The direct effect of lobeglitazone, a new thiazolidinedione, on pancreatic beta cells: A comparison with other thiazolidinediones

Kwon, Min Jeong; Lee, Yong Jae; Jung, Hwa Jin; Shin, Huiyoung; Kim, Tae Nyun; Lee, Soon Hee; Rhee, Byoung Doo; Kim, Mi-Kyung; Park, Jeong Hyun

doi:10.1016/j.diabres.2019.04.006

Cited by 28 publications

(20 citation statements)

References 51 publications

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“…6,7,10,11 Lobeglitazone also showed beneficial effects on β-cell survival and function against hyperglycaemia that were comparable with those of other TZDs. 12,13 In line with those studies, our study added evidence that lobeglitazone was comparable with sitagliptin, in terms of improving glycaemic control with better tolerance. In addition, favourable changes were observed in HDL-C, TG, FFA and adiponectin levels with lobeglitazone compared with sitagliptin in this study.…”

Section: Discussionsupporting

confidence: 84%

“…There has been accumulating evidence from randomized controlled trials regarding the efficacy and safety of lobeglitazone 6,7,10,11 . Lobeglitazone also showed beneficial effects on β‐cell survival and function against hyperglycaemia that were comparable with those of other TZDs 12,13 . In line with those studies, our study added evidence that lobeglitazone was comparable with sitagliptin, in terms of improving glycaemic control with better tolerance.…”

Section: Discussionsupporting

confidence: 83%

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Efficacy and safety of lobeglitazone versus sitagliptin as an add‐on to metformin in patients with type 2 diabetes with two or more components of metabolic syndrome over 24 weeks

Kim

Yoon

et al. 2020

Diabetes Obesity Metabolism

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We aimed to evaluate the efficacy and safety profile of lobeglitazone compared with sitagliptin as an add‐on to metformin in patients with type 2 diabetes as well as other components of metabolic syndrome. Patients inadequately controlled by metformin were randomly assigned to lobeglitazone (0.5 mg, n = 121) or sitagliptin (100 mg, n = 126) for 24 weeks. The mean changes in HbA1c of the lobeglitazone and sitagliptin groups were −0.79% and −0.86%, respectively; the between‐group difference was 0.08% (95% confidence interval, −0.14% to 0.30%), showing non‐inferiority. The proportion of patients having two or more factors of other metabolic syndrome components decreased to a greater extent in the lobeglitazone group than in the sitagliptin group (−11.9% vs. −4.8%; P < .0174). Favourable changes in the lipid metabolism were also observed with lobeglitazone, which had a similar safety profile to sitagliptin. Lobeglitazone was comparable with sitagliptin as an add‐on to metformin in terms of efficacy and safety.

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Section: Discussionsupporting

confidence: 84%

Section: Discussionsupporting

confidence: 83%

Efficacy and safety of lobeglitazone versus sitagliptin as an add‐on to metformin in patients with type 2 diabetes with two or more components of metabolic syndrome over 24 weeks

Kim

Yoon

et al. 2020

Diabetes Obesity Metabolism

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“…However, in terms of bone metabolism, lobeglitazone has been reported to have no detrimental effect on bone mineral density while pioglitazone exhibits negative effects [28,29]. In an in vivo study of db/db (diabetic) mice, lobeglitazone showed beneficial effects on beta cell survival and function and was comparable to other TZDs [30]. Several studies have evaluated the efficacy of pioglitazone on the UACR.…”

Section: Discussionmentioning

confidence: 99%

Comparative Efficacy of Lobeglitazone Versus Pioglitazone on Albuminuria in Patients with Type 2 Diabetes Mellitus

et al. 2020

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Introduction: The aim of this analysis was to evaluate the efficacy of lobeglitazone on albuminuria at 24 weeks of follow-up in patients with type 2 diabetes mellitus (T2DM) compared with pioglitazone using data from a randomized, double-blinded phase III trial. Methods: In the phase III trial, patients who were inadequately controlled with metformin Kyung-Soo Kim and Sangmo Hong contributed equally to the work.

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“…So far, several drugs, including DPP-4 inhibitors (14), GLP-1 analogs (15), and thiazolidinediones (16), have shown to be effective in protecting islet β-cells as well as in controlling blood glucose. However，Novel, safe and more efficient drugs aiming to protect and maintain islet β-cells are still in urgent need.…”

Section: Introductionmentioning

confidence: 99%

Tectorigenin enhances PDX1 expression and protects pancreatic β-cells by activating ERK and reducing ER stress

Yao

Chen

et al. 2020

Journal of Biological Chemistry

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Pancreas/duodenum homeobox protein 1 (PDX1) is an important transcription factor that regulates islet β-cell proliferation, differentiation, and function. Reduced expression of PDX1 is thought to contribute to β-cell loss and dysfunction in diabetes. Thus, promoting PDX1 expression can be an effective strategy to preserve β-cell mass and function. Previously, we established a PDX1 promoter-dependent luciferase system to screen agents that can promote PDX1 expression. Natural compound tectorigenin (TG) was identified as a promising candidate that could enhance the activity of the promoter for PDX1 gene. In this study, we first demonstrated that TG could promote the expression of PDX1 in β-cells via activating extracellular signal-related kinase (ERK), as indicated by increased phosphorylation of ERK; this effect was observed under either normal or glucotoxic/lipotoxic conditions. We then found that TG could suppress induced apoptosis and improved the viability of β-cells under glucotoxicity and lipotoxicity by activation of ERK and reduction of reactive oxygen species (ROS) and endoplasmic reticulum (ER) stress. These effects held true in vivo as well: prophylactic or therapeutic use of TG could obviously inhibit ER stress and decrease islet β-cell apoptosis in the pancreas of mice given a high-fat/high-sucrose diet (HFHSD), thus dramatically maintaining or restoring β-cell mass and islet size respectively. Accordingly, both prophylactic and therapeutic use of TG improved HFHSD impaired glucose metabolism in mice, as evidenced by ameliorating hyperglycemia and glucose intolerance. Taken together, TG, as an agent promoting PDX1 expression exhibits strong protective effects on islet β-cells both in vitro and in vivo.

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The direct effect of lobeglitazone, a new thiazolidinedione, on pancreatic beta cells: A comparison with other thiazolidinediones

Cited by 28 publications

References 51 publications

Efficacy and safety of lobeglitazone versus sitagliptin as an add‐on to metformin in patients with type 2 diabetes with two or more components of metabolic syndrome over 24 weeks

Efficacy and safety of lobeglitazone versus sitagliptin as an add‐on to metformin in patients with type 2 diabetes with two or more components of metabolic syndrome over 24 weeks

Comparative Efficacy of Lobeglitazone Versus Pioglitazone on Albuminuria in Patients with Type 2 Diabetes Mellitus

Tectorigenin enhances PDX1 expression and protects pancreatic β-cells by activating ERK and reducing ER stress

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