Lithocholic acid and derivatives: Antibacterial activity
| Autor: | Macia C. S. de Almeida, Patricia G. G. do Nascimento, Gilvandete M. P. Santiago, Telma L. G. Lemos, José Galberto Martins da Costa, Henrique Douglas Melo Coutinho, Ayla Márcia Cordeiro Bizerra, Juliana M. O. Souza |
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| Rok vydání: | 2015 |
| Předmět: |
Staphylococcus aureus
Lithocholic acid Clinical Biochemistry Molecular Conformation Bacillus cereus Microbial Sensitivity Tests medicine.disease_cause Biochemistry Microbiology Structure-Activity Relationship chemistry.chemical_compound Endocrinology Escherichia coli medicine Molecular Biology Pharmacology Dose-Response Relationship Drug biology Chemistry Organic Chemistry Aminoglycoside Neomycin biology.organism_classification Anti-Bacterial Agents Amikacin Pseudomonas aeruginosa Lithocholic Acid Antibacterial activity medicine.drug |
| Zdroj: | Steroids. 104:8-15 |
| ISSN: | 0039-128X |
| DOI: | 10.1016/j.steroids.2015.07.007 |
| Popis: | In order to develop bioactive lithocholic acid derivatives, we prepared fifteen semi-synthetic compounds through modification at C-3 and/or C-24. The reactions showed yields ranging from 37% to 100%. The structures of all compounds obtained were identified on the basis of their spectral data (IR, MS, 1D- and 2D-NMR). The activity of lithocholic acid and derivatives was evaluated against the growth of Escherichia coli, Staphylococcus aureus, Bacillus cereus and Pseudomonas aeruginosa. The derivative 3α-formyloxy-5β-cholan-24-oic acid (LA-06) showed the best activity, with MIC values of 0.0790 mM against E. coli (Ec 27) and B. cereus in both cases, and 0.0395 mM against S. aureus (ATCC 12692). Lithocholic acid and the derivatives with MIC⩽1.2 mM were evaluated on the susceptibility of some bacterial pathogens to the aminoglycoside antibiotics neomycin, amikacin and gentamicin was evaluated. There are no previously reported studies about these compounds as modifiers of the action of antibiotics or any other drugs. |
| Databáze: | OpenAIRE |
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