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Overview
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Background
Helioxanthin derivative 5-4-2, an analogue of helioxanthin (ACH126447), is a small-molecule inhibitor of HBV, HSV-1and HSV-2 virus with EC50 values of 0.08 μM, 0.29 μM and 0.16 μM, respectively [1].Helioxanthin derivative 5-4-2 is a lactam and has been reported to inhibit the HBV DNA and RNA and viral protein expression [2]. Helioxanthin derivative 5-4-2 has significant anti-virus activity with EC50 values of 0.08 μM, 0.29 μM and 0.16 μM for HBV(hepatitis B virus), HSV-1(herpes simplex virus type 1) and HSV-2(herpes simplex virus type 2), respectively [1]. In addition, Helioxanthin derivative 5-4-2 inhibited HBV replication by post-transcriptional down-regulation of necessary transcription factors [3]. Helioxanthin derivative 5-4-2 has also exhibited potent anti-HCV (hepatitis C virus) activity with 55% inhibition at 1.0 μM and 80%inhibition at 3.0 μM [1].
[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.
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