Insulin signaling: A potential signaling pathway for the stimulatory effect of kaempferitrin on glucose uptake in skeletal muscle

Cazarolli, Luisa Helena; Pereira, Danielle Fontana; Kappel, Virgínia Demarchi; Folador, Poliane; Figueiredo, Maria dos Santos Reis Bonorino; Pizzolatti, Moacir Geraldo; Silva, Fátima Regina Mena Barreto

doi:10.1016/j.ejphar.2013.02.029

Cited by 47 publications

(27 citation statements)

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“…The glucose transporter isoforms GLUT4 and GLUT1 are highly expressed in muscle cells, with GLUT4 being more abundant in an intracellular compartment from which it is quickly translocated to the plasma membrane as a response to insulin challenge. Both insulin-dependent and non-insulin-dependent diabetes were shown to reduce glucose utilization in muscle either due to a defective expression or dysregulation in GLUT4 translocation [3], [18]. In the present study, glucose uptake was found to be normal in the control group treated with no insulin.…”

Section: Resultssupporting

confidence: 41%

Novel Benzoxazine-Based Aglycones Block Glucose Uptake In Vivo by Inhibiting Glycosidases

et al. 2014

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Glycoside hydrolases catalyze the selective hydrolysis of glycosidic bonds in oligosaccharides, polysaccharides, and their conjugates. β-glucosidases occur in all domains of living organisms and constitute a major group among glycoside hydrolases. On the other hand, the benzoxazinoids occur in living systems and act as stable β-glucosides, such as 2-(2,4-dihydroxy-7-methoxy-2H-1,4-benzoxazin-3(4H)-one)-β-D-gluco-pyranose, which hydrolyse to an aglycone DIMBOA. Here, we synthesized the library of novel 1,3-benzoxazine scaffold based aglycones by using 2-aminobenzyl alcohols and aldehydes from one-pot reaction in a chloroacetic acid catalytic system via aerobic oxidative synthesis. Among the synthesized benzoxazines, 4-(7-chloro-2,4-dihydro-1H-benzo[d][1,3]oxazin-2-yl)phenol (compound 7) exhibit significant inhibition towards glucosidase compared to acarbose, with a IC50 value of 11.5 µM. Based upon results generated by in silico target prediction algorithms (Naïve Bayesian classifier), these aglycones potentially target the additional sodium/glucose cotransporter 1 (where a log likelihood score of 2.70 was observed). Furthermore, the in vitro glucosidase activity was correlated with the in silico docking results, with a high docking score for the aglycones towards the substrate binding site of glycosidase. Evidently, the in vitro and in vivo experiments clearly suggest an anti-hyperglycemic effect via glucose uptake inhibition by 4-(7-chloro-2,4-dihydro-1H-benzo[d][1,3]oxazin-2-yl)phenol in the starved rat model. These synthetic aglycones could constitute a novel pharmacological approach for the treatment, or re-enforcement of existing treatments, of type 2 diabetes and associated secondary complications.

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Section: Resultssupporting

confidence: 41%

Novel Benzoxazine-Based Aglycones Block Glucose Uptake In Vivo by Inhibiting Glycosidases

et al. 2014

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“…As previously reported, there are two signaling pathways leading to GLUT4 translocation to PM (Fullerton et al, 2012; Cazarolli et al, 2013), including the activation of PI3K and the activation of AMPK. In this study, when the L6 cells were incubated with compound C for 30 min before addition of ST-EtOAc, the translocation of GLUT4 to PM caused by ST-EtOAc stimulation was mainly inhibited by the addition of compound C ( Figure 2B ).…”

Section: Discussionmentioning

confidence: 62%

Hypoglycemic Activity and the Potential Mechanism of the Flavonoid Rich Extract from Sophora tonkinensis Gagnep. in KK-Ay Mice

Deng

Han

et al. 2016

Front. Pharmacol.

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This study investigated the active principles, hypoglycemic activity and potential mechanisms of the flavonoid rich extract from Sophora tonkinensis Gagnep. (ST-EtOAc) in KK-Ay diabetic mice. An off-line semipreparative liquid chromatography-nuclear magnetic resonance (LC-NMR) and liquid chromatography-ultraviolet-electrospray ionization mass spectrometry (LC-UV–ESIMS) protocol was performed to determine 13 flavonoids from ST-EtOAc. ST-EtOAc administrated orally to the KK-Ay mice significantly increased their sensibility to insulin, reduced fasting blood-glucose levels and blood lipid indexes such as triglyceride and cholesterol. Moreover, ST-EtOAc exhibited a strong effect of stimulation on glucose transporter 4 (GLUT4) translocation by 2.7-fold in L6 cells. However, the selective AMP-activated protein kinase (AMPK) inhibitor compound C can completely inhibit the activation of the AMPK pathway and prevent the GLUT4 translocation caused by ST-EtOAc. In vivo, phosphorylation of the AMPK expression in the liver and skeletal muscle was measured. The results showed phosphorylation of the AMPK had been improved and GLUT4 expression had been also enhanced. In this paper, we conclude that, ST-EtOAc seems to have potential beneficial effects on the treatment of type 2 diabetes mellitus with the probable mechanism of stimulating GLUT4 translocation modulated by the AMPK pathway.

