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Mitochondrial uncouplers inhibit oncogenic E2F1 activity and prostate cancer growth.
Cell Rep Med
December 2024
Georgia Cancer Center, Augusta University, Augusta, GA 30912, USA; Department of Biochemistry and Molecular Biology, Medical College of Georgia, Augusta University, Augusta, GA 30912, USA. Electronic address:
Mitochondrial uncouplers dissipate proton gradients and deplete ATP production from oxidative phosphorylation (OXPHOS). While the growth of prostate cancer depends on OXPHOS-generated ATP, the oncogenic pathway mediated by the transcription factor E2F1 is crucial for the progression of this deadly disease. Here, we report that mitochondrial uncouplers, including tizoxanide (TIZ), the active metabolite of the Food and Drug Administration (FDA)-approved anthelmintic nitazoxanide (NTZ), inhibit E2F1-mediated expression of genes involved in cell cycle progression, DNA synthesis, and lipid synthesis.
View Article and Find Full Text PDFEco-sustainable chromatographic method for the determination of favipiravir and nitazoxanide for COVID-19: application to human plasma.
BMC Chem
January 2025
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Nile Valley University (NVU), El Fayoum, 63518, Egypt.
Coronavirus disease 2019 (COVID-19), an extremely contagious illness, has posed enormous challenges to healthcare systems around the world. Although the evidence on COVID-19 management is growing, antiviral medication is still the first line of treatment. Therefore, it is critical that effective, safe, and tolerable antivirals be available to treat early COVID-19 and stop its progression.
View Article and Find Full Text PDFFormulation and Characterization of β-Cyclodextrins-Nitazoxanide Inclusion Complexes: Enhanced Solubility, In Vitro Drug Release, and Antiviral Activity in Vero Cells.
Pharmaceutics
November 2024
Department of Chemistry, College of Science, King Saud University, Riyadh 11451, Saudi Arabia.
Nitazoxanide (NTX) exhibits promising therapeutic potential; its effectiveness is constrained by its low oral bioavailability due to its poor water solubility and limited permeability. This study focused on developing a complex of NTX with β-cyclodextrins (β-CDs), specifically β-CD and hydroxypropyl-β-cyclodextrin (Hβ-CD), to enhance the solubility and antiviral activity of NTX. The formation of the β-CD:NTX in an aqueous solution was verified using UV-visible spectroscopy, confirming a 1:1 inclusion complex.
View Article and Find Full Text PDFNitazoxanide controls virus viability through its impact on membrane bioenergetics.
Sci Rep
December 2024
Institut Cochin, INSERM, CNRS, Université de Paris, 75014, Paris, France.
Viruses are dependent on cellular energy metabolism for their replication, and the drug nitazoxanide (Alinia) was shown to interfere with both processes. Nitazoxanide is an uncoupler of mitochondrial oxidative phosphorylation (OXPHOS). Our hypothesis was that mitochondrial uncoupling underlies the antiviral effects of nitazoxanide.
View Article and Find Full Text PDFClinical Experience With Ivermectin and Nitazoxanide in the Management of COVID-19 Among Mexican Out- and Inpatients.
Cureus
November 2024
Biotechnology, Laboratorio Nacional LANSEIDI, Mexico City, MEX.
Background and objective The use of ivermectin and nitazoxanide in the treatment of coronavirus disease 2019 (COVID-19) has been a subject of controversy. In this study, we aimed to describe our clinical experience in treating COVID-19 patients with these drugs in Mexico. Material and methods The study involved out- and inpatient clinical assessments of COVID-19 patients conducted in Mexico City from September 2020 to November 2021.
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