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Cytotoxic quassinoids from Ailanthus altissima.
Yan Wang1, Wen-Jing Wang, Chang Su
1Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Jinan University, Guangzhou 510632, PR China.
Bioorganic & Medicinal Chemistry Letters
|January 8, 2013
Summary
Two novel quassinoids from Ailanthus altissima bark show potent cytotoxic effects against human hepatoma cells. Some compounds demonstrated significant activity against multidrug-resistant cancer cells.
Area of Science:
- Natural Products Chemistry
- Pharmacology
- Medicinal Chemistry
Background:
- Ailanthus altissima bark is a source of bioactive compounds.
- Quassinoids are a class of natural products with diverse biological activities.
- Hepatocellular carcinoma (HCC) remains a significant global health challenge.
Purpose of the Study:
- To isolate and characterize new quassinoids from Ailanthus altissima.
- To evaluate the in vitro cytotoxic potential of isolated quassinoids against human hepatoma cell lines.
- To investigate activity against multidrug-resistant cancer cells.
Main Methods:
- Extraction of Ailanthus altissima bark using 95% ethanol.
- Structure elucidation of new compounds using spectroscopic methods (UV, IR, HR-ESI-MS, 1D and 2D NMR).
- In vitro cytotoxicity assays against Hep3B, HepG2, and HepG2/ADM cell lines.
Main Results:
- Two new quassinoids, altissinol A (1) and B (7), were identified along with 12 known quassinoids.
- Compounds 1-7 exhibited potent cytotoxic activity against Hep3B and HepG2 human hepatoma cell lines.
- Compounds 2, 3, and 5 showed enhanced cytotoxicity against multidrug-resistant HepG2/ADM cells, being more sensitive than Doxorubicin (DOX).
Conclusions:
- Ailanthus altissima bark is a valuable source of cytotoxic quassinoids.
- Altissinol A and B represent novel additions to the quassinoid family.
- These findings suggest potential for developing new therapeutic agents for hepatocellular carcinoma, including drug-resistant cases.
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