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首页> 外文期刊>Medicinal chemistry >Bicyclol: a novel drug for treating chronic viral hepatitis B and C.
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Bicyclol: a novel drug for treating chronic viral hepatitis B and C.

机译：双环醇：一种用于治疗慢性乙型和丙型病毒性肝炎的新型药物。

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Chronic viral hepatitis B and C are diseases worldwide. At present, the number of effective and safe drugs for treatment of HBV and HCV is still limited. In order to develop novel anti-viral hepatitis drug, a number of analogues of the active component schizandrin C from Fructus Schiznadrae, a Chinese herb used in the therapy of viral hepatitis, were synthesized. Bicyclol, one of the analogues, was demonstrated to have actions of anti-hepatitis virus replication in duck hepatitis model and 2.2.15 cell line, anti-experimental liver injury induced by hepatotoxins such as CCl4, acetaminophen and ConA, and anti-liver fibrosis in rats and mice. The active mechanism of bicyclol might be anti-apoptosis of hepatocytes through multiple signaling pathways mainly inducing the expressions of hepatic heat shock proteins (HSP27 and HSP70), molecular chaperons. Clinical trial was performed by double blind, randomized and positive control or placebo method in multi-medical centers in China. Patients received bicyclol 25mg thrice daily for six months, then stopped treatment and followed up for 3 months. Oral administration of bicyclol normalized the elevated serum transaminases (ALT, AST) by approximately 50% in chronic viral hepatitis B and C, and also showed certain level of inhibiting HBV and HCV replication. No noticeable adverse reaction has been observed. In combination therapy of bicyclol with interferon alpha, lamivudine and adefovir dipivoxil in HBV or HCV, bicyclol may potentiate the anti-viral efficacy and reduce YMDD mutant and side effects. In 2004 China FDA issued license to manufacture bicyclol. Since then bicyclol has been widely used to treat chronic HBV and HCV in China.
机译：慢性乙型和丙型病毒性肝炎是全世界的疾病。目前，用于治疗HBV和HCV的有效和安全的药物数量仍然有限。为了开发新的抗病毒性肝炎药物，合成了许多来自于Fructus Schiznadrae（一种用于治疗病毒性肝炎的中草药）的活性成分五味子素C的类似物。双环醇是一种类似物，在鸭肝炎模型和2.2.15细胞系中具有抗肝炎病毒复制的作用，由肝毒素如CCl4，对乙酰氨基酚和ConA诱导的抗实验肝损伤以及抗肝纤维化的作用。在大鼠和小鼠中。双环醇的活性机制可能是通过多种信号通路抗肝细胞凋亡，主要诱导肝热休克蛋白（HSP27和HSP70），分子伴侣蛋白的表达。通过双盲，随机和阳性对照或安慰剂方法在中国的多个医疗中心进行了临床试验。患者每天三次三次服用双环25mg，持续六个月，然后停止治疗并随访3个月。在慢性乙型和丙型肝炎病毒中口服双环醇可使血清转氨酶（ALT，AST）升高约50％，并显示出一定程度的抑制HBV和HCV复制。没有观察到明显的不良反应。在双环酚与干扰素α，拉米夫定和阿德福韦酯联用治疗HBV或HCV中，双环酚可增强抗病毒效力并降低YMDD突变体和副作用。 2004年，中国食品药品监督管理局（FDA）颁发了生产双环醇的许可。从那时起，双环醇在中国被广泛用于治疗慢性HBV和HCV。

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