• YAKHAK HOEJI
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• v.20 no.1
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• pp.19-26
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• 1976

Sixteen compounds of 2-aminobenzothiazole derivatives were synthesized from alkyl ($C_{1-5}$) p-aminosalicylate by thiocyanation reaction. The NMR spectra of synthesized compounds showed that they were actually mixture of 5-hydroxy-6-alk-oxycarbonyl-2-aminobenzothiazole [alkoxy=methoxy(Ia), ethoxy (IIa), n-propoxy (IIIa), iso-propoxy (IVa), n-butoxy (Va), iso-butoxy (VIa), n-amoxy (VIIa), iso-amoxy(VIIIa)] and 7-(1b), ethoxy(IIb), n-propoxy(IIIb), iso-propoxy(IVb), n-butoxy(Vb), iso-butpxy (VIb), n-amoxy (VIIb), iso-amoxy (VIIIb)]. The mixtures of two isomeric benzothiazole were separated by two isomers varied with the kind of alkyl chain in alkyl p-aminosalicylate. These compounds were subjected to the test for antimicrobial activities using Staphylococcus aureus and Escherichia coli by tube dilutioin method. The seven compounds, Ia, IIa, IIIa, VIa, IIIb, IVb and Vb showed inhibition of the growth of S. aureus at the concentration of 10${\mu}$g/ml. As to the growth of E. coli, IVb, VIb, VIIb, and VIIIb were observed inhibition at the concentration of 1${\mu}$g/ml. Ia, IIa, IIIa, VIIa, Va, VIIIa, and IIb exhibited potential antimicrobial activities against showed inhibition of the growth of E.coli at the concentration of 100${\mu}$/ml.

• Journal of Pharmaceutical Investigation
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• v.19 no.3
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• pp.145-154
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• 1989

Methyl methacrylate-butyl methacrylate copolymer (MMBM)-povidone (PVP) films were investigated as a potential topical drug delivery system for the controlled release of econazole nitrate as a model drug. The effect of changes in film composition, drug concentration, film thickness, pH and temperature of release medium on the in vitro release of econazole nitrate were studied. The release rate constant was found to be increased with increasing povidone content in dry films. Drug release followed zero-order kinetics in the initial stage and then release rate increased gradually with time, espicially in the films having larger proportions of PVP. The release rate was found to be dependent on drug content, film thickness, the pH and temperature of release medium. Antimicrobial test showed that microbial growth was inhibited markedly with increasing proportions of PVP in films. Also drug content and film thickness affected the antimicrobial activity.

• Food Engineering Progress
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• v.21 no.1
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• pp.36-41
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• 2017

The release profiles of nisin from nisin-incorporating gel foods and the antimicrobial activities of the gels on the growth of Brochothrix thermosphacta in an aqueous system containing the gels have been investigated. A linear regression model was applied to determine the diffusion coefficient (D) for the diffusion of nisin in the gel. The antimicrobial activities of nisin released from 1, 2 and 3% (w/v) agar gels on the growth of B. thermosphacta in a broth medium with and without nisin were investigated. The D decreased from $1.2{\times}10^{-2}$ to $8.2{\times}10^{-3}$ and $6.4{\times}10^{-3}cm^2/s$ as the agar concentration in the gel increased from 1 to 2 and 3% (w/v), demonstrating the diffusion rate in the gels can be controlled by the agar concentration in gel. The agar gel incorporating nisin inhibited the B. thermosphacta growth in the broth medium by prolonging the lag phase. The growth inhibition was enhanced by the addition of nisin in the medium. The results of this study exhibited that the gel food is a feasible nisin delivery system with a controlled release achieved by the adjustment of agar concentration in the system, demonstrating the potential of nisin-incorporating gel for preserving particulate-containing drinks.

• Microbiology and Biotechnology Letters
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• v.50 no.1
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• pp.157-163
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• 2022

Alcoholic liver disease (ALD), which encompasses alcoholic steatosis, alcoholic hepatitis, and alcoholic cirrhosis, is a major cause of morbidity and mortality worldwide. Although the economic and health impacts of ALD are clear, few advances have been made in its prevention or treatment. We recently demonstrated that the insect-derived antimicrobial peptide CopA3 exerts anti-apoptotic and anti-inflammatory activities in various cell systems, including neuronal cells and colonic epithelial cells. Here, we tested whether CopA3 inhibits ethanol-induced liver injury in mice. Mice were intraperitoneally injected with ethanol only or ethanol plus CopA3 for 24 h and then liver injury and inflammatory responses were measured. Ethanol enhanced the production of proinflammatory cytokines, tumor necrosis factor (TNF)-α, interleukin (IL)-1β, interferon (IFN)-γ, and IL-10. It also induced hepatocyte apoptosis and ballooning degeneration in hepatocytes. Notably, all these effects were eliminated or significantly reduced by CopA3 treatment. Collectively, our findings demonstrate that CopA3 ameliorates ethanol-induced liver cell damage and inflammation, suggesting the therapeutic potential of CopA3 for treating ethanol-induced liver injury.

