β-Aminopropionitrile (BAPN) is a specific irreversible lysine oxidase (LOX) inhibitor with an IC50 value of approximately 3-8μM [1]. β Aminopropionitrile targets the active site of LOX or LOXL isoenzymes [2]. β-Aminopropionitrile can cross-link elastin fibers and collagen fibers to maintain the homeostasis of the elastic layer [3].
In vitro, β-Aminopropionitrile (500μM) treated cervical cancer HeLa and SiHa cells for 48 hours, inactivating LOX activity and significantly inhibiting hypoxia-induced cell invasion. The invasion ability of the two cell lines was inhibited by 50% and 60% respectively[4]. β-Aminopropionitrile (1.0mg/mL, approximately 14.3μM) treated LX-2 cells for 24 hours and significantly down-regulated the expression of LOXL2 and α-SMA induced by TGF β [5].
In vivo, β-Aminopropionitrile (100 mg/kg) added to the drinking water of rats fed a high-fat diet for 6 weeks reduced fasting blood glucose and insulin levels, reduced homeostasis model assessment (HOMA) index, and improved obesity and adipose tissue fibrosis. phenomenon [6]. Adding β-Aminopropionitrile (1000 mg/kg) to drinking water and feeding C57BL/6 male mice for 4 weeks significantly reduced the weight of the mice and reduced plasma triglyceride and cholesterol levels [7].
References:
[1] Bhave G, Cummings C F, Vanacore R M, et al. Peroxidasin forms sulfilimine chemical bonds using hypohalous acids in tissue genesis[J]. Nature chemical biology, 2012, 8(9): 784-790.
[2] Rodriguez H M, Vaysberg M, Mikels A, et al. Modulation of lysyl oxidase-like 2 enzymatic activity by an allosteric antibody inhibitor[J]. Journal of biological chemistry, 2010, 285(27): 20964-20974.
[3] Kawai T, Takayanagi T, Forrester S J, et al. Vascular ADAM17 (a Disintegrin and Metalloproteinase Domain 17) Is Required for Angiotensin II/β-Aminopropionitrile–Induced Abdominal Aortic Aneurysm[J]. Hypertension, 2017, 70(5): 959-963.
[4] Yang X, Li S, Li W, et al. Inactivation of lysyl oxidase by β-aminopropionitrile inhibits hypoxia-induced invasion and migration of cervical cancer cells[J]. Oncology reports, 2013, 29(2): 541-548.
[5] Cheng F, Yang F, Wang Y, et al. Mesenchymal stem cell-derived exosomal miR-27b-3p alleviates liver fibrosis via downregulating YAP/LOXL2 pathway[J]. Journal of Nanobiotechnology, 2023, 21(1): 195.
[6] Miana M, Galán M, Martínez-Martínez E, et al. The lysyl oxidase inhibitor β-aminopropionitrile reduces body weight gain and improves the metabolic profile in diet-induced obesity in rats[J]. Disease models & mechanisms, 2015, 8(6): 543-551.
[7] Ren W, Liu Y, Wang X, et al. β-Aminopropionitrile monofumarate induces thoracic aortic dissection in C57BL/6 mice[J]. Scientific reports, 2016, 6(1): 28149.
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