Chang C J, Ashendel C L, Geahlen R L, McLaughlin J L, Waters D J
Department of Medicinal Chemistry and Pharmacognosy, Purdue University, West Lafayette, Indiana 47907, USA.
In Vivo. 1996 Mar-Apr;10(2):185-90.
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.
在正常细胞向恶性细胞转化过程中，信号转导被认为会被细胞癌基因或肿瘤抑制基因改变。这一观点为从天然来源发现基于癌基因的抗癌药物提供了一个有吸引力的靶点。由癌基因编码或调控的蛋白激酶被用于初步筛选药用植物的潜在抗肿瘤活性。对虎杖和湖北栾树粗提物进行蛋白酪氨酸激酶导向的分级分离，已分离出三类不同的蛋白酪氨酸激酶抑制剂，即蒽醌类、二苯乙烯类和黄酮类。蒽醌类抑制剂大黄素对src-Her-2/neu和ras癌基因表现出高度选择性活性。
