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AdipoRon

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https://www.readbyqxmd.com/read/27627895/promigratory-and-proangiogenic-effects-of-adiporon-on-bone-marrow-derived-mesenchymal-stem-cells-an-in-vitro-study
#1
Sara Malih, Massoud Saidijam, Kamran Mansouri, Mona Pourjafar, Maryam Sadat Tafakh, Fahimeh Talebzadeh, Rezvan Najafi
OBJECTIVES: To investigate the effect of AdipoRon on major factors involved in survival, migration and neovascularization of rat bone marrow-derived mesenchymal stem cells. RESULTS: AdipoRon promoted the MSCs viability. Real-time PCR indicated that the expression of cyclooxygenase-2 (COX-2), hypoxia-inducible factor-1 (HIF-1) C-X-C chemokine receptor type 4 (CXCR4), C-C chemokine receptor type 2 (CCR2), vascular endothelial growth factor matrix metalloproteinase-2 (MMP-2) and MMP-9 were upregulated in AdipoRon-treated MSCs compared to control groups...
September 15, 2016: Biotechnology Letters
https://www.readbyqxmd.com/read/27516150/hepatoprotective-effects-of-adiporon-against-d-galactosamine-induced-liver-injury-in-mice
#2
Ying Wang, Yumeng Wan, Guihong Ye, Pu Wang, Xiaowen Xue, Guanzhong Wu, Boping Ye
Adiponectin is an antidiabetic and antiatherogenic adipokine, which plays distinct roles in the balance of energy homoeostasis. As an insulin sensitizing hormone, adiponectin exerts multiple biological effects by the specific receptors (AdipoR1 and AdipoR2), through activation of AMP-activated protein kinase (AMPK) and peroxisome proliferator-activated receptor (PPAR)α pathways. AdipoRon, an orally active synthetic small-molecule AdipoR agonist, shows very similar effects to adiponectin in vitro and in vivo, which could be a promising therapeutic approach for obesity-related disorders...
October 10, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27137743/adiponectin-regulates-contextual-fear-extinction-and-intrinsic-excitability-of-dentate-gyrus-granule-neurons-through-adipor2-receptors
#3
D Zhang, X Wang, B Wang, J C Garza, X Fang, J Wang, P E Scherer, R Brenner, W Zhang, X-Y Lu
Post-traumatic stress disorder (PTSD) is characterized by exaggerated fear expression and impaired fear extinction. The underlying molecular and cellular mechanisms of PTSD are largely unknown. The current pharmacological and non-pharmacological treatments for PTSD are either ineffective or temporary with high relapse rates. Here we report that adiponectin-deficient mice exhibited normal contextual fear conditioning but displayed slower extinction learning. Infusions of adiponectin into the dentate gyrus (DG) of the hippocampus in fear-conditioned mice facilitated extinction of contextual fear...
May 3, 2016: Molecular Psychiatry
https://www.readbyqxmd.com/read/27003122/identification-and-characterization-of-in-vitro-and-in-vivo-generated-metabolites-of-the-adiponectin-receptor-agonists-adiporon-and-112254
#4
Josef Dib, Andreas Thomas, Philippe Delahaut, Eric Fichant, Wilhelm Schänzer, Mario Thevis
Peroxisome proliferator-activated receptors (PPARs), peroxisome proliferator-activated receptor γ coactivator 1α (PGC-1α), sirtuin 1 (SIRT1) and adenosine monophosphate-activated protein kinase (AMPK) are regulators of transcriptional processes and effects of exercise and pseudo-exercise situations. Compounds occasionally referred to as endurance exercise mimetics such as AdipoRon and 112254, both adiponectin receptor agonists, can be used to simulate the physiology of endurance exercise via pathways including these transcriptional regulators...
