Intestinal absorption of berberine and 8-hydroxy dihydroberberine and their effects on sugar absorption in rat small intestine

  • Shi-chao Wei (魏世超)
  • Su Dong (董 苏)
  • Li-jun Xu (徐丽君)Email author
  • Chen-yu Zhang (张晨宇)


The intestinal absorption of berberine (Ber) and its structural modified compound 8-hydroxy dihydroberberine (Hdber) was compared, and their effects on the intestinal absorption of sugar by perfusion experiment were investigated in order to reveal the mechanism of low dose and high activity of Hdber in the treatment of hyperglycemia. The absorption of Hdber and Ber in rat small intestine was measured by in situ perfusion. High performance liquid chromatography (HPLC) was used to determine the concentrations of Hdber and Ber. In situ perfusion method was also used to study the effects of Hdber and Ber on sugar intestinal absorption. Glucose oxidase method and UV spectrophotometry were applied to examine the concentrations of glucose and sucrose in the perfusion fluid. The results showed that the absorption rate of Ber in the small intestine was lower than 10%, but that of Hdber was larger than 70%. Both Hdber and Ber inhibited the absorption of glucose and sucrose at the doses of 10 and 20 μg/mL. However, Hdber presented stronger activity than Ber (P<0.01). It is suggested that Hdber is absorbed easily in rat small intestine and that its inhibitory effect on the absorption of sugar is better than Ber.

Key words

berberine 8-hydroxy dihydroberberine perfusion absorption high performance liquid chromatography sugar 


