In vitro effect of ursolic acid on the inhibition of Mycobacterium tuberculosis and its cell wall mycolic acid

Jyoti, Md. Anirban; Zerin, Tamanna; Kim, Tae Hyun; Hwang, Taehyun; Jang, Woong Sik; Nam, Kwanghee; Song, Ho‐Yeon

doi:10.1016/j.pupt.2015.05.005

Cited by 34 publications

(21 citation statements)

References 35 publications

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“…The results of this experiment correspond well with those of a previous study, which reported that ursolic acid reduces mycolic acid levels [15] Resazurin is reduced to resorufin, which is pink when the mycobacteria grow. viability strongly suggests that DFC-2 is highly effective in reducing mycolic acid levels in M. tuberculosis [15].…”

Section: Lc-ms/ms Analysis Of Total Mycolate In Dfc-2-treated M Tubesupporting

confidence: 90%

“…The drug concentrations and time points used were selected after considering previously published studies [14,15]. After drug treatment, RNA samples from three biological replications were extracted with an RNAprotect bacteria reagent kit (Qiagen) as described by the manufacturer's protocol.…”

Section: Rna Isolation Rt-pcr and Microarraymentioning

confidence: 99%

“…M4537) was used. Quantification of mycolic acids was evaluated by LC-MS/MS as previously described [15].…”

Section: Quantification Of Mycolic Acidsmentioning

confidence: 99%

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In Vitro Effect of DFC-2 on Mycolic Acid Biosynthesis in Mycobacterium tuberculosis

Kim

Seo

Mahmud

et al. 2017

Journal of Microbiology and Biotechnology

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DFC-2, a methyl 5-[2-(dimethylamino)ethoxy]-7,12-dioxo-7,12-dihydrodinaphtho[1,2-b:2',3'-d]furan-6-carboxylate, is reported to have antitubercular effects against . At concentrations ranging from 0.19 to 0.39 μg/ml, DFC-2 inhibited both drug-susceptible and -resistant strains of. Microarray analyses were employed to gain insights into the molecular mechanisms of DFC-2's action in . The most affected functional gene category was "lipid biosynthesis," which is involved in mycolic acid synthesis. The decrease in transcription of genes related to mycolic acid synthesis was confirmed by RT-PCR. Furthermore, we found that DFC-2 triggered a reduction in mycolic acid levels, showing a similar pattern to that of mycolic acid synthesis inhibitor isoniazid. These results may explain how this compound kills mycobacteria efficiently by inhibiting mycolic acid synthesis.

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Section: Lc-ms/ms Analysis Of Total Mycolate In Dfc-2-treated M Tubesupporting

confidence: 90%

Section: Rna Isolation Rt-pcr and Microarraymentioning

confidence: 99%

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In Vitro Effect of DFC-2 on Mycolic Acid Biosynthesis in Mycobacterium tuberculosis

Kim

Seo

Mahmud

et al. 2017

Journal of Microbiology and Biotechnology

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“…In previous reports, various types of plant triterpenoids have been reported to exhibit antitubercular activity (Akihisa et al 2005; Jyoti et al 2015). However, few studies have focused on the intracellular inhibitory activity of triterpenoids in M.tb infection.…”

Section: Discussionmentioning

confidence: 98%

Saxifragifolin D attenuates phagosome maturation arrest in Mycobacterium tuberculosis-infected macrophages via an AMPK and VPS34-dependent pathway

Zhou

et al. 2017

AMB Expr

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Saxifragifolin D (SD), a traditional Chinese medicine, is a pentacyclic triterpenoid compound first isolated from Androsace umbellata. Various plant triterpenoids have been reported to exhibit antitubercular activity. In this study, THP-1-derived macrophages were infected with an attenuated M. tuberculosis (M.tb) strain, H37Ra. Intracellular replication of M.tb was evaluated by counting the colonies after 4 weeks of incubation. The results indicated that SD treatment reduced the intracellular replication of M.tb in THP-1-derived macrophages but not in A549 cells. We performed a phagosome maturation test using confocal microscopy and found that SD treatment partially attenuated the phagosome arrest induced by M.tb infection. These effects were dependent on a VPS34-associated pathway. Immunoprecipitation assays showed that SD increased intracellular UVRAG-linked VPS34, the active VPS34 complex II. However, SD had no effect on the total VPS34 pool. Moreover, the results indicated that the SD-mediated increase in VPS34 complex II activity was mediated by an AMPK-dependent pathway. Collectively, these data indicate that SD may be a promising candidate for treatment of M.tb.

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“…The preparation of cells for SEM study was done as described by Jyoti et al [27]. MTB cells in their early log phase were washed by PBS and harvested by centrifugation.…”

Section: Preparation Of Cells For Semmentioning

confidence: 99%

Molecular Docking, Dynamics Simulation, and Scanning Electron Microscopy (SEM) Examination of Clinically Isolated <i>Mycobacterium tuberculosis</i> by Ursolic Acid: A Pentacyclic Triterpenes

et al. 2019

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The purpose of this study was to analyze the inhibitory action of ursolic acid (UA) as an antitubercular agent by computational docking studies and molecular dynamics simulations. The effect of UA on the cell wall of Mycobacterium tuberculosis (MTB) was evaluated by using Scanning Electron Microscopy (SEM). UA was used as a ligand for molecular interaction and investigate its binding activities to a group of proteins involved in the growth of MTB and the biosynthesis of the cell wall. Computational docking analysis was performed by using autodock 4.2.6 based on scoring functions. UA binding was confirmed by 30 ns molecular dynamics simulation using gromacs 5.1.1. H37Rv sensitive strain and isoniazid-resistant strain were used in the SEM study. UA showed to have the optimum binding affinity to inhA (Two-trans-enoyl-ACP reductase enzyme involved in elongation of fatty acid) with the binding energy of -9.2 kcal/mol. The dynamic simulation showed that the UA-inhA complex relatively stable and found to establish hydrogen bond with Thr196 and Ile194. SEM analysis confirms that UA treatment in both sensitive strain and resistant strain affected the morphology cell wall of MTB. This result indicated that UA could be one of the potential ligands for the development of new antituberculosis drugs.

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In vitro effect of ursolic acid on the inhibition of Mycobacterium tuberculosis and its cell wall mycolic acid

Cited by 34 publications

References 35 publications

In Vitro Effect of DFC-2 on Mycolic Acid Biosynthesis in Mycobacterium tuberculosis

In Vitro Effect of DFC-2 on Mycolic Acid Biosynthesis in Mycobacterium tuberculosis

Saxifragifolin D attenuates phagosome maturation arrest in Mycobacterium tuberculosis-infected macrophages via an AMPK and VPS34-dependent pathway

Molecular Docking, Dynamics Simulation, and Scanning Electron Microscopy (SEM) Examination of Clinically Isolated <i>Mycobacterium tuberculosis</i> by Ursolic Acid: A Pentacyclic Triterpenes

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