Novel antitumor activities of Kushen flavonoids In Vitro and In Vivo

作者：Mingyu Sun, Jun Han, Jifeng Duan, Yumin Cui, Tao Wang, Weihan Zhang, Wei Liu, Jian-Rong Hong, Minghui Yao, Sidong Xiong, Xiaoqiang Yan · 发表于：Phytotherapy Research · 年份：2006 · DOI：10.1002/ptr.2066 · 被引用次数：74 · 研究领域：Bioactive natural compounds、Biological Activity of Diterpenoids and Biflavonoids、Synthesis of Organic Compounds

Kushen (KS), the dried roots of Sophora flavescens Aiton, has a long history of use in traditional Chinese medicine to treat inflammatory diseases and cancer. Kushen alkaloids (KS-As) and Kushen flavonoids (KS-Fs) are the well characterized components in KS. KS-As have been considered biologically active and developed in China as anticancer drugs. In an effort to screen novel antitumor agents from botanicals, more potent antitumor activities were identified in KS-Fs than in KS-As. KS-Fs were able to inhibit the growth of a panel of tumor cell lines and enhanced the antitumor activities of Taxol in vitro. The antitumor activities of KS-Fs and Kur, a single KS-Fs compound, were demonstrated in murine and xenograft human tumor models. Further, it was shown that KS-Fs and Kur were able to enhance the effect of Taxol to inhibit the growth of H460 and Eca-109 xenograft tumors. In addition, peripheral blood cell counts were not significantly affected in normal mice treated with KS-Fs at 200 mg/kg/day for 2 weeks. These results suggest that KS-Fs may be developed as novel antitumor agents and that the currently marketed KS-As drugs in China may have missed the major antitumor activities in Kushen.