Identification of lipid metabolism-targeting compounds active against drug-resistant M. tuberculosis

Singh, Alok; Karaulia, Pratiksha; Yadav, Pragya; Narender, Tadigoppula; Singh, Satyendra; Sashidhara, Koneni V.; Pandey, Amit; Chopra, Sidharth; Dasgupta, Arunava

doi:10.1016/j.jgar.2016.07.003

Cited by 6 publications

(2 citation statements)

References 5 publications

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“…These results agree with previous studies showing that CUR is a potential anti-Mtb agent [65]. It has been demonstrated that CUR has a minimum concentration inhibitory (MIC) activity of 16 µg/mL against drug-susceptible Mtb H37Rv, isoniazid-resistant Mtb H37Rv, rifampicin-resistant H37Rv, streptomycin-resistant H37Rv and ethambutol-resistant H37Rv [66]. The effect of CUR against Mtb could be direct, affecting the bacterial lipid metabolism since lipids and their metabolism is critical to all aspects of mycobacterial infection, pathogenicity, and persistence in the host [66].…”

Section: Discussionsupporting

confidence: 92%

“…It has been demonstrated that CUR has a minimum concentration inhibitory (MIC) activity of 16 µg/mL against drug-susceptible Mtb H37Rv, isoniazid-resistant Mtb H37Rv, rifampicin-resistant H37Rv, streptomycin-resistant H37Rv and ethambutol-resistant H37Rv [66]. The effect of CUR against Mtb could be direct, affecting the bacterial lipid metabolism since lipids and their metabolism is critical to all aspects of mycobacterial infection, pathogenicity, and persistence in the host [66]. CUR can also inhibit bacterial intracellular growth and promote sensible drug strain clearance, as demonstrated in differentiated THP-1 human monocytes, primary human alveolar macrophages, and Raw 264.7 cells infected with Mtb H37Rv or MDR clinical isolates [67,68], by promoting caspase-3-dependent apoptosis and autophagy.…”

Section: Discussionmentioning

confidence: 99%

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Effect of Curcumin in Experimental Pulmonary Tuberculosis: Antimycobacterial Activity in the Lungs and Anti-Inflammatory Effect in the Brain

Lara-Espinosa

Arce-Aceves

López-Torres

et al. 2022

IJMS

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Tuberculosis (TB) is one of the ten leading causes of death worldwide. Patients with TB have been observed to suffer from depression and anxiety linked to social variables. Previous experiments found that the substantial pulmonary inflammation associated with TB causes neuroinflammation, neuronal death, and behavioral impairments in the absence of brain infection. Curcumin (CUR) is a natural product with antioxidant, anti-inflammatory and antibacterial activities. In this work, we evaluated the CUR effect on the growth control of mycobacteria in the lungs and the anti-inflammatory effect in the brain using a model of progressive pulmonary TB in BALB/c mice infected with drug-sensitive mycobacteria (strain H37Rv). The results have shown that CUR decreased lung bacilli load and pneumonia of infected animals. Finally, CUR significantly decreased neuroinflammation (expression of TNFα, IFNγ and IL12) and slightly increased the levels of nuclear factor erythroid 2-related to factor 2 (Nrf2) and the brain-derived neurotrophic factor (BDNF) levels, improving behavioral status. These results suggest that CUR has a bactericidal effect and can control pulmonary mycobacterial infection and reduce neuroinflammation. It seems that CUR has a promising potential as adjuvant therapy in TB treatment.

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Section: Discussionsupporting

confidence: 92%

Section: Discussionmentioning

confidence: 99%

Effect of Curcumin in Experimental Pulmonary Tuberculosis: Antimycobacterial Activity in the Lungs and Anti-Inflammatory Effect in the Brain

Lara-Espinosa

Arce-Aceves

López-Torres

et al. 2022

IJMS

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Sacubitril‐Based Urea and Thiourea Derivatives as Novel Inhibitors for Anti‐Tubercular against Dormant Tuberculosis

et al. 2021

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In the present study, we have attempted to identify Sacubitril derivatives as lead compounds for dormant tuberculosis. A total of twenty‐one compounds belongs to a series of the Sacubitril derivatives 5(a–u) were synthesized using (2R,4S)‐5‐([1,1′‐biphenyl]‐4‐yl)‐4‐(amino)‐2‐methylpentanoic acid ethyl ester hydrochloride with different isocyanates and isothiocyanates. All the compounds structures were determined by 1H & 13C NMR spectroscopy, mass spectrometry, and CHN analysis. Compound, 5 r, the structure confirmed by single‐crystal X‐ray diffraction analysis (SXRD). The newly synthesized compounds were screened for their in vitro antituberculosis activity (anti‐TB) against dormant Mycobacterium tuberculosis H37Rv (ATCC27294). Among the twenty‐one compounds, 5 p and 5 q were exhibited good potent anti‐TB activity compared to the standard drug Ethambutol. Further, the anti‐TB activities of the compounds (5 p and 5 q) were evaluated against M. tuberculosis (Mtb) using the nutrient starvation model (NSM). Moreover, these two compounds, 5 p and 5 q have shown significant inhibition of growth of Mtb as compared to the control. To determine the toxicity nature, the potent anti‐TB active compounds were evaluated against RAW 264.7 cells. Further, the anti‐TB activities of all these compounds have shown a good correlation to their in‐silico molecular docking analysis by exhibiting strong interactions with the inhibitor Mur‐B.

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Ultrasonication-ionic liquid synergy for the synthesis of new potent anti-tuberculosis 1,2,4-triazol-1-yl-pyrazole based spirooxindolopyrrolizidines

Pogaku

Krishna

Sriram

et al. 2019

Bioorganic & Medicinal Chemistry Letters

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Identification of lipid metabolism-targeting compounds active against drug-resistant M. tuberculosis

Cited by 6 publications

References 5 publications

Effect of Curcumin in Experimental Pulmonary Tuberculosis: Antimycobacterial Activity in the Lungs and Anti-Inflammatory Effect in the Brain

Effect of Curcumin in Experimental Pulmonary Tuberculosis: Antimycobacterial Activity in the Lungs and Anti-Inflammatory Effect in the Brain

Sacubitril‐Based Urea and Thiourea Derivatives as Novel Inhibitors for Anti‐Tubercular against Dormant Tuberculosis

Ultrasonication-ionic liquid synergy for the synthesis of new potent anti-tuberculosis 1,2,4-triazol-1-yl-pyrazole based spirooxindolopyrrolizidines

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