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Marine Drugs and Novel
medicinal agents from marine
sources
S Laxman
B.Pharma 4th
semester
TRINITY COLLEGE OF PHARMACEUTICAL SCIENCES.
PEDDAPALLI, TELANGANA STATE
What are
marine drugs?
□ Marine drugs: the drugs obtained from marine
organisms such as bacteria, virus, algae, fungi,
sponges etc.
Examples: shark & Cod-Liver Oils, agar-agar etc.
□ Marine Drugs are extensively used by Chinese and
Japanese people since ancient times.
□ In recent years significant number of novel
metabolites with potential applications have been
discovered from the marine organisms.
Why Marine
Sources?
□ The oceans are earth’s most bio diverse enviornment.Marine
sources have good biological and chemical diversity.
□ Genetic diversity eventually leads to chemical diversity which is a
source of promising new drugs.
□ Marine toxins were found to possess an extremely high potency
with regard to their pharmacological actions.
□ Relatively lower toxic side effects.
Cont...□ Due to the nature of highly harsh chemical and physical conditions in marine
environment , the organisms produce a variety of molecules with unique
structural features and exhibit various types of biological activities.
□ Trends in drug discovery from natural sources stresses on investigation of
the marine eco-system to explore various complex entities.
□ These complex entities are the sources of new leads for treatment of many
diseases such as cancer, aids, inflammatory conditions & a large variety of
viral, bacterial& fungal diseases.
Classification of Marine Drugs
The vast amounts of newer and potent drug molecules derived from the
wide spectrum of marine organisms across the world has been classified
based on their nature of pharmacological actions as shown below:
•Anti-bacterial agents
•Anti-Viral agents
•Antifungal agents
•Anticancer agents
Contd...
•Cardio vascular Active Drugs
•Marine Toxins
•Anti-Microbial Substances
•Anti-inflammatory agents
•Marine Toxins
•miscellaneous pharmacologically active substances
Antibacterial Agents
Compound Biological
name Source
Chemical Structure Uses
Acanthellin-1 Acanthella Active against
o mycobactenumacuta
(sponge)
• • •■ I
L.Filiformischondriol Antimicrobial
(red algae) agent.
PrepadfenoJ Laurenciajohns AntimicrobialBr
tonil (red agent.Cl
algae)
n.
Antiviral Agents
Compound Biological Chemical structure Uses
name source
Avarol Disidea avara Used in the
u(sponge) treatment of
AIDS.
Disidea avara Its also used inAvarone
(sponge) the treatment of
AIDS.
It have the ability
to cross B.B.B
Eudistomin-A Eudistoma It inhibit
immunodeficiencyoivaceu m
virus.
Antifungal Agents
Compoun Biological Chemical Structure Uses
d name source
Zonarol Dictyopteris
zonoroid (brown
algae)
It has fungidal
property.
Isozonorol
Dictyopteris
zonoroid (brown
algae)
' dp
dp
w
i^P _
Antifungal agent.
Thelphin
Thelepus
setosus
(annelida)
JZT}) Antimicrobial
agent.
Antimicrobial agents
Compound Biological Chemical structure Uses
name source
Laurinterol Laurenciajoh
nstonii (red algae)
Active
antimicrobial
agent.
Aeroplysinin-1 Verongia
Aerophoba
(sponge)
Br
C3
Antimicrobial
agent.
Of
Bromopyrones Ptilonia
Australasica
They are toxic as
well as
Antimicrobial
agent.
Anticancer Agents
Cardiovascular Agents
Compound Biological Chemical
structure
Uses
name source
Eldoisin Eledonemoschata Stimulate extra
(Cephalopod) vascular smooth
muscle.
ShowsOctapamine Octopus vulgaris
Adrenergic
responses.
Act as
Neurotransmitter
Marine ToxinsCompound Biological source Chemical structure Uses
name
Saxitoxin Gonyaulax Hypotensive
effectcalenella NH
(dinoflag ell ate)
NHHO
NI
NH
Holothurin-A Helixpomatia Haemolyti
(sea cucumber) activity
'S
~TJ
~ Antifungal
X activity
-xpc
Aplysins Aplysiadepilans Toxical agent
(sea hare)
Anti BioticsCompound Biological Chemical structure Uses
name source
Cephalosporin
-c
Istamycin-A
Istamycin-B
Cephalosporium
acrimonium
(fungus)
Streptomyces
tenjimarien sis
Streptomyces
tenjimarien sis
Antibiotic agent.
