A Randomized, Open-label, Single Dose, Two-way Crossover Clinical Trial to Investigate the Pharmacokinetics, Safety, and Tolerability of the Combination of Gemigliptin/Rosuvastatin 50/20 mg in Comparison to Each Component Gemigliptin 50 mg and Rosuvastatin 20 mg Administered in Healthy Male Volunteers

This study is to evaluate the safety/tolerability and pharmacokinetics of the combinations of gemigliptin 50mg and rosuvastatin 20mg in comparison to each component administered alone in healthy male volunteers.

Start Date01 Mar 2016

Sponsor / Collaborator

LG Life Sciences Ltd.

NCT02126358 / CompletedPhase 3

A Multicenter, Randomized, Placebo-controlled, Double-blind, Phase III Trial to Evaluate the Efficacy and Safety of the Fix-dose Combination Therapy With Gemigliptin 50mg and Rosuvastatin 20mg With Type 2 Diabetes and Dyslipidemia

To evaluate the efficacy and safety of the fix-dose combination therapy with Gemigliptin 50mg and Rosuvastatin 20mg with type 2 diabetes and dyslipidemia

Start Date01 May 2014

Sponsor / Collaborator

LG Life Sciences Ltd.

NCT01702298 / CompletedPhase 3

An Open-label Study to Assess the Safety and Tolerability of MK-0431D for the Treatment of Patients With Type 2 Diabetes Mellitus (T2DM) With Inadequate Glycemic Control on Metformin Monotherapy

The purpose of this study is to examine the safety and tolerability of sitagliptin 100 mg/simvastatin 40 mg FDC (MK-0431D) in Vietnamese participants with type 2 diabetes mellitus with inadequate glycemic control on metformin.

Start Date07 Dec 2012

Sponsor / Collaborator

Merck Sharp & Dohme Corp.

100 Clinical Results associated with HMG-CoA reductase x DPP-4

100 Translational Medicine associated with HMG-CoA reductase x DPP-4

0 Patents (Medical) associated with HMG-CoA reductase x DPP-4

Literatures (Medical) associated with HMG-CoA reductase x DPP-4

03 Aug 2023·Molecules (Basel, Switzerland)

Resveratrol Mitigates Bisphenol A-Induced Metabolic Disruptions: Insights from Experimental Studies.

Article

Author: Rehman, Kanwal ; Rehman, Qudsia ; Chauhdary, Zunera ; Akash, Muhammad Sajid Hamid ; Fatima, Mutayyba ; Nadeem, Ahmed ; Mir, Tahir Maqbool

The aim of this study was to investigate the disruptions of metabolic pathways induced by bisphenol A (BPA) and explore the potential therapeutic intervention provided by resveratrol (RSV) in mitigating these disruptions through the modulation of biochemical pathways. Wistar albino rats were divided into three groups: group 1 served as the control, group 2 received 70 mg/Kg of BPA, and group 3 received 70 mg/kg of BPA along with 100 mg/Kg of RSV. After the treatment period, various biomarkers and gene expressions were measured to assess the effects of BPA and the potential protective effects of RSV. The results revealed that BPA exposure significantly increased the serum levels of α-amylase, α-glucosidase, G6PC, insulin, HbA1c, HMG-CoA reductase, FFAs, TGs, DPP-4, MDA, and proinflammatory cytokines such as TNF-α and IL-6. Concurrently, BPA exposure led to a reduction in the levels of antioxidant enzymes such as catalase (CAT), glutathione peroxidase (GPx), and superoxide dismutase (SOD), as well as GLUT4 and HDL cholesterol. However, the administration of RSV along with BPA significantly ameliorated these alterations in the biomarker levels induced through BPA exposure. RSV treatment effectively reduced the elevated levels of α-amylase, α-glucosidase, G6PC, insulin, HbA1c, HMG-CoA reductase, FFAs, TGs, DPP-4, MDA, and proinflammatory cytokines, while increasing the levels of antioxidant enzymes, GLUT4, and HDL cholesterol. Furthermore, BPA exposure suppressed the mRNA expression of glucokinase (GCK), insulin-like growth factor 1 (IGF-1), and glucose transporter 2 (GLUT2) and up-regulated the mRNA expression of uncoupling protein 2 (UCP2), which are all critical biomarkers involved in glucose metabolism and insulin regulation. In contrast, RSV treatment effectively restored the altered mRNA expressions of these biomarkers, indicating its potential to modulate transcriptional pathways and restore normal metabolic function. In conclusion, the findings of this study strongly suggest that RSV holds promise as a therapeutic intervention for BPA-induced metabolic disorders. By mitigating the disruptions in various metabolic pathways and modulating gene expressions related to glucose metabolism and insulin regulation, RSV shows potential in restoring normal metabolic function and counteracting the adverse effects induced by BPA exposure. However, further research is necessary to fully understand the underlying mechanisms and optimize the dosage and duration of RSV treatment for maximum therapeutic benefits.

