文章基本信息

标题：Induction of Apoptotic Cell Death by Synthetic Naringenin Derivatives in Human Lung Epithelial Carcinoma A549 Cells
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作者：Eung-Ryoung Lee ; Yong-Jin Kang ; Hye-Yeon Choi 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2007
卷号：30
期号：12
页码：2394-2398
DOI：10.1248/bpb.30.2394
出版社：The Pharmaceutical Society of Japan
摘要：Although flavonoids, which are both qualitatively and quantitatively one of the largest groups of natural products, exhibit a variety of beneficial health effects, the exact molecular mechanism of the cellular activities is still not fully explained and there currently exists a lack of evidence for any relationship between the structure–activity relationship and apoptosis-inducing activity. In order to determine the importance of the OH group or substitution of the 5 or carbon-7 in the diphenylpropane skeleton of flavonoids, we originally synthesized several modified naringenin derivatives, including 7- O -benzyl naringenin (KUF-1) and 7- O -(MeO- L -Leu- D -Pro-carbonylmethyl) naringenin (KUF-7). Treatment with KUF-1 or KUF-7 resulted in significant apoptosis-inducing effects concomitant with chromatin condensation, caspase activation, and intracellular ROS production. Our data indicate that originally synthesized naringenin derivatives, KUF-1 and KUF-7 differentially regulate the apoptosis of A549 cells via intracellular ROS production coupled with the concomitant activation of the caspase cascade signaling pathway, thereby implying that hydroxylation or substitution at Carbon-7 is critical for the apoptosis-inducing activity of flavonoids.
关键词：flavonoid;synthetic naringenin derivative;reactive oxygen species;apoptosis;lung cancer;A549