LD50 681 (mg/kg, in mice), Actinopy

681 LD50 (mg/kg, pada tikus), Actinopyga mauritianadikumpulkan dari Lakshadweep di bulan Oktober yang menunjukkan hipotensif dan antimikrobakegiatan LD50 215 (mg/kg, pada tikus), dan Thelenata ananas dikumpulkan dariLakshadweep menunjukkan aktivitas antimikroba, LD50 56.2 (mg/kg, pada tikus).Ekstrak Holothuria ichinitis dikumpulkan dari Mandapam, Tamilnadu,pada bulan April dan H. impotium yang dikumpulkan dari Lakashadweep pada bulan April ditemukanberacun, 26,1 LD50 dan 38.3 (mg/kg, pada tikus) masing-masing. SpesiesMoluska yang menunjukkan aktivitas adalah: Nerita spp. dikumpulkan dari Mandapam, 116 bioaktif alami produk kelautanTamilnadu, pada bulan Januari yang menunjukkan CNS stimulan aktivitas, LD50 68.1 (mg/kg, di dalamtikus); Gurita vulgaris dikumpulkan dari Okha, Gujarat, di bulan Desember yang dipamerkanaktivitas spasmolytic, LD50 1000 (mg/kg, pada tikus) dan Onchidium verruculatumdikumpulkan dari Mandapam, Tamilnadu, pada bulan Mei menunjukkan aktivitas hypoglycaemic,LD50 lebih dari 1000 (mg/kg, pada tikus). Kemampuan Octopi untuk melumpuhkanmangsa sebelum menelan, dengan sekresi kelenjar ludah posterior telah lamatelah diketahui. Agen aktif yang hadir dalam kelenjar ludah guritatelah ditemukan untuk menjadi campuran berat molekul rendah amina, peptida,dan proteinaceous materials.87 Ghiretti et al88 terisolasi aktif proteinaceoussebagian kecil dari kelenjar ludah gurita valgaris dan O. macropus.Sementara penulis ini menemukan bahwa racun dari Octopi lumpuh danhipotensi tindakan, penyelidikan pada gurita vulgaris menunjukkan hanyaspasmolytic tindakan.Empat puluh invertebrata laut milik moluska, Coelentrata,Echinodermata dan Porifera telah diuji untuk antibakteri, antijamur,antiamoebic, obat, antivirus, antifertility, hypoglycaemic dan luasberbagai aktivitas farmakologis. Ini, tiga ekstrak dipamerkankegiatan antiimplantation dan hypoglycaemic; empat ditemukan beracun, limapunya aktivitas antivirus terhadap EMCV dan atau RDV, tujuh memberikan buktihipotensif aktivitas, sementara sembilan ekstrak ditemukan diuretik. Salah satuekstrak memiliki efek stimulan CNS, dan salah satu memiliki oxytoxic kegiatan maupunsebagai rendah susunan abortifacient aktivitas. Selain delapan ekstrak mengungkapkan lebihdari satu jenis activity.89 spesies Coelenterata yang menunjukkan aktivitasadalah: Acropora corymbosa dikumpulkan dari Kadmai pulau, Lakshadweep, dalamJanuari menunjukkan aktivitas CVS, Acropora formika dikumpulkan dari yang samawilayah menunjukkan aktivitas diuretik, LD50 2.15 (mg/kg, pada tikus), Acropora humilisdikumpulkan dari pulau Kadmai, Lakshadweep, pada bulan Januari dipamerkan antivirusaktivitas melawan Ranikhet penyakit virus, LD50 lebih dari 1000 (mg/kg, di dalamtikus), Alcyonaria spp. dikumpulkan dari wilayah sama dipamerkan diuretik,dan hypoglycaemic, kegiatan, LD50 3.16 (mg/kg, pada tikus); Montiporadivaricata dikumpulkan dari Krusadai pulau, Tamilnadu, pada bulan September yang menunjukkanhypoglycaemic activity, LD50 1000 (mg/kg, in mice), Paracondylacts spp.collected from Chandipur, Orissa, in April showed antiimplantation activityin rats, LD50 more than 1000 (mg/kg in mice); Zoanthus spp. collected fromVeraval, Gujarat, in April showed cardiovascular effects. The species ofCrustacean which showed activity is Eurythoe complanata collected fromChandipur in April showed diuretic activity. The species of Echinodermatawhich showed activity are: Pentaceraster regulus collected from Rameswarm,Tamilnadu, in September showed diuretic and antiviral activity againstEncephalomyocaritis virus; Ischnochiton campus collected from Orissa inMarch exhibited antiimplantation activity in rats and CNS activity, LD5026.1 (mg/kg, in mice); Modiolus striatulus collected from Krishnapuram,Orissa in February showed diuretic activity, Terebralia palustris, collectedfrom South Andaman in April showed cardiovascular effects. The species ofBioactivity of Marine Organisms 117Porifera which showed activity are: Axinella andamanensis collected fromthe Red Skin island, South Andaman, in April showed cardiovascular activity,LD50 46.4 (mg/kg, in mice), Callyspongia spinosissima collected fromRameswaram, Tamilnadu, in September showed antiviral activity againstRanikhet Disease virus and Encephalomyocarditis virus; Heteronema erectafrom Red Skin island, South Andaman in September exhibited hypoglycaemicactivity, Sigmadocia pumlla from Rameswaram, Tamilnadu, in Septembershowed, diuretic, antiimplantation activity in rats and cardiovascular effect;Spirastrella inconstans from Krusadai island, Tamilnadu, in Septemberexhibited diuretic activity, LD50 more than 1000 (mg/kg, in mice andSpirastrella inconstans var. digitata from Rameswarm, Tamilnadu, inSeptember showed antiviral activity against Encephalomyocarditis virus.Many Coelenterates produce toxins or other biologically active metabolitesnot only for self-defence but at times to capture prey. Echinoderms areknown to contain polyhydroxysteroids and saponins. Most of these