01 Apr 2023·Pharmacological Research

Therapeutic potential of reserpine in metabolic syndrome: An evidence-based study

Letter

Author: Verma, Kanika ; Paliwal, Sarvesh ; Sharma, Swapnil

A review.Udaya Pratap Singh, and Prashant Gahtori comments pertaining to high fat diet, interventional duration, diseased model used, histopathol. and mol. docking in the article dealing with the therapeutic potential of reserpine in metabolic syndrome: An evidence based study is discussed.Diet-Induced Obesity (DIO) rodent models are frequently used in studies on the pathways implied in the development of metabolic syndrome (MS).Indeed, docking study of Reserpine with various receptors e.g., soluble epoxide hydrolase (sEH), PPARg , PI3K/Akt, DPP4, GRP, HMG-CoA reductase, Glucokinase, and SREBP, was performed to evaluate the binding potential of the Reserpine with various target involved in the pathophysiol. of MS.Since manuscript explicitly deals with the ability of Reserpine to bind to the sEH enzyme and produce pharmacol. activity pertaining to amelioration of MS, it would be redundant to include preliminary in-silico screening per - formed on various targets.

01 Dec 2022·Journal of Food Biochemistry

Antioxidant and enzyme inhibitory properties of sacha inchi ( Plukenetia volubilis ) protein hydrolysate and its peptide fractions

Article

Author: Kreungngernd, Danchai ; Aluko, Rotimi E. ; Suwanangul, Saranya ; Sangsawad, Papungkorn ; Ruttarattanamongkol, Khanitta

The objective of this study was to determine the in vitro activities such as antioxidant and inhibitions of angiotensin converting enzyme, dipeptidyl peptidase-IV, prolyl oligopeptidase, and 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase of sacha inchi protein hydrolysate (SPH) and its membrane ultrafiltration peptide fractions. SPH was prepared after hydrolysis of sacha inchi protein using papain followed by separation into peptide fractions (F1: <1 kDa, F2: 1-3 kDa, F3: 3-5 kDa, and F4: 5-10 kDa) via ultrafiltration membranes. SPH and the peptide fractions were tested for multifunctional properties, specifically functional ability as antioxidants and enzyme inhibitors. Surface hydrophobicity was an important contributing factor to the activity of antioxidative peptides. The DPPH inhibitory activity of F4 was significantly higher (p < .05) than activities of the SPH and other fractions. The smaller peptides with <1 kDa size (F1) showed the most potent (p < .05) antioxidant properties based on the stronger scavenging of ABTS, DPPH, and superoxide radicals in addition to better attenuation of linoleic acid peroxidation. Moreover, the F1 was also the strongest inhibitor of angiotensin converting enzyme, dipeptidyl peptidase-IV, prolyl oligopeptidase inhibition, and 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase based on the lower IC₅₀ values. It was concluded that the smaller size of the F1 peptides was the main determinant of its strong antioxidant and enzyme inhibition potency, which could be taken as an advantage to formulate functional foods and nutraceuticals with potential activities in ameliorating some of the chronic human diseases. PRACTICAL APPLICATIONS: The results of present study indicate that SPH and its ultrafiltration fractions are potential sources of antihypertensive, antidiabetic, inhibition of POP, reduced cholesterol, and strong antioxidant peptides. The strong angiotensin converting enzyme, dipeptidyl peptidase-IV, prolyl oligopeptidase inhibition, and 3-hydroxy-3-methyl-glutaryl-coenzyme inhibitory efficiency of the F1 peptides (MW < 1 kDa) suggest potential utility as an antihypertensive, antidiabetic agent, reduce cholesterol and brain plasticity and memory formation because the small peptide size could enhance absorption from the gastrointestinal tract. Overall, results from this study indicate that SPH, especially the F1 peptides may have applications as ingredients for the formulation of functional foods and nutraceuticals.

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