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. 2008 Sep;43(9):1865-77.
doi: 10.1016/j.ejmech.2007.11.021. Epub 2007 Dec 7.

Evaluation of Ursolic Acid Isolated From Ilex Paraguariensis and Derivatives on Aromatase Inhibition

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Evaluation of Ursolic Acid Isolated From Ilex Paraguariensis and Derivatives on Aromatase Inhibition

Simone C B Gnoatto et al. Eur J Med Chem. .

Abstract

The inhibitory potency of ursolic acid extracted from Ilex paraguariensis, a plant used in South American population for a tea preparation known as maté, and its derivatives to inhibit aromatase activity was assessed and compared to a phytoestrogen apigenin and a steroidal aromatase inhibitor 4-hyroxyandrostenedione (4-OHA). Among all compounds tested only ursolic acid 1 showed an efficient and dose-dependent aromatase inhibition with IC50 value of 32 microM as did apigenin (IC50=10 microM), whereas IC50 value of 4-OHA was 0.8 microM. Our results show that the incorporation of a metallocene moiety into the ursolic acid derivatives decreases the aromatase inhibition. Moreover, comparison of the structure/inhibitory potency relationship of compounds indicates that the presence of cycle A and the configuration of C3-OH and C17-COOH seems to be more favourable to recognize the active site of aromatase and to block its activity.

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