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Alpinetin enhances cholesterol efflux and inhibits lipid accumulation in oxidized low‐density lipoprotein‐loaded human macrophages
Author(s) -
Jiang Zhengming,
Sang Haiqiang,
Fu Xin,
Liang Ying,
Li Ling
Publication year - 2015
Publication title -
biotechnology and applied biochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 70
eISSN - 1470-8744
pISSN - 0885-4513
DOI - 10.1002/bab.1328
Subject(s) - abca1 , abcg1 , liver x receptor alpha , scavenger receptor , cholesterol , efflux , chemistry , liver x receptor , gene knockdown , reverse cholesterol transport , apolipoprotein b , lipoprotein , high density lipoprotein , microbiology and biotechnology , medicine , endocrinology , biology , biochemistry , transcription factor , nuclear receptor , transporter , apoptosis , gene
Alpinetin is a natural flavonoid abundantly present in the ginger family. Here, we investigated the effect of alpinetin on cholesterol efflux and lipid accumulation in oxidized low‐density lipoprotein (ox‐LDL)‐treated THP‐1 macrophages and human peripheral blood monocyte‐derived macrophages (HMDMs). After exposing THP‐1 macrophages to alpinetin, cholesterol efflux was determined by liquid scintillator. The mRNA and protein levels of peroxisome proliferator‐activated receptor gamma (PPAR‐ γ ), liver X receptor alpha (LXR‐α), ATP‐binding cassette transporter A1 (ABCA1), and ABCG1 and scavenger receptor class B member 1 were determined by reverse‐transcriptase PCR (RT‐PCR) and Western blot analysis, respectively. Alpinetin promoted apolipoprotein A‐I‐ and high‐density‐lipoprotein‐mediated cholesterol efflux and elevated PPAR‐γ and LXR‐α mRNA and protein expression in a dose‐dependent fashion in ox‐LDL‐treated THP‐1 macrophages and HMDMs. Small interfering RNA‐mediated silencing of PPAR‐γ or LXR‐α dose dependently reversed alpinetin‐increased cholesterol efflux in THP‐1 macrophages, indicating the involvement of PPAR‐γ and LXR‐α in alpinetin‐promoted cholesterol efflux. Alpinetin inhibited ox‐LDL‐induced lipid accumulation and enhanced the expression of ABCA1 and ABCG1 mRNA and protein, which was reversed by specific knockdown of PPAR‐γ or LXR‐α. Taken together, our results reveal that alpinetin exhibits positive effects on cholesterol efflux and inhibits ox‐LDL‐induced lipid accumulation, which might be through PPAR‐ γ /LXR‐ α /ABCA1/ABCG1 pathway.