Old and New TB Drugs: Mechanisms of Action and Resistance

Kolyva, Anastasia S.; Karakousis, Petros C.

doi:10.5772/30992

Cited by 12 publications

(4 citation statements)

References 132 publications

(113 reference statements)

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“…INH, RIF and SM resistance have even been associated with low or no fitness costs [2,4]. Table 1 summarizes the literature data [7,[13][14][15] on the roles of the major antibiotics used to treat TB and known genes involved in drug-resistance, as well as the mechanisms thought to be responsible for drug-resistance. Drug resistant phenotype in Mtb is associated exclusively with mutations at specific positions in bacterial genomes.…”

Section: Genetic Mechanisms Of Drug Resistance In Mtbmentioning

confidence: 99%

Clade-Specific Distribution of Antibiotic Resistance Mutations in the Population of Mycobacterium tuberculosis - Prospects for Drug Resistance Reversion

Niekerk¹,

Pierneef²,

Reva³

et al. 2018

Basic Biology and Applications of Actinobacteria

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Tuberculosis, caused by Mycobacterium tuberculosis (Mtb), is a leading cause of death in humans worldwide. The emergence of antibiotic-resistant strains of Mtb is a threat to tuberculosis control. A general belief is that drug resistance is acquired by Mtb during antibiotic treatment by accumulation of spontaneous mutations. Also, it is known that the drug resistance mutations (DRM) have an associated fitness cost, reducing the transmissibility and virulence of resistant strains. In this work we show that many canonical DRM are clade specific; i.e. they occur only in specific genetic lineages of Mtb and depend on a specific genetic context necessary for the reduction of the fitness cost and sustainability of the drug resistance phenotype. Dependence of the drug resistance on occurrence of genetic variants of multiple genes and specific activities of the encoded proteins allows combating the drug resistance by impairing the global genetic context. A new drug, FS-1, reverses antibiotic resistance by compromising this genetic context and aggravating the fitness cost of DRM.

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Section: Genetic Mechanisms Of Drug Resistance In Mtbmentioning

confidence: 99%

Clade-Specific Distribution of Antibiotic Resistance Mutations in the Population of Mycobacterium tuberculosis - Prospects for Drug Resistance Reversion

Niekerk¹,

Pierneef²,

Reva³

et al. 2018

Basic Biology and Applications of Actinobacteria

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“…Isoniazid (INH) has been in clinical use for nearly 50 years as a first‐line drug for the prevention and treatment of tuberculosis (TB). It is a prodrug with approved therapeutic applications [10–11] . A wide number of Schiff base complexes exhibit good anti TB, [12–13] antibacterial, [14] anti‐fungal [15] and anti‐cancer [16–17] activities.…”

Section: Introductionmentioning

confidence: 99%

“…It is a prodrug with approved therapeutic applications. [10][11] A wide number of Schiff base complexes exhibit good anti TB, [12][13] antibacterial, [14] anti-fungal [15] and anti-cancer [16][17] activities. Due to the greater therapeutic importance of INH, it is used against bacterial infections [18] in a broad spectrum.…”

Section: Introductionmentioning

confidence: 99%

Selective Detection of Copper Ions and Biological Activities of Isoniazid Schiff Bases

et al. 2023

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Following mechanical milling, the condensation reaction of the corresponding heterocyclic aldehydes with Isoniazid yields the Schiff base (E)‐N′‐((1H‐pyrrol‐2‐yl) methylene)isonicotinohydrazide (S1) and (E)‐N′‐(Thiophen‐2‐ylmethylene)isonicotinohydrazide (S2) supported heterocyclic derivatives. The structures of the Schiff bases, S1 and S2 were confirmed by 1H NMR, 13C NMR and IR spectroscopy. Copper ions (Cu2+) were trapped by S1 in DMSO to form the yellow‐coloured complex Cu‐(E)‐N′‐((1H‐pyrrol‐2‐yl)methylene) isonicotinohydrazide (Cu2++S1) with high sensitivity and selectivity. But the same ligand S1 could not be able to capture other metal ions tested for this work (namely, Co2+, Ni2+, Zn2+, Mn2+, Hg2+, Cd2+, Pb2+, Fe2+, and Fe3+) in DMSO. UV‐visible spectroscopic results confirmed the complex formation (Cu2++S1) with copper ions, but not with the other ions. Analysis of non‐covalent interactions (NCI) of ligand S1 with Ni2+, Cu2+ and Zn2+ in DMSO were investigated by density functional theory (DFT). NCI analysis of S1 by Cu2+ ions in DMSO was in good agreement with the experimental results. S2 did not react with any metal ions used in this study to form a complex in DMSO and the same was confirmed by UV‐Visible spectra. Reasonably good antibacterial activity was observed with S1, S2, Cu2++S1 compared to amoxicillin against Gram‐negative bacteria (K. pneumoniae, E. coli), Gram‐positive bacteria (S. aureus, S. pneumoniae), and fungal strain (C. albicans).

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“…Despite impressive therapeutic progresses in the battle against infections, microorganisms are still a threat to mankind (Chiang et al, 2010;Kolyva and Karakousis, 2012). With hundreds of antibacterial molecules, major concerns remain about the emergence of resistant and multidrug-resistant pathogens (Strateva and Yordanov, 2009;Chiang et al, 2010).…”

Section: Introductionmentioning

confidence: 99%

Evaluation of antimycobacterial rhamnolipid production from non-cytotoxic strains of Pseudomonas aeruginosa isolated from rhizospheric soil of medicinal plants

Mishra

Dubey

Yabaji

et al. 2016

IJBR

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Rhamnolipids (RLs) are the bacterial derived biosurfactants and known for a wide range of industrial and therapeutic applications. They exhibit potent anti-bacterial activity against various gram positive, gram negative and acid fast bacteria including Mycobacterium tuberculosis. Since, Pseudomonas is one of the largest known genuses containing a variety of rhamnolipid producing strains. Therefore, in this study, we selectively isolated the Pseudomonas aeruginosa strains from the rhizospheric soil of the Indian plants of medicinal value, e.g. Azadirachta Indica and Ficus spp., and evaluated them for their natural ability to produce antibacterial rhamnolipids. The bacteria were identified on the basis of 16s rRNA sequencing and biochemical characterization. Among 33 of P. aeruginosa isolates from different soil samples, four isolates showed potent inhibitory activity against methicillin resistant Staphylococcus aureus (MRSA) and fast grower mycobacterial spp. The inhibitory potential of the isolates was found to be correlated with their ability to produce RLs in the medium. The industrial viability of the strains was assessed on the basis of cytotoxicity determining alternative allele, exoS/exoU and cell mediated cytotoxicity against murine macrophages J774.1. The newly isolated strains harbor exoS allele and exhibits lower cell mediated cytotoxicity on macrophage cell line as compared to the clinical strains PA-BAA-427 and PA-27853 used as a control in this study.

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Old and New TB Drugs: Mechanisms of Action and Resistance

Cited by 12 publications

References 132 publications

Clade-Specific Distribution of Antibiotic Resistance Mutations in the Population of Mycobacterium tuberculosis - Prospects for Drug Resistance Reversion

Clade-Specific Distribution of Antibiotic Resistance Mutations in the Population of Mycobacterium tuberculosis - Prospects for Drug Resistance Reversion

Selective Detection of Copper Ions and Biological Activities of Isoniazid Schiff Bases

Evaluation of antimycobacterial rhamnolipid production from non-cytotoxic strains of Pseudomonas aeruginosa isolated from rhizospheric soil of medicinal plants

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