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Marine Drugs: Novel Medicinal Agents from Marine Sources

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Dr. Siddhi Upadhyay
Dr. Siddhi Upadhyay

#pharmacy #pharmacognosy #phytochemistry #phytoconstituents #drsiddhiupadhyay #sigmainstituteofpharmacy #marinedrugs

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MARINE PHARMACOGNOSY DR. SIDDHI UPADHYAY ASSOCIATE PROFESSOR AND H.O.D. DEPARTMENT OF PHARMACOGNOSY AND PHYTOCHEMISTRY SIGMA INSTITUTE OF PHARMACY, BAKROL, WAGHODIA, VADODARA.
Definition of Marine Pharmacognosy  Marine pharmacognosy is the branch of pharmacognosy, which is mainly concern with the naturally occurring substance of medicinally value from marine. 2
Classification of marine drugs  Antiviral agent  Anticancer agent  Antimicrobial agent  Cardiovascular agent  Antibiotics  Anti-inflammatory agent  Anthelmentic  Anticoagulant  Prostaglandins  Marine toxins  Anti-parasitic agent  Agrochemical usage  spirulina 3
Marine algae 1. Chynophyceae (Blue green algae). 2. Chlorophyceae (Green algae). 3. Phacophyceae (Brown algae). 4. Rhodophyceae (Red algae) 4
5 Organism Chemical compd. Physiological effects Tethya crypta(sponge) Ara-A Antiviral Trididemnum species (Tumicate) Diademnins Antiviral & antitumor Eudistoma olivaceum (Tumicate) Eudistomin A & β-carbolines Inhibit immune deficiency virus & high therapeutic index & ability to cross BBB Potential used in treatment of AIDS Disidea avara (Sponge) Avarol & avarone Inhibit immune deficiency virus & high therapeutic index & ability to cross BBB Potential used in treatment of AIDS Ascidian lissocillium patella (Sponge) Patellazole-B High potency against Herpis simplex virus Laminaria (Brown algae) Sulphated poly saccharide flucoidan Inhibit both DNA & RNA of HSV & HIV ANTIVIRAL AGENT
6 NH2 EUDISTOMIN A AVAROL AVARONE
7 Organism Chemical compd. Physilogical effect Cryptotethya crypta Ara-c (cytosine arabinose) Treatment of acute mylogenous leukemia & human acute leukemia Pseudoplexaura porosa Crassian acetate(cyclic diterpens) Cytotoxic to human leukemia Simularia flexibilis Simularine Cytotoxic Aplidium spp. Geranyl hydroquinone Cytotoxic to leukemia & mammary carcinoma Aplysia angasi Aplysistatin Antileukemic Halielona viridis Halitoxin Antitumor Trididemnum spp. Didemnins A,B,C Potent inhibitor of L-1210 leukemic cell ANTICANCER AGENT
8 HOH CH2 OH Ara-C • Adult and child hood leukemia treatment. • Useful in acute granuloma leukemia. • More effective in combination with thoguinine and daunorubicine. Crassian acetate simularine
9 Geranyl hydroquinone O Aplysistatin Bryostatin: Buguna neritina M/A: • Activation of protein kinase C & Arachidonic acid metabolite release. • Both Bryostatin 1&2 the efficiency of interleukin-2 initiating the development of invivo primed cytotoxic T lymphocytes.
