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MARINE
Novel medicinal agents from
marine sources
COMPILED BY
DR NISHA SHARMA
Marine drugs
• Oceans cover more than 70% of the earth’s surface with over 200,000
invertebrates and algal species.
• Commonly used Drugs obtained from marine organisms which are
being used are shark & cod-liver oils, sodium alginate, agar-agar, and
chitin etc.
• Classification
Class Examples
Antibiotic compunds Cycloeudesmol, variabilin, Ircinin-1
Anti inflammatory & anti spasmodic Manoalide, Tetrado toxin
Antimicrobial compd Holotoxin ABC, Tholepin, eunicin acanthelin
Cardiovascular active compd Anthopleurins, Laminine, Eptatretin, saxitoxin,
spongosine, eledosin, ATX-II, Autonomium
Anti cancer (cytotoxic) Ara-c, crassin acetate simularin.
Marine toxins compds Ciguatoxin, Palytoxin, Saxitoxin, Brevetoxin
Miscellaneous compd Kainic acid, Domoic acid, Aplysinopsin.
ANTIBIOTICS COMPOUNDS
Organism Antibiotic Substance
Marine bacterium, Pseudomonas bromutilis 2, 4 - Dibromo - 6 - (3, 4, 5 tribromopyrrole
- 2 - yl) phenol
Red algae, Chondria oppositiclada Cycloeudesmol
Sponge, Ircinia strobilina and Ircinia oros Variabilin, Ircinin – 1
Sponge, Verongia archery 3, 5 - dibromo - 4 - hydroxy benzene-1
acetamide
ANTI INFLAMMATORY COMPOUNDS
Organism Anti inflammatory
Substance
MOA/ uses
Luffariella variabilis (sponge) Manoalide (analgesic also) it acts by direct inactivation
of phospholipase A2enzyme
present in some neurotoxins
and also has a role in
synthesis of prostaglandins
Phyllospongia dendyi; sponge dendalone 3hydroxy
butyrate
Antiinflammatroy
soft coral, Sinularia flexibilis flexibilide
Brown algae, Caulocystis
cephalornithos.
6-n-tridecyl salicylic acid
Flustra foliaceae, a Swedish
marine moss.
Flustramine A& B Muscle relaxant
liver and ovaries of puffer
fishes
Tetradotoxin strong antispasmodic.
ANTI MICROBIAL COMPOUNDS
Organism ANTIMICROBIAL
Sea cucumber, Stichopus japonicus Holotoxin A, B and C (steroida glycoside)
antifungal in nature Zonarol and iso-zonarol
Brown algae, Dictyopteris zonaroides Tetrabromoheptanone
Red algae, Bonnemaisonia hemifera Four isomers of polyhalo 3 butene - 2 - one and
seven isomers of polythaloacetones.
Red algae, Asparogopsis taxiformis. Aeroplysinin-1 (+)
Sponge, Verongia aerophoba Aeroplysinin-1 (-)
Sponge, Agelas oroides 2 - cyano - 4, 5 – dibromo pyrrole
Red algae, Laurencia pacifica and L.
filformis.
Prepacifenol
Annelida, Thelepsus setosus Tholpin
Sea hare, Aplysia californica Debromolaurenterol
Gorgonian corals, Eunicia mammosa Eunicin
Acanthella acuta Acanthelin -1 (active against Mycobacterium)
CARDIOVASCULAR ACTIVE SUBSTANCES
Organism Compounds
peptides obtained from coelenterates
Anthropleura xanthogrammica
A. elegantissima
Anthopleurins: (AP - A and AP - B);
type C (AP – C)
aneural bronchial hearts of pacific
hogfish viz. Eptatretus stoutii.
Eptatretin
marine algae, Laminaria angustata Laminine
Octopus macropus, O. vulgaris and
Eledone moschata
D (–) Octopamine
Saxidomus giganteus, and California
mussel, Mytilus californianus.
Saxitoxin
sea anemones ATX – II (POLYPEPTIDE)
Sea cucumbers, Holothuroidae family Holothurins (triterpenoids moiety)
star fishes of family Asteroidae asterosaponins (steroidal aglycone)
Caribbean sponge Crypotethia crypta. Spongosine (nucleoside)
posterior salivary glands of cephalopod
Eledone moschata.
Eledosin
ANTICANCER SUBSTANCES
Organism Compounds
Caribbean sponges: spongosine and
spongouridine.
