title: Characterization of the transportation of berberine in Coptidis rhizoma extract through rat primary cultured cortical neurons.
abstract: The aim of this study was to investigate the transport behavior and efflux of berberine through the primary culture cortical neurons. High-performance liquid chromatography coupled with an UV-vis detector at 347 nm was applied. The mobile phase was 0.05 m potassium dihydrogen phosphate solution (containing 0.5% triethylamine, pH 3.0)-acetonitrile (73:27, v/v). Neurons were incubated with Coptidis rhizoma extract 6.5 microg/mL (containing 1.91 microg/mL berberine) and verapamil, KCN or cimetidine for 2 h, and then lysed in methanol to extract intracellular berberine. A 20 microL aliquot of sample was injected into the HPLC system to determine berberine concentration. The results showed that metabolic inhibitor KCN and P-glycoprotein inhibitor verapamil could increase berberine concentration within the neurons, indicating that efflux of berberine was energy-dependent and P-glycoprotein was likely to be involved. Moreover, the organic cation transporter inhibitor cimetidine could decrease berberine concentration within the neurons, suggesting that the organic cation transporter might be involved in the berberine transport process.
authors.affiliation: Laboratory of Pharmaceutical Sciences, Department of Biological Sciences and Biotechnology, Tsinghua University, Beijing 100084, People's Republic of China.
authors.forename: Yunyun
authors.initials: Y
authors.lastname: Chen
authors.forename: Xueli
authors.initials: X
authors.lastname: Wang
authors.forename: Hong
authors.initials: H
authors.lastname: Sun
authors.forename: Dongming
authors.initials: D
authors.lastname: Xing
authors.forename: Jun
authors.initials: J
authors.lastname: Hu
authors.forename: Zhuohan
authors.initials: Z
authors.lastname: Wai
authors.forename: Lijun
authors.initials: L
authors.lastname: Du
mesh_terms: D000818:Animals; D000831:Animals, Newborn; D001599:Berberine / Q000737:chemistry / Q000493:pharmacokinetics*; D001693:Biological Transport, Active; D018929:Cell Culture Techniques; D002478:Cells, Cultured; D002540:Cerebral Cortex / Q000166:cytology / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid / Q000295:instrumentation / Q000379:methods; D002927:Cimetidine / Q000378:metabolism; D039323:Coptis / Q000737:chemistry; D000089042:Coptis chinensis; D004305:Dose-Response Relationship, Drug; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000493:pharmacokinetics*; D006023:Glycoproteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D015394:Molecular Structure; D009474:Neurons / Q000378:metabolism*; D027701:Organic Cation Transport Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D051381:Rats; D013053:Spectrophotometry; D014700:Verapamil / Q000378:metabolism
chemical_list: D004365:Drugs, Chinese Herbal; D006023:Glycoproteins; D027701:Organic Cation Transport Proteins; D001599:Berberine; D002927:Cimetidine; D014700:Verapamil; C107393:Coptidis rhizoma extract