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

• Journal of Microbiology and Biotechnology
• /
• v.31 no.12
• /
• pp.1632-1642
• /
• 2021

Tuberculosis is a highly contagious disease caused by Mycobacterium tuberculosis. It affects about 10 million people each year and is still one of the leading causes of death worldwide. About 2 to 3 billion people (equivalent to 1 in 3 people in the world) are infected with latent tuberculosis. Moreover, as the number of multidrug-resistant, extensively drug-resistant, and totally drug-resistant strains of M. tuberculosis continues to increase, there is an urgent need to develop new anti-tuberculosis drugs that are different from existing drugs to combat antibiotic-resistant M. tuberculosis. Against this background, we aimed to develop new anti-tuberculosis drugs using probiotics. Here, we report the anti-tuberculosis effect of Pediococcus acidilactici PMC202 isolated from young radish kimchi, a traditional Korean fermented food. Under coculture conditions, PMC202 inhibited the growth of M. tuberculosis. In addition, PMC202 inhibited the growth of drug-sensitive and -resistant M. tuberculosis- infected macrophages at a concentration that did not show cytotoxicity and showed a synergistic effect with isoniazid. In a 2-week, repeated oral administration toxicity study using mice, PMC202 did not cause weight change or specific clinical symptoms. Furthermore, the results of 16S rRNA-based metagenomics analysis confirmed that dysbiosis was not induced in bronchoalveolar lavage fluid after oral administration of PMC202. The anti-tuberculosis effect of PMC202 was found to be related to the reduction of nitric oxide. Our findings indicate that PMC202 could be used as an anti-tuberculosis drug candidate with the potential to replace current chemical-based drugs. However, more extensive toxicity, mechanism of action, and animal efficacy studies with clinical trials are needed.

• The Journal of Internal Korean Medicine
• /
• v.21 no.4
• /
• pp.555-563
• /
• 2000

Objective : In order to know the antibacterial effects of Kyungok-go against Mycobacteria tuberculosis, Methods : In this study, I inverstigated these effects in terms of combination of other antibiotics with and without Kyungok-go on several different media conditions. Results: On Ogawa medium, Kyungok-go of the $10{\mu}/ml$ concentration showed the anti-Mycobacteria tuberculosis activity against antibiotic drug-sensitive strain. On Middle-blue medium, Kyungok-go of the $10{\mu}/ml$ concentration showed the anti-Mycobacteria tuberculosis activity against antibiotic drug-sensitive strain. Kyungok-go showed the anti mycobacteria tuberculosis activity with the meaningful result above a certain concentration. The resistance against M, tuberculosis as the concentration of Kyungok-go was decreased significantlly on the high concentration($500{\mu}/ml$) When rifampicin and Kyungok-go were used together, the resistance was decreased with the statistical significance as to the persistant antibacterial effect against M. tuberculosis, When ciprofloxacin and Kyungok-go were used together, the resistance was decreased with the statistical significance as to the persistant antibacterial effect against M. tuberculosis, The combination of treatment, Kyungok-go with both rifampicin and ciprofloxacin, showed much better antibacterial effect against M, tuberculosis than antibiotics alone. Conclusions : This study shows that Kyungok-go has antibacterial effect against M. tuberculosis and in the combination of treatment, Kyungok-go with antibiotics, showed much better antibacterial effect against M. tuberculosis than antibiotics alone,.

• Journal of Mushroom
• /
• v.9 no.4
• /
• pp.190-193
• /
• 2011

Inonotus obliquus is a traditional medicine mushroom that was developed from traditional medicine originating in ancient. It has been applied for cancer or immunotherapy, but its effect on pulmonary tuberculosis is not reported. Therefore, we measured the pulmonary tuberculosis therapeutic effect of methyl alcohol extract from MGIT 960 system with fluorescent indicator. Inonotus obliquus extract showed 14 day more inhibitory activity than the positive control. In addition, the anti-pulmonary tuberculosis activity of Inonotus obliquus was $50{\mu}m$. These results suggest that Inonotus obliquus methyl alcohol extracts could contribute to inhibition of pulmonary tuberculosis.

• Journal of Microbiology and Biotechnology
• /
• v.25 no.6
• /
• pp.946-950
• /
• 2015

Recently, it has become a struggle to treat tuberculosis with the current commercial antituberculosis drugs because of the increasing emergence of multidrug-resistant (MDR) tuberculosis and extensively drug-resistant (XDR) tuberculosis. We evaluated here the antimycobacterial activity of tamoxifen, known as a synthetic anti-estrogen, against eight drugsensitive or resistant strains of Mycobacterium tuberculosis (TB), and the active intracellular killing of tamoxifen on TB in macrophages. The results showed that tamoxifen had antituberculosis activity against drug-sensitive strains (MIC, 3.125-6.25 µg/ml) as well as drugresistant strains (MIC, 6.25 to 12.5 µg/ml). In addition, tamoxifen profoundly decreased the number of intracellular TB in macrophages in a dose-dependent manner.

• Bulletin of the Korean Chemical Society
• /
• v.32 no.11
• /
• pp.3996-4000
• /
• 2011

In an attempt to find a new class of anti microbial agents, a series of thiazolidinone and their 5-arylidene derivatives containing 4-(4-methyl benzamido)-benzoyl moiety were synthesized via the reaction of benzocaine with appropriate chemical reagents. These compounds were screened for their antibacterial activity against Gram-positive bacteria (Bacillus subtilis and Bacillus thuringiensis), Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and antifungal activity against Botrytis fabae, Fusarium oxysporan and Candida albicans. On the other hand the synthesized compounds were also screened for their anti tubercular activity. IR, $^1H$ NMR, $^{13}C$ NMR and MS spectral analyses established the structures of the newly synthesized compounds. The results revealed that some of these compounds have shown promising antimicrobial and anti tubercular activity in comparison with standard drugs.

