Inhibition of neuraminidase activity by polyphenol compounds isolated from the roots of Glycyrrhiza uralensis |
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Authors: | Young Bae Ryu Jang Hoon Kim Su-Jin Park Jong Sun Chang Mun-Chual Rho Ki-Hwan Bae Ki Hun Park Woo Song Lee |
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Affiliation: | 1. Bioindustry Technology Research Center and AI Control Material Research Center, Korea Research Institute of Bioscience and Biotechnology, Jeongeup 580-185, Republic of Korea;2. Division of Applied Life Science (BK 21 Program), EB-NCRC, Institute of Agriculture and Life Science, Graduate School of Gyeongsang National University, Jinju 660-701, Republic of Korea;3. College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea |
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Abstract: | 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, IC50 = 9.0 μM) and glycyrol (14, IC50 = 3.1 μM) 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. |
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