Yoo Kyung Mi, Kim Sanghee, Moon Bo Kyung, Kim Sung Soo, Kim Kyung Tack, Kim Sun Yeou, Choi Sang Yoon
Korea Food Research Institute, Songnam, Korea.
Arch Pharm (Weinheim). 2006 May;339(5):238-41. doi: 10.1002/ardp.200500228.
Resveratrol has been identified as a potent anticancer agent in a variety of studies. In this study, several resveratrol derivatives were synthesized and investigated in the search for an anticancer agent with higher efficacy than resveratrol. During our examination of cancer cell lines, compounds C, F, and G evidenced higher inhibitory activity than resveratrol with regard to the growth of PC-3 and LNCaP human prostate cancer cells. Moreover, four derivatives of resveratrol evidenced potent growth inhibitory activity (IC50 0.01-0.04 microM) in LNCaP cells. The levels of activity in these derivatives were 25-100 times stronger than that associated with resveratrol (IC50 1.0 microM). Our results suggested that compounds C, D, F, and G might function as anticancer agents on prostate tumors. This study also contains a discussion regarding the structure-activity relationships of several resveratrol derivatives.
在多项研究中,白藜芦醇已被确认为一种有效的抗癌剂。在本研究中,合成并研究了几种白藜芦醇衍生物,以寻找一种比白藜芦醇具有更高疗效的抗癌剂。在我们对癌细胞系的检测过程中,化合物C、F和G在抑制PC-3和LNCaP人前列腺癌细胞生长方面表现出比白藜芦醇更高的活性。此外,四种白藜芦醇衍生物在LNCaP细胞中表现出强大的生长抑制活性(IC50为0.01 - 0.04微摩尔)。这些衍生物的活性水平比白藜芦醇(IC50为1.0微摩尔)强25 - 100倍。我们的结果表明,化合物C、D、F和G可能对前列腺肿瘤起到抗癌剂的作用。本研究还包含了关于几种白藜芦醇衍生物构效关系的讨论。