• Archives of Pharmacal Research
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• v.29 no.1
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• pp.16-25
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• 2006

A novel series of 1-(1-benzofuran-2-yl-ethylidene)-4-substituted thiosemicarbazides (2a-d) along with some derived ring systems: substituted-2,3-dihydro-thiazoles(3a-c, 4a-f) and thiazolidin-4-ones(5a-d and 6a-d), were synthesized. In addition, cyanoacetic acid-(1-benzofuran-2-yl-ethylidene) hydrazide(7) was used to prepare another new series of compounds consisting of substituted pyridin-2(1H)-ones(8a-c); 2-thioxo-2,3-dihydro-thiazoles(9a-d) and 2-thioxo-2,3-dihydro-6H-thiazolo[4,5-d]pyrimidin-7-ones (10a-c, 11a-c). The absolute configuration of compound 5c was determined by X-ray crystallography. The compounds prepared were evaluated for their in vitro anti-HIV, anticancer, antibacterial, and antifungal activities. Among the tested compounds, compounds 5c and 9a produced a significant reduction ㅐ ㄹ the viral cytopathic effect (93.19% and 59.55%) at concentrations $>2.0{\times}10^{-4}\;M\;and\;2.5{\times}10^{-5}\;M$respectively. Compound 9a was confirmed to have moderate anti-HIV activity. Compounds 2a, 2d, and 5c showed mild antifungal activity. However, none of the tested compounds showed any significant anticancer activity.

• Journal of Physiology & Pathology in Korean Medicine
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• v.20 no.4
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• pp.909-913
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• 2006

The antioxidative activity was observed in the ethyl acetate extract $(IC_{50},\;119{\pm}0.16\;{\mu}g/mL)$ from Pueraria thunbergiana. The DPPH radical scavenging effect of this extract was comparable with that of synthetic antioxdant, BHA $(IC_{50},\;88.39{\pm}1.1\;{\mu}g/mL){\times}\;10^{-3}\;{\mu}M$. Pueraria thunbergiana extracts against microorganisms were evaluated in terms of the minimum inhibitory concentrations (MIC). In general, C. albicans was stronger antimicrobial activity than the other microorganisms. in vitro the antitoxic activity of extracts of Pueraria thunbergiana on NIH 373 fibroblasts was evaluated by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide) method. Generally, detoxification effect by the extracts of Pueraria thunbergiana increased in proportion to the concentrations. When $10\;{\mu}g/mL$ of the hexane extract of Pueraria thunbergiana was treated it showed the highest antitoxic effects (p<0.01). These results suggest that the crude extract of P. thunbergiana has a potential therapeutic activity.

• Journal of Microbiology and Biotechnology
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• v.29 no.6
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• pp.962-972
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• 2019

Non-typhoidal Salmonella (NTS) is one of the most frequent causes of bacterial foodborne illnesses. Considering that the main reservoir of NTS is the intestinal tract of livestock, foods of animal origin are regarded as the main vehicles of Salmonella infection. In particular, poultry colonized with Salmonella Typhimurium (S. Typhimurium), a dominant serotype responsible for human infections, do not exhibit overt signs and symptoms, thereby posing a potential health risk to humans. In this study, comparative genomics approaches were applied to two S. Typhimurium strains, ST1539 and ST1120, isolated from a duck slaughterhouse and a pig farm, respectively, to characterize their virulence and antimicrobial resistance-associated genomic determinants. ST1539 containing a chromosome (4,905,039 bp; 4,403 CDSs) and a plasmid (93,876 bp; 96 CDSs) was phylogenetically distinct from other S. Typhimurium strains such as ST1120 and LT2. Compared to the ST1120 genome (previously deposited in GenBank; CP021909.1 and CP021910.1), ST1539 possesses more virulence determinants, including ST64B prophage, plasmid spv operon encoding virulence factors, genes encoding SseJ effector, Rck invasin, and biofilm-forming factors (bcf operon and pefAB). In accordance with the in silico prediction, ST1539 exhibited higher cytotoxicity against epithelial cells, better survival inside macrophage cells, and faster mice-killing activity than ST1120. However, ST1539 showed less resistance against antibiotics than ST1120, which may be attributed to the multiple resistanceassociated genes in the ST1120 chromosome. The accumulation of comparative genomics data on S. Typhimurium isolates from livestock would enrich our understanding of strategies Salmonella employs to adapt to diverse host animals.

• Mycobiology
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• v.47 no.1
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• pp.87-96
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• 2019

Fungi produce various secondary metabolites that have beneficial and harmful effects on other organisms. Those bioactive metabolites have been explored as potential medicinal and antimicrobial resources. However, the activities of the culture filtrate (CF) and metabolites of whiterot fungus (Schizophyllum commune) have been underexplored. In this study, we assayed the antimicrobial activities of CF obtained from white-rot fungus against various plant pathogens and evaluated its efficacy for controlling anthracnose and gray mold in pepper plants. The CF inhibited the mycelial growth of various fungal plant pathogens, but not of bacterial pathogens. Diluted concentrations of CF significantly suppressed the severity of anthracnose and gray mold in pepper fruits. Furthermore, the incidence of anthracnose in field conditions was reduced by treatment with a 12.5% dilution of CF. The active compound responsible for the antifungal and disease control activity was identified and verified as schizostatin. Our results indicate that the CF of white-rot fungus can be used as an eco-friendly natural product against fungal plant pathogens. Moreover, the compound, schizostatin could be used as a biochemical resource or precursor for development as a pesticide. To the best of our knowledge, this is the first report on the control of plant diseases using CF and active compound from white-rot fungus. We discussed the controversial antagonistic activity of schizostatin and believe that the CF of white-rot fungus or its active compound, schizostatin, could be used as a biochemical pesticide against fungal diseases such as anthracnose and gray mold in many vegetables.

