Helioxanthin 8-1 Chemical Properties

Melting point:

318-320 °C

Density 

1.548±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

Soluble in DMSO

form 

Powder

pka

10.56±0.20(Predicted)

color 

Light yellow to yellow

Helioxanthin 8-1 Usage And Synthesis

Uses

Helioxanthin 8-1 is an analogue of helioxanthin, exhibites significant in vitro anti-HBV/HCV/HSV-1/HIV activity with EC50 of >5/10/1.4/15 uM. IC50 value: >5/10/1.4/15 uM(HBV/HCV/HSV-1/HIV) [1] Target: Antiviral agent The cyclic hydrazide 28(Helioxanthin 8-1) showed the most potent antiHBV activity among those helioxanthin analogues tested. In addition, compound 28 exhibited moderately potent activity against HIV. It would therefore be promising to study helioxanthin analogues that contain a six-membered ring instead of the five-membered ring found in the lactam [1]. 8-1 exhibited effective inhibition on DHBV replication. The combination of 8-1 with 3TC resulted in additional anti-DHBV activity. Viral induced cells displayed higher susceptibility to 8-1 treatment than non-induced cells. HBV X protein might not be an essential factor in the initiation of the biological activity of 8-1, as demonstrated by its absence in DHBV [2].

Biological Activity

helioxanthin 8-1, an analogue of helioxanthin (ach126447), is an inhibitor of hbv and hiv virus with ec50 values of 0.03 μm and 2.7 μm, respectively [1].helioxanthin 8-1 is the cyclic hydrazide derivative of helioxanthin and has shown significant in vitro antivirus activity with ec50 values of 0.03 μm and 2.7 μm for hbv and hiv, respectively [1]. in the ds-tet5 cells, helioxanthin 8-1 can inhibit duck hepatitis b virus (dhbv) dna synthesis with a mean ic50 value of 0.25±0.05 μm. besides, in induced cells and non-induced ds-tet5 cells, helioxanthin 8-1 has cytotoxic effect with cc50 values of 18±2 μm and 45±3 μm, respectively, by using an mtt assay [2].

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] ying c1, tan s, cheng yc. helioxanthin analogue 8-1 inhibits duck hepatitis b virus replication in cell culture. antivir chem chemother. 2010;21(2):97-103.

Helioxanthin 8-1(840529-13-7)Related Product Information

• Helioxanthin derivative 5-4-2