Bioassay-guided isolation of aldose reductase inhibitors from Artemisia dracunculus
Bioassay-guided isolation of aldose reductase inhibitors from Artemisia dracunculus
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DOI：
10.1016/j.phytochem.2006.05.015
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发表时间：
2006-07-01
期刊：
影响因子：
3.8
通讯作者：
Raskin, Ilya
中科院分区：
文献类型：
--
作者：
Logendra, Sithes;Ribnicky, David M.;Raskin, Ilya
龙蒿的乙醇提取物。具有抗糖尿病活性，作为可能的醛糖还原酶（ALR 2）抑制剂，ALR 2是参与糖尿病并发症的关键酶。在3.75 μ g/mL时，总提取物抑制ALR 2活性40%，而槲皮苷，一种已知的ALR 2抑制剂，抑制其活性54%。用总乙醇提取物进行抑制ALR 2活性的化合物的生物活性引导的分级和分离，得到在3.75 μ g/mL下ALR 2抑制活性范围为58%至77%的四种生物活性化合物。经LC/MS、H-1 NMR、C-13 NMR和2DNMR等波谱分析，鉴定为4，5-二-O-咖啡酰奎尼酸、Davidigenin、6-demethoxycapillarisin和2 '，4'-dihydroxy-4-methoxydihydrochalcone。这是首次从A.和4，5-二-O-咖啡酰奎尼酸、6-去甲氧基茵陈素和2 ′，4 ′-二羟基-4-甲氧基二氢查耳酮的ALR 2抑制活性。这些结果提示了A.龙血竭用于改善糖尿病并发症。(c)2006爱思唯尔有限公司保留所有权利。
An ethanolic extract of Artemisia dracunculus L. having antidiabetic activity was examined as a possible aldose reductase (ALR2) inhibitor, a key enzyme involved in diabetic complications. At 3.75 mu g/mL, the total extract inhibited ALR2 activity by 40%, while quercitrin, a known ALR2 inhibitor, inhibited its activity by 54%. Bioactivity guided fractionation and isolation of the compounds that inhibit ALR2 activity was carried out with the total ethanolic extract yielding four bioactive compounds with ALR2 inhibitory activity ranging from 58% to 77% at 3.75 mu g/mL. Using LC/MS, H-1 NMR, C-13 NMR and 2D NMR spectroscopic analyses, the four compounds were identified as 4,5-di-O-caffeoylquinic acid, davidigenin, 6-demethoxycapillarisin and 2',4'-dihydroxy-4-methoxydihydrochalcone. This is the first report on their isolation from A. dracunculus and the ALR2 inhibitory activity of 4,5-di-O-caffeoylquinic acid, 6-demethoxycapillarisin and 2',4'-dihydroxy-4-methoxydihydrochalcone. These results suggest a use of the extract of A. dracunculus for ameliorating diabetic complications. (c) 2006 Elsevier Ltd. All rights reserved.