Helioxanthin derivative 5-4-2

Helioxanthin derivative 5-4-2 is an analogue of helioxanthin, exhibites significant in vitro anti-HBV activity with EC50 of 0.08 uM in HepG2.2.15 cells. IC50 value: 0.08 uM (EC50) [1][2] Target: Anti-HBV Helioxanthin derivative 5-4-2 had potent anti-HBV activities in HepG2.2.15 cells, with the EC50s of 1 and 0.08 microM, respectively. The lamivudine-resistant HBV, L526M/M550V double mutant strain, was also sensitive to helioxanthin and 5-4-2. This class of compounds not only inhibited HBV DNA, but also decreased HBV mRNA and HBV protein expression. The EC50 of HBV DNA inhibition was consistent with the EC50 of HBV 3.5 Kb transcript inhibition, which was 1 and 0.09 microM for helioxanthin and 5-4-2 respectively.

[1]Yeo H, et al. Synthesis and antiviral activity of helioxanthin analogues. J Med Chem. 2005 Jan 27;48(2):534-46.|[2]Li Y, et al. Inhibition of hepatitis B virus gene expression and replication by helioxanthin and its derivative. Antivir Chem Chemother. 2005;16(3):193-201.