Ara –C: 1 - α - D - arabinofuranosyl cytosine
or cytosine arabinoside.
Used in acute myelogenous leukemia and
human acute leukemia,
Caribbean gorgonian,
Pseudoplexaura porosa (soft corals)
Crassin acetate cyclic diterpene
human leukemic and HeLa cells in-vitro.
Soft coral Sinularia flexibilis simularin, dihydrosimularin and
simulariolide.
Gorgonian coral Asperdiol
Aplidium species geranyl hydroquinone (cytotoxic to
leukemia and mammary carcinoma)
Sea hare Aplysia angasi aplysistatin (antileukemic)
Sponge Haliclona viridis; halitoxin (antitumour)
Algae Lyngbya majuscula;
Sea sqirt Ecteinascidia turbinata.
majusculamine - C (inhibitor of X - 5563
myeloma)
MARINE TOXINS
Organism Compounds Effects
Gonyaulax catenella
G. tamarensis
saxitoxin depolarises membranes, permeability
alteration to Na+
Haliclona rubens holotoxin potent neuromuscular blocker
Gambier discus
toxicus
maitotoxin stimulates calcium channels in insect
skeletal muscles
Palythoa species palytoxin most potent coronary vasoconstrictor
Lophogorgia rigida lophotoxin neuromuscular blocker
Ptychodiscus brews brevetoxin positive inotropic and arrhythmogenic
Gambier discus
toxicus
ciguatoxin respiratory depression and bradycardia
Babylonia japonica neosurugatoxin potent blocker of sympathetic ganglia
and a specific blocker of nicotinic Ach
receptors
MISCELLLANEOUS COMPOUNDS
Organism Compounds Effects
red algae: Digenea
simplex
Kainic acid potent convulsant, antiascariatic
activity.
red algae Chondria
armata
domoic acid activity against ascaris and pinworm.
marine annelid,
Lumbriconeris
heteropoda
nereistoxin insecticide due to its ganglion blocking
effects
Sponge Didemnins A, B
and C
against Herpes simplex type-2 virus in
mice
Sponge Ara - Aadenine
arabinoside
Herpes encephalitis.
yellow sponge,
Verongia spengeli
aplysinopsin antidepressant action in animals,
cytotoxic activity.
Eucheuma, Chondrus
and Gigartina
carrageenan anticoagulant agent.

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MARINE origin- Novel DRUGS/ medicine.pptx

  • 1. MARINE Novel medicinal agents from marine sources COMPILED BY DR NISHA SHARMA
  • 2. Marine drugs • Oceans cover more than 70% of the earth’s surface with over 200,000 invertebrates and algal species. • Commonly used Drugs obtained from marine organisms which are being used are shark & cod-liver oils, sodium alginate, agar-agar, and chitin etc. • Classification Class Examples Antibiotic compunds Cycloeudesmol, variabilin, Ircinin-1 Anti inflammatory & anti spasmodic Manoalide, Tetrado toxin Antimicrobial compd Holotoxin ABC, Tholepin, eunicin acanthelin Cardiovascular active compd Anthopleurins, Laminine, Eptatretin, saxitoxin, spongosine, eledosin, ATX-II, Autonomium Anti cancer (cytotoxic) Ara-c, crassin acetate simularin. Marine toxins compds Ciguatoxin, Palytoxin, Saxitoxin, Brevetoxin Miscellaneous compd Kainic acid, Domoic acid, Aplysinopsin.
  • 3. ANTIBIOTICS COMPOUNDS Organism Antibiotic Substance Marine bacterium, Pseudomonas bromutilis 2, 4 - Dibromo - 6 - (3, 4, 5 tribromopyrrole - 2 - yl) phenol Red algae, Chondria oppositiclada Cycloeudesmol Sponge, Ircinia strobilina and Ircinia oros Variabilin, Ircinin – 1 Sponge, Verongia archery 3, 5 - dibromo - 4 - hydroxy benzene-1 acetamide
  • 4. ANTI INFLAMMATORY COMPOUNDS Organism Anti inflammatory Substance MOA/ uses Luffariella variabilis (sponge) Manoalide (analgesic also) it acts by direct inactivation of phospholipase A2enzyme present in some neurotoxins and also has a role in synthesis of prostaglandins Phyllospongia dendyi; sponge dendalone 3hydroxy butyrate Antiinflammatroy soft coral, Sinularia flexibilis flexibilide Brown algae, Caulocystis cephalornithos. 6-n-tridecyl salicylic acid Flustra foliaceae, a Swedish marine moss. Flustramine A& B Muscle relaxant liver and ovaries of puffer fishes Tetradotoxin strong antispasmodic.
