Sulfamethoxazole is a bacteriostatic sulfonamide antibiotic [1]. Sulfamethoxazole competitively inhibits bacterial dihydropteroate synthase (DHPS), blocking folate synthesis and thereby interfering with DNA and protein synthesis [2-3]. Sulfamethoxazole is widely used to treat urinary tract infections, respiratory tract infections, and gastrointestinal infections [4].
In E. coli, after Sulfamethoxazole (1.6mg/mL; 24h) treatment, the activity of bacterial was significantly inhibited [5]. In mouse pancreatic β cells, Sulfamethoxazole (0.1-10mM; 3h) treatment inhibits the channel current of KATP and the inhibition is dose-dependent [6].
In Toxoplasma gondii infected mouse model, Sulfamethoxazole (300mg/kg; po; 24d) significantly decreased mortality among the infected WT C57BL/6 and GKO mice [7]. In danio rerio, Sulfamethoxazole (250ppm; embryo culture;5d) induces brain capillary toxicity by upregulating VEGF and chemokine signaling [8].
References:
[1]. Rudy B C, Senkowski B Z. Sulfamethoxazole[M]//Analytical profiles of drug substances. Academic Press, 1973, 2: 467-486.
[2]. Fernández-Villa D, Aguilar M R, Rojo L. Folic acid antagonists: antimicrobial and immunomodulating mechanisms and applications[J]. International journal of molecular sciences, 2019, 20(20): 4996.
[3]. Cheong M S, Seo K H, Chohra H, et al. Influence of sulfonamide contamination derived from veterinary antibiotics on plant growth and development[J]. Antibiotics, 2020, 9(8): 456.
[4]. Petri W A. Sulfonamides, trimethoprim, sulfamethoxazole, quinolones, and agents for urinary tract infections[J]. Goodman & Gilman’s the pharmacological basis of therapeutics. New York (NY): McGraw Hill, 2006: 1111-1125.
[5]. Park H B, Wei Z, Oh J, et al. Sulfamethoxazole drug stress upregulates antioxidant immunomodulatory metabolites in Escherichia coli[J]. Nature microbiology, 2020, 5(11): 1319-1329.
[6]. Ogata H, Kitamura S, Fujiwara M, et al. Dose dependent effect of sulfamethoxazole on inhibiting KATP channel of mouse pancreatic β cell[J]. Dose-Response, 2023, 21(3): 15593258231203611.
[7]. Norose K, Aosai F, Mun H S, et al. Effects of sulfamethoxazole on murine ocular toxoplasmosis in interferon-γ knockout mice[J]. Investigative ophthalmology & visual science, 2006, 47(1): 265-271.
[8]. Xu Y, Luo L, Chen J. Sulfamethoxazole induces brain capillaries toxicity in zebrafish by up-regulation of VEGF and chemokine signalling[J]. Ecotoxicology and Environmental Safety, 2022, 238: 113620.
Sulfamethoxazole是一种抑菌磺酰胺类抗生素 [1]。Sulfamethoxazole竞争性抑制细菌二氢叶酸合酶（DHPS），阻断叶酸合成，从而干扰DNA和蛋白质合成 [2-3]。Sulfamethoxazole广泛用于治疗泌尿道感染、呼吸道感染和胃肠道感染 [4]。
在大肠杆菌中，Sulfamethoxazole（1.6mg/mL；24h）处理后，细菌活性受到显著抑制 [5]。在小鼠胰腺β细胞中，Sulfamethoxazole（0.1-10mM；3h）处理可抑制KATP通道电流，且这种抑制作用呈剂量依赖性 [6]。
在弓形虫感染的小鼠模型中，Sulfamethoxazole（300mg/kg；口服；24d）显著降低了感染的野生型C57BL/6小鼠和GKO小鼠的死亡率 [7]。在斑马鱼中，Sulfamethoxazole（250ppm；胚胎培养；5d）通过上调VEGF和趋化因子信号传导诱导脑毛细血管毒性 [8]。