Novel antitumor activities of Kushen flavonoids in vitro and in vivo.
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.
Sun
Mingyu
M
Department of Biology, Hutchison Medipharma Ltd., Zhang Jiang Hi-Tech Park, Shanghai 201203, China.
Han
Jun
J
Duan
Jifeng
J
Cui
Yumin
Y
Wang
Tao
T
Zhang
Weihan
W
Liu
Wei
W
Hong
Jianrong
J
Yao
Minghui
M
Xiong
Sidong
S
Yan
Xiaoqiang
X
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D045744:Cell Line, Tumor / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects*; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D051379:Mice; D008813:Mice, Inbred ICR; D008517:Phytotherapy; D018517:Plant Roots; D051381:Rats; D017207:Rats, Sprague-Dawley; D014183:Transplantation, Heterologous
D000972:Antineoplastic Agents, Phytogenic; D004365:Drugs, Chinese Herbal; C494416:kushen