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“…O restante, 31 artigos foram utilizados na pesquisa, e apresentados na Tabela 1, em que estão listadas as espécies de Bauhinia L. que possuem ensaios relacionados à atividade hipoglicemiante e respectivas fontes de referência. RUSSO et al, 1990;SILVA et al, 2002a;PEPATO et al, 2002, JORGE et al, 2004SOUZA et al, 2004;LINO et al, 2004;VASCONCELOS et al, 2004;MENEZES et al, 2007;CUNHA et al, 2010;CURCIO et al, 2012;CAZAROLLI et al, 2013;FARAG et MARTINEZ et al, 2009;MESHRAM et al, 2013B. thonningii OJEZELE, ABATAN, 2011B.…”

Section: Resultsunclassified

Experimental Studies With Species of Bauhinia (Fabaceae) to Evaluate the Antidiabetic Activity

Paula

2016

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RESUMO:Modelos de estudo in vivo e in vitro e em enzimas/receptores são utilizados quando se pretende comprovar a ação farmacológica de um determinado extrato e/ou princípio ativo obtido de plantas, além de elucidar o mecanismo de ação. O objetivo deste estudo foi realizar um levantamento da literatura sobre quais os ensaios que já foram realizados com plantas do gênero Bauhinia L. para verificar a atividade hipoglicemiante, e quais as espécies pesquisadas. Para isso, foi realizado uma revisão da literatura através de busca eletrônica nas bases de dados Pubmed, Science direct, Lilacs e na biblioteca eletrônica Scielo, publicados no período de 1995 à 2015 (20 anos), utilizando como descritores "Bauhinia" and "extract" and "hypoglycemic" or " seus correspondentes em português, "Bauhinia" e "extrato" e antidiabetic" "hipoglicêmica" ou "antidiabético". Foram localizados artigos relacionados à pesquisa com doze espécies de Bauhinia L. A Bauhinia forficata é a que mais apresenta estudos sobre o tema, sendo localizado 13 artigos, seguida da B. variegata com 4 estudos. Foi possível verificar que pouco se conhece sobre a atividade hipoglicemiantes das espécies de Bauhinia L., e que mais estudos são necessários para comprovar o uso popular. Palavras-chave: pata de vaca, planta medicinal, diabetes ABSTRACT:In vivo and in vitro and in enzymes / receptors study models are used when you want to prove the pharmacological action of a particular extract and / or active ingredient from plants, as well as elucidate the mechanism of action. The aim of this study was to survey the literature on which trials have already been conducted with the genus Bauhinia L. plans to check the hypoglycemic activity, and what the surveyed species. For this, we conducted a literature review through electronic search on Pubmed, Science direct, Lilacs and electronic library SciELO, published from 1995 to 2015 (20 years), using as keywords "Bauhinia" and "extract "and" hypoglycemic "or" Antidiabetic "their equivalents in Portuguese," Bauhinia "and" extrato "and" hipoglicêmico "or" anti-diabético". Research-related articles were found with twelve species of Bauhinia L. The Bauhinia forficata is the one that presents studies on the subject, being located 13 articles, followed by B. variegata , 4 studies. It observed that little is known about the hypoglycemic activity of the species of Bauhinia L., and that further studies are needed to confirm the popular use.

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Insulin signaling: A potential signaling pathway for the stimulatory effect of kaempferitrin on glucose uptake in skeletal muscle

Cited by 47 publications

References 46 publications

Novel Benzoxazine-Based Aglycones Block Glucose Uptake In Vivo by Inhibiting Glycosidases

Novel Benzoxazine-Based Aglycones Block Glucose Uptake In Vivo by Inhibiting Glycosidases

Hypoglycemic Activity and the Potential Mechanism of the Flavonoid Rich Extract from Sophora tonkinensis Gagnep. in KK-Ay Mice

Experimental Studies With Species of Bauhinia (Fabaceae) to Evaluate the Antidiabetic Activity

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