Abstract
The root of Sophora flavescens has been reported to possess antitumor activity in Sarcoma 180, lymphoid leukemia 1210 and melanotic melanoma. We have isolated four cytotoxic flavonoids with a lavandulyl side-chain at C8 and tested for their effects on human myeloid leukemia HL-60 cells and human hepatocarcinoma HepG2 cells, in terms of inhibition of proliferation and induction of apoptosis. They showed potent antiproliferative effects with IC 50 values from 11.3 μ m to 18.5 μ m in HL60 cells and from 13.3 μ m to 36.2 μ m in HepG2 cells. Treatment of HL-60 cells with the lavandulylflavonoids induced apoptosis in a dose-dependent manner. Apoptosis was judged by the detection of DNA fragmentation by agarose gel electrophoresis and the degree of apoptosis was quantified by a sandwich enzyme immunoassay. The hydration of C4‴C5‴ double bond with or without C3 hydroxylation caused a complete loss of cytotoxicity. These results suggest that the lavandulyl side-chain is essential for the activity of the flavonoids isolated from S. flavescens which may be used as cancer chemotherapeutic and chemopreventive agents.
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