20S Proteasome Inhibitory Activity of Flavonoids isolated from Spatholobus suberectus

作者：Shim Sang Hee^*

来源：Phytotherapy Research, 2011, 25(4): 615-618.

DOI：10.1002/ptr.3342

• 20S proteasome inhibitor
• Spatholobus suberectus
• isoliquiritigenin
• genistein
• 7-hydroxyflavanone

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 IC(50) values of 4.88 +/- 1.5, 9.26 +/- 1.2 and 5.21 +/- 1.5 mu M, respectively.

• 出版日期2011-4