Absorption and Metabolism of Piceatannol in Rats

Setoguchi, Yuko; Oritani, Yukihiro; Ito, Ryouichi; Inagaki, Hideaki; Maruki‐Uchida, Hiroko; Ichiyanagi, Tsuyoshi; Ito, Tatsuhiko

doi:10.1021/jf404694y

Cited by 90 publications

(115 citation statements)

References 34 publications

(67 reference statements)

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“…23) The particular effect will depend on the structure of the compound, and stilbenes such as resveratrol and piceatannol are polyphenols that show the most promise for beneficial health effects. We previously investigated the absorption and metabolism of piceatannol in rats, 24) and the area under the time-concentration curve for intact piceatannol was two-times higher than that of intact resveratrol. After administration of piceatannol, isorhapontigenin, an O-methyl piceatannol metabolite, was detected in the intact form in rat plasma.…”

Section: Discussionmentioning

confidence: 99%

Piceatannol Lowers the Blood Glucose Level in Diabetic Mice

Uchida-Maruki

Inagaki

Ito

et al. 2015

Biological & Pharmaceutical Bulletin

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We previously found that passion fruit (Passiflora edulis) seeds contained a high amount of piceatannol (3,5,3′,4′-trans-tetrahydroxystilbene), a natural analog of resveratrol (3,5,4′-trans-trihydroxystilbene). Resveratrol has been proposed as a potential anti-metabolic disorder compound, by its activation of sirtuin and AMP-activated protein kinase. Many reports show that resveratrol ameliorates diet-induced obesity and insulin resistance. However, it is not known whether piceatannol also affects diet-induced obesity. We explored the effect of piceatannol on high fat diet-fed mice. The results showed that piceatannol did not affect high fat diet-induced body weight gain or visceral fat gain in mice. However, piceatannol did reduce fasting blood glucose levels. Furthermore, to explore the potential of passion fruit seed extract containing piceatannol as a functional food, passion fruit seed extract was administered in a genetic diabetic mouse model (db/db mice). Single administration of passion fruit seed extract, as well as piceatannol reduced the blood glucose levels of these db/db mice. These results suggest that piceatannol and passion fruit seed extract may have potential application in the prevention of diabetes.Key words piceatannol; passion fruit seed; antidiabetic activity; high fat diet; db/dbThe incidence of metabolic syndrome is increasing worldwide due to aging and changes in lifestyle. In particular, this increase is largely attributed to the rise in the prevalence of obesity, and this common metabolic disorder is associated with increased risk of cardiovascular diseases and type II diabetes, and the latter substantially decreases quality of life and increases health care costs. It is difficult to strictly control blood glucose levels over the long term, even though many anti-diabetic medications are clinically available. Therefore, the development of functional foods that can prevent or improve type II diabetes is an urgent matter.Resveratrol is a natural component of several plants, including grapes, berries, and peanuts. Resveratrol displays widespread functions and has several health-promoting effects owing to its anti-cancer, anti-inflammation, and antioxidant activity.1) Recently, resveratrol has been proposed as a potential anti-metabolic syndrome compound because of its role in activating sirtuin and AMP-activated protein kinase (AMPK).2-5) Indeed, several studies have shown that resveratrol protects mice against diet-induced obesity.6-8) Resveratrol has also been shown to have a favorable effect on glucose metabolism in humans.9,10) However, it should be noted that no weight loss has been reported after resveratrol treatment in any human study. 11)Piceatannol is a hydroxylated analog of resveratrol and is also found in various plants, including grapes and rhubarb. Although piceatannol shows activities similar to resveratrol, its levels in plants are significantly lower than those of resveratrol, 12) and it has therefore received far less research attention. We previously found that passion...

