Anti-diabetic effects of pentamethylquercetin in neonatally streptozotocin-induced diabetic rats

Yan, Wei; Xin, Xin; Jin, Zhendong; Yan, Hongyuan; Li, Xianhui; Wu, Jianzhao; Jin, Man-Wen

doi:10.1016/j.ejphar.2011.06.022

Cited by 27 publications

(15 citation statements)

References 27 publications

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“…Very recently, several studies described the metabolismregulating properties of PMQ, including glucose-lowering effects and upregulation of adiponectin production [21,22]. In the present study, we show for the first time that PMQ reduces body weight, serum glucose, lipid and insulin levels, as well as improving insulin resistance in MSG mice.…”

Section: Discussionsupporting

confidence: 50%

“…We have previously reported that PMQ upregulated adiponectin levels in 3T3-L1 adipocytes [21] and had glucose-lowering effects in a neonatally streptozotocin-induced rat model of diabetes [22]. Although PMQ has been reported to have glucose-lowering effects, the molecular targets of this compound have not been revealed and a more comprehensive analysis of its role in metabolic disorders has not been undertaken.…”

Section: Introductionmentioning

confidence: 99%

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Pentamethylquercetin generates beneficial effects in monosodium glutamate-induced obese mice and C2C12 myotubes by activating AMP-activated protein kinase

Shen

Han

et al. 2012

Diabetologia

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Aims/hypothesis Pentamethylquercetin (PMQ) has recently been shown to have glucose-lowering properties. Here, we aimed to characterise the effectiveness and underlying mechanisms of PMQ for ameliorating metabolic disorders in vivo and vitro. Methods We generated a mouse model of obesity by neonatal administration of monosodium glutamate (MSG) and used it to assess the properties of PMQ as a treatment for metabolic disorders. We also investigated the possible underlying mechanisms of PMQ in the prevention of metabolic disorders. Results Compared with normal mice, MSG mice had metabolic disorders, including central obesity, hyperinsulinaemia, insulin resistance, hyperglycaemia, hyperlipidaemia, decreased phosphorylation of AMP-activated protein kinase (AMPK) and acetyl-CoA carboxylase (ACC), and downregulated levels of GLUT4 in gastrocnemius muscles. In MSG mice, PMQ treatment (5, 10, 20 mg/kg daily) reduced body weight gain, waist circumference, adipose tissue mass, serum glucose, triacylglycerol and total cholesterol, while improving insulin resistance, activating AMPK and increasing ACC phosphorylation and GLUT4 abundance. In C2C12 myotubes, PMQ (10 μmol/l) increased glucose consumption by ∼65%. PMQ treatment (1-10 μmol/l) also activated AMPK, increased ACC phosphorylation and GLUT4 abundance, and upregulated the expression of some key genes involved in fatty acid oxidation. Conclusions/interpretation These findings suggest that PMQ can ameliorate metabolic disorders at least in part via stimulation of AMPK activity.

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Section: Discussionsupporting

confidence: 50%

Section: Introductionmentioning

confidence: 99%

Pentamethylquercetin generates beneficial effects in monosodium glutamate-induced obese mice and C2C12 myotubes by activating AMP-activated protein kinase

Shen

Han

et al. 2012

Diabetologia

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“…PMQ is a flavonoid compound and has been shown to have great anti-diabetic effects on streptozotocin-induced diabetic rats 22 and anti-obesity effects on MSG mice 17 . In this study, we found that PMQ could attenuate TG accumulation in 3T3-L1 adipocytes, combat hyperglycemia and hyperlipidemia and attenuate HFD-induced increases in the epididymal WAT mass in C57BL/6 mice.…”

Section: Discussionmentioning

confidence: 99%

“…PMQ can also be used to treat metabolic disease to improve glucose tolerance and insulin sensitivity in MSG-induced obese mice 17 and diabetic rats 22 through a process unrelated to insulin release. We found PMQ can increase Glut-4 and Cebp/α expression in 3T3-L1 adipocytes and the epididymal fat of HFD mice, thereby augmenting glucose consumption in fat cells, a change that may reduce serum glucose and lipid levels and appears to be at least partially responsible for the anti-metabolic disorder effects of this chemical.…”

