Modulatory effects of verapamil in rifampicin activity against Mycobacterium tuberculosis.
| Title: | Modulatory effects of verapamil in rifampicin activity against Mycobacterium tuberculosis. |
|---|---|
| Authors: | Caleffi-Ferracioli KR; Laboratory of Medical Bacteriology, Department of Clinical Analysis & Biomedicine, State University of Maringa, Parana, Brazil.; Cardoso RF; Laboratory of Medical Bacteriology, Department of Clinical Analysis & Biomedicine, State University of Maringa, Parana, Brazil.; de Souza JV; Laboratory of Medical Bacteriology, Department of Clinical Analysis & Biomedicine, State University of Maringa, Parana, Brazil.; Murase LS; Laboratory of Medical Bacteriology, Department of Clinical Analysis & Biomedicine, State University of Maringa, Parana, Brazil.; Canezin PH; Laboratory of Medical Bacteriology, Department of Clinical Analysis & Biomedicine, State University of Maringa, Parana, Brazil.; Scodro RB; Laboratory of Medical Bacteriology, Department of Clinical Analysis & Biomedicine, State University of Maringa, Parana, Brazil.; Ld Siqueira V; Laboratory of Medical Bacteriology, Department of Clinical Analysis & Biomedicine, State University of Maringa, Parana, Brazil.; Pavan FR; Department of Biological Sciences, School of Pharmaceutical Sciences, Paulista State University, Araraquara, Sao Paulo, Brazil. |
| Source: | Future microbiology [Future Microbiol] 2019 Feb; Vol. 14, pp. 185-194. Date of Electronic Publication: 2019 Jan 16. |
| Publication Type: | Journal Article; Research Support, Non-U.S. Gov't |
| Language: | English |
| Journal Info: | Publisher: Taylor & Francis Country of Publication: England NLM ID: 101278120 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1746-0921 (Electronic) Linking ISSN: 17460913 NLM ISO Abbreviation: Future Microbiol Subsets: MEDLINE |
| Imprint Name(s): | Publication: 2024- : [Milton Park, Oxfordshire] : Taylor & Francis; Original Publication: London : Future Medicine |
| MeSH Terms: | Antitubercular Agents/*pharmacology ; Drug Resistance, Multiple, Bacterial/*drug effects ; Mycobacterium tuberculosis/*drug effects ; Rifampin/*pharmacology ; Verapamil/*pharmacology; Bacterial Proteins/drug effects ; Bacterial Proteins/genetics ; Bacterial Proteins/metabolism ; Catalase/genetics ; DNA-Directed RNA Polymerases/genetics ; Membrane Transport Proteins/drug effects ; Membrane Transport Proteins/genetics ; Membrane Transport Proteins/metabolism ; Mycobacterium tuberculosis/genetics ; Mycobacterium tuberculosis/metabolism ; Oxidoreductases/genetics ; Tuberculosis, Multidrug-Resistant/microbiology ; Brazil ; Drug Synergism ; Drug Therapy, Combination ; Gene Expression Regulation, Bacterial ; Genotype ; Humans ; Microbial Sensitivity Tests ; Mutation ; Time Factors |
| Abstract: | Aim: To evaluate modulatory effect of verapamil (VP) in rifampicin (RIF) activity and its effect in efflux pumps (EPs) transcript levels in Mycobacterium tuberculosis.; Materials & Methods: RIF and VP minimal inhibitory concentration, combinatory effect and detection of mutations were determined in 16 isolates. EPs transcript levels were determined in four isolates by real-time PCR after exposure to drugs.; Results: VP showed good combinatory effect among RIF-resistant isolates. This effect was also observed in the relative transcript levels of EPs, mainly after 72 h of exposure, depending on the EP gene, genotype and the resistance profile of the isolate.; Conclusion: Additional regulatory mechanisms in the EP activities, as well as, interactions with other drug-specific resistance mechanisms need further investigation in M. tuberculosis. |
| Contributed Indexing: | Keywords: efflux pump inhibitor; gene regulation; multidrug transporters; real-time PCR; resistance; rifampicin; synergism; tuberculosis; verapamil |
| Substance Nomenclature: | 0 (Antitubercular Agents); 0 (Bacterial Proteins); 0 (Membrane Transport Proteins); 0 (rpoB protein, Mycobacterium tuberculosis); CJ0O37KU29 (Verapamil); EC 1.- (Oxidoreductases); EC 1.11.1.6 (Catalase); EC 1.11.1.6 (katG protein, Mycobacterium tuberculosis); EC 1.3.1.9 (InhA protein, Mycobacterium); EC 2.7.7.6 (DNA-Directed RNA Polymerases); VJT6J7R4TR (Rifampin) |
| Entry Date(s): | Date Created: 20190117 Date Completed: 20190513 Latest Revision: 20190513 |
| Update Code: | 20260130 |
| DOI: | 10.2217/fmb-2018-0277 |
| PMID: | 30648892 |
| Database: | MEDLINE |
Journal Article; Research Support, Non-U.S. Gov't