Kt. Lee et al., Tectorigenin, an isoflavone of Pueraria thunbergiana Benth., induces differentiation and apoptosis in human promyelocytic leukemia HL-60 cells, BIOL PHAR B, 24(10), 2001, pp. 1117-1121
Cytotoxic effects of six isoflavonoids, tectorigenin, glycitein, tectoridin
, glycitin, 6"-O-xylosyltectoridin, and 6"-O-xylosylglycitin isolated from
the flower of Pueraria thunbergiana BENTH. together with genistein, a known
differentiation and apoptosis inducer, were examined. Among these isoflavo
noids, tectorigenin and genistein exhibited cytotoxicity against various hu
man cancer cells; glycitein showed only mild cytotoxicity. These results su
ggest that the isoflavone structure and 5-hydroxyl group are crucial for th
e cytotoxic properties and that glycosides are inactive. Moreover, tectorig
enin induced differentiation of human promyelocytic leukemia HL-60 cells to
granulocytes and monocytes/macrophages, and caused apoptotic changes of DN
A in the cells, as did genistein. Tectorigenin also inhibited autophosphory
lation of epidermal growth factor (EGF) receptor by EGF and decreased the e
xpression of Bcl-2 protein, with less activity than genistein. From these r
esults, tectorigenin may be a possible therapeutic agent for leukemia.