MARINE

Marine drugs Pharmacognosy

PHARMACOGNOSY
BY:
Submitted by:
Sweaty Salone KINJAN MEHTA.
M.Pharm 1st sem ( pharmacognosy and phytochemistry)
SMT.Hamdard
Jamia N.M. PADALIYA PHARMACY COLLEGE.
INTRODUCTION
In the domain of drugs and medicine which are either
obtain or synthesized by terrestrial organisms, our
earth which is covered 70% with oceans and seas, rich
in fauna and flora, it has not been properly explored.
About 5 lakh species of marine organisms have been
reported from the oceans and sea from the various part
of the world. Some of these organisms are
antimicrobial, antiviral, antibiotic, anticancer, anti-
inflammatory, enzyme inhibitors, neurophysiological,
prostaglandins and cardiovascular agents.
CLASSIFICATION
CLASS EXAMPLE
Anleurins, Laminine, Eptaterin,
Cardiovascular Saxitoxin, Spongosine, Eledosin, Atx-
active compounds II, Autonomium.

Cytotoxic Arc-C, Crassin acetate simularin

compounds.

Antimicrobial Holotoxin ABC, Thelpin, eunicin

compounds. acanhelin.

Antibiotic Cycloeudesmol, viriabillin, Iricnin-

compounds. 1.
CONTD..
CLASS EXAMPLE

Crrageenam,
Anticoagulant. laminarin.

PEG1, PEG2, Soft

Prostaglandin. corals and red
algae.

Anti- tubercular Axithonitrile,

agents. aerathionie,
calofianin.
CONTD…
CLASS EXAMPLES

Anti-inflammatory/ Manolide,
Antispasmodic Tetradotoxin.
compounds.

Ciuatoxin, Palytoxin,
Marine Toxins. Saxitoxin,
Brevetoxin.

Miscellaneous Kalinin acid, domoic

compounds. acid, aplysinopsin.
Cardiovascular Active compounds.
1) ANTHOPLEURINS: This are group of peptides
obtained from coelenterates compound i.e. Antropleura
xanthogrammica giving type A and B, and A.
elegantissima giving type C.
AP-A shows strong isotropic effect on NA+ and K+
ATPase, pump heart rate and blood pressure, and in dogs
give cardio tonic activity which is 35% more potent than
digoxin.
2)Eptatretin : found in Hogfish i.e. Eptatretus stoutill.
It is potent cardio stimulant with direct stimulant action
on mammalian myocardium.
CONTD.. CAC.
3) LAMININE: It is an
marine algae, Laminaria
angustata gives this
basic amino compd.
Which gives hypotensive
effect.
4) SAXITOXIN: it shows
hypotensive effect and is
found in butter clam i.e
Saxidomus giganteus
and California mussel.
Contd.. CAC.
5) ATX-II: this is one of the polypeptides found in sea
anemones. It shows potent and dose dependent cardio
tonic response.
6) AUTONOMIUM: this compound has isosteric
structure of adrenaline and ach. And is found in
Verongia fistularis. This compound shows both α
and β adrenergic effects and also exerts cholinergic
activity.
Due to this it may be useful in regulating the
behaviour of the heart.
CONTD.. CAC.
7) SPONGOSINE: chemically it is a
nucleoside9methoxy derivative of adenosine). It is
found in extract of Caribbean sponge Crypotethia
crypta. It reduces both the rate and contraction of the
heart.
8) ELEDOSIN: it is powerful hypotensive compound
obtain from posterior salivary glands of cephalopod
Eledone moschata. It shows strong vasodilator
effects.
CYTOTOXIC (ANTICANCER) DRUGS.
1) ARA-C: it is 1-α-D- arabinofuranosyl cytosine or
cytosine arabinoside.
It is obtained as a synthetic compound based on the
knowledge of naturally occurring moieties present on
Carrabin sponge, i.e. Spongosine and
Spongouridine.
It is used in the treatment of acute myelogenous
leukemia and human acute leukaemia for therapeutic
purposes. It is active against Erlich carcinoma,
sarcoma-180, L-1210 leukaemia in mice.
Contd. Anticancer..
2)CRASSIN ACETATE: it is a member of cyclic diterpenes
obtain from carrabian gorgonian, Pseudoplexaura
porosa which is cytotoxic to human leukeamia.
Other constituents from cembranoid is Asperidol- a non
lactonic cembranoid from gorgonian coral.
3) BEYOSTATIN: Antileukeamic, it causes inactivation of
protein kinase by arachnoids pathway.
4) DOLASTSTIN: obtain from seahorse Dolabella
auriculata. Varieties are: Dolastatin-10, Dolastastin –H
Isodolastatin—H.
CONTD… ANTICANCER.
ELEATHROMBIN: it is toxic to cancer cell presence
of TAXOL- a sesquiterpene oil.
Alpidium species: contains which is cytotoxic to
leukaemia and mammary carcinoma.
ANTI- MICROBIAL COMPOUNDS
A large no. of antimicrobial compunds have been
detected from the marine organisms like sea
cucumber, marine algae, sponges, sea hare, gorgonian
corals and red algae.
Other antibiotics that are obtain from marine sources
are Cephalosporin's, Istamycin, Zonarol and
isozonarol and tetra bromo heptane.
The organisms and their antimicrobial principles are
listed here.
Anti microbial principles from marine
source.
Marine organisms Antimicrobial compounds

