Title

Interference by Naturally Occurring Fatty Acids in A Noncellular Enzyme-Based Aromatase Bioassay

Document Type

Article

Publication Date

4-1-2006

Publication Title

Journal of Natural Products

Abstract

Natural product drug discovery efforts frequently utilize noncellular screening assays. Fatty acids are commonly found in natural product extracts, and some have been shown to interfere with noncellular assays. Several pure fatty acids were tested using a noncellular aromatase assay, with the unsaturated analogues showing strong inhibitory activity, while the saturated analogues were inactive. Unsaturated fatty acids were further tested against SK-BR-3 hormone-independent human breast cancer cells that overexpress aromatase and were found to be inactive. In natural product screening efforts, especially using plant seeds, it is recommended that extracts active in noncellular bioassays should be dereplicated for the presence of fatty acids prior to bioassay-guided fractionation.

Comments

This research was supported by a University Fellowship from the University of Illinois at Chicago (to M.J.B.), NIH grant R01 CA73698 (P.I., R.W.B.), The Ohio State University Comprehensive Cancer Center (OSUCCC) Breast Cancer Research Fund (to R.W.B.), and the OSUCCC Chemoprevention Program (to A.D.K.).

DOI

10.1021/np050513p

Volume

69

Issue

4