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Monday, 3 August 2015

Current knowledge and pharmacological profile of berberine: An update

European Journal of Pharmacology
Volume 761, 15 August 2015, Pages 288–297
Review



doi:10.1016/j.ejphar.2015.05.068
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Abstract

Berberine, a benzylisoquinoline alkaloid, occurs as an active constituent in numerous medicinal plants and has an array of pharmacological properties. It has been used in Ayurvedic and Chinese medicine for its antimicrobial, antiprotozoal, antidiarrheal and antitrachoma activity. Moreover, several clinical and preclinical studies demonstrate ameliorative effect of berberine against several disorders including metabolic, neurological and cardiological problems. This review provides a summary regarding the pharmacokinetic and pharmacodynamic features of berberine, with a focus on the different mechanisms underlying its multispectrum activity. Studies regarding the safety profile, drug interactions and important clinical trials of berberine have also been included. Clinical trials with respect to neurological disorders need to be undertaken to exploit the beneficiary effects of berberine against serious disorders such as Alzheimer's and Parkinson's disease. Also, clinical studies to detect rare adverse effects of berberine need to be initiated to draw a complete safety profile of berberine and strengthen its applicability.

Abbreviations

  • 5-HT, 5-hydroxytryptamine;
  • 6-OHDA, 6-hydroxydopamine;
  • AChE, acetylcholinesterase;
  • AD, Alzheimer's disease;
  • AMPK, AMP-activated protein kinase;
  • BBB, blood brain barrier;
  • BChE, butyrylcholinestesrase;
  • CD, cluster of differentiation;
  • Cdk, cyclin-dependent kinase;
  • Cmax, maximum serum concentration;
  • CNS, central nervous system;
  • COX, cyclooxygenase;
  • DA, dopamine;
  • DMBA, 7,12-Dimethylbenz(a)anthracene;
  • ERK, extracellular signal-regulated kinase;
  • GFAP, glial fibrillary acidic protein;
  • GPx, glutathione peroxidase;
  • GSK, glycogen synthase kinase;
  • HIV, human immunodeficiency virus;
  • ip, intra-peritoneal;
  • IC, inhibitory concentration;
  • IGF, Insulin-like growth factor;
  • iNOS, inducible nitric oxide synthase;
  • JNK, Jun N-terminal kinase;
  • ka, apparent first-order absorption rate constant;
  • ke, apparent first-order elimination rate constant;
  • MAO, monoamine oxidase;
  • MAPK, mitogen activated protein kinase;
  • MDA, malondialdehyde MIC, minimum inhibitory concentration;
  • MMP, matrix metalloproteases;
  • MPTP, 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine;
  • NE, nor-epinephrine;
  • NF-kB, nuclear factor-kB;
  • Nrf2, nuclear factor erythroid 2-related factor 2;
  • po, per oral;
  • PD, parkinson's disease;
  • PGE2, prostaglandin E2;
  • P-gp, P-glycoprotein;
  • PI3K, phosphatidylinositol-3kinase;
  • SD, Spargue–Dawley;
  • SOD, superoxide dismutase;
  • STZ, streptozotocin;
  • TDS, ter die sumendum;
  • TGF-β1, transforming growth factor-β1;
  • TNF-α, tumor necrosis factor-α

Chemical compounds studied in this article

  • Berberine (PubChem CID: 2353);
  • Berbamine (PubChem CID: 10170);
  • Verapamil (PubChem CID: 2520);
  • Daunomycin (PubChem CID: 30323);
  • Thalifendine (PubChem CID: 3084288);
  • Berberrubine (PubChem CID: 72704);
  • Jatrorrhizine (PubChem CID: 72323);
  • Streptazotocin (PubChem CID: 29327);
  • 6-OHDA (PubChem CID: 4624);
  • Mitoxantrone (PubChem CID: 4212);
  • 5-hydroxytryptamine (PubChem CID: 5202)

Keywords

  • Berberine;
  • Immunomodulation;
  • Oxidative stress;
  • Pharmacodynamics;
  • Pharmacokinetics

Corresponding author. Fax: +91 172 2543101.
Copyright © 2015 Elsevier B.V. All rights reserved.
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