Enhancing the bioavailability of resveratrol by combining it with piperine.
Jeremy J. Johnson,Minakshi Nihal,Imtiaz A. Siddiqui,Cameron O. Scarlett,Howard H. Bailey,Hasan Mukhtar,Nihal Ahmad +6 more
TLDR
Piperine significantly improves the in vivo bioavailability of resveratrol through inhibiting its glucuronidation, thereby slowing its elimination and further detailed research is needed to study the mechanism of improved bioavailability via its combination with piperine.Abstract:
Scope 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. Methods and results 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. Conclusion 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.read more
Citations
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Dietary Intake of (-)-Epigallocatechin-3-gallate against Aging and Cancers: Nanoencapsulation of Multi- Rings Still Requires New Rounds!
TL;DR: Interestingly, emergent studies suggest that nano-encapsulated polyphenols might overcome some limitations frequently observed with dietary bulk-polyphenols (e.g. bioavailability, pharmacokinetics, targeting, efficacy, toxicity and safety), subsequently potentiating their biological effects.
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Bioavailability Enhancement of Poorly Soluble Drugs: The Holy Grail in Pharma Industry.
Mamunur Rashid,Mohd Yaseen Malik,Sandeep Singh,Swati Chaturvedi,Jiaur R. Gayen,Muhammad Wahajuddin +5 more
TL;DR: The use of novel methods such as nano- based formulations, bio-enhancers, solid dispersion, lipid-and polymer-based formulations provide a wide range of applications in not only improving the solubility and permeability of the poorly bioavailable drugs but also improve the stability, and targeting of the drug to specific tissues.
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Adipogenic effects of piperlonguminine in 3T3-L1 cells and plasma concentrations of several amide constituents from Piper chaba extracts after treatment of mice
Itadaki Yamaguchi,Hisashi Matsuda,Hailong Zhang,Makoto Hamao,Chihiro Yamashita,Yuichiro Kogami,Haruka Kon’i,Megumi Murata,Seikou Nakamura,Masayuki Yoshikawa +9 more
TL;DR: Piperlonguminine increased mRNA levels of adiponectin, glucose transporter 4, and fatty acid-binding protein (aP2) but, unlike troglitazone, piper longuminine did not activate PPARγ directly in a nuclear receptor cofactor assay.
Journal ArticleDOI
Piperine Alters the Pharmacokinetics and Anticoagulation of Warfarin in Rats
TL;DR: It is concluded that piperine could be a potent inhibitor of cytochrome P450 metabolism of warfarin in vivo and, contrary to the expectation, may reduce the plasma concentration and anticoagulation of warFarin.
Journal ArticleDOI
Supplementation with Resveratrol, Piperine and Alpha-Tocopherol Decreases Chronic Inflammation in a Cluster of Older Adults with Metabolic Syndrome
Raúl Francisco Pastor,Marisa G. Repetto,Fabiana Lairion,Alberto Lazarowski,Amalia Merelli,Zulma Manfredi Carabetti,Isabel Pastor,Elena Pastor,Laura Valeria Iermoli,Carlos Amadeo Bavasso,Roberto Héctor Iermoli +10 more
TL;DR: This is the first study showing a chronic inflammation decrease in MetS patients due to the administration of a biopower Resveratrol-piperine and alpha tocopherol dietary supplement together with conventional therapy.
References
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Influence of Piperine on the Pharmacokinetics of Curcumin in Animals and Human Volunteers
TL;DR: The study shows that in the dosages used, piperine enhances the serum concentration, extent of absorption and bioavailability of curcumin in both rats and humans with no adverse effects.
Journal ArticleDOI
High absorption but very low bioavailability of oral resveratrol in humans
TL;DR: The dietary polyphenol resveratrol has been shown to have chemopreventive activity against cardiovascular disease and a variety of cancers in model systems, but it is not clear whether the drug reaches the proposed sites of action in vivo after oral ingestion, especially in humans.
Journal ArticleDOI
PKSolver: An add-in program for pharmacokinetic and pharmacodynamic data analysis in Microsoft Excel
TL;DR: The PKSolver provided pharmacokinetic researchers with a fast and easy-to-use tool for routine and basic PK and PD data analysis with a more user-friendly interface and its output could be generated in Microsoft Word in the form of an integrated report.