BEC hydrochloride is a slow-binding and competitive Arginase II inhibitor with Ki of 0.31 μM and 30 nM at pH 7.5 and pH 9.5, respectively[3]. Administration of the arginase inhibitor BEC (S-(2-boronoethyl)-l-cysteine) decreased arginase activity and caused alterations in NO homeostasis, which were reflected by increases in S-nitrosylated and nitrated proteins in the lungs from inflamed mice. BEC enhanced perivascular and peribronchiolar lung inflammation, mucus metaplasia, NF-kappaB DNA binding, and mRNA expression of the NF-kappaB-driven chemokine genes CCL20 and KC, and lead to further increases in airways hyperresponsiveness[4]. BEC is associated with a decline in FEV1(forced expiratory volume in 1 second), and a consistently high BEC is an independent risk factor for an accelerated decline in FEV1[5].
BEC·HCl 细胞实验
Cell Line
Concentration
Treated Time
Description
References
MAF cells
500 μM
48 h
To evaluate the inhibitory effect of BEC on arginase activity in MAF cells. Results showed that BEC inhibited arginase activity in MAF cells.
Cell Mol Life Sci. 2021 Jan;78(2):661-673.
Bovine retinal endothelial cells
10 μM
24 h
Under high glucose conditions, BEC treatment reversed the decrease in NO release, indicating that arginase inhibition restores NO bioavailability.
Front Immunol. 2013 Jul 3;4:173.
peritoneal cells
90 μM
48 h
To evaluate the effect of BEC on CD3ζ re-expression, results showed that BEC could restore CD3ζ expression
Parasit Vectors. 2020 Feb 6;13(1):49.
BEC·HCl 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c mice
Staphylococcus aureus bloodstream infection model
Intraperitoneal injection
50 mg/kg
Once daily for 14 days
BEC enhanced NO production by inhibiting arginase activity, thereby protecting mice from Staphylococcus aureus infection
Front Immunol. 2020 Jul 28;11:1639
Zucker rats
Obese Zucker rat model
Intraperitoneal injection
55.6μg/hour
Continuous for 6 days
BEC improves endothelial function and reduces blood pressure in obese Zucker rats by inhibiting arginase activity.
Obesity (Silver Spring). 2015 Feb;23(2):383-90
Rat
STZ-induced diabetic rats
Ex vivo pretreatment
100 μM
45 minutes
BEC pretreatment partially restored the endothelial-dependent vasodilation of the central retinal arteries in STZ-induced diabetic rats
Diabetologia. 2013 Mar;56(3):654-62
BALB/c mice
Sub-acute and chronic models of allergic airways inflammation
Nebulized administration
40 μg/g
Single dose, 15 minutes before pulmonary function testing
BEC significantly attenuated the CAP+O3-induced increase in AHR, completely reversing the exacerbation of symptoms in OVA/OVA mice
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