Yang Xian-Ying, Liu Ai-Lin, Liu Shu-Jing, Xu Xiao-Wei, Huang Lin-Fang
Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100193, China.
College of Pharmacy and Chemistry, Dali University, Yunnan 671000, China.
Molecules. 2016 Aug 27;21(9):1138. doi: 10.3390/molecules21091138.
To screen for influenza virus neuraminidase inhibition and to provide a reference for the clinical treatment of influenza using traditional Chinese medicines (TCM). In this study, 421 crude extracts (solubilized with petroleum ether, ethanol, ethyl acetate, and aqueous solvents) were obtained from 113 TCM. The medicine extracts were then reacted with oseltamivir, using 2'-(4-methylumbelliferyl)-α-D-N-acetylneuraminic acid (MUNANA) as the substrate, to determine influenza virus neuraminidase activity using a standard fluorimetric assay. It was found that Chinese medicine extracts from Pyrola calliantha, Cynanchum wilfordii, Balanophora involucrata and Paeonia delavayi significantly inhibited neuraminidase activity at a concentration of 40 μg/mL. Dose-dependent inhibitory assays also revealed significant inhibition. The IC50 range of the TCM extracts for influenza virus neuraminidase was approximately 12.66-34.85 μg/mL, respectively. Some Chinese medicines have clear anti-influenza viral effects that may play an important role in the treatment of influenza through the inhibition of viral neuraminidase. The results of this study demonstrated that plant medicines can serve as a useful source of neuraminidase (NA) inhibitors and further investigation into the pharmacologic activities of these extracts is warranted.
筛选流感病毒神经氨酸酶抑制作用，为中医药治疗流感提供临床参考。本研究从113种中药中获得了421种粗提物（用石油醚、乙醇、乙酸乙酯和水性溶剂溶解）。然后将药物提取物与奥司他韦反应，以2'-(4-甲基伞形酮基)-α-D-N-乙酰神经氨酸（MUNANA）为底物，采用标准荧光测定法测定流感病毒神经氨酸酶活性。发现鹿蹄草、白薇、蛇菰和滇牡丹的中药提取物在浓度为40μg/mL时能显著抑制神经氨酸酶活性。剂量依赖性抑制试验也显示出显著抑制作用。中药提取物对流感病毒神经氨酸酶的IC50范围分别约为12.66 - 34.85μg/mL。一些中药具有明确的抗流感病毒作用，可能通过抑制病毒神经氨酸酶在流感治疗中发挥重要作用。本研究结果表明，植物药可作为神经氨酸酶（NA）抑制剂的有用来源，有必要进一步研究这些提取物的药理活性。
