生物活性 | |||
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描述 | Telbivudine, an orally active thymidine nucleoside analog, is a potent antiviral inhibitor of hepatitis B virus (HBV) replication[3]. Telbivudine reverses B19V-induced dysregulation of BIRC3 (Baculoviral Inhibitor of apoptosis Repeat-Containing protein 3), thus, intervening in the apoptosis pathway and protecting susceptible cells from cell death[4]. Telbivudine given for 4 weeks resulted in an 8-log reduction of woodchuck hepatitis virus DNA, and a 3.8-log reduction of hepatitis B virus DNA in human. After 52 weeks of telbivudine treatment there was an approximate 6-log reduction of hepatitis B virus DNA levels, hepatitis B virus DNA became undetectable by PCR assay in 61% of patients. Its antiviral efficacy is significantly better than lamivudine[5]. In vitro assays revealed that telbivudine treatment induced TGF-β1 expression in human macrophagic cells. Telbivudine treatment enhanced the proportion of serum IgG-Fc agalactosylation in cirrhotic patients, which was associated with enhanced levels of TGF-β1 and IgG[6]. Telbivudine exerts endothelial-protective effects in B19V-infected endothelial cells and improves chronic myocarditis associated with B19V transcriptional activity[7]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.13mL 0.83mL 0.41mL |
20.64mL 4.13mL 2.06mL |
41.28mL 8.26mL 4.13mL |
参考文献 |
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