Mechanisms of antidiabetic effects of flavonoid rutin

Ghorbani, Ahmad

doi:10.1016/j.biopha.2017.10.001

Cited by 378 publications

(247 citation statements)

References 64 publications

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“…Similar to islets from T2D organ donors, exhibiting β-cell dysfunction and increased expression of pro-inflammatory cytokines, exposure of non-diabetic islets to high glucose concentrations (24–72 h) results in an increased expression of pro-inflammatory signals that negatively impact β-cell function [3, 7, 11]. The data presented here show that the Gpr142 expression in islets is important to maintain a fully functioning β-cell machinery since Gpr142-KD is associated with the release of a panel of cytokines that are mediators of an inflammatory response [25].…”

Section: Discussionmentioning

confidence: 99%

The functional impact of G protein-coupled receptor 142 (Gpr142) on pancreatic β-cell in rodent

Al-Amily

Dunér

Groop

et al. 2019

Pflugers Arch - Eur J Physiol

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We have recently shown that the G protein-coupled receptor 142 (GPR142) is expressed in both rodent and human pancreatic β-cells. Herein, we investigated the cellular distribution of GPR142 within islets and the effects of selective agonists of GPR142 on glucose-stimulated insulin secretion (GSIS) in the mouse islets and INS-1832/13 cells. Double-immunostaining revealed that GPR142 immunoreactivity in islets mainly occurs in insulin-positive cells. Potentiation of GSIS by GPR142 activation was accompanied by increased cAMP content in INS-1832/13 cells. PKA/Epac inhibition markedly suppressed the effect of GPR142 activation on insulin release. Gpr142 knockdown (Gpr142-KD) in islets was accompanied by elevated release of MCP-1, IFNγ, and TNFα during culture period and abolished the modulatory effect of GPR142 activation on the GSIS. Gpr142-KD had no effect on Ffar1, Ffar2, or Ffar3 mRNA while reducing Gpr56 and increasing Tlr5 and Tlr7 mRNA expression. Gpr142-KD was associated with an increased expression of Chrebp, Txnip, RhoA, and mitochondrial Vdac1 concomitant with a reduced Pdx1, Pax6, and mitochondrial Vdac2 mRNA levels. Long-term exposure of INS-1832/13 cells to hyperglycemia reduced Gpr142 and Vdac2 while increased Chrebp, Txnip, and Vdac1 mRNA expression. GPR142 agonists or Bt2-cAMP counteracted this effect. Glucotoxicity-induced decrease of cell viability in Gpr142-KD INS-1 cells was not affected by GPR142-agonists while Bt2-cAMP prevented it. The results show the importance of Gpr142 in the maintenance of pancreatic β-cell function in rodents and that GPR142 agonists potentiate GSIS by an action, which most likely is due to increased cellular generation of second messenger molecule cAMP.Electronic supplementary materialThe online version of this article (10.1007/s00424-019-02262-7) contains supplementary material, which is available to authorized users.

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Section: Discussionmentioning

confidence: 99%

The functional impact of G protein-coupled receptor 142 (Gpr142) on pancreatic β-cell in rodent

Al-Amily

Dunér

Groop

et al. 2019

Pflugers Arch - Eur J Physiol

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“…The therapeutic uses of phenolic compounds have attracted much interest as they exert a wide range of bioactivities, including antioxidant [38][39][40], antibacterial [41][42][43], antifungal [43][44][45], anti-inflammatory [46,47], and anticancer [48,49] activities. Therefore, the phenolic content can be used as an important indicator of biological attributes of plant extracts.…”

Section: Phytochemical Compositionmentioning

confidence: 99%

Multiple pharmacological approaches on Fibigia eriocarpa extracts by in vitro and computational assays

Zengin

Lobine

Mollica

et al. 2018

Fundamemntal Clinical Pharma

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The ethyl acetate, methanolic, and water extracts of Fibigia eriocarpa were assessed for a panoply of bioactivities. Total phenolic and flavonoid content were quantified as well as individual phenolic compounds by HPLC-DAD. The in vitro antioxidant and enzyme (acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, α-amylase, and α-glucosidase) inhibitory potential of the extracts were evaluated. In silico molecular docking was used to investigate possible interaction between dominant compounds and selected enzymes. Vanillin (303 μg/g extract), apigenin (270 μg/g extract), and kaempferol (180 μg/g extract) were the main compounds in the ethyl acetate extract, while the methanolic extract was characterized by the presence of vanillin, rutin, and apigenin (616, 616 and 252 μg/g extract, respectively). (+)-catechin (1422 μg/g extract) was the main compound in the water extracts. The ethyl acetate extract was found to be a superior source of antioxidant compounds and enzyme inhibitors against above-mentioned enzymes. Docking studies revealed that p-hydroxybenzoic and (+)-catechin have the best scores for tyrosinase, while kaempferol and apigenin showed the best binding pose for α-glucosidase, AChE, and BChE. Results amassed herein are the first report on the phytochemical and biological attributes of F. eriocarpa, which tend to validate the pharmacological uses of this plant as an alternative medicine.

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“…Flavonoids are common markers in botanical drugs or plant extracts that exhibit biological activity in multiple systems, but present poor bioavailability . This is the case of quercetin‐3‐ O ‐rutinoside (rutin), a glycosylated flavonoid with broad therapeutic interest due to its antidiabetic effect, among other demonstrated pharmacological activity . Its low bioavailability is a result of its low aqueous solubility and intestinal metabolism, when rutin turns into quercetin (its aglycone) and other by‐products …”

Section: Introductionmentioning

confidence: 99%

Matrix effects of the hydroethanolic extract and the butanol fraction of calyces fromPhysalis peruvianaL. on the biopharmaceutics classification of rutin

Moré

Feltrin

Brambila

et al. 2020

Journal of Pharmacy and Pharmacology

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Objectives The Biopharmaceutics Classification System (BCS) categorizes active pharmaceutical ingredients according to their solubility and permeability properties, which are susceptible to matrix or formulation effects. The aim of this research was to evaluate the matrix effects of a hydroethanolic extract of calyces from Physalis peruviana L. (HEE) and its butanol fraction (BF), on the biopharmaceutics classification of their major compound, quercetin‐3‐O‐rutinoside (rutin, RU). Methods Rutin was quantified by HPLC‐UV, and Caco‐2 cell monolayer transport studies were performed to obtain the apparent permeability values (Papp). Aqueous solubility was determined at pH 6.8 and 7.4. Key findings The Papp values followed this order: BF > HEE > RU (1.77 ± 0.02 > 1.53 ± 0.07 > 0.90 ± 0.03 × 10−5 cm/s). The lowest solubility values followed this order: HEE > RU > BF (2.988 ± 0.07 > 0.205 ± 0.002 > 0.189 ± 0.005 mg/ml). Conclusions According to these results, rutin could be classified as BCS classes III (high solubility/low permeability) and IV (low solubility/low permeability), depending on the plant matrix. Further work needs to be done in order to establish how apply the BCS for research and development of new botanical drugs or for bioequivalence purposes.

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Mechanisms of antidiabetic effects of flavonoid rutin

Cited by 378 publications

References 64 publications

The functional impact of G protein-coupled receptor 142 (Gpr142) on pancreatic β-cell in rodent

The functional impact of G protein-coupled receptor 142 (Gpr142) on pancreatic β-cell in rodent

Multiple pharmacological approaches on Fibigia eriocarpa extracts by in vitro and computational assays

Matrix effects of the hydroethanolic extract and the butanol fraction of calyces fromPhysalis peruvianaL. on the biopharmaceutics classification of rutin

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