title: Pharmacokinetics and blood-brain barrier penetration of (+)-catechin and (-)-epicatechin in rats by microdialysis sampling coupled to high-performance liquid chromatography with chemiluminescence detection.
abstract: (+)-Catechin (C) and (-)-epicatechin (EC), as the basic monomer units of flavanols, can be widely found in natural products or medicinal herbs. Recent pharmacological studies have revealed that C and EC exhibit good neuroprotective effects. However, there is little information about pharmacokinetic profiles in the brain and in vivo BBB penetration of C and EC. In this paper, an ultrasensitive method using high-performance liquid chromatography (HPLC) with chemiluminescence (CL) detection was developed for the analysis of microdialysis samples. The detection limits for C and EC in Ringer's solution were 1.0 and 1.2 ng/mL, respectively. The intraday and interday accuracies for C and EC in Ringer's solution ranged from -3.0 to 4.4%, and the intraday and interday precisions were below 5.2%. The mean in vivo recoveries of C and EC in microdialysis probes were 33.7% and 26.5% in blood while 38.3% and 29.1% in brain. Pharmacokinetic parameters were estimated using the statistical moment method after iv administration (C and EC, 20 mg/kg of body weight) in rats. Brain-to-blood (AUC(brain)/AUC(blood)) distribution ratios were 0.0726 ± 0.0376 for C and 0.1065 ± 0.0531 for EC, indicating that C and EC could pass through the BBB, which is further evidence of their neuroprotective effects.
authors.affiliation: Anhui Key Laboratory of Bioactivity of Natural Products, School of Pharmacy, Anhui Medical University, Hefei, P R China.
authors.forename: Liang
authors.initials: L
authors.lastname: Wu
authors.forename: Qun-Lin
authors.initials: QL
authors.lastname: Zhang
authors.forename: Xiao-Yue
authors.initials: XY
authors.lastname: Zhang
authors.forename: Chen
authors.initials: C
authors.lastname: Lv
authors.forename: Jun
authors.initials: J
authors.lastname: Li
authors.forename: Ye
authors.initials: Y
authors.lastname: Yuan
authors.forename: Fang-Xiong
authors.initials: FX
authors.lastname: Yin
mesh_terms: D000818:Animals; D001812:Blood-Brain Barrier / Q000378:metabolism*; D002392:Catechin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D004355:Drug Stability; D008163:Luminescent Measurements / Q000379:methods*; D008297:Male; D017551:Microdialysis; D018696:Neuroprotective Agents / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D012680:Sensitivity and Specificity
chemical_list: D018696:Neuroprotective Agents; D002392:Catechin