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Drugs that Destabilize Microtubules

Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...
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An Efficient and Rapid HPLC-QQQ-MS Method for the Quantitation of Tropane Alkaloids in Medicinal Plants
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Bisbenzylisoquinoline alkaloids from Cocculus pendulus.

Atta-ur-Rahman1, Atia-tul-Wahab, S Zia Sultani

  • 1H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan. hej@cyber.net.pk

Natural Product Research
|May 30, 2009
PubMed
Summary

Researchers isolated new and known bisbenzylisoquinoline alkaloids from Cocculus pendulus. These compounds demonstrated significant inhibitory effects on acetylcholinesterase and butyrylcholinesterase enzymes.

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Area of Science:

  • Natural Product Chemistry
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Cocculus pendulus is a plant source of bioactive alkaloids.
  • Bisbenzylisoquinoline alkaloids are known for diverse pharmacological activities.
  • Cholinesterase inhibition is a key target for treating neurodegenerative diseases.

Purpose of the Study:

  • To isolate and characterize alkaloids from Cocculus pendulus.
  • To evaluate the cholinesterase inhibitory potential of isolated compounds.

Main Methods:

  • Phytochemical investigation of Cocculus pendulus extract.
  • Isolation of compounds using chromatographic techniques.
  • Structure elucidation via spectroscopic methods (NMR, MS).
  • In vitro assays for acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibition.

Main Results:

  • A new bisbenzylisoquinoline alkaloid, 1,2-dihydrokurramine (1), was identified.
  • Four known bisbenzylisoquinoline alkaloids (2-5) and one morphinan alkaloid (6) were isolated.
  • All isolated bisbenzylisoquinoline alkaloids exhibited inhibitory activity against AChE and BuChE.

Conclusions:

  • Cocculus pendulus is a valuable source of bisbenzylisoquinoline alkaloids.
  • The identified bisbenzylisoquinoline alkaloids possess significant cholinesterase inhibitory properties.
  • These findings suggest potential therapeutic applications for neurodegenerative disorders.