AKR7A3

Last update 23 Jan 2025

Basic Info

Synonyms

AFAR2, AFB1 aldehyde reductase 2, AFB1-AR 2

+ [3]

Introduction

Can reduce the dialdehyde protein-binding form of aflatoxin B1 (AFB1) to the non-binding AFB1 dialcohol. May be involved in protection of liver against the toxic and carcinogenic effects of AFB1, a potent hepatocarcinogen.

100 Clinical Results associated with AKR7A3

100 Translational Medicine associated with AKR7A3

0 Patents (Medical) associated with AKR7A3

335

Literatures (Medical) associated with AKR7A3

01 Dec 2024·Fundamental & Clinical Pharmacology

The β₂‐adrenergic receptor agonist formoterol attenuates necrosis and apoptosis in the rat myocardium under experimental stress‐induced cardiac injury

Article

Author: Gusakova, Svetlana V. ; Naryzhnaya, Natalia V. ; Maslov, Leonid N. ; Gorbunov, Aleksandr S. ; Derkachev, Ivan A. ; Logvinov, Sergey V. ; Sirotina, Maria A. ; Kurbatov, Boris K. ; Kilin, Mikhail ; Mustafina, Liliia R.

AbstractBackgroundCurrently, there is no effective therapy for takotsubo syndrome (stress‐induced cardiac injury in humans) in the clinics. It has previously been shown that β2‐adrenergic receptor (β2‐AR) agonist formoterol reduces cardiomyocyte injury in experimental takotsubo syndrome.ObjectivesThe aim of this study was to investigate whether formoterol prevents apoptosis and necrosis of cardiomyocytes and endothelial cells in stress‐induced cardiomyopathy.MethodsStress‐induced cardiac injury was induced by immobilization of rats for 2, 6, and 24 hours.ResultsThe myocardium of stressed rats showed a reduction in contractility and histological manifestations of cardiomyocyte damage: karyopyknosis, perinuclear edema of cardiomyocytes and endothelial cells, and microcirculation disturbances augmented with extended exposure to stress. In addition, apoptosis of endothelial cells was detected 6 hours after the onset of stress and peaked at 24 hours. Apoptosis of cardiomyocytes significantly gained only after 24 hours of stress exposure. These morphological alterations were associated with increased levels of serum creatine kinase‐MB, syndecan‐1, and thrombomodulin after 24 hours of stress. Administration of β2‐AR agonist formoterol (50 μg/kg) four times during 24‐hour stress exposure led to the improvement in myocardial inotropy, decrease in the severity of histological signatures, reduction in the number of TUNEL‐positive cardiomyocytes, serum creatine kinase‐MB, syndecan‐1, and thrombomodulin levels.ConclusionPresent data suggest that apoptosis and necrosis of cardiomyocytes and necrosis of endothelial cells in stress‐induced cardiac injury can be mitigated by activation of the β2‐AR. However, formoterol did not eliminate completely cardiomyocyte apoptosis, histological alterations, or endothelium injury markers under stress.

01 Oct 2024·Journal of Chromatography A

Target-specific affinity separation of the bioactive compounds from herbal extract using the spin column packed with the immobilized protein microspheres prior to LC-MS analysis

Article

Author: Han, Yaokun ; Wang, Yunshan ; Zhao, Shoucheng ; Wang, Taotao ; Li, Xia ; Xiao, Chaoni ; Liu, Pei ; Li, Qian

Excellent pretreatments before instrumental analysis are critical for separation and determination of target compounds for discovery of new drugs from herb medicines. We developed a rapid and highly-selective method to separate the bioactive compounds from herbal extract using protein affinity-selection spin column, which was packed with the new sorbent materials from integrating the recombinant β₂-adrenoceptor (β₂-AR) directly out of cell lysates onto the surface of microspheres. Protein affinity-selection spin column was placed in a centrifugal tube, where after the non-specific binders were released to the filtrate under the operational centrifugation, the specific binders on the spin column were cleaned with a washing solvent for LC-MS analysis. The known agonists of β₂-AR were retained/released on protein affinity-selection spin column but not on control column, demonstrating the method with good recovery (79.4∼95.7 %) and high repeatability (RSD < 3.5 %). The adsorption features of three ligands on the spin column were described best by Prism saturation binding model, and the high-affinity binding and the large binding capacity of the spin column make it feasible to trap the trace analytes effectively. It was applied in separating bioactive compounds from Alstoniae Scholaris extract, two of which were identified as picrinine and oleanolic acid in combination with LC-MS and verified as the potential agonists towards β₂-AR though molecular docking and cell experiments. Our study demonstrated that, the spin column with the immobilized protein sorbents in the centrifugal filter device represents a promising tool, enabling rapid and target-specific affinity separation of the bioactive compounds from herbal extract.

01 Oct 2024·Biochemical Pharmacology

Molecular targets of PXR-dependent ethanol-induced hepatotoxicity in female mice

Article

Author: Nnamani, Daniel O ; Twum, Elizabeth ; Mah'moud, Mia ; Gebreyesus, Lidya H ; Yue Cui, Julia ; Ofosu-Boateng, Malvin ; Gonzalez, Frank J ; Gyamfi, Maxwell A ; Kim, Sarah ; Neequaye, Prince ; Choi, Sora

The pregnane X receptor (PXR, NR1I2), a xenobiotic-sensing nuclear receptor signaling potentiates ethanol (EtOH)-induced hepatotoxicity in male mice, however, how PXR signaling modulates EtOH-induced hepatotoxicity in female mice is unknown. Wild type (WT) and Pxr-null mice received 5 % EtOH-containing diets or paired-fed control diets for 8 weeks followed by assessment of liver injury, EtOH elimination rates, histology, and changes in gene and protein expression; microarray and bioinformatic analyses were also employed to identify PXR targets in chronic EtOH-induced hepatotoxicity. In WT females, EtOH ingestion significantly increased serum ethanol and alanine aminotransferase (ALT) levels, hepatic Pxr mRNA, constitutive androstane receptor activation, Cyp2b10 mRNA and protein, oxidative stress, endoplasmic stress (phospho-elF2α) and pro-apoptotic (Bax) protein expression. Unexpectedly, EtOH-fed female Pxr-null mice displayed increased EtOH elimination and elevated levels of hepatic acetaldehyde detoxifying aldehyde dehydrogenase 1a1 (Aldh1a1) mRNA and protein, EtOH-metabolizing alcohol dehydrogenase 1 (ADH1), and lipid suppressing microsomal triglyceride transport protein (MTP) protein, aldo-keto reductase 1b7 (Akr1b7) and Cyp2a5 mRNA, but suppressed CYP2B10 protein levels, with evidence of protection against chronic EtOH-induced oxidative stress and hepatotoxicity. While liver injury was not different between the two WT sexes, female sex may suppress EtOH-induced macrovesicular steatosis in the liver. Several genes and pathways important in retinol and steroid hormone biosynthesis, chemical carcinogenesis, and arachidonic acid metabolism were upregulated by EtOH in a PXR-dependent manner in both sexes. Together, these data establish that female Pxr-null mice are resistant to chronic EtOH-induced hepatotoxicity and unravel the PXR-dependent and -independent mechanisms that contribute to EtOH-induced hepatotoxicity.

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AKR7A3

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