10 Xenia: Xenia elongata M/A: Inhibit the mitochondrial Respiraration in cancer cells. Nephthea: Contain bioactive compd. M/A:  5α- reductase inhibitor  Quite active in prostate cancer cell. They are androgen dependent  Inhibit the coversion of testosterone into dihydrotestosterone
11 Organism Chemical compd. Physiological effect Cephalosporium acremonium Cephalosporin (Antibiotic) Inhibit bacterial cell wall formation, enzyme transpeptidase responsible cross-linking,peptidoglycan synthesis,penicillin binding protein Dictopteris zonoroids (Brown algae) Zonorol, isozonorol Antimicrobial Ptilonia qustralasica Bromopyrone Compd. Have halogen but not to toxic as antimicrobial Bonnemaisonia hemifera (Red algae) Tetrabromoheptanone Antimicrobial Eunicia mammosa (Gorgonian corals) Eunicin Antimicrobial Acanthela acuta Acanthelin Active against mycobacterium ANTIMICROBIAL AGENT
12 CEPHALOSORIN-C OH ZONOROL BROMOPYRONE N=C C=CH2 CH3 CH3 CH3 H ACANTHELIN-1
13 CARDIOVASCULAR AGENTS Cardiotonic Hypotensive compd (Compd. Showing positive ionotropic activities) Marine peptide Marine glycosides Marine nucleoside Hypotensive peptides
14 Cardiotonic 1) Marine peptides Organism Chemical compd. Physiological effects Anthopleura xanthogrannica Anthopleurin A,B,C Anthopleurin A has cardiotonic activities Heart stimulant activities 4 times more than natural cardiac glycosides Anemonia sulcata Anemonia toxin II Comprising 47 amino acid & exibit dose dependent cardiotonic activities Anthopleura eleantissima Anthopleurin C Produce cardiotonic effects in dog. 35 times potent compaired to digoxin with very less toxicity
15 Octopus macropus Octapamine D(-) form 3 times more potent than L(+) form. Neurotransmitter Verongia fistularis Autonomium chloride Exerts both α & β adrenergic effects. Cholinergic action 2) Marine glycosides sulphated Non sulphated • Holothurins • Astrosaponins: obtained fron star fishes (Asteroidae) H—C—CH2NH2 OH OCTAPAMINE
16 Hypotensive compd. 1) Marine neucleosides Spongosine: Cryptotethya crypta (sponge). Reduce both rate and force of contraction of heart. Doridosine: Anisodoris nobilis. Most potent hypotensive marine nucleoside. It lowers the normal temperature of body.
17 2) Hypotensive peptides Aaptamine: Aaptos aaptos α- adrenergic blocking effects Hymenin Urotensin I & II 3) Other compds. Laminine: laminaria angustata Saxitoxin: saxidomus gigantus Eledosin: eledone moschata (cephalopod) powerful effects obtained from posterior salivary gland of cephalopod.
18 ANTIBIOTICS Organism Chemical compd. Physiological effects Cephalosporium acremonium Cephalosporin Inhibit bacterial cell wall formation, enzyme transpeptidase responsible cross- linking,peptidoglycan synthesis,penicillin binding protein. Pseudomonas bromutilis (Marine bacterium) 2,4-dibromo-6-phenol Antibiotic Chondria oppositiclada (Red algae) Cycloudesmol Antibiotic Ircinia strobilina (Spong) Venabilin Ircinin-1 Antibiotic
19 Br 2,4 dibromo-6-phenol variabilin Ircinin-1 cycloeudesmol
20 Organism Chemical compd. Physiological effects Luffariella variabilis Manoalide (NSAID) Act by direct inactivation of phospholipase A2 which is present in some neurotoxin & also role in synthesis of prostaglandins in humans. Analgesic and selective antiinflammatory activities. Rivularia firma Series of novel bindoles Oedema and acts on CNS Puffer fishes (Liver and Ovaries) Tetradotoxin Strong anti-spasmodic Flusra foliaceal Flustramine A&B Muscle relexant Sinularia flexibilis Flexibilide Anti-inflammatory agent ANTI-INFLAMMATORY AGENT
21 Organism Chemical compd. Physiological effects Digenia simplex (Red algae) α- kainic acid Broad specrum anthelmentic. Effect against parasitic round worm, whip worm, tape worm Chondria armata (Red algae) Domoic acid Anthelmentic agent Laminaria anguststa Laminine Anthelmentic, smooth muscle relaxant and hypotensive Sea cucumber Cucumechinoside F antiprotozoal ANTI-PARASITIC AGENTS
22 CH2 COOH α- kainic acid CH2 COOH Domoic acid
23 Organism Chemical compd. Physiological effects Iridaea laminarioides Galaxtan sulphuric acid Anti-coagulants Chondrus cryspus Carragenans Anti-coagulants, invitro activation of thrombin Fucus vasiculosus Flucoidan Anticoagulant, antithrobin through heparin cofactor II ANTI-COAGULANT
24 MARINE TOXINS The marine toxins are caused due to either external metabolites or endotoxins Palytoxin Red tide toxins Cigualera toxin 1) Palytoxin: [PTX]  Initially reported from the pacific ocean by moore & scheuer.  B.S: obtained from zonathid coral of the genus Polythoa found in both pacific & carrabian ocean.  Most poisoneous non protein compound.
