Academic Journal

Pharmacokinetics of pure silybin diastereoisomers and identification of their metabolites in rat plasma

التفاصيل البيبلوغرافية
العنوان: Pharmacokinetics of pure silybin diastereoisomers and identification of their metabolites in rat plasma
المؤلفون: Petr Marhol, Petr Bednář, Petra Kolářová, Rostislav Večeřa, Jitka Ulrichová, Eva Tesařová, Eva Vavříková, Marek Kuzma, Vladimír Křen
المصدر: Journal of Functional Foods, Vol 14, Iss , Pp 570-580 (2015)
بيانات النشر: Elsevier, 2015.
سنة النشر: 2015
المجموعة: LCC:Nutrition. Foods and food supply
مصطلحات موضوعية: Silybin, Silibinin, Silybin glucuronide, Silybin sulfate, Silymarin, Benzofuranone, Nutrition. Foods and food supply, TX341-641
الوصف: The flavonolignan silybin (isolated from the fruits of the milk thistle, Silybum marianum), is a mixture of two diastereoisomers and has anticancer, chemoprotective, hepatoprotective and dermatoprotective properties. This compound is largely used in various functional foods, nutraceutics and food supplements. The pharmacokinetic profiles of optically pure silybins (silybin A and silybin B) were monitored in rat plasma after the intragastric administration (200 mg⋅kg−1 of body weight) of each diastereoisomer. Free (unconjugated) and total (free + conjugated) silybins were monitored for 6 hours by HPLC-PDA. The metabolic profiles of each silybin diastereoisomer were completely different. Our results clearly demonstrate that silybin B (Cmax = 14.50 µg⋅mL−1, Tmax = 2.6 hours, T1/2 = 2.9 hours; total silybin B) was absorbed faster and in a substantially higher amount than silybin A (Cmax = 1.05 µg⋅mL−1, Tmax = 3.9 hours, T1/2 = 2.2 hours; total silybin A). The oral bioavailability of silybin B was estimated to be 0.3%. The AUC 0→6 h (area under the curve) value of total silybin B was 20-fold higher than that of silybin A. SPE-UPLC-MS/MS (solid phase extraction-ultra performance liquid chromatography) was used to identify glucuronides and sulfates (in several isomeric forms) as dominant metabolites of silybin B in rat plasma. Silybin B-7-O-β-glucuronide was the major plasma metabolite of silybin B.
نوع الوثيقة: article
وصف الملف: electronic resource
اللغة: English
تدمد: 1756-4646
Relation: http://www.sciencedirect.com/science/article/pii/S1756464615000936; https://doaj.org/toc/1756-4646
DOI: 10.1016/j.jff.2015.02.031
URL الوصول: https://doaj.org/article/7c0855f118aa411bb18b2b243b913bef
رقم الانضمام: edsdoj.7c0855f118aa411bb18b2b243b913bef
قاعدة البيانات: Directory of Open Access Journals
الوصف
تدمد:17564646
DOI:10.1016/j.jff.2015.02.031