Robustaflavone, a potential non-nucleoside anti-hepatitis B agent.
Robustaflavone, a potential non-nucleoside anti-hepatitis B agent.
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DOI：
10.1016/s0166-3542(98)00033-3
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发表时间：
1998-08
影响因子：
7.6
通讯作者：
D. Zembower;Y. M. Lin;M. Flavin;F. C. Chen;B. Korba
中科院分区：
文献类型：
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作者：
D. Zembower;Y. M. Lin;M. Flavin;F. C. Chen;B. Korba
鲁布他黄酮是一种从漆树中分离出来的天然双黄酮类化合物，被发现是 2.2.15 细胞中乙型肝炎病毒 (HBV) 复制的有效抑制剂，有效浓度 (EC50) 为 0.25 μM，选择性指数 (SI, IC50/EC90) 为 153。 鲁布他黄酮六乙酸酯抑制 HBV 复制，EC50 为 0.73 μM，但浓度高达 1000 μM 时未表现出细胞毒性。鲁棒黄酮与喷昔洛韦和拉米夫定的组合显示出协同抗HBV活性，当组合比率与EC50效价比率相似时具有最显着的效果。因此，鲁棒黄酮和喷昔洛韦 1:1 组合的 EC50 为 0.11 μM，SI 为 684，而鲁棒黄酮和拉米夫定 10:1 组合的 EC50 为 0.054 μM，SI 为 894。使用 Combostat® 程序对组合数据进行统计分析，证实鲁棒黄酮与喷昔洛韦和拉米夫定均表现出协同作用。拉米夫定。
Robustaflavone, a naturally occurring biflavanoid isolated from Rhus succedanea, was found to be a potent inhibitor of hepatitis B virus (HBV) replication in 2.2.15 cells, with an effective concentration (EC50) of 0.25 μM, and a selectivity index (SI, IC50/EC90) of 153. Robustaflavone hexaacetate inhibited HBV replication with an EC50of 0.73 μM, but exhibited no cytotoxicity at concentrations up to 1000 μM. Combinations of robustaflavone with penciclovir and lamivudine displayed synergistic anti-HBV activity, having the most pronounced effects when the combination ratios were similar to the ratio of EC50potencies. Thus, a 1:1 combination of robustaflavone and penciclovir exhibited an EC50of 0.11 μM and an SI of 684, while a 10:1 combination of robustaflavone and lamivudine exhibited an EC50of 0.054 μM and an SI of 894. Statistical analyses of the combination data using the Combostat® program confirmed that robustaflavone exhibited synergism with both penciclovir and lamivudine.