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Section: Discussionmentioning

confidence: 99%

Piceatannol Lowers the Blood Glucose Level in Diabetic Mice

Uchida-Maruki

Inagaki

Ito

et al. 2015

Biological & Pharmaceutical Bulletin

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“…Isorhapontigenin and rhapontigenin are both forms of O -methyl piceatannol [7]. Resveratrol-3- O -glucuronide, resveratrol-4′- O -glucuronide and resveratrol-3- O -sulfate are metabolites of resveratrol.…”

Section: Resultsmentioning

confidence: 99%

“…In the present study, isorhapontigenin and rhapontigenin showed SIRT1 induction effects in THP-1 cells. After intragastric administration of piceatannol, isorhapontigenin was detected in both the intact and conjugated forms, and rhapontigenin was detected only in conjugated form [7]. Therefore, after piceatannol intake, isorhapontigenin could contribute to the upregulation of SIRT1 additively with intact piceatannol.…”

Section: Discussionmentioning

confidence: 99%

“…After centrifugation, the supernatant was evaporated, and solvent was removed from the pellet by freeze-drying. The concentration of piceatannol in the lyophilized powder was measured using high-performance liquid chromatography (HPLC) analysis as previously described [7]. The powder contained piceatannol (85.4 μg/mg) as a primary polyphenol.…”

Section: Methodsmentioning

confidence: 99%

“…To elucidate the bioavailability and metabolism of piceatannol, we investigated the absorption and metabolism of piceatannol in rats [7]. After intragastric administration of piceatannol, isorhapontigenin, an O -methyl piceatannol metabolite, was detected in the intact form in rat plasma.…”

Section: Introductionmentioning

confidence: 99%

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Piceatannol and Its Metabolite, Isorhapontigenin, Induce SIRT1 Expression in THP-1 Human Monocytic Cell Line

et al. 2014

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Piceatannol is a phytochemical that is present in large amounts in passion fruit (Passiflora edulis) seeds, and is an analog of resveratrol. Recently, the absorption and metabolism of piceatannol were investigated in rats, and isorhapontigenin, O-methyl piceatannol, was detected as a piceatannol metabolite in rat plasma. To elucidate the function of piceatannol and its metabolites, we investigated the expression of sirtuin 1 (SIRT1) in THP-1 monocytic cells after treatment with piceatannol and its metabolites, and compared their effects with those of resveratrol and its metabolites. Piceatannol and resveratrol upregulated the expression levels of SIRT1 mRNA and SIRT1 protein. An extract of passion fruit seeds, which contained high levels of piceatannol, also upregulated SIRT1 mRNA expression. As for the metabolites, isorhapontigenin upregulated SIRT1 mRNA expression, whereas resveratrol glucuronides and sulfate did not affect SIRT1 expression. These findings indicate that after intake of piceatannol, not only piceatannol itself, but also its metabolite, isorhapontigenin, contributed to the upregulation of SIRT1 expression.

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Exploring the therapeutic potential of naturally occurring piceatannol in non‐communicable diseases

Gandhi,

Mahant,

Sharma

et al. 2023

BioFactors

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Piceatannol is a naturally occurring hydroxylated resveratrol analogue that can be found in a variety of fruits and vegetables. It has been documented to have a wide range of beneficial effects, including anti‐inflammatory, antioxidant, anti‐aging, anti‐allergic, antidiabetic, neuroprotective, cardioprotective, and chemopreventive properties. Piceatannol has significantly higher antioxidant activity than resveratrol. Piceatannol has been shown in preclinical studies to have the ability to inhibit or reduce the growth of cancers in various organs such as the brain, breast, lung, colon, cervical, liver, prostate, and skin. However, the bioavailability of Piceatannol is comparatively lower than resveratrol and other stilbenes. Several approaches have been reported in recent years to enhance its bioavailability and biological activity, and clinical trials are required to validate these findings. This review focuses on several aspects of natural stilbene Piceatannol, its chemistry, and its mechanism of action, and its promising therapeutic potential for the prevention and treatment of a wide variety of complex human diseases.

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Absorption and Metabolism of Piceatannol in Rats

Cited by 90 publications

References 34 publications

Piceatannol Lowers the Blood Glucose Level in Diabetic Mice

Piceatannol Lowers the Blood Glucose Level in Diabetic Mice

Piceatannol and Its Metabolite, Isorhapontigenin, Induce SIRT1 Expression in THP-1 Human Monocytic Cell Line

Exploring the therapeutic potential of naturally occurring piceatannol in non‐communicable diseases

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