Abstract:Stevioside is demonstrated to regulate the cholesterol levels in body. The steviol is the main natural hydrolysate of stevioside in the intestine. The regulation of adenosine triphosphate binding cassette transporter A1 protein (ABCA1) in mouse macrophages J774A via steviol was studied and its possible molecular mechanism was investigated. The conditions and concentration of steviol were first established by MTT method. The detection of western blot, immunofluorescence and quantitative fluorescence PCR confirmed that steviol could significantly increase the expression of ABCA1 at protein and gene transcription level in collaboration with 8-(4-chlorophenylthio) adenosine 3',5'-cyclic monophosphate (CPT), the analogue of cyclic adenosine monophosphate (cAMP). Moreover, steviol could significantly up-regulate the expression levels of both mRNA and protein in upstream regulatory genes LXRα and PPARα of ABCA1, however, insignificant regulation on the expression of PPARγ was observed. The regulation of the ABCA1 protein expression through steviol might be related to the expression of PPARα and LXRα. This study is extremely instructive to the subsequent treatment and prevention of atherosclerosis, providing a reference for the application of stevioside in food.