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葡萄柚及葡萄柚汁产品中CYP3A4抑制剂、柚皮苷、柚皮素和补骨脂素的含量。

Content of CYP3A4 inhibitors, naringin, naringenin and bergapten in grapefruit and grapefruit juice products.

作者信息

Ho P C, Saville D J, Coville P F, Wanwimolruk S

机构信息

School of Pharmacy, University of Otago, Dunedin, New Zealand.

出版信息

Pharm Acta Helv. 2000 Apr;74(4):379-85. doi: 10.1016/s0031-6865(99)00062-x.

DOI:10.1016/s0031-6865(99)00062-x
PMID:10812937
Abstract

The flavonoids, naringin and naringenin and the furanocoumarin, bergapten (5-methoxypsoralen), were detected in some fresh grapefruit and commercial grapefruit juices but were not detected in other fruit juices tested (orange; orange with apple base; dark grape; orange and mango with apple base; orange, peach, passion fruit juice). The contents of these three grapefruit constituents in commercial juice and fresh grapefruit varied from brand to brand and also from lot to lot. Juice was prepared from the fresh fruit via different methods (by hand, squeezer or blender). The naringin content, after hand-squeeze, ranged from 115 to 384 mg/l. With hand-squeeze juice production, bergapten was not detected (less than 0.5 mg/l) in two varieties of grapefruit, and naringenin was usually not in detectable levels (less than 2 mg/l) in three varieties. All three constituents were present in New Zealand grapefruit preparations (including juice by hand-squeeze) and different lots showed variation in content (1.5-, 2.3- and 4.7-fold for naringin, naringenin and bergapten, respectively). Differences in the concentrations of these three constituents, which have potential for drug interaction, may contribute to the variability in pharmacokinetics of CYP3A4 drugs and some contradictory results of drug interaction studies with grapefruit juice.

摘要

在一些新鲜葡萄柚和市售葡萄柚汁中检测到了黄酮类化合物柚皮苷和柚皮素以及呋喃香豆素补骨脂素(5-甲氧基补骨脂素),但在其他测试的果汁(橙汁;苹果味橙汁;黑葡萄汁;苹果味橙芒果汁;橙桃西番莲果汁)中未检测到。市售果汁和新鲜葡萄柚中这三种葡萄柚成分的含量因品牌和批次而异。通过不同方法(手工、榨汁机或搅拌机)从新鲜水果中制备果汁。手工榨汁后,柚皮苷含量在115至384毫克/升之间。采用手工榨汁生产时,在两个葡萄柚品种中未检测到补骨脂素(低于0.5毫克/升),在三个品种中柚皮素通常也未达到可检测水平(低于2毫克/升)。这三种成分均存在于新西兰葡萄柚制品中(包括手工榨汁的果汁),不同批次的含量存在差异(柚皮苷、柚皮素和补骨脂素的含量分别相差1.5倍、2.3倍和4.7倍)。这三种具有药物相互作用潜力的成分浓度的差异,可能导致CYP3A4药物药代动力学的变异性以及一些葡萄柚汁药物相互作用研究结果相互矛盾。

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