In vitro cytotoxic activity of isolated acridones alkaloids from Zanthoxylum leprieurii Guill. et Perr

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• 作者：Rost ; M. Ngoumfo ; Jean-Bosco Jouda ; Ferdin ; T. Mouafo ; Justin Komguem ; Cé ; line D. Mbazoa ; Tze Chieh Shiao ; Mohammed I. Choudhary ; Hartmut Laatsch ; Jean Legault ; André ; Pichette ; René ; Roy
• 关键词：Acridones ; Cytotoxity ; Lung carcinoma ; Colorectal adenocarcinoma
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2010
• 出版时间：15 May 2010
• 年：2010
• 卷：18
• 期：10
• 页码：3601-3605
• 全文大小：384 K

文摘

Chemical investigation of the roots and fruits of Zanthoxylum leprieurii Guill. et Perr. led to the isolation of three new alkaloids including two acridone derivatives, 3-hydroxy-1,4-dimethoxy-10-methyl-9-acridone (2) and 3-hydroxy-1,2-dimethoxy-10-methyl-9-acridone (3) named helebelicine A and B, respectively, and one secobenzo[c]phenantridine, 10-O-demethyl-12-O-methylarnottianamide (10), together with thirteen other compounds. The structures of compounds 2, 3 and 10 as well as those of the known compounds were elucidated by using spectroscopic methods and by comparison with reported data. The brine-shrimp (artemia salina) lethality bioassay of the chloroform extract of the fruits showed modest cytotoxicity with LD₅₀ at 13.1 μg/mL. Isolated compounds 1, 4–6 were found to be moderately active against lung carcinoma cells (A549), colorectal adenocarcinoma cells (DLD-1) and normal cells (WS1) with IC₅₀ values ranging from 27 to 77 μM. In contrast to the positive control etoposide used, the cytotoxicity of the most active compound 4 was found to be selective against cancer cells in comparison to normal cells WS1 with IC₅₀ of 51 ± 8 μM and 4.3 ± 0.4 μM, respectively.