Phenylpropanoid glucosides from Tadehagi triquetrum inhibit oxLDL-evoked foam cell formation through modulating cholesterol homeostasis in RAW264.7 macrophages.

The phenylpropanoid glucosides from Tadehagi triquetrum were found to be beneficial to glucose and lipid metabolism in vitro. Herein, we investigated the effects of these compounds on oxidised low-density lipoprotein (oxLDL)-induced foam cell formation in RAW264.7 macrophages, aiming to evaluate their potential utility in prevention of atherosclerosis. Our results showed that three out of seven phenylpropanoid glucosides significantly inhibited oxLDL-evoked foam cell formation. These three compounds remarkably inhibited cholesterol influx and enhanced cholesterol efflux. Treatment with compounds 3, 4 and 7 significantly down-regulated the expression of scavenge receptors 1 (SR-1) and cluster of differentiation 36 (CD36) and increased the expression ATP-binding cassette transporters A1 and G1 (ABCA1 and ABCG1). Analyses of structure-activity relationships revealed that cinnamyl group was the most pivotal group for their activities. This work provided phenomenon that these phenylpropanoid glucosides are effective regulator of cholesterol influx/efflux and may be useful in leading for development of anti-atherosclerotic agents.