Phytotherapy Research, 2011, 25(4):615-8.

20S Proteasome Inhibitory Activity of Flavonoids isolated from Spatholobus suberectus

Sang Hee Shim

School of Biotechnology, Yeungnam University, Gyeongsan 712-749, South Korea

The promising biological role of the ubiquitin proteasome pathway (UPP) in cancer therapy has recently emerged. Inhibition of proteasome has been proposed as a new therapeutic target for treatment of cancer. Bioassay-guided fractionation of a MeOH extract of the stems of Spatholobus suberectus resulted in seven compounds, liquiritigenin (1), isoliquiritigenin (2), genistein (3), daidzein (4), medicarpin (5), 7-hydroxyflavanone (6) and formononetin (7), which were evaluated for the first time for their inhibitory effect on 20S proteasome. Among the isolated compounds, 2, 3 and 6 exhibited inhibitory activities on human 20S proteasome with IC50 values of 4.88 ± 1.5, 9.26 ± 1.2 and 5.21 ± 1.5 µm, respectively.

英国《植物疗法研究》，2011年4月

从鸡血藤中分离的黄酮类化合物抑制20S 蛋白酶体的活性

辛桑河

韩国岭南大学生物工程学院

最近在肿瘤治疗中出现了具有前景生物作用的泛素蛋白酶体通路 (UPP)。蛋白酶体的抑制作用被认为是治疗癌症的新治疗靶点。根据生物鉴定指导分馏鸡血藤茎的甲醇提取物可以得到七种化合物、 甘草素 (1)、 异甘草素 (2)、 金雀异黄素 (3)、 大豆苷元 (4)、 美迪紫檀素 (5)、 7-羟基磺烷酮（6） 和芒柄花素 (7)，第一次评价了它们对 20S 蛋白酶体的抑制作用。在这些分离得到的化合物中，2、 3 和 6 分别展出 IC50 值为 4.88 ± 1.5，9.26 ± 1.2 和 5.21 ± 1.5 um抑制20S 蛋白酶体的活性。