Enhancement of Berberine Hypoglycemic Activity by Oligomeric Proanthocyanidins
文献类型：期刊论文
| 作者 | Zhang, Haoyue2; Wang, Xueping2; Wang, Ting1; Chen, Kaixian2 ; Wang, Heyao1; Jia, Qi2; Li, Yiming2
|
| 刊名 | Molecules (Basel, Switzerland)
 |
| 出版日期 | 2018-12-14 |
| 卷号 | 23期号:12 |
| ISSN号 | 1420-3049 |
| DOI | 10.3390/molecules23123318 |
| 文献子类 | Article |
| 英文摘要 | This study investigated the possible enhancement of berberine's (BB) hypoglycemic activity by oligomeric proanthocyanidins (OPCs) and its underlying mechanism. The hypoglycemic activity of the studied compounds was evaluated in diabetic / mice. The cellular uptake and efflux of BB with or without OPCs were investigated using Caco-2 intestinal cells. A pharmacokinetic study of BB and OPCs was performed in Sprague Dawley (SD) mice by oral administration of the study compounds. Liquid chromatography⁻tandem mass spectrometry (LC⁻MS/MS) was employed to determine the cellular efflux, retention, and the serum concentrations of the compounds. The results revealed that OPCs considerably potentiated the hypoglycemic efficacy of BB in diabetic / mice. In the in vitro experiments, OPCs significantly inhibited the efflux and increased the uptake of the P-glycoprotein (P-gp) substrate rhodamine-123 (R123) and BB in Caco-2 intestinal cells. Moreover, OPCs substantially reduced the expression of P-gp in Caco-2 cells. The inhibition of BB efflux by OPCs was translated into the improved pharmacokinetics in vivo. When co-administered, OPCs obviously increased the average maximum concentration of BB in mice. In summary, this study demonstrated that combination of BB with OPCs could significantly improve the pharmacokinetics and hypoglycemic efficacy of BB, which is valuable for future exploration of the combination of BB and OPCs as oral hypoglycemic agents. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/266314]  |
| 专题 | 药理学第三研究室 |
| 通讯作者 | Zhang, Haoyue; Wang, Xueping; Wang, Ting; Chen, Kaixian; Wang, Heyao; Jia, Qi; Li, Yiming |
| 作者单位 | 1.Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China 2.School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai 201203, China; |
| 推荐引用方式 GB/T 7714 | Zhang, Haoyue,Wang, Xueping,Wang, Ting,et al. Enhancement of Berberine Hypoglycemic Activity by Oligomeric Proanthocyanidins[J]. Molecules (Basel, Switzerland),2018,23(12). |
| APA | Zhang, Haoyue.,Wang, Xueping.,Wang, Ting.,Chen, Kaixian.,Wang, Heyao.,...&Li, Yiming.(2018).Enhancement of Berberine Hypoglycemic Activity by Oligomeric Proanthocyanidins.Molecules (Basel, Switzerland),23(12). |
| MLA | Zhang, Haoyue,et al."Enhancement of Berberine Hypoglycemic Activity by Oligomeric Proanthocyanidins".Molecules (Basel, Switzerland) 23.12(2018). |
入库方式： OAI收割
来源：上海药物研究所
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