proteomicsanalysisrevealsapotentialnewtargetproteinforthelipidloweringeffectofberberine8998
文献类型：期刊论文
| 作者 | u Chengyin1; Liu Gangyi2; Liu Xiaohui3; Gui Yuzhou1; Liu Haiming2; Zheng Hongchao2; Gorecki Darek C4; Patel Asmita V4; Yu Chen2; Wang Yiping1
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| 刊名 | actapharmacologicasinica
 |
| 出版日期 | 2018 |
| 卷号 | 39期号:9页码:1473 |
| 关键词 | DISEASE ATHEROSCLEROSIS IDENTIFICATION CHALLENGES EFFICACY RECEPTOR berberine berberine8998 proteomics lipid-lowering cholesterol triglycerides LDL-C fatty acid metabolism hypercholesterolemia obesity |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2017.200 |
| 英文摘要 | Berberine8998 is a newly synthesized berberine derivative with better lipid-lowering activity and improved absorption. The objective of this study was to investigate the effects of berberine8998 on serum cholesterol and lipid levels in vivo and to examine the mechanisms involved. Hamsters on high-fat diet (HFD) were administered berberine or berberine8998 (50 mg.kg(-1).d(-1), ig) for 3 weeks. Berberine8998 administration significantly lowered the total cholesterol, triglycerides and LDL-C levels in HFD hamsters. Bioinformatics revealed that berberine and berberine8998 shared similar metabolic pathways and fatty acid metabolism was the predominant pathway. Western blot validation results showed that peroxisomal acyl-coenzyme A oxidase 1 (ACOX1) and long-chain fatty acid-CoA ligase 1 (ACSL1), two proteins involved in fatty acid metabolism, were expressed differently in the berberine8998 group than in the untreated group and the berberine treatment group. Biochemistry results showed that berberine8998 significantly lowered the non-esterified fatty acid (NEFA) levels, which may lead to a reduction in TG levels in the berberine8998 treatment group and the differences observed in proteomics analyses. Pharmacokinetic analysis conducted in rats. After administration of berberine or berberine8998 (50 mg/kg, ig), berberine8998 exhibited a remarkably improved absorption with increasing bioavailability by 6.7 times compared with berberine. These findings suggest that berberine8998 lowers cholesterol and lipid levels via different mechanisms than berberine, and its improved absorption makes it a promising therapeutic candidate for the treatment of hypercholesterolemia and obesity. |
| 资助项目 | [Xuhui Central Hospital, Shanghai Clinical Center and the Chinese Academy of Sciences (Shanghai, China)] ; [Shanghai Municipal Commission of Health and Family Planning] |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/284792]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.中国科学院上海药物研究所 2.Xuhui Central Hospital,Shanghai Clinical Center,Chinese Academy of Sciences 3.Department of Proteomics Research,College of Life Sciences and Institutes of Biomedical Sciences,Fudan University 4.School of Pharmacy and Biomedical Sciences,University of Portsmouth |
| 推荐引用方式 GB/T 7714 | u Chengyin,Liu Gangyi,Liu Xiaohui,et al. proteomicsanalysisrevealsapotentialnewtargetproteinforthelipidloweringeffectofberberine8998[J]. actapharmacologicasinica,2018,39(9):1473. |
| APA | u Chengyin.,Liu Gangyi.,Liu Xiaohui.,Gui Yuzhou.,Liu Haiming.,...&Wang Yiping.(2018).proteomicsanalysisrevealsapotentialnewtargetproteinforthelipidloweringeffectofberberine8998.actapharmacologicasinica,39(9),1473. |
| MLA | u Chengyin,et al."proteomicsanalysisrevealsapotentialnewtargetproteinforthelipidloweringeffectofberberine8998".actapharmacologicasinica 39.9(2018):1473. |
入库方式： OAI收割
来源：上海药物研究所
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