Tenofovir is a nucleotide analogue reverse transcriptase inhibitors (NRTIs) which reduces the viral cytopathic effect of HIV-1 (IIIB), HIV-2(ROD) with EC50 of 1.15 μg/ml and 1.12 μg/ml.
Tenofovir demonstrates cytotoxic effects in HK-2 cells, with IC50 values of 9.21 μM at 48 hours and 2.77 μM at 72 hours in MTT assays. It lowers ATP levels, increases oxidative stress and protein carbonylation, and induces apoptosis through mitochondrial damage in these cells [1]. Tenofovir combined with M48U1, each formulated in 0.25% HEC, inhibits replication of both R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, including several laboratory and patient-derived HIV-1 strains. This combination exhibits synergistic antiretroviral effects against R5-tropic HIV-1BaL infection and is non-toxic to PBMCs [2].
体内研究
Tenofovir Disoproxil Fumarate administered at doses of 20, 50, 140, or 300 mg/kg shows dose-dependent effectiveness in preventing vaginal HIV transmission in BLT humanized mice, significantly reducing HIV transmission at 50, 140, and 300 mg/kg [3].
Tenofovir Disoproxil Fumarate (0.5, 1.5, or 5.0 mg/kg/day, pO.) leads to a dose-dependent reduction in serum viremia in woodchucks with chronic WHV infection and is safe and effective in this model [4].
体外研究
Tenofovir demonstrates cytotoxic effects in HK-2 cells, with IC50 values of 9.21 μM at 48 hours and 2.77 μM at 72 hours in MTT assays. It lowers ATP levels, increases oxidative stress and protein carbonylation, and induces apoptosis through mitochondrial damage in these cells [1].
Tenofovir combined with M48U1, each formulated in 0.25% HEC, inhibits replication of both R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, including several laboratory and patient-derived HIV-1 strains. This combination exhibits synergistic antiretroviral effects against R5-tropic HIV-1BaL infection and is non-toxic to PBMCs [2].
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