Recent studies indicated that andrographolide was a potential anti-HIV therapeutic agent. In the paper, the synthesis of a series of andrographolide derivatives was described and their anti-HIV activities were evaluated in vitro. As compared with TI, compounds 5c, 5d and 5i showed moderate inhibitory activities on the cytopathic effect with TI above 10. Among the derivatives, compound 5i was the best one with TI > 51.
Keywords: Andrographolide, anti-HIV, derivatives, synthesis, cytopathic effect, HIV/AIDS, alkaloids, polysaccharides, flavonoids, triterpenes, lactones, sapon-ins, Andrographis paniculata, protein-mediated syncytia, HL60 cells, CD4+ lymphocyte level, HIV-1 RNA, lipopoly-saccharides (LPS)-induced tumor necrosis factor, interleukin-6, cyclooxygenase-2, acid anhydride, DMAP, CH2Cl2, propionic anhydride, hexanoic anhydride, benzoyl chloride, triphenylchloromethane, methylmorpholine, dicyclohexylcarbodiimide, C8166 cells, therapeutic index, anti-HIV-1 effects, hin-layer chromatography, DMSO, fetal bovine serum, 96-well microtiter plate, HIV-1 tissue culture infections dose
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