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In vitro: BEC causes significant enhancement of NO-dependent smooth muscle relaxation. In myocytes, BEC augments Ca(2+)-dependent NOS activity and NO production, and increases basal contractility. BEC also inhibits the proliferation of human pulmonary artery smooth muscle cells by decreasing the expression levels of cyclin D1 and CDK4, increasing the expression of p27, and partly reducing the phosphorylation of Akt and ERK.
In vivo: In mice with allergic inflammation (OVA/OVA), BEC enhances peribronchiolar and perivascular inflammation, leads to enhanced NF-κB DNA binding and NF-κB-dependent inflammatory gene expression, and causes an increase in the content of NOx. In rats with pulmonary arterial hypertension, BEC reduces the right ventricle systolic pressure.
| Cell Experiment | |
|---|---|
| Cell lines | RAW264.7 cells |
| Preparation method | cell viability and arginase activity To explore the functional role of endogenous arginase II on the LPS-induced cell death, we investigated the effect of BEC, an arginase inhibitor, on the LPS-induced NO production and cell viability in RAW264.7 cells. Cells were treated with LPS (300 ng/ml) in the presence or absence of BEC, arginase inhibitor for 18 h. BEC (100 μM) did not affect basal arginase activity, however, it significantly inhibit LPS-induced up-regulation of arginase activity. Furthermore, BEC significantly inhibited LPS-induced NO production and cell death in RAW264.7 cells. This data suggested that up-regulated arginase II in response to LPS plays a protective role against LPS-induced cell death in macrophages. |
| Concentrations | 100 μM |
| Incubation time | 18 h |
| Animal Experiment | |
|---|---|
| Animal models | Mice with allergic inflammation (OVA/OVA) |
| Formulation | PBS |
| Dosages | 0.30 mM, 40 μl |
| Administration | oropharyngeal aspiration |
| Molecular Weight | 229.49 |
| Formula | C5H12BNO4S.ClH |
| CAS Number | 222638-67-7 |
| Solubility (25°C) | Water 45 mg/mL DMSO 45 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Khong SM, et al. Br J Pharmacol. Arginase II inhibition prevents nitrate tolerance.
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