Effect of quercetin and glucuronide metabolites on the monoamine oxidase-A reaction in mouse brain mitochondria

Yoshino, Saki; Hara, Aya; Sakakibara, Hiroyuki; Kawabata, Kyuichi; Tokumura, Akira; Ishisaka, Akari; Kawai, Yoshichika; Terao, Junji

doi:10.1016/j.nut.2010.09.002

Cited by 75 publications

(53 citation statements)

References 39 publications

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“…A PK profile of isorhamnetin glucuronide conjugate in normal and CKD rats; B PK profile of quercetin glucuronide conjugate in normal and CKD rats; C PK profile of isorhamnetin sulfate conjugate in normal and CKD rats; D PK profile of quercetin sulfate conjugate in normal and CKD rats; E PK profile of quercetin in normal and CKD rats; F PK profile of isorhamnetin in normal and CKD rats. (Terao et al, 2011;Yoshino et al, 2011). As reported, luteolin monoglucuronide was converted to free aglycone during inflammation using lipopolysaccharide-stimulated human neutrophils (Shimoi et al, 2001).…”

Section: Discussionmentioning

confidence: 66%

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Conjugated metabolites represent the major circulating forms ofAbelmoschus manihot in vivoand show an altered pharmacokinetic profile in renal pathology

Guo

Shang

et al. 2015

Pharmaceutical Biology

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Objective: Flavonoids are main active components of A. manihot, which can be transformed into glucuronide/sulfate conjugates in vivo. Exploring the pharmacokinetic profile of these conjugates is necessary to further elucidate the mechanism of action. Material and method: Flavonoid fraction of A. manihot (FFA) was extracted from A. manihot flower with ethanol. FFA (400 mg/kg) was orally given to normal rats and chronic kidney disease (CKD) model rats. Blood samples were collected at 5, 15, 30, 45, 60, 90, 120, 240, 360, and 720 min after administration. The plasma concentrations of quercetin and isorhamnetin glucuronide/sulfate conjugates were analyzed by UPLC-MS/MS. Results: In normal rats, AUC of quercetin-glucuronide conjugates, isorhamnetin-glucuronide conjugates, quercetin-sulfate conjugates, and isorhamnetin-sulfate conjugates was 459. 45 ± 192.70, 1153.01 ± 697.04, 417.81 ± 220.31, and 2475.19 ± 1085.22 mmol h/L, respectively. While AUC of quercetin and isorhamnetin was 5.47 ± 2.54 and 30.73 ± 25.95 mmol h/L. AUC of the glucuronide-sulfate conjugates of quercetin and isorhamnetin is 125-times higher than that of aglycone (quercetin and isorhamnetin), showing that glucuronide/sulfate conjugates represent the major circulating forms of A. manihot flavonoid in vivo. AUC of isorhamnetinglucuronide conjugates and quercetin-sulfate conjugates was 719.65 ± 619.22 and 275.49 ± 1 60.95 mmol h/L, indicating that less conjugated metabolites were formed in CKD rats compared with normal rats. The ratio of AUC glucuronide/sulfate /AUC aglycone decreased from 125 to 104, which implied the impaired phase II metabolism ability in CKD rat. Discussion and conclusion: Glucuronide-sulfate conjugates provide an important clue for further elucidating the activity of conjugated metabolites and their relationship with the nephroprotective efficacy of A. manihot. It is necessary to take caution when extrapolating pharmacokinetics parameters from healthy animals in designing pharmacological studies.

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Section: Discussionmentioning

confidence: 66%

“…In recent years, there has been a growing interest in the biological function of flavonoid glucuronide-sulfate conjugates (Galindo et al, 2012;Shimoi et al, 2001;Terao et al, 2011;Yoshino et al, 2011). Exploring the pharmacokinetic profile of these conjugates is necessary to further elucidate the mechanism of action.…”

Section: Introductionmentioning

confidence: 99%

Conjugated metabolites represent the major circulating forms ofAbelmoschus manihot in vivoand show an altered pharmacokinetic profile in renal pathology

Guo

Shang

et al. 2015

Pharmaceutical Biology

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“…The pellet was washed with the same buffer using similar centrifugation conditions. Supernatant was used for lipid peroxidation assay or malondialdehyde (MDA)-level estimation, while precipitates were used for MAO estimation (Yoshino et al 2011). Supernatant as such and precipitates after dissolution were also taken for the estimation of total protein content using Lowry method.…”