saponinsare reported to have haemolytic activity. Mostly the secondary metabolitesisolated from hard crust Molluscs are venomous in nature, and are used bythe animals to capture prey. Sponges are by far the most extensively studiedmarine animals. A variety of biologically active constituents have been isolatedfrom sponges.Extracts of marine organisms have been assayed for their cardiovascular90and toxic properties.91 The results of screening of 118 marine organisms(Coral, Alcyoniarians, Molluscs, Echinoderms) found in coastal waters ofIndia, for their toxicity on fish and mice fingerlings as well as their hemolyticactivities are reported.92Echinoderms were found to be toxic to both fish andmice. They also exhibited high order of hemolytic activity. The Alcyoniarianswere found toxic to fish and mice, but had weak hemolytic activity. TheMolluscs, Patelia chathalamus, Trochus spp., Conus spp., Siganus spp. andConus textile were found toxic to fish only, whereas Drupa heptogonalis wasfound lethal only to mice. The coral Acropora formosa and A. milleporaexhibited hemolytic activity and were the only corals toxic to mice. Subergorgiasuberosa, the only gorgonian collected showed lethal toxicity to fish as wellas strong hemolytic activity. The sponges did not show toxic reaction to fishand mice, but exhibited weak hemolytic activity. Specimen of Spirastrellainconstans, Porites lutea, Pocillopora damicornis, Favites abdita, Montiporadigitata and Noditittoria pyramidalis, collected from three different locationsto determine whether their biotoxicity differs with change in ecologicalconditions, showed that their biotoxicities did not differ with ecologicalchanges.4.4 Search of Pharmaceutically Useful CompoundsRinehert et al93 have been searching pharmaceutically useful compoundsfrom marine organisms. Their first effort invovled a survey of marine organismsfor antibacterial and antifungal properties. The bioassay were carried out on118 Bioactive Marine Natural Productsshipboard.94 These were the first systematic shipboard assay for pharmaceuticalactivity, and had many advantages.95,96 The most active antiviral extract inshipboard testing was from a tunicate identified as Eudistoma olivaceum,97but the extract was surprisingly inactive in the secondary assay. However, theextract of the recollected sample proved very active in both primary andsecondary assays against Herpes simplex and other viruses, confirming thevalue of on site assay. Chemical investigation of the bioactive extract ofEudistoma yielded 17 eudistomins having variously substituted β-carbolines.98,99 Although all the isolated compounds exhibited antimicrobialor antiviral activity, the most potent compounds were the tetracyclic eudistominswith the unique oxathiazepine ring. The in vivo testing of these compoundscould not be carried out due to the scarcity of the tunicate and paucity ofmany of the eudistomins. Rinehart et al100,101 have synthesised a number ofthese eudistomins. However, oxathiazepine eudistomins have been preparedin extremely poor yield.The extract of the tunicate Trididemnum solidum was found to have potentantiviral activity in bioassays carried out on shipboard.93 It was also found tobe most cytotoxic. Moreover, these activities were confirmed in in vivotesting at Upjohn,101 USA. Nine major and several minor didemnins havebeen isolated from the extract of T. solidum102-104 which is widely distributedand didemnin-B was relatively abundant in it. Syntheses of some didemninshave been reported.105,106 Didemnins are active in vivo against DNA andRNA viruses. Of these, didemnin-B is the most active. Besides, didemnin-Bexhibits remarkable immunosuppressant activity.107 It is 1000 times as potent
as cyclosporin-A in inhibiting T-cell mitogenesis. It has also been shown in
vivo activity in prolonging skin grafts.96 Unfortunately, didemnin-B is toxic.
Ecteinascidia turbinata is reported to contain a potent antitumour agent.108
An interesting immunoregulatory activity was subsequently observed in the
extract of the organism.109 Later on, cytotoxicity was found in the extract.
Counter current chromatography and TLC bioautography on tissue culture
plates resulted in the isolation of ecteinascidins in yields 10-4 to 10-6 percent.96
All the compounds had either anti-bacterial activity or cytotoxicity against L
1210 leukemia cells.96
Over 300 marine organisms from Okinawan water have been screened for
cytotoxicity, antiviral and antimicrobial activities.110 An extract of a sponge
Theonella spp. was found highly cytotoxic in the assay against P 388 murine
leukemia cells. Bioassay guided separation led to the isolation of an active
constituent designated as misakinolide A, which had IC50 10 ng/ml in in
vitro tests and T/C 145% at a dose of 0.5 mg/kg against P 388 in mice. The
biology and ecology of tropical Holothurians have been reviewed.111 Work
has been conducted on the toxicity of sponges and holothurians.112
5. Actinomycetes
Actinomycetes play a major role in producing antibiotic