GQ-11: A new PPAR agonist improves obesity-induced metabolic alterations in LDLr−/− mice

Abstract

GQ-11 is a partial/dual PPARα/γ agonist that demonstrates anti-diabetic effects. Additionally, it improves the lipid profile and ameliorates chronic inflammation associated with obesity in atherosclerosis-prone mice.

Effects of a new thiazolidine compound (GQ-11) on tissue repair process in models of insulin resistance and ischemia-reperfusion

“…Consistently, previous studies also showed anti-inflammatory effects promoted by GQ-11, through TNF-α, CCL-2 and IL-1β modulation in obese mice (SILVA et al, 2018). Evidences suggest that IL-1β plays a key role in pathophysiology of hepatic I/R injury, some of them attesting that neutrophils and macrophages can contribute to the cytokine maturation, independently of inflammasome (SADATOMO et al, 2017).…”

New Peroxisome Proliferator-Activated Receptor Agonist (GQ-11) Improves Wound Healing in Diabetic Mice

“…Our previous studies indicated beneficial properties of a novel PPAR agonist (GQ-11) that may represent a promising candidate for the therapy of diabetes complications. 15 In this study, our major findings are that GQ-11 induces a pro-healing phenotype both in cultured macrophages and when applied topically to wounds of diabetic mice, which resulted in accelerated re-epithelization and collagen deposition.…”

“…GQ-11 is a new thiazolidine compound, exhibiting partial/dual PPARa/c agonism with classical antidiabetic effects of TZDs, improves lipid profile and reduces chronic inflammation associated with obesity in mice with reduced side effects. 15 Therefore, the aim of this study was to determine whether GQ-11 reduces inflammation and improves wound healing in diabetic mice in basic research, providing better understanding of underlying mechanisms, improving diabetic wound healing clinical trials and purposing a new approach to diabetic wound healing treatment to prevent its complications such as amputations.…”

“…GQ-11 [(Z)-5-((1H-indol-3-yl)methylene)-3-(4methylbenzyl)thiazolidine-2,4-dione] was synthesized as previously described, 15 in the Laboratory of Drug Design and Synthesis of the Federal University of Pernambuco (Recife, Pernambuco, Brazil).…”

“…Sample size calculation was based on evidence from previous preclinical studies for testing TZDs antidiabetic effects. 15,17,18 At 10 weeks of age, animals were anesthetized with isoflurane (3%), the skin shaved and cleaned with 70% alcohol, and four full thickness wounds were created on the dorsum using 8 mm biopsy punch. On day 3 postinjury, after initial inflammatory response was allowed to proceed normally, animals were randomly allocated into three treatment groups (n = 6/group): vehicle (F-127 Ò Pluronic Gel, Sigma-Aldrich, Cat No.…”