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A new antimalarial quassinoid from Simaba orinocensis.
Ilias Muhammad1, Erdal Bedir, Shabana I Khan
1Departments of Pharmacognosy and Pharmacology, Research Institute of Pharmaceutical Sciences, School of Pharmacy, University of Mississippi, University, Mississippi 38677, USA. milias@olemiss.edu
Journal of Natural Products
|May 29, 2004
Summary
A novel quassinoid, orinocinolide, shows potent antimalarial activity comparable to simalikalactone D. While less toxic, orinocinolide demonstrated anticancer properties but lacked activity against Leishmania donovani.
Area of Science:
- Natural Products Chemistry
- Medicinal Chemistry
- Pharmacology
Background:
- The root bark of Simaba orinocensis is a source of bioactive quassinoids.
- Quassinoids have demonstrated potential as antimalarial and anticancer agents.
Purpose of the Study:
- To isolate and characterize new quassinoids from Simaba orinocensis.
- To evaluate the antimalarial, antiparasitic, and anticancer activities of the isolated compounds.
Main Methods:
- Isolation of compounds using chromatographic techniques.
- Structure elucidation using 1D and 2D NMR spectroscopy and chemical derivatization.
- In vitro bioassays to determine IC(50) values against Plasmodium falciparum, Leishmania donovani, and human cancer cell lines.
Main Results:
- Orinocinolide (1) was isolated along with simalikalactone D (2).
- Orinocinolide (1) exhibited potent antimalarial activity against Plasmodium falciparum, comparable to simalikalactone D.
- Compound 1 showed significantly lower toxicity to VERO and HL-60 cells compared to compound 2.
- Simalikalactone D (2) displayed potent activity against Leishmania donovani, whereas orinocinolide (1) was inactive.
- Both compounds inhibited human cancer cell growth, with compound 2 being more potent.
Conclusions:
- Orinocinolide is a promising new antimalarial quassinoid with a favorable toxicity profile.
- Simalikalactone D possesses broad-spectrum activity against malaria, leishmaniasis, and cancer.
- Further investigation into orinocinolide's therapeutic potential is warranted.