Cardiovascular Antimicrobial Antiinflammatory and antibiotic agents of marine origin

Cardiovascular, Antimicrobial, Anti-inflammatory and Antibiotic agents of marine origin

Cardiovascular antimicrobial antiinflammatory and antibiotic agents of marine origin

Cardiovascular antimicrobial antiinflammatory and antibiotic agents of marine origin

Objective

At the end of this
lecture, students will be able to:

• Discuss the different sources of Cardiovascular, antimicrobial, anti-inflammatory and antibiotic agents of marine origin

Marine Cardiovascular drugs

• Cardiotonics

• Marine peptides

• Marine glycosides

Laminin

• Obtained from marine algae Laminaria angustata

• Belongs to the family heterotrimeric glycopoteins composed of heavy chain, designated as alpha and 2 light chains, designated as beta and gamma which are linked by disulphide bonds to form and symmetrical cross shaped structure

• Shows hypotensive effect

Octapamine

• Found in the salivary glands of Octapus vulgaris, O. macropus and Eledone moschata

• Produces cardiovascular adrenergic response

• As neurotransmitter in invertebrates

Octapamine

Saxitoxin (Mussel poison, Clam poison, Paralytic shellfish poison, STX)

• Obtained from the dinoflagellates, Gonyaulax catenella or G. tamarensis

• Exhibits hypotensive effect

Saxitoxin (Mussel poison, Clam poison, Paralytic shellfish poison, STX)

Autonomium chloride

• Obtained from Verongia fistularis

• Exerts both α and β adrenergic effects

• Also exhibits cholinergic action

• Shows CNS stimulant activity

Autonomium chloride

• Polypeptides obtained from marine sources (Sea anemones) includes a polypeptide with 147 aminoacids from Actinia equine exhibiting bradycardia, rapid hypotension and respiratory arrest

• Other polypeptides are obtained from Condylactis gigantean, Parasicyonis action stoloides exhibiting haemolytic and neurotoxic Action

Marine glycosdies – Holothurins and astrosaponins

Holothurins

• Obtained from the family, Holothuroidae and phylum Echinodermata possessing steroidal moiety resembling digitalis

Astrosaponins

• From fishes of family Asteroidae

Eledoisin

• Obtained from the posterior salivary glands of Eledone moschata

• Stimulates extravascular smooth muscle, lacrimal secretion

• Potent vasodilator, hypotensive agent

Hypotensive compounds

Spongosine

• Nucleoside and a methoxy derivative of adenosine

• Obtained from Caribbean sponge, Cryptotetheia crypta

• Exhibits various coronary vasodilation and negative inotropy

• Acts as hypotensive agent

• Reduces force and rate of contraction of heart

Spongosine

Doridosine

• Obtained from nudibranch Anisodoris nobilis

• Most potent hypotensive marine nucleoside

• Exerts hypothermic activity

Doridosine

Hypotensive peptides and other compounds

Aaptamine

• Obtained from Aaptos asptos

• Used as α adrenergic blocking agent

• Causes hypotension

Aaptamine

Hymenin

• Obtained from Hymeniacidon aldis

• Used as α adrenergic blocking agent

• Causes hypotension

Hymenin

Urotensins I and II

• Obtained from specific caudal neurosecretory system of Giltichthys miralilis and from Catostomus commersoni

• Exerts vasodilation and hence hypotension

Marine Antimicrobial agents

Chemical compound

Organism

Uses

Istamycins Streptomyces tenimariensis Effective against gram +ve and – ve organisms
Bromopyrones

Fimbrolides

Laurene

Ptilonia austrulasica

Delisea fimbriata

Laurencia

Have halogen in particular bromine, hence toxic
Holotoxin A, B, C

(Steroidal glycoside)

Sea cucumber, Stichopus
japonicas
Antifungal
Zonarol and isozonarol Dictyopteris zonaroides

(Brown algae)

Antimicrobial
Tetrabromoheptanone Bonnemaisonia hemifera (Red algae) Antimicrobial

 

Aeropolysnin Verongia aerophola (Sponge) Antimicrobial
Prepacifenol Laurencia pacifia, L.filiformis
(Red algae)
Antimicrobial
Thelphin Thelepsus setosul

(Annelida)

Antimicrobial
Eunicin Eucinia mammosa

(Gorgonian corals)

Antimicrobial
Acanthelin Acanthella acuta Against mycobacterium

Marine Antiinflammatory compounds

• A novel bi indoles was isolated from the marine cyanobacterium, Rivularia firma

• The major compound was (+)-7’-mtheoxy -2,3,5,5’ tetrabromo-3, 4’-bi-1H indole; Active against carrageenan & kaolin induced paw edema

Marine Anti inflammatory compounds

• Palaulol, a sesqueterpene from the sponge, Fascaplysinopsis species

Marine Antiinflammatory compounds

• A sesqueterpene furan form the coelenterate, Sinularia species

Marine Antiinflammatory compounds

Other anti-inflammatory compound includes

• Dendalone-3-hydroxybutyrate from the sponge, Phyllospongia dendyi

• Flustramine A and B from the Swedish marine moss Flustra foliaceae

• Tetradotoxin form the globe fish Spheroides rubripes

• 6-n-tridecyl salicylic acid from the brown algae Caulocystis cephalornithos

• Flexibilide from the soft coral, Sinularia flexibilis

• Monalide from the sponge Luffariella variabilis

Marine Antibiotic agents

The naturally occurring antibiotics includes

Okadaic acid (Halochondrine A)

• Obtained from Halichondria sps (Marine black sponge)

• First ionophoric polyether identified in marine organism

Okadaic acid (Halochondrine A)

Acanthifolicin

• Obtained from the sponge, Pandoras acanthifolium

• Possess antibacterial activity and cytotoxic activity

Acanthifolicin

The other antibiotic agents include

• 2,4 dibromo-6-(3,4,5  tribromo  pyrrole-2-yl)-phenol obtained from the Marine bacterium, Pseudomonas bromutilis

2,4 dibromo-6-(3,4,5  tribromo  pyrrole-2-yl)-phenol

• Cycloeudesmol obtained from the red algae Chondria oppsiticlada

Cycloeudesmol

• Variablin and ircinin obtained from the sponge Ircinia strobilina & I. oros

Variablin and ircinin

Variablin and ircinin

• 3,5 dibromo 4 hydroxy benzene-1 acetamide obtained form the sponge, Verongia archeri

3,5 dibromo 4 hydroxy benzene-1 acetamide

Cardiovascular antimicrobial antiinflammatory and antibiotic agents of marine origin Summary

• Compounds used in cardiovascular system – laminin, octapamine, saxitoxin, autonomium chloride, astrosaponins, eledoisin, spongosine, doridosine, aaptamine, hymenin, urotensins etc

• Antimicorbial compounds – Istamycins, Bromopyrones, Fimbrolides, Laurene, Holotoxin A, B, C (Steroidal glycoside), Zonarol and isozonarol, Tetrabromoheptanone, Aeropolysnin, Prepacifenol, Thelphin, Eunicin, Acanthelin

• Anti-inflammatory drugs include novel bi indoles, (+)-7’-mtheoxy – 2,3,5,5’ tetrabromo-3, 4’-bi-1H indole etc

• The various antibiotics compounds are okadaic acid, acanthifolicin, 2,4  dibromo-6-(3,4,5  tribromo pyrrole-2-yl)-phenol, Cycloeudesmol, Variablin and ircinin, 3,5 dibromo 4 hydroxy benzene-1 acetamide etc

                   Dietary Supplement and Nutraceuticals 

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