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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >New monoterpene glycosides and phenolic compounds from Distylium racemosum and their inhibitory activity against ribonuclease H.
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New monoterpene glycosides and phenolic compounds from Distylium racemosum and their inhibitory activity against ribonuclease H.

机译:来自Ribonuclease的抑制活性的新型单萜甙和酚类化合物及其对核糖核酸酶H的抑制活性。

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摘要

Two new monoterpene glycosides, distyloside A-B (1-2), and a new megastigmane glucoside, iso-dihydrodendranthemoside A (3) were isolated from twigs and leaves of Distylium racemosum, along with five known phenolic compounds (4-8). The structures were established via spectroscopic techniques and chemical transformations, and the absolute stereochemistry of 3 was determined by Mosher's esterification. A homogeneous fluorescence resonance energy transfer (FRET) quenching assay was used to determine the inhibitory activity of isolates (1-8) on the ribonuclease H enzymes from HIV-1, 2, human, and Escherichia coli. Among them, 6''-O-galloylsalidroside (6) showed potent inhibitory effects with an IC(50) value of 3.5 muM on HIV-2, and 1.7 muM on human RNase H, respectively.
机译:两种新的单萜糖苷,二硫代吡喃(1-2)和新的Megastigmane葡萄糖苷,异磷脂A(3)分离出卵子瘤的树枝和叶片,以及五种已知的酚类化合物(4-8)。 通过光谱技术和化学转化建立了结构,并通过Mosher酯化确定了3的绝对立体化学。 均匀的荧光共振能量转移(FRET)猝灭测定用于确定HIV-1,2,人和大肠杆菌的核糖核酸酶H酶对中间株(1-8)的抑制活性。 其中,6' - o-galloylsalloside(6)分别显示出与HIV-2的IC(50)值为3.5米的IC(50)值,以及1.7毫安的人RNase H.

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