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LD50 681 (mg/kg, in mice), Actinopyga mauritianacollected from Lakshadweep in October showed hypotensive and antimicrobialactivities LD50 215 (mg/kg, in mice), and Thelenata ananas collected fromLakshadweep showed antimicrobial activity, LD50 56.2 (mg/kg, in mice).The extracts of Holothuria ichinitis collected from Mandapam, Tamilnadu,in April and H. impotium collected from Lakashadweep in April were foundtoxic, LD50 26.1 and 38.3 (mg/kg, in mice) respectively. The species ofMollusca which showed activity are : Nerita spp. collected from Mandapam,116 Bioactive Marine Natural ProductsTamilnadu, in January showed CNS stimulant activity, LD50 68.1 (mg/kg, inmice); Octopus vulgaris collected from Okha, Gujarat, in December exhibitedspasmolytic activity, LD50 1000 (mg/kg, in mice) and Onchidium verruculatumcollected from Mandapam, Tamilnadu, in May showed hypoglycaemic activity,LD50 more than 1000 (mg/kg, in mice). The ability of Octopi to paralyseprey before ingestion, with secretions of posterior salivary glands has longbeen known. The active agents present in the salivary glands of the Octopushave been found to be a mixture of low molecular weight amines, peptides,and proteinaceous materials.87 Ghiretti et al88 isolated an active proteinaceousfraction from the salivary glands of Octopus valgaris and O. macropus.While these authors found that the toxins from Octopi have paralytic andhypotension action, the investigations on Octopus vulgaris indicated onlyspasmolytic action.Forty marine invertebrates belonging to the Mollusca, Coelentrata,Echinodermata and Porifera have been tested for antibacterial, antifungal,antiamoebic, antimalarial, antiviral, antifertility, hypoglycaemic and a widerange of pharmacological activities. Of these, three extracts each exhibitedantiimplantation and hypoglycaemic activities; four were found toxic, fivehad antiviral activity against EMCV and or RDV, seven gave evidence ofhypotensive activity, while nine extracts were found to be diuretic. Oneextract had the CNS stimulant effect, and one had oxytoxic activity as wellas low order of abortifacient activity. Besides eight extracts revealed morethan one type of activity.89 The species of Coelenterata which showed activityare: Acropora corymbosa collected from Kadmai Island, Lakshadweep, inJanuary showed CVS activity, Acropora formica collected from the samelocality showed diuretic activity, LD50 2.15 (mg/kg, in mice), Acropora humiliscollected from the Kadmai Island, Lakshadweep, in January exhibited antiviralactivity against Ranikhet Disease virus, LD50 more than 1000 (mg/kg, inmice), Alcyonaria spp. collected from the same locality exhibited diuretic,and hypoglycaemic, activities, LD50 3.16 (mg/kg, in mice); Montiporadivaricata collected from Krusadai Island, Tamilnadu, in September showedhypoglycaemic 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,97
but the extract was surprisingly inactive in the secondary assay. However, the
extract of the recollected sample proved very active in both primary and
secondary assays against Herpes simplex and other viruses, confirming the
value of on site assay. Chemical investigation of the bioactive extract of
Eudistoma yielded 17 eudistomins having variously substituted β-
carbolines.98,99 Although all the isolated compounds exhibited antimicrobial
or antiviral activity, the most potent compounds were the tetracyclic eudistomins
with the unique oxathiazepine ring. The in vivo testing of these compounds
could not be carried out due to the scarcity of the tunicate and paucity of
many of the eudistomins. Rinehart et al100,101 have synthesised a number of
these eudistomins. However, oxathiazepine eudistomins have been prepared
in extremely poor yield.
The extract of the tunicate Trididemnum solidum was found to have potent
antiviral activity in bioassays carried out on shipboard.93 It was also found to
be most cytotoxic. Moreover, these activities were confirmed in in vivo
testing at Upjohn,101 USA. Nine major and several minor didemnins have
been isolated from the extract of T. solidum102-104 which is widely distributed
and didemnin-B was relatively abundant in it. Syntheses of some didemnins
have been reported.105,106 Didemnins are active in vivo against DNA and
RNA viruses. Of these, didemnin-B is the most active. Besides, didemnin-B
exhibits 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
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