Assessment and modulation of phillyrin absorption by P-gp using Caco-2 cells and MDR1-MDCKII cells

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• 作者：Yun-Xia Li (1) (2) (3)
  Liang-Hong Ye (1) (2) (3)
  Xue-Hua Jiang (4)
  Cheng Peng (1) (2) (3)
  
• 关键词：Phillyrin ; Transportation ; Caco ; 2 cells ; MDR1 ; MDCKII cells ; P ; gp
• 刊名：European Journal of Drug Metabolism and Pharmacokinetics
• 出版年：2011
• 出版时间：March 2011
• 年：2011
• 卷：36
• 期：1
• 页码：41-47
• 全文大小：210KB
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• 作者单位：Yun-Xia Li (1) (2) (3)
  Liang-Hong Ye (1) (2) (3)
  Xue-Hua Jiang (4)
  Cheng Peng (1) (2) (3)
  
  1. Pharmacy College, Chengdu University of Traditional Chinese Medicine, No. 1166, Liutai Road, Chengdu, 610075, People’s Republic of China
  2. The Ministry of Education Key Laboratory of Standardization of Chinese Herbal Medicine, Chengdu, 610075, People’s Republic of China
  3. State Key Laboratory Breeding Base of Systematic Research, Development and Utilization of Chinese Medicine Resources, Chengdu, 610075, People’s Republic of China
  4. West China School of Pharmacy, Sichuan University, Chengdu, 610041, People’s Republic of China
  

文摘

The study was to investigate the absorption mechanism and transport modulation of phillyrin by P-gp in Caco-2 cells and MDR1-MDCKII cells. Three concentrations of phillyrin were tested in transport studies. The absorptive transports of phillyrin in the two cell models were not concentration-dependent which indicated passive diffusion as the dominating process in the test concentrations. The absorptive P app were 7.15, 6.39 and 10.03?×?10??cm?s?, respectively, for different concentrations (2.2, 4.8 and 8.4?μg?ml?) in Caco-2 cells. And the low absorptive P app was consistent with the low oral bioavailability of phillyrin observed in pharmacokinetic experiments. In transport inhibition experiment, the efflux inhibitors, verapamil and GF120918 can increase the absorption of phillyrin in Caco-2 cells which suggested the involvement of efflux transporters. In the further inhibition experiment in MDR1-MDCKII cells, the absorption was greatly increased and the efflux of phillyrin was competitively inhibited by verapamil and GF120918, which confirmed the involvement of P-gp in the efflux of phillyrin.