Cardiovascular, Antimicrobial, Anti-inflammatory 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

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

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

• Exhibits hypotensive effect

Autonomium chloride

• Obtained from Verongia fistularis

• Exerts both α and β adrenergic effects

• Also exhibits cholinergic action

• Shows CNS stimulant activity

• 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

Doridosine

• Obtained from nudibranch Anisodoris nobilis

• Most potent hypotensive marine nucleoside

• Exerts hypothermic activity

Hypotensive peptides and other compounds

Aaptamine

• Obtained from Aaptos asptos

• Used as α adrenergic blocking agent

• Causes hypotension

Hymenin

• Obtained from Hymeniacidon aldis

• Used as α adrenergic blocking agent

• Causes hypotension

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

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

• Palaulol, a sesqueterpene from the sponge, Fascaplysinopsis species

• A sesqueterpene furan form the coelenterate, Sinularia species

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

Acanthifolicin

• Obtained from the sponge, Pandoras acanthifolium

• Possess antibacterial activity and cytotoxic activity

The other antibiotic agents include

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

• Cycloeudesmol obtained from the red algae Chondria oppsiticlada

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

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

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