Welcome to Chinese Journal of Clinical Pharmacology and Therapeutics,Today is Chinese

Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2004, Vol. 9 ›› Issue (9): 970-977.

Previous Articles     Next Articles

Correlation of furanocoumarin composition and rat cytochrome P450 3A inhibition among citrus fruit juices

GUO Lian-Qing, BAO Hao, YANG Juan, CHEN Qiao-Yun1, LIU Yu-Xiu2, LI Jin-Heng, YAMAZOE Yasushi3   

  1. Department of Clinical Pharmacology,1Department of Pharmacy,2Department of Science Research, Jinling Hospital &Clinical School of Medical College of Nanjing University, Nanjing 210002, Jiangsu, China;
    3Division of Drug Metabolism and Molecular Toxicology, Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai 980-8578, Japan
  • Received:2004-06-21 Accepted:2004-07-30 Online:2004-09-26 Published:2020-11-23
  • Contact: GUO Lian-Qing, male, doctor of pharmacy, associate professor, tutor of master, engaged in drug metabolism. Tel:025-80860196 E-mail:guokaku @hotmail.com
  • Supported by:
    Project partly supported by the Scientific Research Foundation for the Returned Overseas Chinese Scholars, State Education Ministry (№0214H010)

Abstract: AIM: To investigate the existence of these compounds in other citrus fruit juices, and check their inhibitory intensities on activity of cytochrome P450 (CYP) 3A.METHODS: Freshly squeezed citrus fruit juices were determined separately for their composition and levels of six furanocoumarins with a gradient highpressure liquid chromatographic (HPLC) method. Inhibition of CYP3A by each juice sample was tested with the activity of testosterone 6β-hydroxylation in liver microsoms of male Sprague-Dawley rats.RESULTS: Comparing with grapefruit juices, the Jaffa sweetie showed almost the same composition and levels of furanocoumarins, and a comparable inhibitory intensity of CYP3A; the Japanese red pommelo, `Guanxi Miyou' and `Jinyou' pommelos showed similar compositions but lower levels of furanocoumarins, and weaker inhibiting intensities of CYP3A; While `Changshan Huyou' pummelos, sweet oranges and mandarins showed less varieties and much lower levels of furanocoumarins, and most of them showed no inhibition of CYP3A.CONCLUSION: Furanocoumarin composition can be an index to predict citrus fruit juice-drug interaction based on CYP3A inhibition; Clinical validations should be conducted on `Guanxi Miyou' pummelo and closely related accessions for their possible drug interactions similar to grapefruit juice.

Key words: psoralens, citrus fruit juice, high-pressure liquid chromatography, cytochrome P450 3A, enzyme inhibition

CLC Number: