teneligliptin hydrobromide  (Solapur Municipal)

Journal: FEBS Open Bio

Article Title: The dipeptidyl peptidase‐4 ( DPP ‐4) inhibitor teneligliptin enhances brown adipose tissue function, thereby preventing obesity in mice

doi: 10.1002/2211-5463.12498

Figure Lengend Snippet: Effects of teneligliptin treatment on HFD ‐induced obesity and obesity‐induced metabolic disorders. Teneligliptin was administered in the drinking water (80 mg·kg −1 ·day −1 ), for a total of 10 weeks, to male 6‐week‐old C57 BL /6N mice also fed a HFD . A and B: Body weight gain (A) and food intake (B) were measured during the administration period. C–F: After 10 weeks of treatment, plasma glucose (C) and triglycerol (D) levels, intraperitoneal WAT weight (E) and hepatic triglycerol accumulation levels (F) were determined. Plasma glucose and triglycerol and hepatic triglycerol levels were determined enzymatically. HFD , high‐fat diet; ND , normal diet; Tene, teneligliptin plus HFD . All the values are means + SE ( n = 5–8). * P < 0.05, ** P < 0.01.

Article Snippet: Teneligliptin hydrobromide hydrate (>95% purity confirmed by HPLC) was kindly provided by Mitsubishi Tanabe Pharma Corporation (Osaka, Japan).

Techniques: Clinical Proteomics

Journal: FEBS Open Bio

Article Title: The dipeptidyl peptidase‐4 ( DPP ‐4) inhibitor teneligliptin enhances brown adipose tissue function, thereby preventing obesity in mice

doi: 10.1002/2211-5463.12498

Figure Lengend Snippet: Body and tissue weights of mice treated with or without teneligliptin for 10 weeks

Article Snippet: Teneligliptin hydrobromide hydrate (>95% purity confirmed by HPLC) was kindly provided by Mitsubishi Tanabe Pharma Corporation (Osaka, Japan).

Techniques:

Journal: FEBS Open Bio

Article Title: The dipeptidyl peptidase‐4 ( DPP ‐4) inhibitor teneligliptin enhances brown adipose tissue function, thereby preventing obesity in mice

doi: 10.1002/2211-5463.12498

Figure Lengend Snippet: Effects of teneligliptin treatment on HFD ‐induced WAT dysfunction. Teneligliptin was administered in the drinking water (80 mg·kg −1 ·day −1 ), for a total of 10 weeks, to male 6‐week‐old C57 BL /6N mice also fed a HFD . (A) iWAT samples embedded in the paraffin were cut into 6‐μm sections, and each section was stained with haematoxylin and eosin. Representative images of iWAT sections are shown (the scale bars in the panels represent 200 μm). The average adipocyte size was determined by image analysis. All values are means + SE ( n = 7–10). (B) mRNA expression levels of genes related to chronic inflammation in eWAT were determined by real‐time RT ‐ PCR . HFD , high‐fat diet; ND , normal diet; Tene, teneligliptin plus HFD . All the values are means + SE ( n = 8–10). * P < 0.05, ** P < 0.01.

Article Snippet: Teneligliptin hydrobromide hydrate (>95% purity confirmed by HPLC) was kindly provided by Mitsubishi Tanabe Pharma Corporation (Osaka, Japan).

Techniques: Staining, Expressing, Quantitative RT-PCR

Journal: FEBS Open Bio

Article Title: The dipeptidyl peptidase‐4 ( DPP ‐4) inhibitor teneligliptin enhances brown adipose tissue function, thereby preventing obesity in mice

doi: 10.1002/2211-5463.12498

Figure Lengend Snippet: Effects of teneligliptin treatment on whole‐body energy expenditure and BAT function in BAT and iWAT . Teneligliptin was administered in the drinking water (80 mg·kg −1 ·day −1 ), for a total of 10 weeks, to male 6‐week‐old C57 BL /6N mice also fed a HFD . A–C: Ten weeks after initial treatment, oxygen consumption rate (A) and RER (B) were measured by indirect calorimetry, and locomotor activity (C) was measured using an infrared sensor under the fed condition for 20 h (dark phase: 10 h; light phase: 10 h). (D) The mRNA and protein expression levels of UCP 1 in BAT were determined by real‐time RT ‐ PCR and immunoblotting, respectively. (E,F) The mRNA and protein expression levels of UCP 1 (E) and the mRNA expression levels of genes related to BAT function (F) in iWAT were determined by immunoblotting (protein expression levels) and real‐time RT ‐ PCR ( mRNA expression levels). HFD , high‐fat diet; ND normal diet; Tene, teneligliptin plus HFD . All the values are means + SE ( n = 7–10). * P < 0.05, ** P < 0.01.

Article Snippet: Teneligliptin hydrobromide hydrate (>95% purity confirmed by HPLC) was kindly provided by Mitsubishi Tanabe Pharma Corporation (Osaka, Japan).

Techniques: Activity Assay, Expressing, Quantitative RT-PCR, Western Blot

Journal: FEBS Open Bio

Article Title: The dipeptidyl peptidase‐4 ( DPP ‐4) inhibitor teneligliptin enhances brown adipose tissue function, thereby preventing obesity in mice

doi: 10.1002/2211-5463.12498

Figure Lengend Snippet: Effects of the soluble form of DPP ‐4 on Ucp1 expression in cultured white adipocytes. A and B: Expression of Dpp4 mRNA in eWAT . The mRNA expression levels of DPP 4 in eWAT from lean control and obese diabetic db/db mice (A), and in the adipocyte fraction (Adipo) and SVF fraction from eWAT (B), were determined by real‐time RT ‐ PCR . C: 10T1/2 cells were induced to differentiate into adipocytes. Six days after the induction of differentiation, cells were treated with or without 1 μ m isoproterenol (Iso), 1 μg· mL −1 sDPP ‐4 and 100 μ m teneligliptin (Tene) for 8 h. After cDNA preparation, Ucp1 mRNA expression levels were determined by real‐time RT ‐ PCR . D: Effects of sDPP ‐4 on 1 μ m forskolin‐induced activation of the Ucp1 promoter. 10T1/2 cells were transfected with pUCP 1‐pro‐Luc and incubated in medium, with or without sDPP ‐4, followed by treatment with 0.5 or 1 μ m forskolin, with or without sDPP ‐4, for an additional 8 h. All the data are shown as mean + SE ( n = 5–6). * P < 0.05, ** P < 0.01.

Article Snippet: Teneligliptin hydrobromide hydrate (>95% purity confirmed by HPLC) was kindly provided by Mitsubishi Tanabe Pharma Corporation (Osaka, Japan).

Techniques: Expressing, Cell Culture, Control, Quantitative RT-PCR, Activation Assay, Transfection, Incubation

Journal: FEBS Open Bio

Article Title: The dipeptidyl peptidase‐4 ( DPP ‐4) inhibitor teneligliptin enhances brown adipose tissue function, thereby preventing obesity in mice

doi: 10.1002/2211-5463.12498

Figure Lengend Snippet: Dipeptidyl peptidase‐4 inhibits β‐adrenoreceptor agonist‐induced Ucp1 expression through activation of ERK signalling. Mouse primary pre‐adipocytes, isolated from iWAT , were induced to differentiate into adipocytes for 6–8 days. (A) ERK protein levels (phosphorylated ERK , P‐ ERK and total ERK , T‐ ERK ) were analysed in adipocytes treated with or without 1 μg· mL −1 sDPP ‐4, 100 μ m teneligliptin (Tene) and 20 μ m PD 98509 ( PD ). (B) Adipocytes were incubated in the presence or absence of sDPP ‐4 and PD 98509 ( PD ) for 12 h. The cells were then treated with or without sDPP ‐4, PD 98509 and/or isoproterenol (Iso) for 8 h, after which the Ucp1 mRNA levels were determined. All the values represent the mean + SE ( n = 4–6). ** P < 0.01. (C) ERK protein levels were analysed in adipocytes treated with or without sDPP ‐4 and 10 μ m GB 83 (a PAR2 inhibitor).

Article Snippet: Teneligliptin hydrobromide hydrate (>95% purity confirmed by HPLC) was kindly provided by Mitsubishi Tanabe Pharma Corporation (Osaka, Japan).

Techniques: Expressing, Activation Assay, Isolation, Incubation

Journal: FEBS Open Bio

Article Title: The dipeptidyl peptidase‐4 ( DPP ‐4) inhibitor teneligliptin enhances brown adipose tissue function, thereby preventing obesity in mice

doi: 10.1002/2211-5463.12498

Figure Lengend Snippet: Metabolic characteristics of mice treated with or without teneligliptin or CL316243 for 7 days

Article Snippet: Teneligliptin hydrobromide hydrate (>95% purity confirmed by HPLC) was kindly provided by Mitsubishi Tanabe Pharma Corporation (Osaka, Japan).

Techniques: Control, Clinical Proteomics

Journal: FEBS Open Bio

Article Title: The dipeptidyl peptidase‐4 ( DPP ‐4) inhibitor teneligliptin enhances brown adipose tissue function, thereby preventing obesity in mice

doi: 10.1002/2211-5463.12498

Figure Lengend Snippet: Effects of teneligliptin or CL 316243 treatment on BAT function in BAT and iWAT . For 7 days, teneligliptin and CL 316243 were administered in the drinking water (80 mg·kg −1 ·day −1 ) and intraperitoneal injection (0.5 mg·kg −1 ·day −1 ) to male 6‐week‐old C57 BL /6N mice fed an HFD , respectively. (A) Liver samples embedded in the paraffin were cut into 5‐μm sections, and each section was stained with haematoxylin and eosin. Representative images of liver sections are shown (the scale bars in the panels represent 100 μm). (B) The mRNA expression levels of Ucp1 and Pgc1a in BAT and iWAT were determined by real‐time RT ‐ PCR . (C) The protein levels of UCP 1 in BAT and iWAT were determined by immunoblotting. All the values are means + SE ( n = 6–9). * P < 0.05, ** P < 0.01 compared with control.

Article Snippet: Teneligliptin hydrobromide hydrate (>95% purity confirmed by HPLC) was kindly provided by Mitsubishi Tanabe Pharma Corporation (Osaka, Japan).

Techniques: Injection, Staining, Expressing, Quantitative RT-PCR, Western Blot, Control

Journal: FEBS Open Bio

Article Title: The dipeptidyl peptidase‐4 ( DPP ‐4) inhibitor teneligliptin enhances brown adipose tissue function, thereby preventing obesity in mice

doi: 10.1002/2211-5463.12498

Figure Lengend Snippet: Proposed schema of preventive effect of teneligliptin on obesity in adipocytes. sDPP ‐4‐mediated ERK activation, acting through PAR 2, suppresses β‐adrenoreceptor‐stimulated UCP 1 upregulation in adipocytes, and teneligliptin treatment could prevent this suppression, suggesting that this mechanism might be related to the teneligliptin‐induced activation of BAT function in vivo . Teneligliptin‐activated BAT function enhances energy expenditure, leading to the prevention of obesity.

Article Snippet: Teneligliptin hydrobromide hydrate (>95% purity confirmed by HPLC) was kindly provided by Mitsubishi Tanabe Pharma Corporation (Osaka, Japan).

Techniques: Activation Assay, In Vivo