Nafamostat Mesylate(FUT-175) is a synthetic serine protease inhibitor [1]. Nafamostat Mesylate reduces inflammatory responses by inhibiting the complement system, reducing cytokine release, and preventing pancreatic enzyme activation [2]. Nafamostat Mesylate is commonly used to treat acute pancreatitis [3-4].
In SW620 cells, Nafamostat Mesylate (80μg/mL; 3h) prevents NF-κB activation and induces apoptosis in irradiated colorectal cancer cells [5]. In MSTO-211H cells, cell viability was significantly reduced after Nafamostat Mesilate (10μM; 48h) treatment [6]. In YCU-L891 and YCU-H891 cells, Nafamostat Mesylate (10μM; 48h) inhibited the proliferation of two HNSCC cell lines [7].
In choline deficient ethionine diet mice model, Nafamostat Mesylate (20mg/kg; ip; 5d) inhibited the redistribution of cathepsin B activity and the activation of trypsinogen [8]. In xenograft pancreatic cancer mice model, Nafamostat Mesylate (30μg/g; ip; 6 weeks) enhances oxaliplatin-induced tumor growth inhibition [9].
References:
[1]. Mellgren K, Skogby M, Friberg L G, et al. The influence of a serine protease inhibitor, nafamostat mesilate, on plasma coagulation, and platelet activation during experimental extracorporeal life support (ECLS)[J]. Thrombosis and haemostasis, 1998, 79(02): 342-347.
[2]. He Q, Wei Y, Qian Y, et al. Pathophysiological dynamics in the contact, coagulation, and complement systems during sepsis: Potential targets for nafamostat mesilate[J]. Journal of intensive medicine, 2024, 4(04): 453-467.
[3]. Wisner J R, Ozawa S, Renner I G. The effects of nafamostat mesilate (FUT-175) on caerulein-induced acute pancreatitis in the rat[J]. International journal of pancreatology, 1989, 4(4): 383-390.
[4]. Keck T, Balcom J H, Antoniu B A, et al. Regional effects of nafamostat, a novel potent protease and complement inhibitor, on severe necrotizing pancreatitis[J]. Surgery, 2001, 130(2): 175-181.
[5]. Sugano H, Shirai Y, Horiuchi T, et al. Nafamostat mesilate enhances the radiosensitivity and reduces the radiation-induced invasive ability of colorectal cancer cells[J]. Cancers, 2018, 10(10): 386.
[6]. Sutoh T, Fukuda I, Kimura D, et al. Nafamostat mesilate (FUT-175) inhibits cell growth and invasion of malignant pleural mesothelioma cell line, MSTO-211H[J]. Hirosaki Medical Journal, 2010, 61(1): 19-25.
[7]. Yamashita Y, Ishiguro Y, Sano D, et al. Antitumor effects of Nafamostat mesilate on head and neck squamous cell carcinoma[J]. Auris Nasus Larynx, 2007, 34(4): 487-491.
[8]. Hirano T, Takeuchi S. A New Protease Inhibitor, Nafamostat Mesilate (FUT-175), Protects Pancreatic Acinar Cells in CDE-Diet-lnduced Pancreatitis in Mice[J]. Digestive surgery, 1993, 10(4): 182-188.
[9]. Gocho T, Uwagawa T, Furukawa K, et al. Combination chemotherapy of serine protease inhibitor nafamostat mesilate with oxaliplatin targeting NF-κB activation for pancreatic cancer[J]. Cancer Letters, 2013, 333(1): 89-95.
Nafamostat Mesylate(FUT-175)是一种合成的丝氨酸蛋白酶抑制剂 [1]。Nafamostat Mesylate通过抑制补体系统、减少细胞因子释放和阻止胰腺酶活化来减轻炎症反应 [2]。Nafamostat Mesylate常用于治疗急性胰腺炎 [3-4]。
在 SW620 细胞中，Nafamostat Mesylate（80μg/mL；3h）可抑制NF-κB活化并诱导受照射的结直肠癌细胞凋亡 [5]。在MSTO-211H细胞中，Nafamostat Mesylate（10μM；48h）处理后细胞活力显著降低 [6]。在YCU-L891和YCU-H891细胞中，Nafamostat Mesylate（10μM；48h）抑制了两种HNSCC细胞系的增殖 [7]。
在胆碱缺乏的乙硫氨酸饮食小鼠模型中，Nafamostat Mesylate（20mg/kg；ip；5d）抑制了组织蛋白酶B活性的重新分布和胰蛋白酶原的活化 [8]。在异种移植胰腺癌小鼠模型中，Nafamostat Mesylate（30μg/g；ip；6周)增强了奥沙利铂诱导的肿瘤生长抑制作用 [9]。