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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Administration of resveratrol: What formulation solutions to bioavailability limitations?
TL;DR: An increasing number of recent studies have aimed at designing novel resveratrol formulations to overcome its poor solubility, limited stability, high metabolization and weak bioavailability, which is a barrier to the development of therapeutic applications.
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The Role of Resveratrol in Cancer Therapy
Jeong-Hyeon Ko,Gautam Sethi,Jae-Young Um,Muthu K. Shanmugam,Frank Arfuso,Alan Prem Kumar,Anupam Bishayee,Kwang Seok Ahn +7 more
TL;DR: The current focus of this review is resveratrol’s in vivo and in vitro effects in a variety of cancers, and intracellular molecular targets modulated by this polyphenol.
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Resveratrol and cancer: focus on in vivo evidence
TL;DR: This review highlights the in vivo effects of resveratrol treatment on breast, colorectal, liver, pancreatic, and prostate cancers and suggests that many factors need to be considered before resver atrol can be used for human cancer prevention or therapy.
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Resveratrol and clinical trials: the crossroad from in vitro studies to human evidence.
Joao Tomé-Carneiro,Mar Larrosa,Antonio González-Sarrías,Francisco A. Tomás-Barberán,María Teresa García-Conesa,Juan Carlos Espín +5 more
TL;DR: This review will focus on the currently available evidence regarding resveratrol’s effects on humans obtained from randomized clinical trials and provide a critical outlook for further research on this molecule that is evolving from a minor dietary compound to a possible multi-target therapeutic drug.
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Dietary phytochemicals and cancer chemoprevention: a review of the clinical evidence.
TL;DR: The data regarding select phytochemicals including curcumin, resveratrol, lycopene, folates and tea polyphenols are summarized with emphasis on the clinical evidence supporting the efficacy of these compounds in high-risk populations.
References
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Pharmacokinetic and safety profile of trans‐resveratrol in a rising multiple‐dose study in healthy volunteers
Luís Pereira de Almeida,Manuel Vaz-da-Silva,Amílcar Falcão,Eva Soares,Raquel Costa,Ana I. Loureiro,Carlos Fernandes-Lopes,José-Francisco Rocha,Teresa G. Nunes,Lyndon C. Wright,Patrício Soares-da-Silva +10 more
TL;DR: In conclusion, repeated administration was well-tolerated but produced relatively low plasma concentrations of trans-resveratrol, despite the high doses and short dosing interval used.
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Cancer chemopreventive activity of resveratrol.
TL;DR: Evidence indicated that resveratrol selectively suppresses the transcriptional activation of cytochrome P‐450 1A1 and inhibits the formation of carcinogen‐induced preneoplastic lesions in a mouse mammary organ culture model, holding great promise for future development as a chemopreventive agent that may be useful for several disorders.
Journal Article
Biochemical basis of enhanced drug bioavailability by piperine: evidence that piperine is a potent inhibitor of drug metabolism.
C.K. Atal,R K Dubey,J. Singh +2 more
TL;DR: It is demonstrated that piperine is a nonspecific inhibitor of drug metabolism which shows little discrimination between different cytochrome P-450 forms.
Journal ArticleDOI
Chemoprevention by resveratrol: molecular mechanisms and therapeutic potential
TL;DR: There is growing evidence that resveratrol can prevent or delay the onset of various cancers, heart diseases, ischemic and chemically induced injuries, pathological inflammation and viral infections.
Journal ArticleDOI
Resveratrol modulates drug- and carcinogen-metabolizing enzymes in a healthy volunteer study
H-H. Sherry Chow,Linda L. Garland,Chiu Hsieh Hsu,Donna R. Vining,Wade M. Chew,Jessica A. Miller,Marjorie Perloff,James A. Crowell,David S. Alberts +8 more
TL;DR: It is concluded that resveratrol can modulate enzyme systems involved in carcinogen activation and detoxification, which may be one mechanism by which resver atrol inhibits carcinogenesis.