Antigiardial activity of isoflavones from Dalbergia frutescens bark
Antigiardial activity of isoflavones from Dalbergia frutescens bark
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DOI：
10.1021/np000010d
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发表时间：
2000-10-01
影响因子：
5.1
通讯作者：
Walker, LA
中科院分区：
文献类型：
--
作者：
Khan, IA;Avery, MA;Walker, LA
从黄檀（Dalbergia frutescens）中分离得到芒柄花黄素（1）、栗树素（5）、odoratin（6）、黄豆黄素（7）、假结合素（8）、藤黄素（9）和cuneatin（10），并测定了它们的抗贾第鞭毛虫活性。在这些化合物中，芒柄花素（1）是最有效的抗心血管药物，其IC 50值为30 ng/mL（约0.1 μ M），而当前选择的药物甲硝唑的IC 50值为100 ng/mL（约0.6 μ M）。还评价了与芒柄花黄素密切相关的三种异黄酮[大豆黄酮（2）、鹰嘴豆素A（3）和染料木黄酮（4）]，但它们的活性至少比1低100倍。因此，芒柄花素（1）可能是开发新的抗心血管药物的一个有趣的线索，也是一个新的机制靶点的探针。
Several isoflavones [formononetin (1), castanin (5), odoratin (6), glycitein (7), pseudebaptogenin (8), fujikinetin (9), and cuneatin (10)] were isolated from Dalbergia frutescens, and their antiprotozoal activities were determined against Giardia intestinalis. Among these compounds, formononetin (1) was the most potent antigiardial agent, with an IC50 value of 30 ng/mL (approximately 0.1 muM), as compared to the value for metronidazole, the current drug of choice, of 100 ng/mL (approximately 0.6 muM). Three isoflavones closely related to formononetin [daidzein (2), biochanin A (3) and genistein (4)] were also evaluated, but they were at least 100 times less active than 1. Formononetin (1) may thus be an interesting lead for development of new antigiardial agents eras a probe for a new mechanistic target.