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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Inhibition of neuraminidase activity by polyphenol compounds isolated from the roots of Glycyrrhiza uralensis.
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Inhibition of neuraminidase activity by polyphenol compounds isolated from the roots of Glycyrrhiza uralensis.

机译:从甘草根中分离出的多酚化合物对神经氨酸酶活性的抑制作用。

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摘要

We isolated 18 polyphenols with neuraminidase inhibitory activity from methanol extracts of the roots of Glycyrrhiza uralensis. These polyphenols consisted of four chalcones (1-4), nine flavonoids (5-13), four coumarins (14-17), and one phenylbenzofuran (18). When we tested the effects of these individual compounds and analogs thereof on neuraminidase activation, we found that isoliquiritigenin (1, IC(50)=9.0 microM) and glycyrol (14, IC(50)=3.1 microM) had strong inhibitory activity. Structure-activity analysis showed that the furan rings of the polyphenols were essential for neuraminidase inhibitory activity, and that this activity was enhanced by the apioside group on the chalcone and flavanone backbone. In addition, the presence of a five-membered ring between C-4 and C-2' in coumestan was critical for neuraminidase inhibition. All neuraminidase inhibitors screened were found to be reversible noncompetitive inhibitors.
机译:我们从甘草根的甲醇提取物中分离了18种具有神经氨酸酶抑制活性的多酚。这些多酚由四个查耳酮(1-4),九个类黄酮(5-13),四个香豆素(14-17)和一个苯基苯并呋喃(18)组成。当我们测试这些单独的化合物及其类似物对神经氨酸酶活化的影响时,我们发现异黄体生成素(1,IC(50)= 9.0 microM)和甘油(14,IC(50)= 3.1 microM)具有很强的抑制活性。结构活性分析表明,多酚的呋喃环对于神经氨酸酶抑制活性是必不可少的,并且查耳酮和黄烷酮骨架上的apioside基团增强了该活性。此外,香豆素中C-4和C-2'之间存在一个五元环,这对抑制神经氨酸酶至关重要。发现所有筛选的神经氨酸酶抑制剂都是可逆的非竞争性抑制剂。

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