Xanthine oxidase inhibitory activity of Vietnamese medicinal plants

Xanthine oxidase inhibitory activity of Vietnamese medicinal plants
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DOI:
10.1248/bpb.27.1414
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发表时间:
2004-09-01
影响因子:
2
通讯作者:
Kadota, S
Kadota, S
中科院分区:
医学4区
文献类型:
--
作者:
Nguyen, MTT;Awale, S;Kadota, S

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在从越南传统医学中用于治疗痛风和相关症状的96种药用植物制备的288种提取物中,188种在100 μ g/ml下表现出黄嘌呤氧化酶(XO)抑制活性,其中46种具有大于50%的抑制。在50 μ g/ml时,168种提取物具有活性,其中21种具有超过50%的抑制作用。在25 μ g/ml时,146种提取物显示出抑制活性,其中8种显示出超过50%的抑制,而126种提取物在10 μ g/ml时显示出活性,其中2种具有大于50%的抑制。青蒿、云实、艾纳香、菊花的甲醇提取物和Tetracera scandens(庆和省)的甲醇-水提取物表现出较强的XO抑制活性,IC 50值小于20 μ g/ml。结果表明,丁香花的甲醇提取物具有较强的抑菌活性。中华绒螯蟹的IC_(50)值为5.1 μ g/ml。甲醇提取物的活性导向分馏导致咖啡酸(1)、毛地黄黄酮(2)、圣草酚(3)和1,5-二-O-咖啡酰奎宁酸(4)的分离。所有这些化合物均显示出浓度依赖性的XO抑制活性,2的活性(IC 50 1.3 μ m)比临床使用的药物别嘌呤醇(IC 50 2.5 μ m)更有效。
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 mug/ml, with 46 having greater than 50% inhibition. At 50 mug/ml, 168 of the extracts were active, with 21 possessing more than 50% inhibition. At 25jig/ml, 146 extracts exhibited inhibitory activity, with 8 showing over 50% inhibition, while 126 extracts presented activity at 10 mug/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-H2O extract of Tetracera scandens (Khanh Hoa province) exhibited strong XO inhibitory activity with IC50 values less than 20 mug/ml. The most active extract was the MeOH extract of the flower of C. sinense with an IC50 value of 5.1 mug/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 (IC50 1.3 mum) than the clinically used drug, allopurinol (IC50 2.5 mum).