Abstract

MINGUZZI, Sandro; BARATA, Lauro E. S.  and  CORDELL, Geoffrey A.. Cytotoxic derivatives of withanolides isolated from the leaves of Acnistus arborescens. Quím. Nova [online]. 2011, vol.34, n.2, pp. 237-241. ISSN 0100-4042.  http://dx.doi.org/10.1590/S0100-40422011000200013.

In view of anticancer activity of 7 β-acetoxywithanolide D (2) and 7β-16α-diacetoxywithonide D (3), isolated from the leaves of Acnistus arborescens (Solanaceae), five withanolide derivatives were obtained and their structures were determined by NMR, MS and IV data analysis. The in vitro anticancer activity of these derivatives was evaluated in a panel of cancer cell lines: human breast (BC-1), human lung (Lu1), human colon (Col2) and human oral epidermoid carcinoma (KB). Compounds 2a (acetylation of 2), 3b (oxidation of 3) and 2c (hydrogenation of 2) exhibited the highest anticancer activity against human lung cancer cells, with ED₅₀ values of 0.19, 0.25 and 0.63 μg/mL, respectively.

Keywords : Acnistus arborescens; withanolides derivatives; human lung cancer.