• Journal of Microbiology and Biotechnology
• /
• v.29 no.8
• /
• pp.1221-1229
• /
• 2019

Mycobacterium tuberculosis, a causative pathogen of tuberculosis (TB), still threatens human health worldwide. To find a novel drug to eradicate this pathogen, we tested taurine-5-bromosalicylaldehyde Schiff base (TBSSB) as an innovative anti-mycobacterial drug using Mycobacterium smegmatis as a surrogate model for M. tuberculosis. We investigated the antimicrobial activity of TBSSB against M. smegmatis by plotting growth curves, examined the effect of TBSSB on biofilm formation, observed morphological changes by scanning electron microscopy and transmission electron microscopy, and detected differentially expressed proteins using two-dimensional gel electrophoresis coupled with mass spectrometry. TBSSB inhibited mycobacterial growth and biofilm formation, altered cell ultrastructure and intracellular content, and inhibited cell division. Furthermore, M. smegmatis adapted itself to TBSSB inhibition by regulating the metabolic pathways and enzymatic activities of the identified proteins. NDMA-dependent methanol dehydrogenase, NAD(P)H nitroreductase, and amidohydrolase AmiB1 appear to be pivotal factors to regulate the M. smegmatis survival under TBSSB. Our dataset reinforced the idea that Schiff base-taurine compounds have the potential to be developed as novel anti-mycobacterial drugs.

• Korean Journal of Clinical Laboratory Science
• /
• v.54 no.2
• /
• pp.125-132
• /
• 2022

The prevalence of multidrug-resistant TB (MDR-TB) and extensively drug-resistant TB (XDR-TB) are increasing. We analyzed the patterns of drug resistance and tracking period days of acquiring anti-mycobacterial resistance. From January 2010 to December 2019, drug susceptibility tests (DST) were performed by the absolute concentration method using the Löwenstein-Jensen solid medium and pyrazinamidase activity test (to assess pyrazinamide resistance) in samples from patients who were referred to the Green Cross Laboratories in Yongin. Among the cases that showed resistance to one or more anti-tuberculosis drugs, 55 patients (33.1%) were resistant to isoniazid (INH) at the time of initial referral, and the rates for the development of resistant anti-tuberculosis drugs were ethambutol (EMB) (26.6%), rifampicin (RFP) (21.9%), quinolones (QUI) (21.9%) and pyrazinamide (PZA) (10.9%), in that order. In the cases sensitive to all 10 anti-tuberculosis drugs initially, the development of resistance to INH was the most frequent, seen in 43 patients (7.2%). The average follow-up period was 435.6 days, and the resistance development was observed in the order of INH (7.2%), RFP (3.9%), SM (1.9%), QUI (0.7%), amikacin (AMK) (0.5%), and EMB (0.5%). The conversion of susceptible strains to resistant strains is an important warning sign for the patient, especially in cases of conversion to MDR or XDR. This information would be helpful for improving patient care during TB treatment.

• Tuberculosis and Respiratory Diseases
• /
• v.65 no.6
• /
• pp.522-526
• /
• 2008

A 63-year old woman was admitted to our hospital for an evaluation of thrombocytopenia. She had been diagnosed with tuberculous pericarditis three months earlier in a local clinic and treated with anti-tuberculosis medication. Two months later, thrombocytopenia developed. The medication was subsequently stopped because it was suspected that the anti-tuberculosis medication, particularly rifampin, might have caused the severe platelet reduction. However, the thrombocytopenia was more aggravated. A bone marrow biopsy was performed, which showed moderate amounts of histiocytes with active hemophagocytosis. This finding strongly suggested that the critical thrombocytopenia had been caused by hemophagocytic syndrome, not by the side effects of the anti-tuberculosis medication. Furthermore, the development of hemophagocytosis might have been due to an uncontrolled tuberculosis infection and its associated aberrant immunity. Therefore, she was started with both standard anti-tuberculosis medication and chemotherapy using etoposide plus steroid. One month after the initiation of treatment, the thrombocytopenia had gradually improved and she was discharged in a tolerable condition. At the third month of the follow-up, her platelet level and ferritin, the activity marker of hemophagocytic syndrome, was within the normal range.

• Korean Journal of Food Science and Technology
• /
• v.46 no.1
• /
• pp.94-99
• /
• 2014

The present study aimed to evaluate the in vitro antimycobacterial effects of hop plant, Humulus japonicus. Methanol extract of H. japonicus (MeOH extract) showed strong direct bactericidal effects against Mycobacterium tuberculosis in vitro. Furthermore, the MeOH extract significantly inhibited M. tuberculosis growth in human macrophages. When five fractions obtained from MeOH extract were examined using the same methods, the hexane and ethyl acetate fractions showed bactericidal effects against M. tuberculosis in vitro, whereas the butanol and water fractions inhibited M. tuberculosis growth in macrophages. Because H. japonicus extract exhibited antimycobacterial activity against both free M. tuberculosis in culture medium and intracellular M. tuberculosis in human macrophages, this plant might be a good candidate for development of a new anti-tuberculosis drug.