The synthesis of deoxycholic acid (DCA)- and cholic acid (CA)-derived mixed tetraoxanes revealed that N-(2-dimethylamino)ethyl derivatives are potent antimalarials in vitro and in vivo. The tetraoxanes presented in this paper are dual inhibitors: besides curing mice in vivo without observed toxic effects, they kill cancer cell lines at very low concentrations. For example, DCA and CA derivatives 16 and 25 cured 3/5 (160 mg/kg/day) and 2/5 (40 mg/kg/day, MTD >960 mg/kg), respectively, and they were extremely active against melanoma LOX IMVI cancer, LC50 = 22 nM and 69 nM, respectively.
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http://dx.doi.org/10.1021/jm070684m | DOI Listing |
ACS Infect Dis
January 2024
Laboratory of Nanotechnology and Chemical Biology, Regional Centre for Biotechnology, 3rd Milestone Faridabad-Gurgaon Expressway, NCR Biotech Cluster, Faridabad 121001, Haryana, India.
Biofilm infections are mainly caused by Gram-positive bacteria (GPB) like , Gram-negative bacteria (GNB) like , and fungi like . These infections are responsible for antimicrobial tolerance, and commensal interactions of these microbes pose a severe threat to chronic infections. Treatment therapies against biofilm infections are limited to eradicating only 20-30% of infections.
View Article and Find Full Text PDFEur J Med Chem
March 2023
Ferrier Research Institute, Victoria University of Wellington, 69 Gracefield Rd, Lower Hutt, 5040, New Zealand.
Recent discoveries have demonstrated that the physiological function of bile acids extends to the regulation of diverse signaling processes through interactions with nuclear and G protein-coupled receptors, most notably the Farnesoid-X nuclear receptor (FXR) and the G protein-coupled bile acid receptor 1 (GPBAR1, also known as TGR5). Targeting such signaling pathways pharmacologically, i.e.
View Article and Find Full Text PDFNPJ Biofilms Microbiomes
November 2022
Department of Biology, Texas A&M University, College Station, TX, 77843, USA.
The Clostridioides difficile pathogen is responsible for nosocomial infections. Germination is an essential step for the establishment of C. difficile infection (CDI) because toxins that are secreted by vegetative cells are responsible for the symptoms of CDI.
View Article and Find Full Text PDFMolecules
December 2021
N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, SB RAS, 9, Lavrent'ev Ave., 630090 Novosibirsk, Russia.
Kidney360
May 2021
Division of Renal Diseases, Department of Medicine, University of Colorado Anschutz Medical Campus, Aurora, Colorado.
Background: Our metabolome approach found that levels of circulating, free deoxycholic acid (DCA) is associated with the severity of vascular calcification in patients with CKD. However, it is not known whether DCA directly causes vascular calcification in CKD.
Methods: Using various chemicals and animal and cell culture models, we investigated whether the modulation of DCA levels influences vascular calcification in CKD.
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