Nguyen Mai Thanh Thi, Awale Suresh, Tezuka Yasuhiro, Tran Quan Le, Kadota Shigetoshi
Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, 2630 Sugitani, Toyama 930-0194, Japan.
Chem Pharm Bull (Tokyo). 2005 Aug;53(8):984-8. doi: 10.1248/cpb.53.984.
From the MeOH extract of Vietnamese Caesalpinia sappan, a novel biogenetically exclusive benzindenopyran, with a new carbon framework, neoprotosappanin (1), and a new compound, protosappanin A dimethyl acetal (3), were isolated together with protosappanin E-2 (2), neosappanone A (4), and 13 previously reported phenolic compounds (5-17). Their structures were elucidated on the basis of spectroscopic data. Compounds 1-4, 7, 13, and 15-17 showed significant xanthine oxidase inhibitory activity in a concentration-dependent manner, and sappanchalcone (17) showed the most potent activity with an IC50 value of 3.9 microM, comparable to that of positive control allopurinol (IC50, 2.5 microM). The kinetic study of these inhibitors indicated that they are competitive inhibitors, the same as allopurinol, except for 1 and 16 which are noncompetitive inhibitors.
从越南苏木的甲醇提取物中，分离出一种新型生源独特的苯并茚并吡喃（具有新的碳骨架，即新原苏木素（1））、一种新化合物原苏木素A二甲基缩醛（3），以及原苏木素E - 2（2）、新苏木酮A（4）和13种先前报道的酚类化合物（5 - 17）。它们的结构通过光谱数据得以阐明。化合物1 - 4、7、13以及15 - 17呈现出浓度依赖性的显著黄嘌呤氧化酶抑制活性，其中苏木查耳酮（17）表现出最强的活性，IC50值为3.9微摩尔，与阳性对照别嘌呤醇（IC50，2.5微摩尔）相当。对这些抑制剂的动力学研究表明，除了1和16为非竞争性抑制剂外，它们与别嘌呤醇一样都是竞争性抑制剂。
