Helioxanthin derivative 5-4-2

Helioxanthin derivative 5-4-2是helioxanthin (ACH126447)的类似物,是HBV\HSV-1和HSV-2的小分子抑制剂,EC50值分别为0.08 μM\0.29 μM和0.16 μM [1].

Helioxanthin derivative 5-4-2是一种内酰胺,对HBV的 DNA\RNA及病毒蛋白表达具有抑制作用[2].Helioxanthin derivative 5-4-2具有显著的抗病毒活性,对HBV(肝炎B 病毒), HSV-1(1型单纯疱疹病毒)和HSV-2(2型单纯疱疹病毒)的EC50值分别为0.08 μM\0.29 μM 和0.16 μM [1] .另外,Helioxanthin derivative 5-4-2通过对必需转录因子的转录后下调,抑制HBV复制[3].Helioxanthin derivative 5-4-2具有有效抗HCV(肝炎病毒C)活性,1.0 μM能够抑制 55%,3.0 μM能够抑制80% [1].

参考文献：
[1].  Yeo H1, Li Y, Fu L, Zhu JL, Gullen EA, Dutschman GE, Lee Y, Chung R, Huang ES, Austin DJ, Cheng YC. Synthesis and antiviral activity of helioxanthin analogues. J Med Chem. 2005 Jan 27;48(2):534-46.
[2].  Li Y1, Fu L, Yeo H, Zhu JL, Chou CK, Kou YH, Yeh SF, Gullen E, Austin D, ChengYC.Inhibition of hepatitis B virus gene expression and replication by helioxanthin and its derivative. Antivir Chem Chemother. 2005;16(3):193-201.
[3].  Stein LL1, Loomba R. Drug targets in hepatitis B virus infection. Infect Disord Drug Targets. 2009 Apr;9(2):105-16.