Differential cellular uptake and metabolism of curcuminoids in monocytes/macrophages: regulatory effects on lipid accumulation (1044.5)

Abstract

Curcumin (CUR), also known as diferuloylmethane, is obtained from the rhizome of turmeric (Curcuma Longa L.) and is present in dried turmeric powder at a concentration of 2‐5%. CUR has been shown to have several physiological activities, and we have previously shown that CUR may increase lipid accumulation in cultured THP‐1 monocytes/macrophages, but tetrahydrocurcumin (THC), an in vivo metabolite of CUR, had no such effect. In the present study, we have hypothesized that different cellular uptake and/or metabolism of CUR and THC might be a possible explanation for the previously observed differences in their effects on lipid accumulation in THP‐1. Chromatography with tandem mass spectrometry revealed that CUR was readily taken up by THP‐1 monocytes/macrophages and slowly metabolized to hexahydrocurcumin sulfate. In contrast, uptake of THC was low. In parallel with CUR uptake, an increased lipid uptake was observed in THP‐1 macrophages but not with THC or with another CUR metabolite and structurally related compounds. From these results, it is possible to deduce that CUR and THC are taken up and metabolized differently in THP‐1 cells, which determine their biological activity. The remarkable differential cellular uptake of CUR, relative to THC and other similar molecules, may imply that the CUR uptake into cells may occur via a transporter.Grant Funding Source: USDA agreement# 58‐1950‐0‐014