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首页> 外文期刊>Bioorganic and medicinal chemistry >Neuraminidase inhibitory activities of flavonols isolated from Rhodiola rosea roots and their in vitro anti-influenza viral activities.
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Neuraminidase inhibitory activities of flavonols isolated from Rhodiola rosea roots and their in vitro anti-influenza viral activities.

机译：玫瑰红景天根中黄酮醇的神经氨酸酶抑制活性及其体外抗流感病毒活性。

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摘要

Five flavonols (3, 5, and 9-11) were isolated from Rhodiola rosea, and compared with commercially available flavonoids (1, 2, 4, 6-8, and 12-14) to facilitate analysis of their structure-activity relationship (SAR). All compounds (1-14) showed neuraminidase inhibitory activities with IC(50) values ranging from 0.8 to 56.9 microM. The in vitro anti-influenza virus activities of flavonoids 1-6, 8-12, and 14 were evaluated using two influenza viral strains, H1N1 (A/PR/8/34) and H9N2 (A/Chicken/Korea/MS96/96), testing their ability to reduce virus-induced cytopathic effect (CPE) in MDCK cells. We found that the activity of these compounds ranged from 30.2 to 99.1 microM against H1N1- and 18.5 to 133.6 microM against H9N2-induced CPE. Of compounds 1-14, gossypetin (6) exhibited the most potent inhibitory activity, with IC(50) values of 0.8 and 2.6 microM on neuraminidases from Clostridium perfringens and recombinant influenza virus A (rvH1N1), respectively. In contrast, kaempferol (3) exhibited the highest activity against two influenza viruses, H1N1 and H9N2 with EC(50) values of 30.2 and 18.5 microM, respectively. Activity depended on the position and number of hydroxy groups on the flavonoids backbone. In kinetic studies, all isolated compounds behaved as noncompetitive inhibitors.
机译：从玫瑰红景天中分离出5种黄酮醇（3、5和9-11），并与市售的黄酮类化合物（1、2、4、6-8和12-14）进行比较，以方便分析其结构-活性关系（ SAR）。所有化合物（1-14）均显示神经氨酸酶抑制活性，IC（50）值范围为0.8至56.9 microM。使用两种流感病毒株H1N1（A / PR / 8/34）和H9N2（A / Chicken / Korea / MS96 / 96）评价了类黄酮1-6、8-12和14的体外抗流感病毒活性），测试它们在MDCK细胞中降低病毒诱导的细胞病变效应（CPE）的能力。我们发现这些化合物的抗H1N1活性为30.2至99.1 microM，抗H9N2诱导的CPE为18.5至133.6 microM。在化合物1-14中，棉酚（6）表现出最强的抑制活性，对产气荚膜梭菌和重组流感病毒A（rvH1N1）的神经氨酸酶的IC（50）值分别为0.8和2.6 microM。相反，山奈酚（3）对两种流感病毒H1N1和H9N2表现出最高的活性，EC（50）值分别为30.2和18.5 microM。活性取决于类黄酮主链上羟基的位置和数量。在动力学研究中，所有分离的化合物均表现为非竞争性抑制剂。

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