Proteomics analysis reveals a potential new target protein for the lipid-lowering effect of Berberine8998
文献类型：期刊论文
| 作者 | Yu, Cheng-yin3,4; Liu, Gang-yi5; Liu, Xiao-hui1,2; Gui, Yu-zhou4; Liu, Hai-ming5; Zheng, Hong-chao5; Gorecki, Darek C.3; Patel, Asmita, V3; Yu, Chen5; Wang, Yi-ping4
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| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2018-09 |
| 卷号 | 39期号:9页码:1473-1482 |
| 关键词 | berberine berberine8998 proteomics lipid-lowering cholesterol triglycerides LDL-C fatty acid metabolism hypercholesterolemia obesity |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2017.200 |
| 文献子类 | Article |
| 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. |
| WOS关键词 | DISEASE ; ATHEROSCLEROSIS ; IDENTIFICATION ; CHALLENGES ; EFFICACY ; RECEPTOR |
| 资助项目 | Xuhui Central Hospital, Shanghai Clinical Center and the Chinese Academy of Sciences (Shanghai, China)[10431903400] ; Shanghai Municipal Commission of Health and Family Planning[ZK2012A39] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000442758500007 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279600]  |
| 专题 | 药理学第一研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Yu, Chen |
| 作者单位 | 1.Fudan Univ, Coll Life Sci, Dept Prote Res, Shanghai 200032, Peoples R China; 2.Fudan Univ, Inst Biomed Sci, Shanghai 200032, Peoples R China 3.Univ Portsmouth, Sch Pharm & Biomed Sci, Portsmouth PO1 2DT, Hants, England; 4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 5.Chinese Acad Sci, Xuhui Cent Hosp, Shanghai Clin Ctr, Shanghai 200031, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Yu, Cheng-yin,Liu, Gang-yi,Liu, Xiao-hui,et al. Proteomics analysis reveals a potential new target protein for the lipid-lowering effect of Berberine8998[J]. ACTA PHARMACOLOGICA SINICA,2018,39(9):1473-1482. |
| APA | Yu, Cheng-yin.,Liu, Gang-yi.,Liu, Xiao-hui.,Gui, Yu-zhou.,Liu, Hai-ming.,...&Wang, Yi-ping.(2018).Proteomics analysis reveals a potential new target protein for the lipid-lowering effect of Berberine8998.ACTA PHARMACOLOGICA SINICA,39(9),1473-1482. |
| MLA | Yu, Cheng-yin,et al."Proteomics analysis reveals a potential new target protein for the lipid-lowering effect of Berberine8998".ACTA PHARMACOLOGICA SINICA 39.9(2018):1473-1482. |
入库方式： OAI收割
来源：上海药物研究所
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