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High-Performance Liquid Chromatography
Published in Adorjan Aszalos, Modern Analysis of Antibiotics, 2020
Joel J. Kirschbaum, Adorjan Aszalos
Nifuroxazide is used in the treatment of acute bacterial diarrhea. It was assayed in plasma using a 5-μm octadecylsilane column (150 x 4.6 mm) and a mobile phase of water acidified with phosphoric acid to pH 2.5-acetonitrile (70:30) flowing at 1 ml/min through a detector set to 362 nm [458]. Responses were linear from 2 to 200 ng/ml. The relative standard deviation at 2 ng/ml was 15%, with 90% recovered; at 200 ng/ml, 100% was recovered with a relative standard deviation of 3%.
The Renewal of Interest in Nitroaromatic Drugs
Published in Venkatesan Jayaprakash, Daniele Castagnolo, Yusuf Özkay, Medicinal Chemistry of Neglected and Tropical Diseases, 2019
Nicolas Primas, Caroline Ducros, Patrice Vanelle, Pierre Verhaeghe
As with the Chagas disease, nifuroxazide derivatives were also tested against the kinetoplastid L. donovani. Although nifuroxazide (29) belongs to the family of 5-nitrofurans, far better results were obtained by replacing the furan ring by a thiophene ring. The antileishmanial activities obtained on the promastigote form of the parasite were below the micromolar value for two compounds (78–79) (Figure 21) (Rando et al. 2008). Similar activity was demonstrated by compound (79) based on the 5-nitrofuran ring against L. infantum promastigotes. With its two nitro groups, the mutagenicity of this compound may be questionable (Petri e Silva et al. 2016). Structures and in vitro anti-L. donovani activities of nifuroxazide analogs (78–79).
Renoprotective effect of nifuroxazide in diabetes-induced nephropathy: impact on NFκB, oxidative stress, and apoptosis
Published in Toxicology Mechanisms and Methods, 2018
Nehal M. Elsherbiny, Sawsan A. Zaitone, Hala M. F. Mohammad, Mohamed El-Sherbiny
Nifuroxazide is an intestinal broad-spectrum antibiotic that showed security to a certain extent in clinical applications (Jia et al. 2017). Safety of nifuroxazide has been reported in human (Nelson et al. 2008) as well as in tumor-bearing mice (Yang et al. 2015). Interestingly, nifuroxazide is reported as strong inhibitor of STAT3 activation. STAT3 is a transcription factor that mediates the signal of various inflammatory cytokines and growth factors (Chung and Vadgama 2015). Various triggers activates STAT3 including inflammatory cytokines, advanced glycation end products and high glucose. Once activated, phosphorylation is translocated to nucleus and induced expression of multiple pro-inflammatory and angiogenic genes (Gao et al. 2018). Constitutive activation STAT3 is pathogenic and targeting STAT3 has been reported to be effective in various diseases including DN and DM (Said et al. 2018). On the other hand, NFκB has been reported as crucial regulator of inflammatory events associated with DN. Indeed, increased nuclear translocation of NFκB has been demonstrated in both experimental and human DN (Kuhad and Chopra 2009). Interestingly, both STAT3 and NFκB share common target genes that regulate cell proliferation, survival, inflammation, and immune response. Moreover, activated STAT3 was also reported to contribute to constitutive activation of NFκB in inflammation and cancer (He and Karin 2011). We found that nifuroxazide treatment reduced diabetes-triggered NFκB nuclear translocation in renal tissue, suggesting a crosstalk between STAT3 and NFκB in DN.