Antiviral effects of saikosaponins on human coronavirus 229E in vitro
Antiviral effects of saikosaponins on human coronavirus 229E in vitro
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DOI：
10.1111/j.1440-1681.2006.04415.x
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发表时间：
2006-07-01
影响因子：
2.9
通讯作者：
Lin, Chun-Ching
中科院分区：
文献类型：
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作者：
Cheng, Pei-Win;Ng, Lean-Teik;Lin, Chun-Ching
1.柴胡皂苷代表一组齐墩果烷衍生物，通常为糖苷，存在于许多植物科中。从药用植物如柴胡属分离的柴胡皂苷，异形虫属和玄参具有多种生物活性，特别是抗肝炎、肾炎、抗肝癌、抗炎、免疫调节和抗菌作用.本研究的目的是检测柴胡皂苷（A、B-2、C和D）的抗病毒活性及其作用方式。使用2，3-双[2-甲氧基-4-硝基-5-磺基苯基]-5-[（苯基氨基）羰基-2H-氢氧化四唑]（XTT）测定，结果显示所有测试的柴胡皂苷在0.25-25 μ mol/L的浓度下显示抗病毒活性，其中柴胡皂苷B-2的活性最强（IC 50 = 1.7 +/- 0.1 μ mol/L）。有趣的是，柴胡皂苷A（50%细胞毒性（CC 50）浓度= 228.1 +/- 3.8 μ mol/L;选择性指数（SI）= 26.6）和B-2（CC 50 = 383.3 +/- 0.2 μ mol/L; SI = 221.9）在达到抗病毒活性的浓度下对靶细胞均未表现出细胞毒性作用。在加入时间研究中，在感染前（-4至-1 h）、合并感染（0 h）和感染后（1-4 h）的不同时间加入6 μ mol/L的柴胡皂苷B-2后，显著抑制人冠状病毒229 E感染。此外，柴胡皂苷B-2对病毒的粘附和穿透也有抑制作用.目前的结果表明，柴胡皂苷B-2具有有效的抗病毒活性，其作用方式可能涉及干扰病毒复制的早期阶段，如病毒的吸收和穿透。
1. Saikosaponins represent a group of oleanane derivatives, usually as glucosides, that are found in a number of plant families. Saikosaponins isolated from medicinal plants such as Bupleurum spp., Heteromorpha spp. and Scrophularia scorodonia have been reported to possess various biological activities, specifically antihepatitis, antinephritis, antihepatoma, anti-inflammation, immunomodulation and antibacterial effects.2. The aim of the present study was to examine the anticoronaviral activity of saikosaponins (A, B-2, C and D) and their mode of action. Using the 2,3-bis[2-methoxy-4-nitro-5-sulfophenyl]-5-[(phenylamino) carbonyl-2H-tetrazolium hydroxide] (XTT) assay, results showed that all saikosaponins tested demonstrated antiviral activity at concentrations of 0.25-25 mu mol/L, with the strongest activity being noted for saikosaponin B-2 (IC50 = 1.7 +/- 0.1 mu mol/L). Interestingly, both saikosaponins A (50% cellular cytotoxicity (CC50) concentration = 228.1 +/- 3.8 mu mol/L; selectivity index (SI) = 26.6) and B-2 (CC50 = 383.3 +/- 0.2 mu mol/L; SI = 221.9) exhibited no cytotoxic effects on target cells at concentrations that achieved antiviral activity. In the time-of-addition studies, saikosaponin B-2, at 6 mu mol/L, significantly inhibited human coronavirus 229E infection following its addition at various time pre-infection (-4 to -1 h), coinfection (0 h) and post-infection (1-4 h). Furthermore, saikosaponin B-2 also showed an inhibitory effect on viral attachment and penetration.3. The present results indicate that saikosaponin B-2 has potent anticoronaviral activity and that its mode of action possibly involves interference in the early stage of viral replication, such as absorption and penetration of the virus.