• Archives of Pharmacal Research
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• v.27 no.7
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• pp.713-719
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• 2004

Several analogues of the general formulae 2-methoxy-9-substituted acridine and 6-chloro-2-methoxy-9-substituted acridine were synthesized and evaluated in vitro at 6.25 $\mu\textrm{g}$/mL against M. tuberculosis $H_{37}Rv$. Compounds 15 and 17 showed potential antitubercular activity with 100％ inhibition to the virulent mycobacterium.

• Korean Journal of Microbiology
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• v.46 no.2
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• pp.134-139
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• 2010

Mycobacterium tuberculosis (Mtb) is one of the most successful pathogens to infect one third of world population. Th1-mediated immunity against Mtb infection is known as critical to express mycobacteriostatic function but it is not sufficient to resolve the infection. In this study, to verify the possibility Mtb itself change the gene expression to survive against host immune response, expression pattern of selected H37Rv genes, 16S rRNA, acr, fbpA, aceA, and ahpC, during the course of infection was measured with absolute quantitation method using real-time RT-PCR. The total number of transcripts of 16S rRNA increased during the course of infection, which was coincide with the increasing CFU. The total number of fbpA transcripts per CFU, which encode typical secreted Mtb antigen, Ag85A, increased for 10 days of infection before decreasing. The number of transcripts of acr per CFU, which encode heat shock protein, ${\alpha}$-crystallin, increased during the infection, and ahpC and aceA, they both are enzymes produced in oxidative stressful condition, increased for 20 days and then slightly decreased on day 30. These findings are one of survival strategy of pathogen evading host immune response lead to persistent infection inside host cells.

• Biomedical Science Letters
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• v.15 no.4
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• pp.295-300
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• 2009

Tuberculosis caused by Mycobacterium tuberculosis (MTB) still remains to be the most dreadful infectious disease affecting almost every country. In the present study, we developed a simple and rapid but accurate and sensitive assay method for detecting MTB using microplate hybridization assay. For this, a selective region of the rpoB gene was used to design PCR primers, and MTB and Mycobacterium genus-specific probe molecules. The specificity of the assay was confirmed using fifteen different mycobacterial reference strains and twelve different non-mycobacterial reference strains, and the sensitivity was determined to be 100 fg using genomic DNA of MTB reference strain, H37Rv. Subsequently, a total of 62 sputum samples with diverse smear scores and culture positive results were used to evaluate the kit performance. In brief, the specificity and the sensitivity of the assay were 100% and 98.4%, respectively.

• Journal of Microbiology and Biotechnology
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• v.29 no.9
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• pp.1401-1411
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• 2019

Mycobacterial cell walls comprise thick and diverse lipids and glycolipids that act as a permeability barrier to antibiotics or other chemical agents. The use of OH radicals from a non-thermal plasma jet (NTPJ) for the inactivation of mycobacteria in aqueous solution was adopted as a novel approach. Addition of water vapor in a nitrogen plasma jet generated OH radicals, which converted to hydrogen peroxide ($H_2O_2$) that inactivated non-pathogenic Mycobacterium smegmatis and pathogenic Mycobacterium tuberculosis H37Rv. A stable plasma plume was obtained from a nitrogen plasma jet with 1.91 W of power, killing Escherichia coli and mycobacteria effectively, whereas addition of catalase decreased the effects of the former. Mycobacteria were more resistant than E. coli to NTPJ treatment. Plasma treatment enhanced intracellular ROS production and upregulation of genes related to ROS stress responses (thiolrelated oxidoreductases, such as SseA and DoxX, and ferric uptake regulator furA). Morphological changes of M. smegmatis and M. tuberculosis H37Rv were observed after 5 min treatment with $N_2+H_2O$ plasma, but not of pre-incubated sample with catalase. This finding indicates that the bactericidal efficacy of NTPJ is related to the toxicity of OH and $H_2O_2$ radicals in cells. Therefore, our study suggests that NTPJ treatment may effectively control pulmonary infections caused by M. tuberculosis and nontuberculous mycobacteria (NTM) such as M. avium or M. abscessus in water.

• Tuberculosis and Respiratory Diseases
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• v.43 no.6
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• pp.842-851
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• 1996