25  Linear polycyclic compd. Having mol.formula is C129 H223 N3 O54.  Use: Coronary vasocostrictor Anti-anginal Chemotherapeutic agent 2) Red tide toxins:  Star was the pionear in reporting red tide toxin from gulf of mexico.  Red tide due to red coloured peridinin, carotanoids natural pigment by imparting to water brown to red coloration.
26 Red tide organism Toxin present G.S Physiological effects Protogonyaulax cartenella GTXs & STXs Japan, south america & pacific ocean Block membrane by Na+ conductance Axexandrium tamarense GTXs & STXs North atlantic Block membrane by Na+ conductance Ptychodiscus Brevetoxin Gulf of mexico +ve ionotropic effects & array thromogenic Gymnodinium catenatum GTXs & PX Japan Paralytic syndrom GTX Gonyautoxins STX saxitoxin PX protogonyautoxin
27 Tetradotoxin: [TTX]  Obtained from ovaries & liver of globe fish & puffer fish.  TTX bind with Na+ channel on outside of exitable membranes there by inducing Na+ influx in exchange for K+  Cause depolarization immediately. Brevetoxin:  Effects on Na+ influx & voltage sensitive channel. 3)Ciguatera toxin: Ciguatoxin (CTX) Maitotoxin (MTX)
28 i) Ciguatoxin  It is a poison due to indigestion of blue green algae.  B.S: obtained from gymnothorax javanicus  Characterized by diarrhoea, vomiting & sometimes acute neurological problems ii) Maitotoxin  B.S: obtained from gambierdiscus toxicus Lophotoxin : lophogorgia rigida  Neuromuscular blocker  Irriversible post synaptic blockage at neuromuscular junction
29 NH2 Saxitoxin CHO O OAC Lophotoxin
30 SPIRULINA  B.S: Spirulina is a the blue green algae Spirulina pletensis or S. maxima.  Family: oscillatoriaceae  G.S: Cultivated in USA, Thiland, Mexico, India and China  Group of algae responsible for photosynthesis.  Link between green plants and bacteria.  It has a soft cell made up of complex sugars and protein.  Different from most algae that it is easily digested.  Source of food contain neutraceutical having antioxidant, probiotic and phytonutrients.
31  Chemical composition: protein: 50-70% proteineous nitrogen: 11.36% total organic nitrogen: 13.35% nitrogen from nucleic acid: 1.9% net protein utilization: 62% lipid: 5-6%  Having essential fat which composed of oleic, linoleic, gamma linoleic, palmitic acid.  40% of fat including sulpholipids have anti-HIV activity.  Contain β- carotine having anti-oxidant capacity.  Phytocynin- blue green pigment which enhance general immunity and lymphocytic activity against cancer.
32  Biological role:  Immunostimulant activity.  Stimulate production and activity of bone marrow stem cells, macrophages, T-cells, spleen and thymus gland.  Enhances cell nucleus enzyme activity & DNA repair hence used in cancer treatment.  Calcium spirulina inhibit HIV-1, HSV.  Appetite suppresing activity.
