Khan I A, Avery M A, Burandt C L, Goins D K, Mikell J R, Nash T E, Azadegan A, Walker L A
National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, Mississippi 38677, USA.
J Nat Prod. 2000 Oct;63(10):1414-6. doi: 10.1021/np000010d.
Several isoflavones [formononetin (1), castanin (5), odoratin (6), glycitein (7), pseudobaptogenin (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 IC(50) value of 30 ng/mL (approximately 0.1 microM), as compared to the value for metronidazole, the current drug of choice, of 100 ng/mL (approximately 0.6 microM). 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 or as a probe for a new mechanistic target.
从黄檀属植物（Dalbergia frutescens）中分离出了几种异黄酮[芒柄花黄素（1）、紫铆因（5）、奥多拉丁（6）、黄豆黄素（7）、假巴普托皂苷元（8）、藤黄菌素（9）和楔叶豆素（10）]，并测定了它们对肠道贾第虫的抗原虫活性。在这些化合物中，芒柄花黄素（1）是最有效的抗贾第虫药物，其半数抑制浓度（IC50）值为30 ng/mL（约0.1 microM），而目前的首选药物甲硝唑的IC50值为100 ng/mL（约0.6 microM）。还对与芒柄花黄素密切相关的三种异黄酮[大豆苷元（2）、鹰嘴豆芽素A（3）和染料木黄酮（4）]进行了评估，但它们的活性至少比芒柄花黄素低100倍。因此，芒柄花黄素（1）可能是开发新型抗贾第虫药物的一个有意义的先导化合物，或者作为新的作用机制靶点的研究探针。
