In vitro pharmacodynamic evaluation of anti-HIV cholesteryl-phosphoryl zidovudine self-assemblies / 国际药学研究杂志

ABSTRACT

Objective To evaluate the anti-HIV activity of the self-assemblies of cholesteryl-phosphoryl zidovudine (CPZ) and provide evidence for the promising new anti-HIV drug. Methods CPZ self-assemblies were prepared. The MT4 cells infected by HIV-1 were the model to evaluate the anti-HIV activity of CPZ self-assemblies, which based on the generation of combined ceHs, was compared to that of the parent drug-zidovudine (AZT). The cytotoxicity of CPZ self-assemblies as evaluated by the MTT method. Phagocytosis of macrophage to CPZ self-assemblies was evaluated in RAW264. 7 ceHs. Results The anti-HIV activity of CPZ self-assemblies was much higher than that of AZT, with the half effective concentration (EC50) 1/10 to 1/50 that of AZT. The selectivity index (SI) was high, indicating that the self-assemblies were safe. Conclusion CPZ self-assemblies have high anti-HIV activity and is apromisinganti-HIV drug.