June 5, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/26282004/adiporon-a-possible-drug-for-colorectal-cancer-prevention
#5
EDITORIAL
Sara Malih, Rezvan Najafi
Colorectal cancer (CRC) is in the third place of the most common cancers. Certain risk factors can increase the development of CRC, including diet and inheritance. Several studies have shown that there is a potential link between obesity and CRC. Adipose tissue is known to be a largest endocrine organ in the body, with the ability to produce various cytokines including adiponectin. Two types of adiponectin receptor, AdipoR1 and AdipoR2, have been detected in various cancer tissues such as CRC. There is mounting evidence that AdipoR1 signaling occurs mainly through 5' AMP-activated protein kinase (AMPK) and adiponectin inhibits colorectal cancer cell growth via activation of AMPK, thereby suppression of the mammalian target of rapamycin (mTOR) pathway...
September 2015: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
https://www.readbyqxmd.com/read/26037251/adiporon-the-first-orally-active-adiponectin-receptor-activator-attenuates-postischemic-myocardial-apoptosis-through-both-ampk-mediated-and-ampk-independent-signalings
#6
Yanqing Zhang, Jianli Zhao, Rui Li, Wayne Bond Lau, Yue-Xing Yuan, Bin Liang, Rong Li, Er-He Gao, Walter J Koch, Xin-Liang Ma, Ya-Jing Wang
Adiponectin (APN) is a cardioprotective molecule. Its reduction in diabetes exacerbates myocardial ischemia/reperfusion (MI/R) injury. Although APN administration in animals attenuates MI/R injury, multiple factors limit its clinical application. The current study investigated whether AdipoRon, the first orally active molecule that binds APN receptors, may protect the heart against MI/R injury, and if so, to delineate the involved mechanisms. Wild-type (WT), APN knockout (APN-KO), and cardiomyocyte specific-AMPK dominant negative (AMPK-DN) mice were treated with vehicle or AdipoRon (50 mg/kg, 10 min prior to MI) and subjected to MI/R (30 min/3-24 h)...
August 1, 2015: American Journal of Physiology. Endocrinology and Metabolism
https://www.readbyqxmd.com/read/25800023/studies-on-the-collision-induced-dissociation-of-adipor-agonists-after-electrospray-ionization-and-their-implementation-in-sports-drug-testing
#7
Josef Dib, Nils Schlörer, Wilhelm Schänzer, Mario Thevis
AdipoR agonists are small, orally active molecules capable of mimicking the protein adiponectin, which represents an adipokine with antidiabetic and antiatherogenic effects. Two adiponectin receptors were reported in the literature referred to as adipoR1 and adipoR2. Activation of these receptors stimulates mitochondrial biogenesis and results in an improved oxidative metabolism (via adipoR1) and increased insulin sensitivity (via adipoR2). Hence, adipoR agonists are potentially performance enhancing substances and targets of proactive and preventive anti-doping measures...
February 2015: Journal of Mass Spectrometry: JMS
https://www.readbyqxmd.com/read/24172895/a-small-molecule-adipor-agonist-for-type-2-diabetes-and-short-life-in-obesity
#8
Miki Okada-Iwabu, Toshimasa Yamauchi, Masato Iwabu, Teruki Honma, Ken-ichi Hamagami, Koichi Matsuda, Mamiko Yamaguchi, Hiroaki Tanabe, Tomomi Kimura-Someya, Mikako Shirouzu, Hitomi Ogata, Kumpei Tokuyama, Kohjiro Ueki, Tetsuo Nagano, Akiko Tanaka, Shigeyuki Yokoyama, Takashi Kadowaki
Adiponectin secreted from adipocytes binds to adiponectin receptors AdipoR1 and AdipoR2, and exerts antidiabetic effects via activation of AMPK and PPAR-α pathways, respectively. Levels of adiponectin in plasma are reduced in obesity, which causes insulin resistance and type 2 diabetes. Thus, orally active small molecules that bind to and activate AdipoR1 and AdipoR2 could ameliorate obesity-related diseases such as type 2 diabetes. Here we report the identification of orally active synthetic small-molecule AdipoR agonists...
November 28, 2013: Nature
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