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A New Saponin with Anti-HIV-1 Protease Activity from Acacia pennata

机译:具有来自金合欢Pennata的抗HIV-1蛋白酶活性的新皂苷

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摘要

We investigated the phytochemicals from an ethanol extract of Acacia pennata (L.) Willd stems, a Vietnam medicinal plant, which led to the isolation of a new saponin termed 21 beta-O-[(2E)-6-hydroxyl-2,6-dimethy1-2,7-octadienoyl] pitheduloside G (1), as well as pitheduloside G (2), a known saponin. The structures of compounds 1 and 2 were elucidated via spectroscopy and compared with those reported in the literature. The isolates (1 and 2) were tested for their inhibitory effects on human immunodeficiency virus type 1 (HIV-1) protease (PR). We found that the new compound, 21 beta-O-[(2E)-6-hydroxy1-2,6-dimethyl-2,7-octadienoyl] pitheduloside G (1), possessed potent anti-HIV-1 PR activity, with a half-maximum inhibitory concentration (IC50) value of 2.0 +/- 0.2 mu M. In contrast, pitheduloside G (2) exhibited much less inhibition, with an IC50 value of 18 +/- 0.5 mu M. Both compounds were nontoxic in human embryonic kidney 293T cells at concentrations effective against HIV-1 PR. This is the first report regarding the isolation of an anti-HIV-1 PR compound (1) from an Acacia plant species.
机译:我们研究了越南药用植物的乙醇提取物中的乙醇提取物,该植物的乙醇提取物导致了将新的Saponin称为21β-O - [(2E)-6-羟基-2,6 -dimethy1-2,7-odayInoyl] Pitheduloside g(1),以及甲磺酰基G(2),已知的皂苷。通过光谱学阐明化合物1和2的结构,与文献中报道的那些相比。测试分离物(1和2)对人免疫缺陷病毒型1(HIV-1)蛋白酶(PR)的抑制作用。我们发现新化合物,21β-O - [(2E)-6-羟基1-2,6-二甲基-2,7-十八烯酰]甲硅醚G(1)具有效率的抗HIV-1 PR活性,具有相比之下,甲硝基钠G(2)的半最大抑制浓度(IC50)值为2.0 +/-0.2μm。抑制得多,IC50值为18 +/-0.5μm。两种化合物都在毒性中人胚胎肾293T细胞在浓度上有效对抗HIV-1 PR。这是关于从合欢植物物种中分离抗HIV-1 Pr复合物(1)的第一个报告。

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