Tectorigenin, an Isoflavone of Pueraria thunbergiana BENTH., Induces Differentiation and Apoptosis in Human Promyelocytic Leukemia HL-60 Cells

• Published in: Biological & pharmaceutical bulletin Vol. 24; no. 10; pp. 1117 - 1121
• Main Authors: LEE, Kyung-Tae, SOHN, Il-Cheol, KIM, Young-Kwan, CHOI, Jung-Hye, CHOI, Jong-Won, PARK, Hee-Juhn, ITOH, Yoshie, MIYAMOTO, Ken-ichi
• Format: Journal Article
• Language: English
• Published: Tokyo The Pharmaceutical Society of Japan 01.10.2001; Maruzen; Japan Science and Technology Agency
• Subjects: Anti-Inflammatory Agents, Non-Steroidal - pharmacology; Antineoplastic agents; apoptosis; Apoptosis - drug effects; Biological and medical sciences; Blotting, Western; Cell Differentiation - drug effects; Cell Division - drug effects; cytotoxicity; differentiation; DNA Fragmentation - drug effects; Flow Cytometry; Gene Expression - drug effects; General aspects; Genes, bcl-1 - drug effects; Genistein - chemistry; Genistein - pharmacology; HL-60 cell; HL-60 Cells; Humans; isoflavone; Isoflavones - pharmacology; Medical sciences; Pharmacology. Drug treatments; Phosphorylation; Plants, Medicinal - chemistry; Pueraria - chemistry; Spectrometry, Fluorescence; Structure-Activity Relationship; tectorigenin; Antineoplastic agent; Human; Promyelocytic leukemia; Autophosphorylation; Pharmacognosy; Acute; Oriental medicine; Malignant hemopathy; Cell differentiation; Gene expression; Isoflavone derivatives; Biological activity; Medicinal plant; Epidermal growth factor; Structure activity relation; Cell death; Established cell line; Plant origin; Tumor cell; Apoptosis; Biological receptor
• ISSN: 0918-6158; 1347-5215
• DOI: 10.1248/bpb.24.1117

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 isoflavonoids, tectorigenin and genistein exhibited cytotoxicity against various human cancer cells; glycitein showed only mild cytotoxicity. These results suggest that the isoflavone structure and 5-hydroxyl group are crucial for the cytotoxic properties and that glycosides are inactive. Moreover, tectorigenin induced differentiation of human promyelocytic leukemia HL-60 cells to granulocytes and monocytes/macrophages, and caused apoptotic changes of DNA in the cells, as did genistein. Tectorigenin also inhibited autophosphorylation of epidermal growth factor (EGF) receptor by EGF and decreased the expression of Bcl-2 protein, with less activity than genistein. From these results, tectorigenin may be a possible therapeutic agent for leukemia.