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  1. 1.
    Yin J, Zhang H, Ye J. Traditional Chinese medicine in treatment of metabolic syndrome. Endocr Metab Immune Disord Drug Targets, 2008,8(2):99–111PubMedCentralPubMedCrossRefGoogle Scholar
  2. 2.
    Lau CW, Yao XQ, Chen ZY, et al. Cardiovascular actions of berberine. Cardiovasc Drug Rev, 2001,19(3):234–244PubMedCrossRefGoogle Scholar
  3. 3.
    Sack RB, Froehlich JL. Berberine inhibits intestinal secretory response of Vibrio cholerae and Escherichia coli enterotoxins. Infect Immun, 1982,35(2):471–475PubMedCentralPubMedGoogle Scholar
  4. 4.
    Cheng Z, Pang T, Gu M, et al. Berberine-stimulated glucose uptake in L6 myotubes involves both AMPK and p38 MAPK. Biochim Biophys Acta, 2006,1760(11): 1682–1689PubMedCrossRefGoogle Scholar
  5. 5.
    Faik P, Morgan M, Naftalin RJ, et al. Transport and accumulation of 2-deoxy-D-glucose in wild-type and hexokinase-deficient cultured Chinese-hamster ovary (CHO) cells. Biochem J, 1989,260(1):153–155PubMedCentralPubMedGoogle Scholar
  6. 6.
    Gao Z, Chiao P, Zhang X, et al. Coactivators and corepressors of NF-kappaB in IkappaB alpha gene promoter. J Biol Chem, 2005,280(22):21 091–21 098CrossRefGoogle Scholar
  7. 7.
    Gao Z, Zhang X, Zuberi A, et al. Inhibition of insulin sensitivity by free fatty acids requires activation of multiple serine kinases in 3T3-L1 adipocytes. Mol Endocrinol, 2004,18(8):2024–2034PubMedCrossRefGoogle Scholar
  8. 8.
    Yin J, Xing HL, Ye JP. Efficacy of berberine in patients with type 2 diabetes. Metabolism, 2008,57(5):712–717PubMedCentralPubMedCrossRefGoogle Scholar
  9. 9.
    Zhang Y, Li X, Zou D, et al. Treatment of type 2 diabetes and dyslipidemia with the natural plant alkaloid berberine. J Clin Endocrinol Metab, 2008,93(7):2559–2565PubMedCrossRefGoogle Scholar
  10. 10.
    Lee YS, Kim WS, Kim KH, et al. Berberine, a natural plant product, activates AMP-activated protein kinase with beneficial metabolic effects in diabetic and insulin-resistant states. Diabetes, 2006,55(8):2256–2264PubMedCrossRefGoogle Scholar
  11. 11.
    Kong WJ, Zhang H, Song DQ, et al. Berberine reduces insulin resistance through protein kinase C-dependent up-regulation of insulin receptor expression. Metabolism, 2009,58(1):109–119PubMedCrossRefGoogle Scholar
  12. 12.
    Zhang H, Wei J, Xue R, et al. Berberine lowers blood glucose in type 2 diabetes mellitus patients through increasing insulin receptor expression. Metabolism, 2010,59(2):285–292PubMedCrossRefGoogle Scholar
  13. 13.
    Li GS, Liu XH, Zhu H, et al. Berberine-improved visceral white adipose tissue insulin resistance associated with altered sterol regulatory element-binding proteins, liver x receptors, and peroxisome proliferator-activated receptors transcriptional programs in diabetic hamsters. Biol Pharm Bull, 2011,34(5):644–654PubMedCrossRefGoogle Scholar
  14. 14.
    Yin J, Hu R, Chen M, et al. Effects of berberine on glucose metabolism in vitro. Metabolism, 2002,51(11): 1439–1443PubMedCrossRefGoogle Scholar
  15. 15.
    Gu Y, Zhang Y, Shi X, et al. Effect of traditional Chinese medicine berberine on type 2 diabetes based on comprehensive metabolomics. Talanta, 2010,81(3):766–772PubMedCrossRefGoogle Scholar
  16. 16.
    Liu L, Yu YL, Yang JS, et al. Berberine suppresses intestinal disaccharidases with beneficial metabolic effects in diabetic states, evidences from in vivo and in vitro study. Naunyn Schmiedebergs Arch Pharmacol, 2010,381(4): 371–381PubMedCrossRefGoogle Scholar
  17. 17.
    Pan GY, Huang ZJ, Wang GJ, et al. The antihyperglycaemic activity of berberine arises from a decrease of glucose absorption. Planta Med, 2003,69(7):632–636PubMedCrossRefGoogle Scholar
  18. 18.
    Chen W, Fan D, Meng L, et al. Enhancing effects of chitosan and chitosan hydrochloride on intestinal absorption of berberine in rats. Drug Dev Ind Pharm, 2012,38(1): 104–110PubMedCrossRefGoogle Scholar
  19. 19.
    Pan GY, Wang GJ, Liu XD, et al. The involvement of P-glycoprotein in berberine absorption. Pharmacol Toxicol, 2002,91(4):193–197PubMedCrossRefGoogle Scholar
  20. 20.
    Xu LJ, Lu FE, Wei SC. Comparison of therapeutic effects between 8-hydroxy dihydroberberine and berberine hydrochlorde on ype 2 diabetes mellitus in rats. Zhong Xi Yi Jie He Yan Jiu (Chinese), 2009,1(4):173–176Google Scholar
  21. 21.
    Xu LJ, Lu FE, Wei SC. Effects on improving 3T3-L1 lipocyte insulin resistance induced by high FFA and high glucose of 8-Hydroxydihydroberberine. Yao Xue Xue Bao (Chinese), 2009,11(44):1304–1308Google Scholar
  22. 22.
    Lv XY, Li J, Zhang M, et al. Enhancement of sodium caprate on intestine absorption and antidiabetic action of berberine. AAPS Pharm Sci Tech, 2010,11(1):372–382CrossRefGoogle Scholar
  23. 23.
    Lee TS, Pan CC, Peng CC, et al. Anti-atherogenic effect of berberine on LXRalpha-ABCA1-dependent cholesterol efflux in macrophages. J Cell Biochem, 2010,111(1): 104–110PubMedCrossRefGoogle Scholar
  24. 24.
    Zeng XH, Zeng XJ, Li YY. Efficacy and safety of berberine for congestive heart failure secondary to ischemic or idiopathic dilated cardiomyopathy. Am J Cardiol, 2003,92(2):173–176PubMedCrossRefGoogle Scholar
  25. 25.
    Pan GY, Wang GJ, Sun JG, et al. Inhibitory action of berberine on glucose absorption. Yao Xue Xue Bao (Chinese), 2003,38(12):911–914Google Scholar

Copyright information

© Huazhong University of Science and Technology and Springer-Verlag Berlin Heidelberg 2014

Authors and Affiliations

  • Shi-chao Wei (魏世超)
    • 1
  • Su Dong (董 苏)
    • 1
  • Li-jun Xu (徐丽君)
    • 2
    Email author
  • Chen-yu Zhang (张晨宇)
    • 1
  1. 1.Department of Pharmacy, Tongji Hospital, Tongji Medical CollegeHuazhong University of Science and TechnologyWuhanChina
  2. 2.Institute of Integrative Traditional Chinese and Western Medicine, Tongji Hospital, Tongji Medical CollegeHuazhong University of Science and TechnologyWuhanChina

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