Oncogene signal transduction inhibitors from medicinal plants.
Signal transduction is believed to be altered by cellular oncogenes or tumor suppressor genes during the transformation of normal cells into malignant cells. This proposition offers an attractive target for oncogene-based anticancer drug discovery from natural sources. Protein kinases encoded or modulated by oncogenes were used to prescreen the potential antitumor activity of medicinal plants. Protein-tyrosine kinase-directed fractionation and separation of the crude extracts of Polygonum cuspidatum and Koelreuteria henryi have led to the isolation of three different classes of protein-tyrosine kinase inhibitors, anthraquinone, stilbene and flavonoid. The anthraquinone inhibitor, emodin, displayed highly selective activities against src-Her-2/neu and ras-oncogenes.
Chang
C J
CJ
Department of Medicinal Chemistry and Pharmacognosy, Purdue University, West Lafayette, Indiana 47907, USA.
Ashendel
C L
CL
Geahlen
R L
RL
McLaughlin
J L
JL
Waters
D J
DJ
D000880:Anthraquinones / Q000494:pharmacology / Q000633:toxicity; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000633:toxicity; D002455:Cell Division / Q000187:drug effects; D004642:Emodin / Q000494:pharmacology / Q000633:toxicity; D006801:Humans; D015394:Molecular Structure; D009369:Neoplasms / Q000378:metabolism / Q000628:therapy; D009857:Oncogenes; D010946:Plants, Medicinal / Q000737:chemistry*; D011493:Protein Kinase C / Q000037:antagonists & inhibitors; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors; D015398:Signal Transduction / Q000187:drug effects*; D013267:Stilbenes / Q000494:pharmacology / Q000633:toxicity; D014407:Tumor Cells, Cultured
D000880:Anthraquinones; D000970:Antineoplastic Agents; D013267:Stilbenes; D011505:Protein-Tyrosine Kinases; D011493:Protein Kinase C; D004642:Emodin