Section: Discussionmentioning

confidence: 99%

Pentamethylquercetin induces adipose browning and exerts beneficial effects in 3T3-L1 adipocytes and high-fat diet-fed mice

Han

Shen

et al. 2017

Sci Rep

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Browning white adipocytes may be a new target in anti-obesity therapy. Pentamethylquercetin (PMQ) has been shown to have anti-obesity effects in monosodium glutamate-induced obese mice. Here, we aimed to study the anti-obesity effects of PMQ in vitro and in vivo and to determine if adipose browning is involved in the mechanism underlying the anti-obesity effects of PMQ. We evaluated the effects of PMQ on cell proliferation, cell differentiation, glucose consumption, cellular lipid metabolism, and related brown gene expression in 3T3-L1 adipocytes. We also investigated the effects of PMQ in a mouse model of high-fat diet (HFD)-induced obesity. Our results demonstrated that PMQ increased the consumption of glucose, inhibited the accumulation of cellular triglycerides (TGs), and induced the expression of brown adipocyte-specific genes, such as uncoupling protein 1 (UCP-1), during the early stage of differentiation in 3T3-L1 adipocytes. In HFD mice, PMQ treatment reduced waist circumference, LEE index, white adipose tissue (WAT) weight and white adipocyte size and increased brown adipose tissue (BAT) weight. Moreover, PMQ treatment induced mitochondrial biogenesis and upregulated UCP-1 expression in WAT. These findings suggest that PMQ may induce browning of adipose tissue, a phenomenon that is at least partly related to its anti-obesity effects.

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“…59) With regard to in vivo study, several attractive studies about antidiabetic and anti-obese effects of 25 in several animal models were reported. [60][61][62][63] The detailed mechanisms of 24 and 25 are still unclear, because many transcriptional factors are involved in agipogenesis. For example, early adipogenic transcription factors [e.g.…”

Section: Methoxyflavonols From the Rhizome Of Kaempferia Parvifloramentioning

confidence: 99%

Search for New Type of PPARγ Agonist-Like Anti-diabetic Compounds from Medicinal Plants

Matsuda

Nakamura

Yoshikawa

2014

Biological & Pharmaceutical Bulletin

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Potent ligands of peroxisome proliferator-activated receptor γ (PPARγ) such as thiazolidinediones (pioglitazone, troglitazone, etc.) improve insulin sensitivity by increasing the levels of adiponectin, an important adipocytokine associated with insulin sensitivity in adipose tissue. Several constituents from medicinal plants were recently reported to show PPARγ agonist-like activity in 3T3-L1 cells, but did not show agonistic activity at the receptor site different from thiazolidinediones. Our recent studies on PPARγ agonist-like constituents, such as hydrangenol and hydrangeic acid from the processed leaves of Hydrangea macrophylla var. thunbergii, piperlonguminine and retrofractamide A from the fruit of Piper chaba, and tetramethylkaempferol and pentamethylquercetin from the rhizomes of Kaempferia parviflora, are reviewed.

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Anti-diabetic effects of pentamethylquercetin in neonatally streptozotocin-induced diabetic rats

Cited by 27 publications

References 27 publications

Pentamethylquercetin generates beneficial effects in monosodium glutamate-induced obese mice and C2C12 myotubes by activating AMP-activated protein kinase

Pentamethylquercetin generates beneficial effects in monosodium glutamate-induced obese mice and C2C12 myotubes by activating AMP-activated protein kinase

Pentamethylquercetin induces adipose browning and exerts beneficial effects in 3T3-L1 adipocytes and high-fat diet-fed mice

Search for New Type of PPARγ Agonist-Like Anti-diabetic Compounds from Medicinal Plants

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