0000000000398643
AUTHOR
A Moran
Clinical concentrations of efavirenz (EFV) reduce cellular proliferation and viability in several human cell lines
Results MTT assays upon 24 h of culture in the presence of the drug revealed reduced viability in the human hepatoma cell line Hep3B (significant for all three concentrations and calculated as 84.59 ± 8.82% decrease for 50 μM EFV), human cervix carcinoma cell line HeLa (71.92 ± 5.49% reduction for 50 μM EFV) and primary Human Umbilical Vein Endothelial cells (HUVEC), (96.76 ± 0.27% reduction for 50 μM EFV). This result was corroborated with 3day-proliferation experiments in which Hep3B were exposed to different concentrations of EFV; a significant reduction (60.1 ± 6.54% after 3 days) was detected with 25 μM EFV whereas cytotoxicity (97.01 ± 1.13% reduction) was observed with 50 μM, however…
Enhanced oxidative stress and increased mitochondrial mass during Efavirenz-induced apoptosis in human hepatic cells
BACKGROUND AND PURPOSE Efavirenz (EFV) is widely used in the treatment of HIV-1 infection. Though highly efficient, there is growing concern about EFV-related side effects, the molecular basis of which remains elusive. EXPERIMENTAL APPROACH In vitro studies were performed to address the effect of clinically relevant concentrations of EFV (10, 25 and 50 µM) on human hepatic cells. KEY RESULTS Cellular proliferation and viability were reduced in a concentration-dependent manner. Analyses of the cell cycle and several cell death parameters (chromatin condensation, phosphatidylserine exteriorization, mitochondrial proapoptotic protein translocation and caspase activation) revealed that EFV trig…