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Dr. R. P. Rajesh,Ph.D,
Scientist C,
Molecular & Nanomedical Sciences,
Sathyabama Institute of Science
and Technology, Chennai-119
Ph: 8072968170
+919994189582
Marine invertebrates
•Marine invertebrates like sponges, molluscs, ascidians, polychaete worms, etc.
are rich sources of novel compounds with potential pharmacological and
biotechnological applications.
•Many invertebrates are sessile with no physical defense mechanisms. So, their
survival depends solely on the production of bioactive secondary metabolites,
which attracted the researchers very much as a potential source of new
medicaments.
•The laurinterol acetate and laurinterol isolated from the sea hare Aplysia
kurodai were also reported from the red alga Laurencia intermedia which shows
the sea hare accumulate these metabolites through ingestion of red alga.
•The bryostatins are macrocyclic lactones isolated from the marine bryozoan
Bugula neritina (Bugulidae).
•Bryostatin 1, one of the most abundant and best studied compounds of this
series, was originally described on the basis of inhibition of growth in murine
P388 lymphocytic leukemia cells at subnanomolar concentrations.
•Kahalaide F, a depsipeptide from the marine mollusc Elysia rufescens found in
Hawaii, is an anticancer agent
Ascidians
•Ascidians are prolific producers of bioactive substances and are a
notable source of nitrogen-bearing secondary metabolites with a wide
range of biological activities
•Didemnin-B from the Caribbean tunicate Trididemnum solidum was the
first marine compound to enter human cancer clinical trial as a purified
natural product
•Two unusual trithiocane derivatives, exhibiting mild antibacterial
activity as well as toxicity towards brine shrimp, were isolated from the
ascidian Perophora viridis collected from North Carolina
•Ecteinascidin, isolated from Ecteinascidia turbinata showed potent
activity in vivo against a variety of mouse tumour cells
•Eudistomins from Eudistoma species exhibited potent antiviral activity
in vitro
•Sebastianines A and B, biologically active pyridoacridine metabolites,
which show cytotoxic activities towards colon cancer cells, were
isolated from a Brazilian ascidian Cystodytes dellechiajei
Few compounds from Ascidian in clinical trials and market
Condition Compound Ascidian Status Origin
Cancer Aplidine Aplidium albicans In Clinical
Trials
Mediterranean
Antiviral Didemnin B Trididemnum
solidum
Withdrawn due
to toxicity
Caribbean
Cancer Dehydrodidemnin B Aplidium albicans In Clinical
Trials
Mediterranean
Cancer Ecteinascidin- 743 Ecteinascidia
turbinata
Market in the
name YondelisR
Caribbean
HIV Cyclodidemniserino
l trisulfate
Didemnum
guttatum
In Clinical
Trials
Palau
HIV Lamellarin a 20
sulfate
Didemnum
obscurum
In Clinical
Trials
Australia
EXTRACTION OF ASCIDIANS
ASCIDIAN
DRIED POWDER
SOLVANT EXTRACTION
ROTARY VACUM EVAPORATOR
CONCENTRATED EXTRACT
EVALUATION OF BIOLOGICAL ACTIVITY
MICE BIOASSAY
ZEBRA FISH BIOASSAY
HEMOLYTIC BIOASSAY
ANTIBACTERIAL ASSAY
ANTICOUGULANT ASSAY
CYTOTOXIC ASSAY
EXTRACT
HR- MS MS
NMR
X-Ray
STRUCTURAL CHARACTERISATION
STRUCTURE
DRUG DEVELOPMENT
PRECLINICAL CLINICAL DRUG
NATURAL PRODUCT FROM ASCIDIANS

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NATURAL PRODUCT FROM ASCIDIANS

  • 1. Dr. R. P. Rajesh,Ph.D, Scientist C, Molecular & Nanomedical Sciences, Sathyabama Institute of Science and Technology, Chennai-119 Ph: 8072968170 +919994189582
  • 2. Marine invertebrates •Marine invertebrates like sponges, molluscs, ascidians, polychaete worms, etc. are rich sources of novel compounds with potential pharmacological and biotechnological applications. •Many invertebrates are sessile with no physical defense mechanisms. So, their survival depends solely on the production of bioactive secondary metabolites, which attracted the researchers very much as a potential source of new medicaments. •The laurinterol acetate and laurinterol isolated from the sea hare Aplysia kurodai were also reported from the red alga Laurencia intermedia which shows the sea hare accumulate these metabolites through ingestion of red alga. •The bryostatins are macrocyclic lactones isolated from the marine bryozoan Bugula neritina (Bugulidae). •Bryostatin 1, one of the most abundant and best studied compounds of this series, was originally described on the basis of inhibition of growth in murine P388 lymphocytic leukemia cells at subnanomolar concentrations. •Kahalaide F, a depsipeptide from the marine mollusc Elysia rufescens found in Hawaii, is an anticancer agent
  • 3. Ascidians •Ascidians are prolific producers of bioactive substances and are a notable source of nitrogen-bearing secondary metabolites with a wide range of biological activities •Didemnin-B from the Caribbean tunicate Trididemnum solidum was the first marine compound to enter human cancer clinical trial as a purified natural product •Two unusual trithiocane derivatives, exhibiting mild antibacterial activity as well as toxicity towards brine shrimp, were isolated from the ascidian Perophora viridis collected from North Carolina •Ecteinascidin, isolated from Ecteinascidia turbinata showed potent activity in vivo against a variety of mouse tumour cells •Eudistomins from Eudistoma species exhibited potent antiviral activity in vitro •Sebastianines A and B, biologically active pyridoacridine metabolites, which show cytotoxic activities towards colon cancer cells, were isolated from a Brazilian ascidian Cystodytes dellechiajei
  • 4. Few compounds from Ascidian in clinical trials and market Condition Compound Ascidian Status Origin Cancer Aplidine Aplidium albicans In Clinical Trials Mediterranean Antiviral Didemnin B Trididemnum solidum Withdrawn due to toxicity Caribbean Cancer Dehydrodidemnin B Aplidium albicans In Clinical Trials Mediterranean Cancer Ecteinascidin- 743 Ecteinascidia turbinata Market in the name YondelisR Caribbean HIV Cyclodidemniserino l trisulfate Didemnum guttatum In Clinical Trials Palau HIV Lamellarin a 20 sulfate Didemnum obscurum In Clinical Trials Australia
  • 5. EXTRACTION OF ASCIDIANS ASCIDIAN DRIED POWDER SOLVANT EXTRACTION ROTARY VACUM EVAPORATOR CONCENTRATED EXTRACT
  • 6. EVALUATION OF BIOLOGICAL ACTIVITY MICE BIOASSAY ZEBRA FISH BIOASSAY HEMOLYTIC BIOASSAY ANTIBACTERIAL ASSAY ANTICOUGULANT ASSAY CYTOTOXIC ASSAY EXTRACT
  • 7. HR- MS MS NMR X-Ray STRUCTURAL CHARACTERISATION STRUCTURE