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菘蓝根来源的芹菜素 B 体外抗人及禽源甲型和乙型流感病毒活性研究。

Antiviral activity of Isatis indigotica root-derived clemastanin B against human and avian influenza A and B viruses in vitro.

机构信息

Macau University of Science and Technology, Taipa, Macau, SAR, PR China.

出版信息

Int J Mol Med. 2013 Apr;31(4):867-73. doi: 10.3892/ijmm.2013.1274. Epub 2013 Feb 7.

DOI:10.3892/ijmm.2013.1274
PMID:23403777
Abstract

Clemastanin B, 7S,8R,8'R-(-)-lariciresinol-4,4'-bis-O-β-D-glucopyranoside, is one of the major lignans extracted from Isatis indigotica root (IIR). In this study, the anti-influenza activities of clemastanin B were evaluated in vitro. Clemastanin B was found to inhibit different subtypes of human (H1N1, including swine-origin H1N1; H3N2 and influenza B) and avian influenza viruses (H6N2, H7N3, H9N2) at different magnitudes of activity (IC50 0.087-0.72 mg/ml) while this compound was inactive against respiratory syncytial virus (RSV), adenovirus 3 (ADV3), parainfluenza virus 3 (PIV3), enterovirus 71 (EV71) and human rhinovirus (HRV). An apparent virus titer reduction was detected when MDCK cells were treated with clemastanin B after viral infection, particularly at the early stage, and the ribonucleoprotein (RNP) of the influenza virus was retained in the nucleus after treatment with clemastanin B. These results demonstrated that clemastanin B targets viral endocytosis, uncoating or RNP export from the nucleus. Furthermore, treatment with clemastanin B did not easily result in the emergence of viral drug resistance. The effects of clemastanin B demonstrated in this study may promote the antiviral study of IIR, but additional studies are required to define the anti-influenza mechanism(s).

摘要

荆芥宁 B,7S,8R,8'R-(-)-松脂醇-4,4'-二-O-β-D-吡喃葡萄糖苷,是从菘蓝根(IIR)中提取的主要木脂素之一。本研究评价了荆芥宁 B 的体外抗流感活性。荆芥宁 B 对不同亚型的人(H1N1,包括猪源 H1N1;H3N2 和 B 型流感)和禽流感病毒(H6N2、H7N3、H9N2)具有不同程度的抑制活性(IC50 为 0.087-0.72mg/ml),而该化合物对呼吸道合胞病毒(RSV)、腺病毒 3(ADV3)、副流感病毒 3(PIV3)、肠道病毒 71(EV71)和人鼻病毒(HRV)均无活性。当 MDCK 细胞在病毒感染后用荆芥宁 B 处理时,明显检测到病毒滴度降低,特别是在早期,并且用荆芥宁 B 处理后流感病毒的核糖核蛋白(RNP)保留在核内。这些结果表明荆芥宁 B 的作用靶点是病毒的内吞作用、脱壳或 RNP 从细胞核输出。此外,荆芥宁 B 的治疗不易导致病毒耐药性的出现。本研究中荆芥宁 B 的作用可能促进对菘蓝抗病毒的研究,但需要进一步研究以确定其抗流感机制。

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