Background : Rifampicin(RFP) is a key component of the antituberculous shon-course chemotherapy and the RFP-resistance is a marker of multi-drug resistant(MDR) M. tuberculosis. rpoB gene encodes the ${\beta}$-subunit of RNA polymerase of M. tuberculosis which is the target of RFP. Recent reports show that rpoB gene mutations are the cause of RFP resistance of M. tuberculosis and the main mechanism of rpoB gene mutation is point mutation. And PCR-SSCP is a rapid and easy method for detecting point mutations. So we performed PCR-SSCP of rpoB gene of M. tuberculosis and compared the result with traditional RFP sensitivity test. Method : The 27 RFP sensitive M. tuberculosis culture isolates and 25 RFP resistant isolates were evaluated. The RFP sensitivity test was done at the Korean Tuberculosis istitute. The DNA was extracted by bead beater method and was amplified with primers TR-8 and TR-9 in a 20ul PCR reaction containing 0.1ul(luCi) [${\alpha}-^{32}P$] - dCTP. After amplification, SSCP was done using non-denaturaring polyacrylamide gel electrophoresis. Then direct sequencing was done in cases of different eletrophoretic mobility compared with that of H37Rv. In 19 cases, we compared PCR-SSCP results with patient's clinical course and the results of traditional RFP sensitivity test. Results : 1) All 27 RFP sensitive M. tuberculosis isolates showed the same electrophoretic mobility compared with that of H37Rv. And all 25 RFP resistant M. tuberculosis isolates showed different electrophoretic mobility. 2) The mechanism of rpoB gene mutation of M. tuberculosis is mainly point mutation. 3) The PCR-SSCP results correlate well with traditional RFP sensitivity and patient's clinical response to antituberculous treatment. Conclusion: The PCR-SSCP of rpoB gene is a very sensitive and rapid mehod in detecting RFP- resistant M. tuberculosis.

• YAKHAK HOEJI
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• v.17 no.4
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• pp.223-234
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• 1973

Sixteen compounds of N-aroyl-N'-(4'-alkoxyphenyl) thiourea derivative, twenty one compounds of N-aeryl-N'(3'-hydroxy-4'-alkoxycar-bonylphenyl) thiourea derivative, three compounds of N-aeroyl-N'-.alpha.-naphthyiourea derivative and three compounds of N-cyanoacetyl-N'-aroyl thiosemicarbazide derivative were syntrhesized as potential antitubercular agent and were subjected to screening test for antitubercular activity against Mycobacterium turberculosis H/sub 37/Rv by tube dilution method in vitro. Of the fourty three eompounds, N-p-cyanobenzoyl-N'-(4'-iso-butoxyphenyl) thiourea, N-p-cyanobenzoyl-N'-(4-n-amoxyphenyl)thiourea, N-furoyl-N'-(3'-hydroxy-4'-ethoxycarbonylphenyl)thiourea, N-p-cyanobenzoyl-N'-(3'-hydroxy-4'-n-butoxycarbonylphenyl)thiourea, N-p-cyanobenzoyl-N'-(3'-hydroxy-4'-n-amoxycarbonylphenyl)thiourea, and N-5-nitrofuroyl-N'(3'-hydroxy-4"-n-amoxycarbonylphrnyl)thiourea showed the growth inhibition of M. tuberculosis H/sub 37/Rv at the coccentraction og 10.mu.g/ml, respectively.

• Korean Journal of Microbiology
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• v.54 no.3
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• pp.222-227
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• 2018

Mycobacterium tuberculosis (MTB)-originated lipid antigen is presented on the antigen-presenting cell surface with CD1b. When monocyte-derived dendritic cells phagocytosed MTB H37Rv (Multiplicity of infection 10, infectivity: 46.89%), the CD1b expression level decreased slowly. Since this was just a live MTB-mediated phenomenon, it was not detected from heat-killed MTB or mycolic acid, which is a unique antigen of MTB. We confirmed that the phosphorylation of CD1b molecules using 2D electrophoresis with staining could phosphorylate and induce the presentation of the lipid antigen using the phagocytosis assay.

• Journal of the Korean Chemical Society
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• v.66 no.3
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• pp.194-201
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• 2022

A simple, efficient, and cost-effective method has been employed for the synthesis of 2,4,5-trisubstituted imidazole derivatives (3a-j) containing quinoline substituent at 2^nd position. Title compounds were obtained by multicomponent reaction (MCR), involving aryl substituted 1,2-diketone, quinoline carbaldehyde and ammonium acetate in the presence of acetic acid solvent under mild reaction conditions. The newly synthesized quinoline containing imidazole derivatives were confirmed through FT-IR, ¹H-NMR, ¹³C-NMR and mass spectral analysis. In-vitro microplate alamar blue assay (MABA) to determine the MIC (minimum inhibitory concentration) values against Mycobacterium tuberculosis H37Rv was performed for the synthesized compounds. The synthesized compounds exhibited activity against Mycobacterium tuberculosis and among which compounds, 3d, 3f and 3i showed good activity. The highest activity was showed with compound 3i. The anti-mycobacterial activity results are well correlated with the computational molecular docking analysis, which was performed for the synthesized compounds prior to the evaluation of the activity.

• The Journal of the Korean Society for Microbiology
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• v.35 no.5_6
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• pp.375-375
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• 2000

• YAKHAK HOEJI
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• v.15 no.3_4
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• pp.93-97
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• 1971

Seventeen novel compounds of thiosemicarbazone derivatives were synthesized and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H$_{37}$Rv and antibacterial activity against Staphylococcus aureus, Escherichia coli. It was found that 4-($\alpha$-naphthyl)-1-(2-furfuraldehyde)-3-thiosemicarbazone was active at 0.01$\mu$g/ml and 1, 1'-(p-phenylene)-4, 4'-bis(phenyl)-2, 2'-dithiosemicarbazide, at 0.01$\mu$g/ml against E. coli, respectively.