Exenatide upregulates gene expression of glucagon‐like peptide‐1 receptor and nerve growth factor in streptozotocin/nicotinamide‐induced diabetic mice

Gümüşlü, Esen; Çine, Naci; Ertan, Merve; Mutlu, Oğuz; Çelikyurt, İpek Komşuoğlu; Ulak, Güner

doi:10.1111/fcp.12329

Cited by 16 publications

(5 citation statements)

References 58 publications

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“…Although there are many available treatments for T2DM [3], there is still a very urgent need to develop new drugs for the treatment of this disease. Recently, the clarification of the molecular mechanisms underlying the development of metabolic syndrome and the identification of novel targets for the prevention and therapy of T2DM have been widely studied by worldwide researchers [4–6]. It has now been clarified that the serum level of transforming growth factor β (TGF‐ β ) increased in patients with T2DM [7,8], and the TGF‐ β /Smad pathway was involved in the emergence of this disease.…”

Section: Introductionmentioning

confidence: 99%

SIS3, a good candidate for the reverse of type 2 diabetes mellitus in mice

Wang

Yan

Cui

et al. 2020

Fundamemntal Clinical Pharma

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TGF‐β signaling plays an extremely important role in the occurrence and development of type 2 diabetes mellitus (T2DM), and the blockade of TGF‐β/Smad3 pathway protests against the high‐fat diet‐induced obesity and diabetes. As a specific small molecule inhibitor of Smad3 protein, the biological activities of compound SIS3 were evaluated by high‐fat diet‐induced T2DM model mice. In vivo results indicated that SIS3 can not only significantly reduce the body weight, fat mass, and fasting blood glucose in high‐fat diet‐induced T2DM model mice, but also improve insulin sensitivity and oral glucose tolerance of high‐fat diet‐induced T2DM model mice after the injection of SIS3 with 5 mg/kg for 45 days.

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Section: Introductionmentioning

confidence: 99%

SIS3, a good candidate for the reverse of type 2 diabetes mellitus in mice

Wang

Yan

Cui

et al. 2020

Fundamemntal Clinical Pharma

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“…Although this finding is preliminary and requires further investigation, it enhances knowledge regarding GLP-1 role in mental disorders. Animal studies have suggested that development of diabetes is associated with a reduction in the expression of GLP-1R in the hippocampus (Gumuslu et al, 2018). In addition, decreased hypothalamic expression of GLP-1R in individuals with type 2 diabetes has been previously documented (Ten Kulve et al, 2016).…”

Section: Discussionmentioning

confidence: 99%

The effect of body mass index on glucagon-like peptide receptor gene expression in the post mortem brain from individuals with mood and psychotic disorders

Mansur

Fries²,

Trevizol³

et al. 2019

European Neuropsychopharmacology

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There is an increasing interest in the putative role of glucagon-like peptide 1 receptor (GLP-1R) agonists as novel therapeutic agents for mental disorders. Herein, we investigated the expressions of GLP-1R and GLP-2R genes, and its relationship with body mass index (BMI), in the post-mortem brain tissue of patients with mood (MD) and psychotic disorders. Brain samples were localized to the dorsolateral prefrontal cortex (dlPFC) (n = 459) and hippocampus (n = 378). After adjustment for age, sex, ethnicity, post-mortem interval (PMI) and BMI, we observed significant differences, between healthy controls and MD subjects, in GLP-1R and GLP-2R gene expression in the dlPFC (β = 1.504, p = 0.004; and β = 1.305, p = 0.011, respectively); whereas in the hippocampus, only GLP-1R expression was significantly associated with MD (β = −1.28, p = 0.029). No significant differences were found in relation to schizophrenia. In addition, we observed a moderating effect of MD diagnosis on the associations between BMI, GLP-1R and GLP-2R expression values in the dlPFC (β = −0.05, p = 0.003; and β = −0.04, p = 0.004, respectively). There was a similar moderating effect for GLP-1R in the hippocampus (β = 0.043, 95% CI 0.003; 0.08 p = 0.03), but in an opposite direction than observed in the dlPFC. This is the first evidence of abnormal gene expression of GLP-1R and GLP-2R in postmortem brain of individuals with MD, providing a rationale for further inquiry and proof of principle interventional studies.

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“…After acclimatization, diabetes was induced in balb/c mice with slight modification, as described earlier [ 67 ]. All overnight-fasted mice were given a single dose of (i.p) injection of STZ 150 mg/kg body weight (BW), dissolved in citrate buffer of 0.1 m after 15 min of nicotinamide at 240 mg/kg BW (i.p).…”

Section: Methodsmentioning

confidence: 99%

Quercetin and Kaempferol as Multi-Targeting Antidiabetic Agents against Mouse Model of Chemically Induced Type 2 Diabetes

Ali,

Hassan,

Ansari

et al. 2024

Pharmaceuticals

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Diabetes, a multifactorial metabolic disorder, demands the discovery of multi-targeting drugs with minimal side effects. This study investigated the multi-targeting antidiabetic potential of quercetin and kaempferol. The druggability and binding affinities of both compounds towards multiple antidiabetic targets were explored using pharmacokinetic and docking software (AutoDock Vina 1.1.2). Our findings showed that quercetin and kaempferol obey Lipinski’s rule of five and exhibit desirable ADMET (absorption, distribution, metabolism excretion, and toxicity) profiles. Both compounds showed higher binding affinities towards C-reactive protein (CRP), interleukin-1 (IL-1), dipeptidyl peptidase-4 (DPP-IV), peroxisome proliferator-activated receptor gamma (PPARG), protein tyrosine phosphatase (PTP), and sodium–glucose co-transporter-1 (SGLT-1) compared to metformin (the positive control). Both quercetin and kaempferol inhibited α-amylase activity (in vitro) up to 20.30 ± 0.49 and 37.43 ± 0.42%, respectively. Their oral supplementation significantly reduced blood glucose levels (p < 0.001), improved lipid profile (p < 0.001), and enhanced total antioxidant status (p < 0.01) in streptozotocin–nicotinamide (STZ-NA)-induced diabetic mice. Additionally, both compounds significantly inhibited the proliferation of Huh-7 and HepG2 (cancer cells) (p < 0.0001) with no effect on the viability of Vero cell line (non-cancer). In conclusion, quercetin and kaempferol demonstrated higher binding affinities towards multiple targets than metformin. In vitro and in vivo antidiabetic potential along with the anticancer activities of both compounds suggest promise for further development in diabetes management. The combination of both drugs did not show a synergistic effect, possibly due to their same target on the receptors.

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Exenatide upregulates gene expression of glucagon‐like peptide‐1 receptor and nerve growth factor in streptozotocin/nicotinamide‐induced diabetic mice

Cited by 16 publications

References 58 publications

SIS3, a good candidate for the reverse of type 2 diabetes mellitus in mice

SIS3, a good candidate for the reverse of type 2 diabetes mellitus in mice

The effect of body mass index on glucagon-like peptide receptor gene expression in the post mortem brain from individuals with mood and psychotic disorders

Quercetin and Kaempferol as Multi-Targeting Antidiabetic Agents against Mouse Model of Chemically Induced Type 2 Diabetes

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