Biological Activity
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].
References
[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.