33 THANK YOU !!! siupa.pharma@gmail.com

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Marine Drugs: Novel Medicinal Agents from Marine Sources

  • 1. MARINE PHARMACOGNOSY DR. SIDDHI UPADHYAY ASSOCIATE PROFESSOR AND H.O.D. DEPARTMENT OF PHARMACOGNOSY AND PHYTOCHEMISTRY SIGMA INSTITUTE OF PHARMACY, BAKROL, WAGHODIA, VADODARA.
  • 2. Definition of Marine Pharmacognosy  Marine pharmacognosy is the branch of pharmacognosy, which is mainly concern with the naturally occurring substance of medicinally value from marine. 2
  • 3. Classification of marine drugs  Antiviral agent  Anticancer agent  Antimicrobial agent  Cardiovascular agent  Antibiotics  Anti-inflammatory agent  Anthelmentic  Anticoagulant  Prostaglandins  Marine toxins  Anti-parasitic agent  Agrochemical usage  spirulina 3
  • 4. Marine algae 1. Chynophyceae (Blue green algae). 2. Chlorophyceae (Green algae). 3. Phacophyceae (Brown algae). 4. Rhodophyceae (Red algae) 4
  • 5. 5 Organism Chemical compd. Physiological effects Tethya crypta(sponge) Ara-A Antiviral Trididemnum species (Tumicate) Diademnins Antiviral & antitumor Eudistoma olivaceum (Tumicate) Eudistomin A & β-carbolines Inhibit immune deficiency virus & high therapeutic index & ability to cross BBB Potential used in treatment of AIDS Disidea avara (Sponge) Avarol & avarone Inhibit immune deficiency virus & high therapeutic index & ability to cross BBB Potential used in treatment of AIDS Ascidian lissocillium patella (Sponge) Patellazole-B High potency against Herpis simplex virus Laminaria (Brown algae) Sulphated poly saccharide flucoidan Inhibit both DNA & RNA of HSV & HIV ANTIVIRAL AGENT
  • 7. 7 Organism Chemical compd. Physilogical effect Cryptotethya crypta Ara-c (cytosine arabinose) Treatment of acute mylogenous leukemia & human acute leukemia Pseudoplexaura porosa Crassian acetate(cyclic diterpens) Cytotoxic to human leukemia Simularia flexibilis Simularine Cytotoxic Aplidium spp. Geranyl hydroquinone Cytotoxic to leukemia & mammary carcinoma Aplysia angasi Aplysistatin Antileukemic Halielona viridis Halitoxin Antitumor Trididemnum spp. Didemnins A,B,C Potent inhibitor of L-1210 leukemic cell ANTICANCER AGENT
  • 8. 8 HOH CH2 OH Ara-C • Adult and child hood leukemia treatment. • Useful in acute granuloma leukemia. • More effective in combination with thoguinine and daunorubicine. Crassian acetate simularine
  • 9. 9 Geranyl hydroquinone O Aplysistatin Bryostatin: Buguna neritina M/A: • Activation of protein kinase C & Arachidonic acid metabolite release. • Both Bryostatin 1&2 the efficiency of interleukin-2 initiating the development of invivo primed cytotoxic T lymphocytes.
