新型亚氨基取代 1,4-萘醌衍生物的抗锥虫活性和细胞毒性。
Antitrypanosomal activities and cytotoxicity of some novel imido-substituted 1,4-naphthoquinone derivatives.
机构信息
Department of Biology, Howard University, Washington DC 20059, USA.
出版信息
Arch Pharm Res. 2012 Jan;35(1):27-33. doi: 10.1007/s12272-012-0103-1. Epub 2012 Feb 2.
Abstract
The antitrypanosomal activities, cytotoxicity, and selectivity indices of eleven imido-substituted 1,4-naphthoquinone derivatives and nifurtimox have been studied. Compared to nifurtimox (IC(50) = 10.67 μM), all the imido-naphthoquinone analogs (IMDNQ1-IMDNQ11) are more potent on Trypanosoma cruzi with IC50 values ranging from 0.7 μM to 6.1 μM (p < 0.05). Studies of the cytotoxic activities of these compounds on a Balb/C 3T3 mouse fibroblast cell line revealed that four of these compounds, IMDNQ1, IMDNQ2, IMDNQ3, and IMDNQ10 displayed selectivity indices of 60.25, 53.97, 31.83, and 275.3, respectively, rendering them significantly (p < 0.05) more selective in inhibiting the parasite growth than nifurtimox (selectivity index = 10.86).
摘要
研究了 11 种亚氨基取代的 1,4-萘醌衍生物和硝呋替莫的抗锥虫活性、细胞毒性和选择性指数。与硝呋替莫（IC（50）= 10.67 μM）相比，所有亚氨基萘醌类似物（IMDNQ1-IMDNQ11）对 Trypanosoma cruzi 的活性更强，IC50 值范围为 0.7 μM 至 6.1 μM（p < 0.05）。对这些化合物在 Balb/C 3T3 小鼠成纤维细胞系上的细胞毒性活性的研究表明，其中 4 种化合物 IMDNQ1、IMDNQ2、IMDNQ3 和 IMDNQ10 的选择性指数分别为 60.25、53.97、31.83 和 275.3，分别比硝呋替莫（选择性指数 = 10.86）更显著地（p < 0.05）选择性抑制寄生虫生长。
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