Biocatalysis of the Anticancer Sipholane Triterpenoids

 

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Abstract

The Red Sea sponge Callyspongia (= Siphonochalina) siphonella is a rich source of sipholane triterpenoids. Biocatalysis of the major sipholanes, sipholenol A (1) and sipholenone A (2), respectively, by Mucor ramannianus ATCC 9628 and Cunninghamella elegans ATCC 7929 afforded four new metabolites 3 - 6 along with sipholenol G and 28-hydroxysipholenol A. Major sipholanes along with their biocatalytic products were investigated for their antiproliferative activity against the highly malignant +SA mouse mammary epithelial cell line. Sipholenone A (2) was the most active sipholane inhibiting +SA cell proliferation with an IC₅₀ value of 20 - 30 μM. Sipholenone A, also, showed cytotoxicity against MCF-7 at a dose of 0.9 μM and antiangiogenic activity in the CAM (chorio-allantoic membrane) assay. This is the first report on anticancer activity of these triterpenoids.

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Prof. Dr. Khalid El Sayed

Department of Basic Pharmaceutical Sciences

College of Pharmacy

University of Louisiana at Monroe

700 University Avenue

Monroe

Louisiana 71209

USA

Phone: +1-318-342-1725

Fax: +1-318-342-1737

Email: elsayed@ulm.edu

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