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越南药用植物的黄嘌呤氧化酶抑制活性

Xanthine oxidase inhibitory activity of Vietnamese medicinal plants.

作者信息

Nguyen Mai Thanh Thi, Awale Suresh, Tezuka Yasuhiro, Tran Quan Le, Watanabe Hiroshi, Kadota Shigetoshi

机构信息

Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, 2630-Sugitani, Toyama 930-0194, Japan.

出版信息

Biol Pharm Bull. 2004 Sep;27(9):1414-21. doi: 10.1248/bpb.27.1414.

Abstract

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).

摘要

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。

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