Comparison of glutathione reductase activity and the intracellular glutathione reducing effects of 13 derivatives of 1′-acetoxychavicol acetate in Ehrlich ascites tumor cells

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• 作者：Shenghui Xu ; Akiko Kojima-Yuasa ; Hideki Azuma ; David Opare Kennedy ; Yotaro Konishi ; Isao Matsui-Yuasa
• 关键词：1′ ; -Acetoxychavicol acetate ; Glutathione ; Glutathione reductase ; Structure– ; activity relationship ; Ehrlich ascites tumor cell
• 刊名：Chemico-Biological Interactions
• 出版年：2010
• 出版时间：14 May 2010
• 年：2010
• 卷：185
• 期：3
• 页码：235-240
• 全文大小：529 K

文摘

In a previous study, we showed that (1′S)-acetoxychavicol acetate ((S)-ACA) caused a rapid decrease in glutathione (GSH) levels less than 15 min after exposure. (S)-ACA-induced cell death was reversed by the addition of N-acetylcysteine. In the current study, we investigated the inhibitory activities of 13 derivatives of (S)-ACA on tumor cell viability, intracellular GSH level and GR activity. Correlations were found among a decrease in cell viability, intracellular GSH levels and the activity of GR in Ehrlich ascites tumor cells treated with the various ACA analogues. A test of the 13 derivatives revealed that the structural factors regulating activity were as follows: (1) the para or 1′-position of acetoxyl group (or other acyl group) was essential, (2) the presence of a C2′–C3′ double or triple bond was essential, and (3) the S configuration of the 1′-acetoxyl group was preferable.