• Journal of Microbiology and Biotechnology
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• v.32 no.8
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• pp.989-1002
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• 2022

Cephalopods, in particular octopus (Octopus vulgaris), have the ability to alter their appearance or body pattern by showing a wide range of camouflage by virtue of their chromatophores, which contain nanostructured granules of ommochrome pigments. Recently, the antioxidant and antimicrobial activities of ommochromes have become of great interest; therefore, in this study, the pH-dependent redox effect of the extraction solvent on the antioxidant potential and the structural characterization of the pigments were evaluated. Cell viability was determined by the microdilution method in broth by turbidity, MTT, resazurin, as well as fluorescence microscopy kit assays. A Live/Dead Double Staining Kit and an ROS Kit were used to elucidate the possible inhibitory mechanisms of ommochromes against bacterial and fungal strains. The results obtained revealed that the redox state alters the color changes of the ommochromes and is dependent on the pH in the extraction solvent. Natural phenoxazinone (ommochromes) is moderately toxic to the pathogens Staphylococcus aureus, Bacillus subtilis, Salmonella Typhimurium and Candida albicans, while the species Pseudomonas aeruginosa and Pseudomonas fluorescens, and the filamentous fungi Aspergillus parasiticus, Alternaria spp. and Fusarium verticillioides, were tolerant to these pigments. UV/visible spectral scanning and Fourier- transform infrared spectroscopy (FTIR) suggest the presence of reduced ommatin in methanol/ HCl extract with high intrinsic fluorescence.

• Korean Journal of Pharmacognosy
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• v.53 no.2
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• pp.87-95
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• 2022

Methicillin resistance Staphylococcus aureus (MRSA) is a gram-positive bacterium, the most commonly isolated bacterial human pathogen. JiYu-san is one of the natural products used to treat diseases in the folk recipe. In this study, we investigated the antimicrobial activity of EtOH 70% extracts of JiYu-san (JYS) against MRSA. The antibacterial activity of JYS against MRSA strain was evaluated using minimum inhibitory concentration (MIC), checkerboard dilution test, and time-kill assay. The effect of JYS on the immune mechanism of MRSA was confirmed through cell membrane permeability tests and energy metabolism tests, and the antibacterial activity mechanism was performed using qRT-PCR and western blot. As a result, in the antibacterial test of JYS, the MIC was measured to be 1.9~1000 ㎍/mL, and synergistic or showed a partial synergistic effect. In addition, JYS showed antibacterial activity in a combination test with DCCD or TX-100. In a study on the mechanism of action of antibacterial activity, it was found that JYS suppressed MRSA resistance genes and proteins. These results suggest that JYS has antibacterial activity and provides great potential as a natural antibiotic by modulating the immune mechanism against MRSA.

• Animal Bioscience
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• v.36 no.7
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• pp.1034-1043
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• 2023

Objective: Two serine protease inhibitors, peptidase inhibitor 3 (PI3) and secretory leukocyte protease inhibitor (SLPI), play important roles in protease inhibition and antimicrobial activity, but their expression, regulation, and function at the maternal-fetal interface in pigs are not fully understood. Therefore, we determined the expression and regulation of PI3 and SLPI in the endometrium throughout the estrous cycle and at the maternal-fetal interface in pigs. Methods: Endometrial tissues during the estrous cycle and pregnancy, conceptus tissues during early pregnancy, and chorioallantoic tissues during mid to late pregnancy were obtained, and the expression of PI3 and SLPI was analyzed. The effects of the steroid hormones estradiol-17β (E2) and progesterone (P4) on the expression of PI3 and SLPI were determined in endometrial explant cultures. Results: PI3 and SLPI were expressed in the endometrium during the estrous cycle and pregnancy, with higher levels during mid to late pregnancy than during the estrous cycle and early pregnancy. Early-stage conceptuses and chorioallantoic tissues during mid to late pregnancy also expressed PI3 and SLPI. PI3 protein and SLPI mRNA were primarily localized to endometrial epithelia. In endometrial explant cultures, the expression of PI3 was induced by increasing doses of P4, and the expression of SLPI was induced by increasing doses of E2 and P4. Conclusion: These results suggest that the PI3 and SLPI expressed in the endometrium and conceptus tissues play an important role in antimicrobial activity for fetal protection against potential pathogens and in blocking protease actions to allow epitheliochorial placenta formation.

