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染料木黄酮的潜在降脂机制。

Potential Lipid-Lowering Mechanisms of Biochanin A.

作者信息

Xue Zhaohui, Zhang Qian, Yu Wancong, Wen Haichao, Hou Xiaonan, Li Dan, Kou Xiaohong

机构信息

School of Chemical Engineering and Technology, Tianjin University , Tianjin 300072, China.

Medical Plant Laboratory, Tianjin Research Center of Agricultural Biotechnology , Tianjin 300381, China.

出版信息

J Agric Food Chem. 2017 May 17;65(19):3842-3850. doi: 10.1021/acs.jafc.7b00967. Epub 2017 May 4.

DOI:10.1021/acs.jafc.7b00967
PMID:28447802
Abstract

Extensive studies have demonstrated that biochanin A (BCA) has a significant hypolipidemic effect. However, its mechanism of action is not clear. In this context, the effect of BCA on a high-fat diet (HFD)-induced hyperlipidemia in mice was determined. The results showed that treatment with a medium dose of biochanin A (BM) significantly decreased low-density lipoprotein cholesterol (LDL-C) 85% (from 1.196 ± 0.183 to 0.181 ± 0.0778 mM) and total cholesterol (TC) 39% (from 5.983 ± 0.128 to 3.649 ± 0.374 mM) levels, increased lipoprotein lipase (LPL) 96% (from 1.421 ± 0.0982 to 2.784 ± 0.177 U/mg protein) and hepatic triglyceride lipase (HTGL) 78% (from 1.614 ± 0.0848 to 2.870 ± 0.0977 U/mg protein) activities, significantly improved fecal lipid levels, and lowered the epididymal fat index in hyperlipidemic mice compared with the HFD control mice (p < 0.05). In vitro, the high antioxidant capacity of BCA was determined by the FRAP assay, ABTS scavenging method, and an ROS assay. In RAW 264.7 macrophages, a dose of 10 μM BCA significantly increased the cholesterol efflux by 18.7% compared with the control cells. Moreover, molecular docking of BCA on cholesterol ester transfer protein (CETP) (Asn24 and Thr27 at the N-terminal; Ala274 and Phe270 at the C-terminal) gave new insights into the role of BCA in preventing cholesterol ester transport.

摘要

广泛的研究表明,染料木黄酮(BCA)具有显著的降血脂作用。然而,其作用机制尚不清楚。在此背景下,确定了BCA对高脂饮食(HFD)诱导的小鼠高脂血症的影响。结果表明,中剂量染料木黄酮(BM)治疗可使低密度脂蛋白胆固醇(LDL-C)显著降低85%(从1.196±0.183降至0.181±0.0778 mM),总胆固醇(TC)降低39%(从5.983±0.128降至3.649±0.374 mM),脂蛋白脂肪酶(LPL)活性增加96%(从1.421±0.0982升至2.784±0.177 U/mg蛋白),肝甘油三酯脂肪酶(HTGL)活性增加78%(从1.614±0.0848升至2.870±0.0977 U/mg蛋白),粪便脂质水平显著改善,与HFD对照小鼠相比,高脂血症小鼠的附睾脂肪指数降低(p<0.05)。在体外,通过FRAP测定、ABTS清除法和ROS测定确定了BCA的高抗氧化能力。在RAW 264.7巨噬细胞中,与对照细胞相比,10 μM剂量的BCA可使胆固醇流出显著增加18.7%。此外,BCA对胆固醇酯转移蛋白(CETP)(N端的Asn24和Thr27;C端的Ala274和Phe270)的分子对接为BCA在预防胆固醇酯转运中的作用提供了新的见解。

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