  • 10. 10 Xenia: Xenia elongata M/A: Inhibit the mitochondrial Respiraration in cancer cells. Nephthea: Contain bioactive compd. M/A:  5α- reductase inhibitor  Quite active in prostate cancer cell. They are androgen dependent  Inhibit the coversion of testosterone into dihydrotestosterone
  • 11. 11 Organism Chemical compd. Physiological effect Cephalosporium acremonium Cephalosporin (Antibiotic) Inhibit bacterial cell wall formation, enzyme transpeptidase responsible cross-linking,peptidoglycan synthesis,penicillin binding protein Dictopteris zonoroids (Brown algae) Zonorol, isozonorol Antimicrobial Ptilonia qustralasica Bromopyrone Compd. Have halogen but not to toxic as antimicrobial Bonnemaisonia hemifera (Red algae) Tetrabromoheptanone Antimicrobial Eunicia mammosa (Gorgonian corals) Eunicin Antimicrobial Acanthela acuta Acanthelin Active against mycobacterium ANTIMICROBIAL AGENT
  • 13. 13 CARDIOVASCULAR AGENTS Cardiotonic Hypotensive compd (Compd. Showing positive ionotropic activities) Marine peptide Marine glycosides Marine nucleoside Hypotensive peptides
  • 14. 14 Cardiotonic 1) Marine peptides Organism Chemical compd. Physiological effects Anthopleura xanthogrannica Anthopleurin A,B,C Anthopleurin A has cardiotonic activities Heart stimulant activities 4 times more than natural cardiac glycosides Anemonia sulcata Anemonia toxin II Comprising 47 amino acid & exibit dose dependent cardiotonic activities Anthopleura eleantissima Anthopleurin C Produce cardiotonic effects in dog. 35 times potent compaired to digoxin with very less toxicity
  • 15. 15 Octopus macropus Octapamine D(-) form 3 times more potent than L(+) form. Neurotransmitter Verongia fistularis Autonomium chloride Exerts both α & β adrenergic effects. Cholinergic action 2) Marine glycosides sulphated Non sulphated • Holothurins • Astrosaponins: obtained fron star fishes (Asteroidae) H—C—CH2NH2 OH OCTAPAMINE
  • 16. 16 Hypotensive compd. 1) Marine neucleosides Spongosine: Cryptotethya crypta (sponge). Reduce both rate and force of contraction of heart. Doridosine: Anisodoris nobilis. Most potent hypotensive marine nucleoside. It lowers the normal temperature of body.
  • 17. 17 2) Hypotensive peptides Aaptamine: Aaptos aaptos α- adrenergic blocking effects Hymenin Urotensin I & II 3) Other compds. Laminine: laminaria angustata Saxitoxin: saxidomus gigantus Eledosin: eledone moschata (cephalopod) powerful effects obtained from posterior salivary gland of cephalopod.
  • 18. 18 ANTIBIOTICS Organism Chemical compd. Physiological effects Cephalosporium acremonium Cephalosporin Inhibit bacterial cell wall formation, enzyme transpeptidase responsible cross- linking,peptidoglycan synthesis,penicillin binding protein. Pseudomonas bromutilis (Marine bacterium) 2,4-dibromo-6-phenol Antibiotic Chondria oppositiclada (Red algae) Cycloudesmol Antibiotic Ircinia strobilina (Spong) Venabilin Ircinin-1 Antibiotic
  • 20. 20 Organism Chemical compd. Physiological effects Luffariella variabilis Manoalide (NSAID) Act by direct inactivation of phospholipase A2 which is present in some neurotoxin & also role in synthesis of prostaglandins in humans. Analgesic and selective antiinflammatory activities. Rivularia firma Series of novel bindoles Oedema and acts on CNS Puffer fishes (Liver and Ovaries) Tetradotoxin Strong anti-spasmodic Flusra foliaceal Flustramine A&B Muscle relexant Sinularia flexibilis Flexibilide Anti-inflammatory agent ANTI-INFLAMMATORY AGENT
  • 21. 21 Organism Chemical compd. Physiological effects Digenia simplex (Red algae) α- kainic acid Broad specrum anthelmentic. Effect against parasitic round worm, whip worm, tape worm Chondria armata (Red algae) Domoic acid Anthelmentic agent Laminaria anguststa Laminine Anthelmentic, smooth muscle relaxant and hypotensive Sea cucumber Cucumechinoside F antiprotozoal ANTI-PARASITIC AGENTS
  • 22. 22 CH2 COOH α- kainic acid CH2 COOH Domoic acid
  • 23. 23 Organism Chemical compd. Physiological effects Iridaea laminarioides Galaxtan sulphuric acid Anti-coagulants Chondrus cryspus Carragenans Anti-coagulants, invitro activation of thrombin Fucus vasiculosus Flucoidan Anticoagulant, antithrobin through heparin cofactor II ANTI-COAGULANT
  • 24. 24 MARINE TOXINS The marine toxins are caused due to either external metabolites or endotoxins Palytoxin Red tide toxins Cigualera toxin 1) Palytoxin: [PTX]  Initially reported from the pacific ocean by moore & scheuer.  B.S: obtained from zonathid coral of the genus Polythoa found in both pacific & carrabian ocean.  Most poisoneous non protein compound.