• Journal of The Korean Society of Integrative Medicine
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• v.11 no.2
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• pp.149-157
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• 2023

Purpose : In this study, to prove the antibacterial effect of Disocorea batatas, which is widely used for food, and to confirm the growth inhibitory effect, the antibacterial activity against L. gasseri, S. mutans, and P. gingivalis was verified. Based on this, it is intended to verify the utility as a preventive and therapeutic composition for dental caries and periodontal disease. Methods : RAW 264.7 cells were used to verify the cell survival rate and NO (Nitric Oxide) inhibitory effect on Disocorea batatas ethanol extract (DBEE). In order to verify the antibacterial effect against L. gasseri, S. mutans, and P. gingivalis, concentrations of 125, 250, and 500 ㎎/㎖ of DBEE were used and measured by the disk diffusion method. In order to confirm the growth inhibitory effect, the absorbance was measured at 600 ㎚ at 3, 6, 12, 18, and 24 hours using the liquid medium dilution method, and the growth inhibitory effect was measured compared to the control group. Results : The cell viability for DBEE was 91 % at 50 ㎎/㎖, and there was no cytotoxicity. The NO production inhibitory effect was shown from 10 ㎍/ml, and the higher the concentration, the greater the inhibitory effect. As for the antimicrobial effect using the disk diffusion method, the higher the concentration, the higher the antibacterial effect. At 125 ㎎/㎖ and 250 ㎎/㎖, S. mutans and L. gasseri showed high antimicrobial activity, and at 500 ㎎/㎖, the antibacterial effect was higher in L. gasseri. The growth inhibitory effect in DBEE was concentration-dependent as the higher the concentration, the higher the growth inhibitory effect, and all of them began to show growth inhibitory effects from 6 hours. Conclusion : Considering that it is widely used as an edible and medicinal material, Disocorea batatas has shown the potential to be used as a substance to prevent and alleviate dental caries and periodontal diseases, and it is believed that further research can be applied to oral health care products.

• Journal of Veterinary Science
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• v.23 no.1
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• pp.6.1-6.8
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• 2022

Background: With limited information available, the association among urinary tract infections, urease-producing bacteria and the presence of magnesium ammonium phosphate (MAP) urolithiasis in canines in Thailand requires more study. Objectives: This study aimed to investigate the association between demographic characteristics of canines and the presence of MAP urolithiasis in canines, and to evaluate antimicrobial susceptibility patterns of bacteria isolated from canine uroliths. Methods: A total of 56 canines admitted for treatment with surgical removal of uroliths were recruited. Demographic characteristics and clinical chemistry data were recorded. Bacteria isolated from the removed uroliths were identified. Chemical compositions of the uroliths were analyzed by Fourier transform infrared spectrometer. Potential risk factors were determined with univariable and multivariable logistic regression analyses. Results: Of 56 canine urolithiasis, bacteria were isolated from uroliths of 38 canines (27 MAP and 11 non-MAP) but not from uroliths of 18 canines (5 MAP and 13 non-MAP). The most common bacteria found in nidus of MAP uroliths was Staphylococcus pseudintermedius (approximately 51%). An antimicrobial resistance was frequently found in Staphylococci isolates (42.86%). Multivariate logistic regression analysis showed that the predictors of MAP urolith in canine urolithiasis were being female (p = 0.044; adjusted odds ratio [OR], 10.22; 95% confidence interval [CI], 1.06-98.24) and the positive urolith culture (p = 0.012; adjusted OR, 8.60; 95% CI, 1.60-46.30). Conclusions: Our results indicate that S. pseudintermedius (a urease-producing bacterium) is the major causative bacteria of MAP uroliths. A positive urolith culture and being female are risk factors of MAP urolithiasis in canines.

• Microbiology and Biotechnology Letters
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• v.51 no.4
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• pp.474-483
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• 2023

Members of the genus Streptomyces produce more than 70% of antibiotics. The rise in antibiotic resistance globally enhanced the search for novel species with the ability to produce new bioactive compounds. This study was initiated to investigate different regions in Jordan for previously uncultured and rare Streptomyces species capable of producing novel antimicrobial compounds especially active against bacteria resistant to antibiotics. A total of 191 Streptomyces strains were isolated from 26 soil samples collected from different geographic regions in Jordan. Isolates were characterized based on colony and cellular morphology as well as using 16S rRNA gene sequencing. These isolates were screened for their ability to produce antibiotics by the perpendicular-cross streak method, and then tested by well diffusion method against tested pathogens. Fifty-four isolates showed potential to produce antimicrobial products especially active against resistant bacteria, 20.1% of the isolates showed inhibitory effect against Staphylococcus aureus, 16.9% against clinical MSSA strains, and 18.0% against MRSA: whereas only 4.2% against Esherichia coli, 3.2% against Klebsiella pneumonia, 2.7% against Pseudomonas aeruginosa, and 10.0% against clinical Candida albicans. Three isolates were selected for further identification due to their antibacterial activity against S. aureus, MRSA, and MSSA. These isolates were identified as follows; Streptomyces aburaviensis DSa3, Streptomyces alboniger SAb7 and Streptomyces misionensis ZAb2, based on cultural, biochemical characteristics and molecular analysis of the 16S rRNA.