Sea cucumber, Stichopus japonicus. Holotoxin A, B, C (steroidal glycoside).

Zonarol and isozonarol (antifungal) &

Brown algae, Dictyopteris zonaroides
Tetrabromoheptane.

4 isomers of polyhalo 3 butene-2-one

Red algae, Bonnemaisonia hemifera.
and 7 isomers of polyhaloacetones.

Red algae. Asparagopsis taxiformis Aeroplysinin-1 (+)

Antimicrobial principles from Marine
sources.
Marine organisms Antimicrobial compounds
Sponge, Verongia aerophoba. Aeroplysinin-1 (-)

Sponge, Agelas, Oroides. 2-cyno-4,5- dibrmopyrrole.

Red algae, Laurencia pacifica and L. filformis. Prepacifenol.

Annelida, Thelepsus setosus. Thelpin.

Sea hare, Aplysia californica. Debromolaurenterol.

Gorgonian corals, Eunica mammosa. Eunicin.

Acanthella acuta Acanthelin-1.

Antimicrobial compounds
Cephalosporin (1950) obtain from marine fungus
Cephalosporium acromonium.
Cephalosporin C is a modification of original
cephalosporin and is widely used as an antibiotic.
It is generally useful where penicillin and ampicillin is
not effective.
Istamycin: it is fermentation source of marine
microorg. Streptomyceus lengimariensis.
It is in-vitro bacteria used those which are resistance
to amino-glycoside antibiotic.
ANTIBIOTIC COMPOUNDS.
Organisms Antibiotic substance
2,4-dibromo-6-(3,4,5
Marine bacterium, trobromopyrrole-2-yl) phenol
Pseudomonas bromutilis.

Red algae, Chondria Cylcloeudesmol.

oppositiclada.

Sponge, Ircinia strobilina Variabillin, Ircinin-1.

and Ircinia oros.

Sponge, Verongia 3,5-dibromo-4-hydroxy

benzene-1 acetamide.
archery
ANTI-INFLAMMATORY AND
ANTISPASMODIC AGENTS
MANNOLIDE: A NSAID compound, has been obtain
from the sponge Luffariella variabilis. It act by direct
inactivtion of phospholipase A2. it is also analgesic.
DENDALONE 3 HYDROXY BUTYRATE: obtain from a
sponge, phyllospongia dendyii.
FLUSTRAMINE A &B: from Flustra foliaceae. A
Swedish marine moss.
TETRADOXIN: obtain from liver and ovary of puffer
fishes is a strong antispamodic.
ANTI- VIRAL, ANTI- HIV AGENTS.
Widely used are Laminalam species which is obtain
from brown algae.
It has anti viral antihiv coagulant activity.
ARA-A: It is obtain from sponge Tetya crypta.
Avarone/ Avaronone: it is obtain from sponge
Disidea ovara it is useful against HIV and is the only
drug cross BBB
DIDEMNIS: These are depsi peptides from Tunicate,
Trididenum species.
Discovery and development of marine drugs
New Drug Development Stages
Natural/Marine product discovery
Chemically modified drug
Discovery unknown structure of compounds
Synthesis, recombinant DNA
Source of leads for product development
Synthetic compounds based on existing compounds
Chemical improvement on drug molecule
Drug candidates
Pre-clinical and clinical trials
Approval process
Marketing new drug products
Marine Drug Delivery
 Bioencapsulation Inhalation

Marine
Sponges Drug Transdermal
Delivery

Oral Transmucosal

Topical
THANK YOU