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BRYOSTATIN & KAHALADIDE
MARINE BIODIVERSITY – ANTICANCER
DRUG DEVELOPMENT
• Various active anticancer agents are derived from
plants and terrestrial microbes.
• The oceans cover about 70% of the earth’s
surface, and the marine environment includes
tremendous biodiversity.
• The isolation of C-nucleosides from the Caribbean
sponge, Cryptotheca crypta, four decades
ago, provided the basis for the synthesis of
cytarabine, the first marine derived anticancer agent
to be developed for clinical use.
OCEANS – A HUB FOR BIODIVERSITY
STATUS OF MARINE RESEARCH
DRUG-LIKE MOLECULES IN PIPELINE
BRYOSTATIN
Bryostatin1 is currently in Oncology Clinical
Phase II
• Bryostatin 1 is a macro cyclic natural lactone isolated
from the marine bryozoan , Bugula neritina .
• It modulates the activity of protein kinase C
(PKC), lacks tumor-promoting activity and shows
differentiation inducing effects in various in vitro and
in vivo models.
• It also has immunomodulatory properties, including
the induction of cytokine release and expansion of
tumor specific lymphocyte populations.
CHEMICAL STRUCTURE
KAHALADIDE F
Kahalalide F is currently in Oncology
Clinical Phase II
• Kahalalide F (KF) is a cyclic peptide derived
from the Hawaiian herbivorous marine species
of mollusc , Elysia rufescens.
• Its diet is the green alga Bryopsis sp.
• It shows antitumor activities both on
transformed cell lines and on tumor
specimens derived from a variety of solid
human tumors.
• The molecular basis of the tumoricidal activity
of KF are not fully established.
The permeabilization of the
plasma membrane leading to
oncosis.
Alterations in lysosome
morphology.
Inhibition of the ErbB3 signaling
pathway.
CHEMICAL STRUCTURE
REFERENCES
• Gilberto Schwartsmann, Adriana Brondani da
Rocha, Roberto GS Berlinck and Jose Jimeno Marine
organisms as a source of new anticancer agents, THE
LANCET Oncology Vol 2 April 2001.
• Dr. Fernando de la Calle Marine Genetic Resources: A
Source of New Drugs, Biodiversity and Genetic Resources
of the Deep Sea ITLOS, Hamburg. Sep, 29th 2007.
• Luis J. Cruz, Juan R. Luque-Ortega, Luis Rivas and
Fernando Albericio Kahalalide F, an Antitumor
Depsipeptide in Clinical Trials, and Its Analogues as
Effective Antileishmanial agents, Molecular
pharmaceutics, Revised Manuscript Received March
7, 2009; Accepted March 24, 2009.
”In one drop of water are found all
the
secrets of the oceans”

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Anti cancerous drug from marine ecosystem

  • 2. MARINE BIODIVERSITY – ANTICANCER DRUG DEVELOPMENT • Various active anticancer agents are derived from plants and terrestrial microbes. • The oceans cover about 70% of the earth’s surface, and the marine environment includes tremendous biodiversity. • The isolation of C-nucleosides from the Caribbean sponge, Cryptotheca crypta, four decades ago, provided the basis for the synthesis of cytarabine, the first marine derived anticancer agent to be developed for clinical use.
  • 3. OCEANS – A HUB FOR BIODIVERSITY
  • 4. STATUS OF MARINE RESEARCH
  • 6. BRYOSTATIN Bryostatin1 is currently in Oncology Clinical Phase II
  • 7. • Bryostatin 1 is a macro cyclic natural lactone isolated from the marine bryozoan , Bugula neritina . • It modulates the activity of protein kinase C (PKC), lacks tumor-promoting activity and shows differentiation inducing effects in various in vitro and in vivo models. • It also has immunomodulatory properties, including the induction of cytokine release and expansion of tumor specific lymphocyte populations.
  • 9. KAHALADIDE F Kahalalide F is currently in Oncology Clinical Phase II
  • 10. • Kahalalide F (KF) is a cyclic peptide derived from the Hawaiian herbivorous marine species of mollusc , Elysia rufescens. • Its diet is the green alga Bryopsis sp. • It shows antitumor activities both on transformed cell lines and on tumor specimens derived from a variety of solid human tumors.
  • 11. • The molecular basis of the tumoricidal activity of KF are not fully established. The permeabilization of the plasma membrane leading to oncosis. Alterations in lysosome morphology. Inhibition of the ErbB3 signaling pathway.
  • 13. REFERENCES • Gilberto Schwartsmann, Adriana Brondani da Rocha, Roberto GS Berlinck and Jose Jimeno Marine organisms as a source of new anticancer agents, THE LANCET Oncology Vol 2 April 2001. • Dr. Fernando de la Calle Marine Genetic Resources: A Source of New Drugs, Biodiversity and Genetic Resources of the Deep Sea ITLOS, Hamburg. Sep, 29th 2007. • Luis J. Cruz, Juan R. Luque-Ortega, Luis Rivas and Fernando Albericio Kahalalide F, an Antitumor Depsipeptide in Clinical Trials, and Its Analogues as Effective Antileishmanial agents, Molecular pharmaceutics, Revised Manuscript Received March 7, 2009; Accepted March 24, 2009.
  • 14. ”In one drop of water are found all the secrets of the oceans”