Macrophages were incubated with 125I-VLDL for 5 h in presence or absence of lipoprotein lipase (LPL) inhibitor, benzene boronic acid (BBA). Both the uptake and degradation of 125I-VLDL by macrophages were saturable, and the uptake and degradation curves were virtually identical. When macrophages were incubated with 125I-VLDL for 10 h in presence of BBA, the uptake and degradation of 125I-VLDL were still saturable. However, in absence of BBA, the uptake and degradation were no longer saturable. The results suggest that with macrophages incubated with VLDL for a shorter period, VLDL was taken up predominantly via receptor pathway, with a longer period of incubation, LPL played a striking role in uptake of VLDL.