Mini Reviews in Medicinal Chemistry, 2012, 12(4):350-362.

The Mechanisms of Anticancer Agents by Genistein and Synthetic Derivatives of Isoflavone

Huan Qiu Li, et al

College of Pharmaceutical Science, Soochow University, Suzhou 215123, PR China

Genistein is the most abundant isoflavone in soybeans. It has exhibited diverse biological activities, among these, its anticancer effects is most noteworthy. Through regulating critical cell cycle genes, genistein can inhibit cancer cell growth in vivo and in vitro. It has been reported that genistein can inhibit activation of NF-κB and Akt signaling pathways to induce cell apopt1osis, both pathways are well known for their function to maintain a balance between cell survival and apoptosis. In order to find out more outstanding anticancer isoflavone agents, against cancers extended synthesis of genistein derivatives has been carried out. Some of these synthetic compounds demonstrated higher anticancer activity with lower doses. Based on these results, genistein and its synthetic derivatives may be an emerging new type of anticancer agents.

荷兰《药物化学短评》，2012年4月

金雀异黄素和大豆异黄酮合成衍生物等抗肿瘤试剂的机制

李焕秋，等

中国苏州大学药物科学院

金雀异黄素是大豆中最丰富的异黄酮。它具有多种生物活性，其中，最值得注意的是其抗肿瘤的作用。通过调控细胞周期的关键基因，金雀异黄素可以在体内和体外抑制癌细胞生长。据报道，金雀异黄素可抑制 NF-κ B 的活化和Akt 信号通路进而诱导细胞 凋亡，众所周知这两种途径被用于维持细胞存活和凋亡之间的平衡。为了找出更多优秀的抗癌异黄酮药物，合成了抗癌症发展的金雀异黄素衍生物。这些合成化合物中的一些表现出较高的抗癌活性和更低的剂量。基于这些结果，金雀异黄素及其合成衍生物可能是一种新兴的新型抗癌药物。