NH2 | OH NH2 jn-viti
is obs
° o • - 1 again!
NH?
J Gr( + )
^ISI"
H
^h
2 In-vitro activity
observed
against Gr(-) and
bacteria.
•: 1
r M
In-vitro activity is
observed aganst
Gr(-) and Gr( + )
bacteria.
Anti Inflammatory
Method to Study
Marine Products
❖ Collection & field identification of the marine
organisms.
❖ Initial Extraction of the organism
❖ Biological assay of the extract.
❖ Partitioning to confirm and enrich bio-activity.
❖ Determination of the polarity of natural
Challenges
Market challenges
Identification of market need, ie, which
bioactivity is needed
Identification of the best marine
organism for specific bioactives
(supported by predicted necessary
volulmes and production schemes for the
chosen market)
Industry-Academia partnerships
Identification of competition targetting
and also of new targets
Intelectual property status
Identification of price tag per unit
(supported by the choosen market)
Identification of production
technologies that support the
possible price level
Desired formulation and route of
administration
Regulatory requirements
Identification of the tests that need to be
performed for approval
Identification of the volume needec for the
final manufacturing and supply
Bioprospecting
MNPs collections for
bioactivity discovery
HTS of MNPs collections
against potential targets
HIT identification
Hit validation with
dereplication follow-up and
MoA assays
]
LEAD identification and
optimization
Pre-clinical studies
Clinical trials
r Biodiversity
Challenges
□ Sampling approaches
□ Taxonomic expertise
□ Biodiversity access/
Sustainability
□ HTS screening crude
versus fractionated extracts coupled
with CC
□ Genome mining and
combinatorial biosynthesis
Market
Supply and Technical
Challenges
Variability/ Identification of MNP
producer
Sustainable supply:
Mariculture and aquaculture
Hemisynthesis or total synthesis
Fermentation of microorganisms
Metagenomics
Re-discovery of the unknown
Sophistication of modern
spectroscopic technics
Virtual Screening
Toxicity and efficacy studies
References:□ https://www.mdpi.com/1660-3397/12/2/1066
□ https://owlcation.com/stem/Marine-Sources-for-Anticancer-Drugs
□ https://www.sciencedaily.com/releases/2018/06/180619123013.htm
□ http://www-actus.univ-ubs.fr/fr/index/articles-chroniques/service-
recherche/marine-drugs.html
□ http://theconversation.com/marine-compound-first-new-natural-
antibiotic-in-decades-16433
□
Thank You…Thank You…

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Laxman marine drugs

  • 1. Marine Drugs and Novel medicinal agents from marine sources S Laxman B.Pharma 4th semester TRINITY COLLEGE OF PHARMACEUTICAL SCIENCES. PEDDAPALLI, TELANGANA STATE
  • 2. What are marine drugs? □ Marine drugs: the drugs obtained from marine organisms such as bacteria, virus, algae, fungi, sponges etc. Examples: shark & Cod-Liver Oils, agar-agar etc. □ Marine Drugs are extensively used by Chinese and Japanese people since ancient times. □ In recent years significant number of novel metabolites with potential applications have been discovered from the marine organisms.
  • 3. Why Marine Sources? □ The oceans are earth’s most bio diverse enviornment.Marine sources have good biological and chemical diversity. □ Genetic diversity eventually leads to chemical diversity which is a source of promising new drugs. □ Marine toxins were found to possess an extremely high potency with regard to their pharmacological actions. □ Relatively lower toxic side effects.
  • 4. Cont...□ Due to the nature of highly harsh chemical and physical conditions in marine environment , the organisms produce a variety of molecules with unique structural features and exhibit various types of biological activities. □ Trends in drug discovery from natural sources stresses on investigation of the marine eco-system to explore various complex entities. □ These complex entities are the sources of new leads for treatment of many diseases such as cancer, aids, inflammatory conditions & a large variety of viral, bacterial& fungal diseases.
  • 5. Classification of Marine Drugs The vast amounts of newer and potent drug molecules derived from the wide spectrum of marine organisms across the world has been classified based on their nature of pharmacological actions as shown below: •Anti-bacterial agents •Anti-Viral agents •Antifungal agents •Anticancer agents
  • 6. Contd... •Cardio vascular Active Drugs •Marine Toxins •Anti-Microbial Substances •Anti-inflammatory agents •Marine Toxins •miscellaneous pharmacologically active substances
  • 7. Antibacterial Agents Compound Biological name Source Chemical Structure Uses Acanthellin-1 Acanthella Active against o mycobactenumacuta (sponge) • • •■ I L.Filiformischondriol Antimicrobial (red algae) agent. PrepadfenoJ Laurenciajohns AntimicrobialBr tonil (red agent.Cl algae) n.