  • 5. ANTI MICROBIAL COMPOUNDS Organism ANTIMICROBIAL Sea cucumber, Stichopus japonicus Holotoxin A, B and C (steroida glycoside) antifungal in nature Zonarol and iso-zonarol Brown algae, Dictyopteris zonaroides Tetrabromoheptanone Red algae, Bonnemaisonia hemifera Four isomers of polyhalo 3 butene - 2 - one and seven isomers of polythaloacetones. Red algae, Asparogopsis taxiformis. Aeroplysinin-1 (+) Sponge, Verongia aerophoba Aeroplysinin-1 (-) Sponge, Agelas oroides 2 - cyano - 4, 5 – dibromo pyrrole Red algae, Laurencia pacifica and L. filformis. Prepacifenol Annelida, Thelepsus setosus Tholpin Sea hare, Aplysia californica Debromolaurenterol Gorgonian corals, Eunicia mammosa Eunicin Acanthella acuta Acanthelin -1 (active against Mycobacterium)
  • 6. CARDIOVASCULAR ACTIVE SUBSTANCES Organism Compounds peptides obtained from coelenterates Anthropleura xanthogrammica A. elegantissima Anthopleurins: (AP - A and AP - B); type C (AP – C) aneural bronchial hearts of pacific hogfish viz. Eptatretus stoutii. Eptatretin marine algae, Laminaria angustata Laminine Octopus macropus, O. vulgaris and Eledone moschata D (–) Octopamine Saxidomus giganteus, and California mussel, Mytilus californianus. Saxitoxin sea anemones ATX – II (POLYPEPTIDE) Sea cucumbers, Holothuroidae family Holothurins (triterpenoids moiety) star fishes of family Asteroidae asterosaponins (steroidal aglycone) Caribbean sponge Crypotethia crypta. Spongosine (nucleoside) posterior salivary glands of cephalopod Eledone moschata. Eledosin
  • 7. ANTICANCER SUBSTANCES Organism Compounds Caribbean sponges: spongosine and spongouridine. Ara –C: 1 - α - D - arabinofuranosyl cytosine or cytosine arabinoside. Used in acute myelogenous leukemia and human acute leukemia, Caribbean gorgonian, Pseudoplexaura porosa (soft corals) Crassin acetate cyclic diterpene human leukemic and HeLa cells in-vitro. Soft coral Sinularia flexibilis simularin, dihydrosimularin and simulariolide. Gorgonian coral Asperdiol Aplidium species geranyl hydroquinone (cytotoxic to leukemia and mammary carcinoma) Sea hare Aplysia angasi aplysistatin (antileukemic) Sponge Haliclona viridis; halitoxin (antitumour) Algae Lyngbya majuscula; Sea sqirt Ecteinascidia turbinata. majusculamine - C (inhibitor of X - 5563 myeloma)
  • 8. MARINE TOXINS Organism Compounds Effects Gonyaulax catenella G. tamarensis saxitoxin depolarises membranes, permeability alteration to Na+ Haliclona rubens holotoxin potent neuromuscular blocker Gambier discus toxicus maitotoxin stimulates calcium channels in insect skeletal muscles Palythoa species palytoxin most potent coronary vasoconstrictor Lophogorgia rigida lophotoxin neuromuscular blocker Ptychodiscus brews brevetoxin positive inotropic and arrhythmogenic Gambier discus toxicus ciguatoxin respiratory depression and bradycardia Babylonia japonica neosurugatoxin potent blocker of sympathetic ganglia and a specific blocker of nicotinic Ach receptors
  • 9. MISCELLLANEOUS COMPOUNDS Organism Compounds Effects red algae: Digenea simplex Kainic acid potent convulsant, antiascariatic activity. red algae Chondria armata domoic acid activity against ascaris and pinworm. marine annelid, Lumbriconeris heteropoda nereistoxin insecticide due to its ganglion blocking effects Sponge Didemnins A, B and C against Herpes simplex type-2 virus in mice Sponge Ara - Aadenine arabinoside Herpes encephalitis. yellow sponge, Verongia spengeli aplysinopsin antidepressant action in animals, cytotoxic activity. Eucheuma, Chondrus and Gigartina carrageenan anticoagulant agent.