  • 25. 25  Linear polycyclic compd. Having mol.formula is C129 H223 N3 O54.  Use: Coronary vasocostrictor Anti-anginal Chemotherapeutic agent 2) Red tide toxins:  Star was the pionear in reporting red tide toxin from gulf of mexico.  Red tide due to red coloured peridinin, carotanoids natural pigment by imparting to water brown to red coloration.
  • 26. 26 Red tide organism Toxin present G.S Physiological effects Protogonyaulax cartenella GTXs & STXs Japan, south america & pacific ocean Block membrane by Na+ conductance Axexandrium tamarense GTXs & STXs North atlantic Block membrane by Na+ conductance Ptychodiscus Brevetoxin Gulf of mexico +ve ionotropic effects & array thromogenic Gymnodinium catenatum GTXs & PX Japan Paralytic syndrom GTX Gonyautoxins STX saxitoxin PX protogonyautoxin
  • 27. 27 Tetradotoxin: [TTX]  Obtained from ovaries & liver of globe fish & puffer fish.  TTX bind with Na+ channel on outside of exitable membranes there by inducing Na+ influx in exchange for K+  Cause depolarization immediately. Brevetoxin:  Effects on Na+ influx & voltage sensitive channel. 3)Ciguatera toxin: Ciguatoxin (CTX) Maitotoxin (MTX)
  • 28. 28 i) Ciguatoxin  It is a poison due to indigestion of blue green algae.  B.S: obtained from gymnothorax javanicus  Characterized by diarrhoea, vomiting & sometimes acute neurological problems ii) Maitotoxin  B.S: obtained from gambierdiscus toxicus Lophotoxin : lophogorgia rigida  Neuromuscular blocker  Irriversible post synaptic blockage at neuromuscular junction
  • 30. 30 SPIRULINA  B.S: Spirulina is a the blue green algae Spirulina pletensis or S. maxima.  Family: oscillatoriaceae  G.S: Cultivated in USA, Thiland, Mexico, India and China  Group of algae responsible for photosynthesis.  Link between green plants and bacteria.  It has a soft cell made up of complex sugars and protein.  Different from most algae that it is easily digested.  Source of food contain neutraceutical having antioxidant, probiotic and phytonutrients.
  • 31. 31  Chemical composition: protein: 50-70% proteineous nitrogen: 11.36% total organic nitrogen: 13.35% nitrogen from nucleic acid: 1.9% net protein utilization: 62% lipid: 5-6%  Having essential fat which composed of oleic, linoleic, gamma linoleic, palmitic acid.  40% of fat including sulpholipids have anti-HIV activity.  Contain β- carotine having anti-oxidant capacity.  Phytocynin- blue green pigment which enhance general immunity and lymphocytic activity against cancer.
  • 32. 32  Biological role:  Immunostimulant activity.  Stimulate production and activity of bone marrow stem cells, macrophages, T-cells, spleen and thymus gland.  Enhances cell nucleus enzyme activity & DNA repair hence used in cancer treatment.  Calcium spirulina inhibit HIV-1, HSV.  Appetite suppresing activity.