Allopurinol sodium is a highly effective and orally active inhibitor of xanthine oxidase, with an IC50 ranging from 0.2 to 50 μM. It is commonly utilized in the study of hyperuricemia and gout. Beyond its primary application, Allopurinol sodium is known to decrease the expression of HIF-1α and HIF-2α proteins, exhibiting potential in reducing hypoxia-induced factors. Additionally, it has demonstrated antidepressant, anti-nociceptive, and anti-leishmanial activities[1].[2].[3].[4].[5].
体内研究
In vivo, when administered orally at a dose of 39 mg/kg daily for 21 consecutive days, Allopurinol sodium shows antidepressant activity in mice[3].
Furthermore, administered intraperitoneally at doses ranging from 10 to 400 mg/kg, it induces significant anti-nociceptive effects in mice[4].
体外研究
In cell-based studies, Allopurinol sodium at concentrations of 0, 10, 100, and 1000 µg/ml over 17 hours significantly reduces the expression of HIF-1α and HIF-2α in HFF (human fibroblasts) and HUVEC (human umbilical vein endothelial cells) cells. Over a 24-hour period at the same concentrations, it also reduces angiogenesis traits in HUVEC cells[5].
Allopurinol sodium/别嘌醇钠 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Mouse aortic endothelial cells
100 μmol/L
4 hours
To investigate the effect of allopurinol on MP-mediated oxidative stress in endothelial cells, results showed that allopurinol had no significant effect on MP-mediated ROS production.
J Am Heart Assoc. 2012 Jun;1(3):e001842.
THP-1 human myeloid leukemia cells
250 μg/ml
1 hour pre-treatment
Pre-treatment with allopurinol attenuated XOD activation/UA production and significantly decreased phospho-S2448 mTOR levels while increasing T2446 phosphorylation.
Sci Rep. 2014 Sep 9;4:6307.
Allopurinol sodium/别嘌醇钠 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Wild-type and AMPD2 knockout mice
Drinking water
1.1 mM
30 weeks
Allopurinol significantly reduced plasma and intrahepatic uric acid levels in MSG + IMP-treated mice and attenuated weight gain and features of metabolic syndrome.
Nat Metab. 2021 Sep;3(9):1189-1201
Mice
Endotoxin-induced bacterial translocation model
Oral gavage
50 mg/kg
Once at 48 and 24 hours before
To investigate the effect of allopurinol on endotoxin-induced bacterial translocation. Results showed that allopurinol significantly reduced endotoxin-induced bacterial translocation and mucosal injury.
J Clin Invest. 1989 Jul;84(1):36-42
C57BL6/J male mice
Western diet-induced obesity model
Drinking water administration
125 mg/L
Continued for 16 weeks
XO inhibition significantly attenuated WD-induced increases in plasma uric acid, vascular XO activity and oxidative stress, in concert with reductions in proteinuria. Further, XO inhibition prevented WD-induced increases in aortic EnNaC expression and associated endothelial and subendothelial stiffness. XO inhibition also reduced vascular pro-inflammatory and maladaptive immune responses induced by consumption of a WD.
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