Section: Biochemical Estimationsmentioning

confidence: 99%

Antidepressant and anxiolytic effects of Garcinia indica fruit rind via monoaminergic pathway

2017

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Depression and anxiety are the most crippling neuropsychiatric disorders of this modern era. These mostly occur as anxiety followed by depression or in mixed state. Therefore, there is an urgent need of a safe and effective treatment, which proves its worth in this ailment. What else than a conventional food would be a better choice for a convenient therapy. Therefore, Garcinia indica, commonly known as Kokam, fruit rind has been used in the present study to investigate its antidepressant and anti-anxiety potential using forced swim test, tail suspension test, and reserpine-induced hypothermia; and elevated plus maze, hole-board test, and light dark model, respectively. Garcinia indica fruit rind given to mice with food for consecutive 14 days at 0.5, 1, and 2% w/w significantly (p \ 0.05) reduced despair behavior in forced swim test, immobility duration in tail suspension test, and also switched the hypothermia (reserpine induced) to normal temperature significantly (p \ 0.05). Garcinia indica significantly (p \ 0.05) raised the time elapsed and count of entries in open arms of elevated plus maze, enhanced incidence of head dipping in holes of hole board along with duration of expending time in lit compartment of light dark model, exhibiting its anti-anxiety effect. Garcinia indica significantly reduced monoamine oxidase and malondialdehyde levels providing support to neuroprotective potential of fruit rind. The mechanistic study showed the participation of G. indica at a 1 -adrenoceptor and D 2 -dopamine receptor, by attenuating prazosin and sulpirideinduced increase in immobility duration. Garcinia indica fruit rind showed a significant antidepressant and anxiolytic effect while no effect on locomotor activity, i.e., no psycho-stimulation.

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“…The resulting aglycone (i.e., quercetin) is then absorbed and metabolized into quercetin glucuronides and glucuronyl sulfates of methylated quercetin, and the quercetin metabolites also show antidepressant effects with oral administration (21). There is a report that quercetin and its glucuronide metabolites affect the monoamine oxidase-A in brain mitochondria and attenuate the breakdown of serotonin (22). There is some possibility that the sleep-improving effect of AVLE is due to this protection against the decomposition of serotonin.…”

Section: Discussionmentioning

confidence: 99%

The Improvement of Sleep by Oral Intake of GABA and <i>Apocynum venetum</i> Leaf Extract

Yasuda

Yamashita

Maru

et al. 2015

Journal of Nutritional Science and Vitaminology, J Nutr Sci Vit

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SummaryThe effects of two food materials, g-aminobutyric acid (GABA) produced by natural fermentation and Apocynum venetum leaf extract (AVLE), on the improvement of sleep were investigated in humans. The electroencephalogram (EEG) test revealed that oral administration of GABA (100 mg) and AVLE (50 mg) had beneficial effects on sleep. GABA shortened sleep latency by 5.3 min and AVLE increased non-rapid eye movement (REM) sleep time by 7.6%. Simultaneous intake of GABA and AVLE shortened sleep latency by 4.3 min and increased non-REM sleep time by 5.1%. The result of questionnaires showed that GABA and AVLE enabled subjects to realize the effects on sleep. These results mean that GABA can help people to fall asleep quickly, AVLE induces deep sleep, and they function complementarily with simultaneous intake. Since both GABA and AVLE are materials of foods and have been ingested for a long time, they can be regarded as safe and appropriate for daily intake in order to improve the quality of sleep.

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Effect of quercetin and glucuronide metabolites on the monoamine oxidase-A reaction in mouse brain mitochondria

Cited by 75 publications

References 39 publications

Conjugated metabolites represent the major circulating forms ofAbelmoschus manihot in vivoand show an altered pharmacokinetic profile in renal pathology

Conjugated metabolites represent the major circulating forms ofAbelmoschus manihot in vivoand show an altered pharmacokinetic profile in renal pathology

Antidepressant and anxiolytic effects of Garcinia indica fruit rind via monoaminergic pathway

The Improvement of Sleep by Oral Intake of GABA and <i>Apocynum venetum</i> Leaf Extract

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