Jayasuriya H, Koonchanok N M, Geahlen R L, McLaughlin J L, Chang C J
Department of Medicinal Chemistry and Pharmacognosy, Purdue University, West Lafayette, Indiana 47907.
J Nat Prod. 1992 May;55(5):696-8. doi: 10.1021/np50083a026.
Bioassay-directed fractionation of a Chinese medicinal plant, Polygonum cuspidatum (Polygonaceae), has led to the discovery of an anthraquinone, emodin [1], as a strong inhibitor of a protein tyrosine kinase (p56lck) partially purified from bovine thymus. Comparison of the IC50 values of emodin for protein tyrosine kinase inhibitory activity with physcion [2] and emodin-O8-D-glucoside [3], also isolated from the same plant, reveal the importance of the hydroxyl groups at C-6 and C-8 for the observed activity.
对一种中药虎杖（蓼科）进行生物测定导向的分级分离，发现了一种蒽醌——大黄素[1]，它是从牛胸腺中部分纯化得到的一种蛋白酪氨酸激酶（p56lck）的强效抑制剂。将大黄素对蛋白酪氨酸激酶抑制活性的半数抑制浓度（IC50）值与同样从该植物中分离得到的大黄素甲醚[2]和大黄素-O8-D-葡萄糖苷[3]进行比较，揭示了C-6和C-8位羟基对于所观察到的活性的重要性。
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