Anti-human immunodeficiency virus activity of polyhydroxy fullerenes in vitro

Polyhydroxy fullerenes (henceforth fullerenols) prepared by three different methods were evaluated for antiviral activity in cell culture. While all the fullerenols were active against HIV-1 in acutely infected primary human lymphocytes (EC50 values of 15-42 mu M in PBMC), none were active against chronically infected H9 cells. The cytotoxicity of the fullerenols ranged from low to very low in PBMC and Vero cells (IC50 greater than or equal to 68-100 mu M), but was more varied in CEM cells (IC50 = 3.4 to > 100 mu M). None of the compounds were as active in PBMC or H9 cells as those for the previously reported Wudl fulleroid and 3'-azido-3'-deoxythymidine (AZT). Two fullerenols had low but selective activity against herpes simplex virus type 1 in Vero cells.