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Identification of Novel PPARγ Partial Agonists Based on Virtual Screening Strategy: In Silico and In Vitro Experimental Validation.
Molecules
October 2024
School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou 511436, China.
Thiazolidinediones (TZDs) including rosiglitazone and pioglitazone function as peroxisome proliferator-activated receptor gamma (PPARγ) full agonists, which have been known as a class to be among the most effective drugs for the treatment of type 2 diabetes mellitus (T2DM). However, side effects of TZDs such as fluid retention and weight gain are associated with their full agonistic activities toward PPARγ induced by the AF-2 helix-involved "locked" mechanism. Thereby, this study aimed to obtain novel PPARγ partial agonists without direct interaction with the AF-2 helix.
View Article and Find Full Text PDFIs fluid retention a cardiovascular risk factor?
Clin Hemorheol Microcirc
October 2024
Department of Family Medicine, Case Western Reserve University School of Medicine, Cleveland, OH, USA.
Endothelial dysfunction, the earliest manifestation of atherosclerosis, can be initiated by both biochemicals and biomechanical forces. Atherosclerosis occurs predominantly at arterial branch points, arterial bifurcations and the curved segments of great arteries. These are the regions that blood flows turbulently.
View Article and Find Full Text PDFThe preventive effectiveness of Crocus sativus extract in treating lung injuries caused by inhaled paraquat in rats.
J Ethnopharmacol
January 2025
Applied Biomedical Research Center, Mashhad University of Medical Sciences, Mashhad, Iran; Department of Physiology, Faculty of Medicine, Mashhad University of Medical Sciences, Mashhad, Iran. Electronic address:
Article Synopsis
- - Paraquat (PQ) is a toxic herbicide that can cause serious lung issues, but Crocus sativus (Cs) has shown promise for treating related respiratory problems due to its anti-inflammatory and antioxidant properties.
- - This study aimed to assess how Cs extract and pioglitazone (Pio) can prevent lung damage and inflammation caused by PQ exposure in rats, comparing their effects to dexamethasone (Dexa).
- - Results indicated that treatments with both Cs and Pio improved lung health and function, with the combination showing the most significant benefits, suggesting Cs could be a viable alternative to traditional treatments like Dexa.
Evaluation of the protective effect of Curcuma longa and PPARγ agonist, pioglitazone on paraquat-induced lung injury in rats.
Immun Inflamm Dis
August 2024
Applied Biomedical Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.
Background: The inhalation of paraquat (PQ), one of the most widely used herbicides in the world, can result in lung injury. Curcuma longa (Cl) has long history in traditional and folk medicine for the treatment of a wide range of disorders including respiratory diseases.
Aim: The aim of the present work was to evaluate the preventive effect of Cl on inhaled PQ-induced lung injury in rats.
Unveiling Pharmacokinetics and Drug Interaction of Linagliptin and Pioglitazone HCl in Rat Plasma Using LC-MS/MS.
Chem Res Toxicol
May 2024
Medicinal Chemistry Department, Faculty of Pharmacy, Suez Canal University, Ismailia 41522, Egypt.
The linagliptin (LIN) and pioglitazone HCl (PIO) combination, currently undergoing phase III clinical trials for diabetes mellitus treatment, demonstrated significant improvements in glycemic control. However, the absence of an analytical method for simultaneous determination in biological fluids highlights a crucial gap. This underscores the pressing need for sensitive bioanalytical methods, emphasizing the paramount importance of developing such tools to advance diabetes management strategies and enhance patient care.
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