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].

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.