Journal
FOOD AND CHEMICAL TOXICOLOGY
Volume 38, Issue 10, Pages 861-865Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0278-6915(00)00079-X
Keywords
Vitex rotundifolia; polymethoxyflavonoids; cytotoxicity; apoptosis; HL-60 cells
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Three polymethoxyflavonoids from the fruit of Vitex rotundifolia, namely 2',3',5-trihydroxy-3,6,7-trimethoxyflavone (Vx-1), vitexicarpin (Vx-5) and artemetin (Vx-6), were tested for their antiproliferative activity in human myeloid leukemia HL-60 cells. They showed a dose-dependent decrease in the growth of HL-60 cells. The concentrations required for 50% inhibition of the growth (IC50) after 96 h were 4.03 mu m, 0.12 mu m and 30.98 mu m for Vx-1, Vx-5 and Vx-6, respectively. Treatment of HL-60 cells with the flavonoids induced morphological changes that are characteristic of apoptosis. We judged the induction of apoptosis by the detection of DNA fragmentation in agarose gel electrophoresis and the degree of apoptosis was quantified by a double-antibody sandwich ELISA and by flow cytometric analysis. The C-3 hydroxyl and C-8 methoxyl groups were found not to be essential for the activity, but the C-3' methoxyl instead of hydroxyl group lowered the antiproliferative, and apoptosis inducing activity. These results suggest that the polymethoxyflavonoids isolated from V. rotundifolia may he used as potential chemopreventive and chemotherapeutic agents. (C) 2000 Elsevier Science Ltd. All rights reserved.
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