Accumulation and metabolism of the anticancer flavonoid 5,7-dimethoxyflavone compared to its unmethylated analog chrysin in the Atlantic killifish

Tsuji, Petra A.; Winn, Richard N.; Walle, Thomas

doi:10.1016/j.cbi.2006.08.023

Cited by 51 publications

(36 citation statements)

References 27 publications

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“…The identification of metabolites indicated that methoxyflavones in KP were mainly metabolized to their demethylated forms and were conjugated to the sulfate and glucuronide forms to a minor extent. Tsuji et al (2006) also found demethylation and glucuronidation of DMF after administration of DMF. The metabolites of KP can be found in rat feces and urine samples after administration of KP, but they were not detected in blood samples.…”

Section: Pharmacokinetics Study Of Methoxyflavones In Kpmentioning

confidence: 86%

“…Walle et al (2007) reported that after oral administration of DMF, it was found mainly in the liver with much higher levels than in plasma, kidney, and lung. Tsuji et al (2006) also reported that after administration of DMF to Atlantic killifish, the highest concentration of DMF was found in liver followed by brain, intestines, gill, and skin. In the current study, the methoxyflavones were detected in brain and testes, indicating their ability to penetrate the blood-brain and bloodtesticular barriers.…”

Section: Pharmacokinetics Study Of Methoxyflavones In Kpmentioning

confidence: 93%

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Pharmacokinetics, Bioavailability, Tissue Distribution, Excretion, and Metabolite Identification of Methoxyflavones in Kaempferia parviflora Extract in Rats

Mekjaruskul¹,

Jay²,

Sripanidkulchai³

2012

Drug Metab Dispos

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ABSTRACT:Kaempferia parviflora (KP) is an herbal plant in the family of Zingiberaceae. KP mainly contains methoxyflavones, especially 5,7-dimethoxyflavone (DMF), 5,7,4-trimethoxyflavone (TMF), and 3,5,7,3,4-pentamethoxyflavone (PMF). The present study was designed to characterize the pharmacokinetics, including bioavailability, distribution, excretion, and identification of metabolites after administration of a KP ethanolic extract. Male rats were orally or intravenously administered a 250 mg/kg concentration of a KP extract, and blood samples were obtained at selected times to determine pharmacokinetic parameters of PMF, TMF, and DMF. For distribution and excretion studies, the organs, urine, and feces samples were collected at various times after oral administration of a larger (750 mg/kg) dose of KP extract. Methoxyflavones in the biological samples were quantified by high-performance liquid chromatography-UV, and the metabolites in urine and feces were further identified by using liquid chromatography-tandem mass spectrometry. After oral administration, concentrations of the three methoxyflavones quickly approached their maximal concentration, ranging from 0.55 to 0.88 g/ml within 1 to 2 h after administration, and then were gradually excreted with half-lives of 3 to 6 h. The methoxyflavones showed low oral bioavailability of 1 to 4%. Three methoxyflavones were detected at their highest levels in liver followed by kidney. They were also found in lung, testes, and brain. After absorption, organ distribution, and metabolism, the components of KP were mainly eliminated through urine in the forms of demethylated, sulfated, and glucuronidated products and as demethylated metabolites in the feces. The parent compounds were found to have 0.79, 1.76, and 3.10% dose recovery in urine and 1.06, 1.77, and 0.96% dose recovery in feces for PMF, TMF, and DMF, respectively. These studies are the first to describe the pharmacokinetics of KP extract to provide the information on blood and tissue levels.

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Section: Pharmacokinetics Study Of Methoxyflavones In Kpmentioning

confidence: 86%

Section: Pharmacokinetics Study Of Methoxyflavones In Kpmentioning

confidence: 93%

Pharmacokinetics, Bioavailability, Tissue Distribution, Excretion, and Metabolite Identification of Methoxyflavones in Kaempferia parviflora Extract in Rats

Mekjaruskul¹,

Jay²,

Sripanidkulchai³

2012

Drug Metab Dispos

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“…Cytochrome P450 isozymes are reported to be responsible for O-demethylad reactions (Honda et al, 2011). For instance, 5,7-dimethoxyflavone was reported metabolized primarily to 5-methoxy-7-hydroxyflavone by recombinant CYP1A1 (Tsuji et al, 2006). In addition, tangeretin, a major flavonoid in citrus fruits, was purportedly metabolized to two O-demethylated metabolites by CYP1A2 and CYP3A4 (Breinholt et al, 2003).…”

Section: Discussionmentioning

confidence: 99%

Metabolism of [6]-Shogaol in Mice and in Cancer Cells

Chen

Lv²,

Soroka³

et al. 2012

Drug Metab Dispos

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ABSTRACT:Ginger has received extensive attention because of its antioxidant, antiinflammatory, and antitumor activities. However, the metabolic fate of its major components is still unclear. In the present study, the metabolism of [6]-shogaol, one of the major active components in ginger, was examined for the first time in mice and in cancer cells. Thirteen metabolites were detected and identified, seven of which were purified from fecal samples collected from

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“…anti-inflammatory, antioxidant [18][19][20][21], anticancer [22,23], muscular metabolismenhancing [24], anti-photoaging [25], phosphodiesterase (PDE)5 inhibitory [26], anti-cardiovascular disease [27], and viral protease inhibitory [28] activities). A large number of studies have investigated the bioactivities of black ginger extract (KPE), which is rich in PMFs [24,[29][30][31][32][33][34][35][36][37].…”

Section: Backgroundsmentioning

confidence: 99%

Enhancement of physical fitness by black ginger extract rich in polymethoxyflavones: a double-blind randomized crossover trial

Toda¹

2016

Integr Mol Med

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Accumulation and metabolism of the anticancer flavonoid 5,7-dimethoxyflavone compared to its unmethylated analog chrysin in the Atlantic killifish

Cited by 51 publications

References 27 publications

Pharmacokinetics, Bioavailability, Tissue Distribution, Excretion, and Metabolite Identification of Methoxyflavones in Kaempferia parviflora Extract in Rats

Pharmacokinetics, Bioavailability, Tissue Distribution, Excretion, and Metabolite Identification of Methoxyflavones in Kaempferia parviflora Extract in Rats

Metabolism of [6]-Shogaol in Mice and in Cancer Cells

Enhancement of physical fitness by black ginger extract rich in polymethoxyflavones: a double-blind randomized crossover trial

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