Naunyn-Schmiedeberg's Archives of Pharmacology

, Volume 381, Issue 4, pp 371–381

Berberine suppresses intestinal disaccharidases with beneficial metabolic effects in diabetic states, evidences from in vivo and in vitro study

  • Li Liu
  • Yun-Li Yu
  • Jian-Song Yang
  • Yang Li
  • Yao-Wu Liu
  • Yan Liang
  • Xiao-Dong Liu
  • Lin Xie
  • Guang-Ji Wang
ORIGINAL ARTICLE

DOI: 10.1007/s00210-010-0502-0

Cite this article as:
Liu, L., Yu, YL., Yang, JS. et al. Naunyn-Schmied Arch Pharmacol (2010) 381: 371. doi:10.1007/s00210-010-0502-0

Abstract

Clinical reports have demonstrated that berberine is a potential antidiabetic agent, but the underlying mechanism is unclear. The purpose of this study was to investigate if berberine exerts its hypoglycemic action via inhibiting intestinal disaccharidases using in vivo and in vitro experiments. Streptozotocin-induced diabetic rats received berberine (100 or 200 mg/kg) orally once daily or acarbose (40 mg/kg) orally twice daily for 5 weeks. Disaccharidase activities and sucrase–isomaltase (SI) complex messenger RNA (mRNA) expression in intestinal regions were assessed. The same treatment was operated in normal rats. Sucrose and maltose loading tests were also documented. In addition, Caco-2 cells were cultured in medium containing berberine or berberine plus chelerythrine. Compound C or H-89 for 5 days, disaccharidase activities, and SI complex mRNA levels were measured. The animal experiments showed that berberine significantly decreased the disaccharidase activities and SI complex mRNA expression both in diabetic rats and normal rats. Berberine can also significantly lower postprandial blood glucose levels induced by sucrose or maltose loading in normal rats. The cellular results showed that berberine may suppress disaccharidase activities and downregulate SI complex mRNA expression in a concentration-dependent manner. Only H-89, an inhibitor of protein kinase A (PKA), may reverse the decrease in disaccharidase activities and SI complex mRNA expression induced by berberine. In conclusion, berberine suppresses disaccharidase activities and SI complex mRNA expression with beneficial metabolic effects in diabetic states. The inhibitory effect, at least partly, involves the PKA-dependent pathway.

Keywords

Diabetes mellitusDisaccharidaseBerberineSucrase–isomaltase complexPKA

Copyright information

© Springer-Verlag 2010

Authors and Affiliations

  • Li Liu
    • 1
  • Yun-Li Yu
    • 1
  • Jian-Song Yang
    • 2
  • Yang Li
    • 1
    • 2
  • Yao-Wu Liu
    • 1
    • 3
  • Yan Liang
    • 1
  • Xiao-Dong Liu
    • 1
  • Lin Xie
    • 1
  • Guang-Ji Wang
    • 1
  1. 1.Key Laboratory of Drug Metabolism and PharmacokineticsChina Pharmaceutical UniversityNanjingChina
  2. 2.DMPK, GlaxoSmithKline (China) R&D Co.ShanghaiChina
  3. 3.Department of PharmacologyXuzhou Medical CollegeXuzhouChina