H Cao1, P Tao. 1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.
Abstract
OBJECTIVE: To find out reliable index for evaluating the anti-hepatitis B virus (HBV) effects in vitro of lamivudine (3TC) and other five anti-HBV drugs. METHODS: The contents of human hepatitis B surface antigen (HBsAg), hepatitis B e antigen (HBeAg) and hepatitis B virus DNA (HBV DNA) in the culture supernatant of 2.2.15 cell line transfected with hepatitis B virus gene were tested after the six anti-hepatitis B virus drugs were added respectively, and the accordance of different indexes was compared. RESULTS: All six drugs, within a certain range, exercised only weak or no inhibitive effect on extracellular HBsAg and HBeAg secreted by 2.2.15 cell line. Lamivudine and 2 3-dideoxy-3-fluoroguanosine (FLG) significantly inhibited the level of HBV DNA, with the 50% inhibition concentration(IC50) of 0.31 mumol/L and 0.53 mumol/L respectively. Acyclovir (ACV) and interferon-alpha(IFN-alpha) also inhibited the HBV DNA with the IC50 of 0.33 mmol/L and 96.18 U/ml respectively. Phosphonoformate (PFA) and ribavirin (RBV) showed none effect on HBV DNA content even at the maximum non-toxic concentrations. CONCLUSION: There is not accordance between the expression activities of proteins of HBsAg and HBeAg and the inhibition of HBV DNA level. HBV DNA level better reflexes the inhibitive effect of different drugs and can be used as an important index for evaluation of anti-HBV effect in vitro.
OBJECTIVE: To find out reliable index for evaluating the anti-hepatitis B virus (HBV) effects in vitro of lamivudine (3TC) and other five anti-HBV drugs. METHODS: The contents of humanhepatitis B surface antigen (HBsAg), hepatitis B e antigen (HBeAg) and hepatitis B virus DNA (HBV DNA) in the culture supernatant of 2.2.15 cell line transfected with hepatitis B virus gene were tested after the six anti-hepatitis B virus drugs were added respectively, and the accordance of different indexes was compared. RESULTS: All six drugs, within a certain range, exercised only weak or no inhibitive effect on extracellular HBsAg and HBeAg secreted by 2.2.15 cell line. Lamivudine and 2 3-dideoxy-3-fluoroguanosine (FLG) significantly inhibited the level of HBV DNA, with the 50% inhibition concentration(IC50) of 0.31 mumol/L and 0.53 mumol/L respectively. Acyclovir (ACV) and interferon-alpha(IFN-alpha) also inhibited the HBV DNA with the IC50 of 0.33 mmol/L and 96.18 U/ml respectively. Phosphonoformate (PFA) and ribavirin (RBV) showed none effect on HBV DNA content even at the maximum non-toxic concentrations. CONCLUSION: There is not accordance between the expression activities of proteins of HBsAg and HBeAg and the inhibition of HBV DNA level. HBV DNA level better reflexes the inhibitive effect of different drugs and can be used as an important index for evaluation of anti-HBV effect in vitro.