Department of Pharmacy Practice, College of Pharmacy, University of Illinois at Chicago, Chicago, IL, USA.
Mol Nutr Food Res. 2011 Aug;55(8):1169-76. doi: 10.1002/mnfr.201100117. Epub 2011 Jun 29.
Resveratrol (3,5,4'-trihydroxystilbene) is a phytoalexin shown to possess a multitude of health-promoting properties in pre-clinical studies. However, the poor in vivo bioavailability of resveratrol due to its rapid metabolism is being considered as a major obstacle in translating its effects in humans. In this study, we examined the hypothesis that piperine will enhance the pharmacokinetic parameters of resveratrol via inhibiting its glucuronidation, thereby slowing its elimination.
Employing a standardized LC/MS assay, we determined the effect of piperine co-administration with resveratrol on serum levels resveratrol and resveratrol-3-O-β-D-glucuronide in C57BL mice. Mice were administered resveratrol (100 mg/kg; oral gavage) or resveratrol (100 mg/kg; oral gavage)+piperine (10 mg/kg; oral gavage), and the serum levels of resveratrol and resveratrol-3-O-β-D-glucuronide were analyzed at different times. We found that the degree of exposure (i.e. AUC) to resveratrol was enhanced to 229% and the maximum serum concentration (C(max)) was increased to 1544% with the addition of piperine.
Our study demonstrated that piperine significantly improves the in vivo bioavailability of resveratrol. However, further detailed research is needed to study the mechanism of improved bioavailability of resveratrol via its combination with piperine as well as its effect on resveratrol metabolism.
白藜芦醇（3,5,4'-三羟基二苯乙烯）是一种植物抗毒素，在临床前研究中显示出多种促进健康的特性。然而，由于其快速代谢，白藜芦醇的体内生物利用度较差，被认为是将其在人体中的作用转化的主要障碍。在这项研究中，我们假设胡椒碱通过抑制其葡萄糖醛酸化来增强白藜芦醇的药代动力学参数，从而减缓其消除。
我们采用标准化的 LC/MS 测定法，研究了胡椒碱与白藜芦醇同时给药对 C57BL 小鼠血清中白藜芦醇和白藜芦醇-3-O-β-D-葡萄糖醛酸水平的影响。小鼠给予白藜芦醇（100mg/kg；口服灌胃）或白藜芦醇（100mg/kg；口服灌胃）+胡椒碱（10mg/kg；口服灌胃），并在不同时间分析血清中白藜芦醇和白藜芦醇-3-O-β-D-葡萄糖醛酸的水平。我们发现，加入胡椒碱后，白藜芦醇的暴露程度（即 AUC）增加到 229%，最大血清浓度（C(max)）增加到 1544%。
我们的研究表明，胡椒碱显著提高了白藜芦醇的体内生物利用度。然而，需要进一步详细研究通过与胡椒碱结合提高白藜芦醇生物利用度的机制及其对白藜芦醇代谢的影响。