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  • 9. Antiviral Agents Compound Biological Chemical structure Uses name source Avarol Disidea avara Used in the u(sponge) treatment of AIDS. Disidea avara Its also used inAvarone (sponge) the treatment of AIDS. It have the ability to cross B.B.B Eudistomin-A Eudistoma It inhibit immunodeficiencyoivaceu m virus.
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  • 11. Antifungal Agents Compoun Biological Chemical Structure Uses d name source Zonarol Dictyopteris zonoroid (brown algae) It has fungidal property. Isozonorol Dictyopteris zonoroid (brown algae) ' dp dp w i^P _ Antifungal agent. Thelphin Thelepus setosus (annelida) JZT}) Antimicrobial agent.
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  • 13. Antimicrobial agents Compound Biological Chemical structure Uses name source Laurinterol Laurenciajoh nstonii (red algae) Active antimicrobial agent. Aeroplysinin-1 Verongia Aerophoba (sponge) Br C3 Antimicrobial agent. Of Bromopyrones Ptilonia Australasica They are toxic as well as Antimicrobial agent.
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  • 17. Cardiovascular Agents Compound Biological Chemical structure Uses name source Eldoisin Eledonemoschata Stimulate extra (Cephalopod) vascular smooth muscle. ShowsOctapamine Octopus vulgaris Adrenergic responses. Act as Neurotransmitter
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  • 19. Marine ToxinsCompound Biological source Chemical structure Uses name Saxitoxin Gonyaulax Hypotensive effectcalenella NH (dinoflag ell ate) NHHO NI NH Holothurin-A Helixpomatia Haemolyti (sea cucumber) activity 'S ~TJ ~ Antifungal X activity -xpc Aplysins Aplysiadepilans Toxical agent (sea hare)
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  • 21. Anti BioticsCompound Biological Chemical structure Uses name source Cephalosporin -c Istamycin-A Istamycin-B Cephalosporium acrimonium (fungus) Streptomyces tenjimarien sis Streptomyces tenjimarien sis Antibiotic agent. NH2 | OH NH2 jn-viti is obs ° o • - 1 again! NH? J Gr( + ) ^ISI" H ^h 2 In-vitro activity observed against Gr(-) and bacteria. •: 1 r M In-vitro activity is observed aganst Gr(-) and Gr( + ) bacteria.
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  • 25. Method to Study Marine Products ❖ Collection & field identification of the marine organisms. ❖ Initial Extraction of the organism ❖ Biological assay of the extract. ❖ Partitioning to confirm and enrich bio-activity. ❖ Determination of the polarity of natural
  • 26. Challenges Market challenges Identification of market need, ie, which bioactivity is needed Identification of the best marine organism for specific bioactives (supported by predicted necessary volulmes and production schemes for the chosen market) Industry-Academia partnerships Identification of competition targetting and also of new targets Intelectual property status Identification of price tag per unit (supported by the choosen market) Identification of production technologies that support the possible price level Desired formulation and route of administration Regulatory requirements Identification of the tests that need to be performed for approval Identification of the volume needec for the final manufacturing and supply Bioprospecting MNPs collections for bioactivity discovery HTS of MNPs collections against potential targets HIT identification Hit validation with dereplication follow-up and MoA assays ] LEAD identification and optimization Pre-clinical studies Clinical trials r Biodiversity Challenges □ Sampling approaches □ Taxonomic expertise □ Biodiversity access/ Sustainability □ HTS screening crude versus fractionated extracts coupled with CC □ Genome mining and combinatorial biosynthesis Market Supply and Technical Challenges Variability/ Identification of MNP producer Sustainable supply: Mariculture and aquaculture Hemisynthesis or total synthesis Fermentation of microorganisms Metagenomics Re-discovery of the unknown Sophistication of modern spectroscopic technics Virtual Screening Toxicity and efficacy studies
  • 27. References:□ https://www.mdpi.com/1660-3397/12/2/1066 □ https://owlcation.com/stem/Marine-Sources-for-Anticancer-Drugs □ https://www.sciencedaily.com/releases/2018/06/180619123013.htm □ http://www-actus.univ-ubs.fr/fr/index/articles-chroniques/service- recherche/marine-drugs.html □ http://theconversation.com/marine-compound-first-new-natural- antibiotic-in-decades-16433 □