechOpen Women in Science 2018” Book Collection. The program aims to support women scientists worldwide whose academic needs include quality assurance, peer-review, fast publishing, collaboration among complementary authors, immediate exposure, and post-publishing citations reporting.
\\n\\nAPPLYING FOR THE “INTECHOPEN WOMEN IN SCIENCE 2018” OPEN ACCESS BOOK COLLECTION
\\n\\nWomen scientists can apply for one book topic, either as an editor or with co-editors, for a publication of an OA book in any of the scientific categories that will be evaluated by The Women in Science Book Collection Committee, led by IntechOpen’s Editorial Board. Submitted proposals will be sent to designated members of the IntechOpen Editorial Advisory Board who will evaluate proposals based on the following parameters: the proposal’s originality, the topic’s relation to recent trends in the corresponding scientific field, and significance to the scientific community.
\\n\\nThe submissions are now closed. All applicants will be notified on the results in due time. Thank you for participating!
\\n"}]'},components:[{type:"htmlEditorComponent",content:"On February 9th, 2018, which marks the official celebration of UNESCO’s International Day of Women and Girls in Science, we have announced we are seeking contributors for the upcoming “IntechOpen Women in Science 2018” Book Collection. The program aims to support women scientists worldwide whose academic needs include quality assurance, peer-review, fast publishing, collaboration among complementary authors, immediate exposure, and post-publishing citations reporting.
\n\nAPPLYING FOR THE “INTECHOPEN WOMEN IN SCIENCE 2018” OPEN ACCESS BOOK COLLECTION
\n\nWomen scientists can apply for one book topic, either as an editor or with co-editors, for a publication of an OA book in any of the scientific categories that will be evaluated by The Women in Science Book Collection Committee, led by IntechOpen’s Editorial Board. Submitted proposals will be sent to designated members of the IntechOpen Editorial Advisory Board who will evaluate proposals based on the following parameters: the proposal’s originality, the topic’s relation to recent trends in the corresponding scientific field, and significance to the scientific community.
\n\nThe submissions are now closed. All applicants will be notified on the results in due time. Thank you for participating!
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