Galangin 3-benzyl-5-methylether derivatives function as an adiponectin synthesis-promoting peroxisome proliferator-activated receptor γ partial agonist

Prenylated Chrysin Derivatives as Partial PPARγ Agonists with Adiponectin Secretion-Inducing Activity

“…13,14 Three PPAR subtypes, PPARα, PPARγ, and PPARδ, have been extensively studied as drug targets in treating human metabolic diseases. 11,12,15,16 Among the three PPAR subtypes, PPARγ plays a pivotal role in regulating adipocyte function. 13,17 The transcriptional activation of PPARγ improves insulin sensitivity and modulates inflammatory processes.…”

“…Adiponectin is an adipocyte-derived cytokine with diverse biological activities, including the improvement of insulin sensitivity, the inhibition of inflammation, and the regulation of metabolic processes . Regarding the increase in ectopic fats in the liver and vascular tissues, many studies have shown that hypoadiponectinemia is associated with human metabolic diseases, such as type II diabetes, fatty liver disease, and atherosclerosis. − Moreover, the relative decrease in circulating adiponectin is linked to an increased risk of obesity-related malignancies, such as hematologic, endometrial, colon, renal, and liver cancers. , Thus, the administration of recombinant adiponectin has been suggested as a possible strategy for treating conditions associated with hypoadiponectinemia. , However, recombinant adiponectin requires extensive post-translational modification and oligomerization, which limits its therapeutic applications. , Therefore, compounds that can promote adiponectin secretion from adipocytes have been proposed as novel therapeutic agents for treating various metabolic diseases and cancers. − …”

“…Cellular adiponectin biosynthesis in adipocytes is mainly regulated by the peroxisome proliferator-activated receptor (PPAR). , Three PPAR subtypes, PPARα, PPARγ, and PPARδ, have been extensively studied as drug targets in treating human metabolic diseases. ,,, Among the three PPAR subtypes, PPARγ plays a pivotal role in regulating adipocyte function. , The transcriptional activation of PPARγ improves insulin sensitivity and modulates inflammatory processes . Recent evidence has shown that PPAR-induced adiponectin secretion alleviates obesity-associated nonalcoholic fatty liver disease (NAFLD). , Many thiazolidinedione (TZD) class PPARγ agonists, highly potent adiponectin secretion-inducing compounds, have been approved as antidiabetic drugs.…”

Discovery of Pan-peroxisome Proliferator-Activated Receptor Modulators from an Endolichenic Fungus, Daldinia childiae

“…The phenotype-based approach is an alternative to target-based methods in discovering novel treatments for metabolic diseases. − The relative serum adiponectin concentration is low in human metabolic diseases and its upregulation has been suggested as a novel therapeutic strategy in human diseases associated with hypoadiponectinemia. , The phenotype-based screening of adiponectin-synthesis-promoting compounds using an adipogenesis model of human bone marrow mesenchymal stem cells (hBM-MSCs) has been used to discover novel dual- or pan-PPAR modulators. ,− …”