Nguyen Mai Thanh Thi, Awale Suresh, Tezuka Yasuhiro, Tran Quan Le, Watanabe Hiroshi, Kadota Shigetoshi
Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, 2630-Sugitani, Toyama 930-0194, Japan.
Biol Pharm Bull. 2004 Sep;27(9):1414-21. doi: 10.1248/bpb.27.1414.
Among 288 extracts, prepared from 96 medicinal plants used in Vietnamese traditional medicine to treat gout and related symptoms, 188 demonstrated xanthine oxidase (XO) inhibitory activity at 100 microg/ml, with 46 having greater than 50% inhibition. At 50 microg/ml, 168 of the extracts were active, with 21 possessing more than 50% inhibition. At 25 microg/ml, 146 extracts exhibited inhibitory activity, with 8 showing over 50% inhibition, while 126 extracts presented activity at 10 microg/ml, with 2 having greater than 50% inhibition. The MeOH extracts of Artemisia vulgaris, Caesalpinia sappan (collected at the Seven-Mountain area), Blumea balsamifera (collected in Lam Dong province), Chrysanthemum sinense and MeOH-H(2)O extract of Tetracera scandens (Khanh Hoa province) exhibited strong XO inhibitory activity with IC(50) values less than 20 microg/ml. The most active extract was the MeOH extract of the flower of C. sinense with an IC(50) value of 5.1 microg/ml. Activity-guided fractionation of the MeOH extract led to the isolation of caffeic acid (1), luteolin (2), eriodictyol (3), and 1,5-di-O-caffeoylquinic acid (4). All these compounds showed significant XO inhibitory activity in a concentration-dependent manner, and the activity of 2 was more potent (IC(50) 1.3 microM) than the clinically used drug, allopurinol (IC(50) 2.5 microM).
从越南传统医学中用于治疗痛风及相关症状的96种药用植物制备的288种提取物中,188种在100微克/毫升时表现出黄嘌呤氧化酶(XO)抑制活性,其中46种抑制率大于50%。在50微克/毫升时,168种提取物有活性,21种抑制率超过50%。在25微克/毫升时,146种提取物表现出抑制活性,8种抑制率超过50%,而在10微克/毫升时,126种提取物有活性,2种抑制率大于50%。黄花蒿、苏木(采自七山地区)、艾纳香(采自林同省)、中华菊以及伏石蕨(庆和省)的甲醇 - 水提取物表现出较强的XO抑制活性,IC50值小于20微克/毫升。活性最强的提取物是中华菊花朵的甲醇提取物,IC50值为5.1微克/毫升。对甲醇提取物进行活性导向分离得到了咖啡酸(1)、木犀草素(2)、圣草酚(3)和1,5 - 二 - O - 咖啡酰奎宁酸(4)。所有这些化合物均以浓度依赖性方式表现出显著的XO抑制活性,且化合物2的活性(IC50 1.3微摩尔)比临床使用的药物别嘌醇(IC50 2.5微摩尔)更强。