• Journal of Plant Biotechnology
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• v.49 no.3
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• pp.257-270
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• 2022

The aim of this work was to prepare a new biodegradable polyhydroxybutyrate (PHB) submicron fiber mat loaded with hypericin-rich Hypericum perforatum raw extract by centrifugal spinning technology, an alternative approach to the traditional method of electrospinning to fabricate nanofibers or microfibers from solutions at high speed and low cost. Hypericins in methanol/acetone extract of H. perforatum were determined by UHPLC-MS/MS and HPLC/PDA. Submicron fiber mats composed of pure PHB or PHB enriched with H. perforatum extract were prepared using a pilot plant demonstrator for the centrifugal spinning technology and characterized by SEM. Singlet oxygen production was quantified by the 1,3-diphenylisobenzofuran (DPIBF) method in hexane. The results proved a significant production of singlet oxygen by the prepared submicron fiber mat. We also found a significant antibacterial activity against the bacterial strain Escherichia coli CCM 5417 by a method in accordance with JIS Z 2801/ISO 22196 standards. The H. perforatum extract-enriched PHB submicron fiber mats showed potential for the development of self-cleaning and antimicrobial air filters.

• Archives of Pharmacal Research
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• v.13 no.1
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• pp.78-81
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• 1990

N-Aryl-N'(4-hydroxy-6-methyl-2-pyrimidinyl)guanidines (IIa-c) were prepared by cyclization of N-arybiguanides (Ia-c) with ethyl acetoacetate. Coupling of compounds (IIa-c) with the appropriate diazotized arylamine gave N-aryl-N'-(5-arylhydrazono-6-methyl-4-oxopyrimidin-2-yl) guanidines (IIIa-f). Whereas, their chlorination with phosphorus oxychloride followed by treatment of N-aryl-N'-(4-Chloro-6-methyl-2-pyrimidinyl)guanidimes (IVac) with the appropriate arylamine afforded the corresponding 4-arylamino derivatives (Vaf). Compounds (IIa-f) were also formed when compounds (1a-c) were treated with ethyl 2-arylhydrazono-3-oxobutyrates. The antimircobial testing of some of the prepared compounds against some pathogenic microorganisms revealed that only two have a marked effect against Escherichia coli.

• Bulletin of the Korean Chemical Society
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• v.28 no.12
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• pp.2338-2343
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• 2007

Under the framework of green chemistry, an efficient and extremely fast procedure for the synthesis of 5a-h through four-step procedure starting from 2-arylidenetetralin-1-one 1a-d under microwave irradiation is described. A considerable increase in the reaction rate has been observed with better yield. The structures of the synthesized compounds have been characterized on the basis of their elemental analysis and spectral data. Synthesized compounds 5a-h was evaluated for their antimicrobial activity. Some of the compounds exhibited appreciable activity.

• Journal of the Korean Society of Food Science and Nutrition
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• v.30 no.3
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• pp.410-414
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• 2001

A new bacteriocin produced by Bacillus licheniformis cy2 was partially purified and characterized. The bacteriocin named as BSCY2 was stable in the pH range of 2.5~9.5. BSCY2 was stable below 4$0^{\circ}C$ and it retained its antimicrobial activity during long tern storage at -2$0^{\circ}C$ and -7$0^{\circ}C$. BSCY2 was inactivated 15 min exposure to temperatures over 8$0^{\circ}C$ and lost 50% of its antimicrobial activity within 2 hr at 7$0^{\circ}C$. BSCY2 was inactivated by proteinase K treatment, which indicates its proteinous nature. Direct detection of the BSCY2 band showing antimicobial activity on Tricine-SDS-PAGE suggested an apparent molecular mass of about 6,500 dalton. These characterizatics of BSCY2 are considered as potential compounds for use in bioindustry.

• Archives of Pharmacal Research
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• v.28 no.9
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• pp.1031-1036
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• 2005

[ $(+)-Lyoniresinol-3{\alpha}-O-\beta-D-glucopyranoside$ ] (1) was isolated from an ethyl acetate extract of the root bark from Lycium chinense Miller, and its structure was determined using 1D and 2D NMR spectroscopy including DEPT, HMQC, and HMBC. $(+)-Lyoniresinol-3{\alpha}-O-\beta-D-glucopyranoside$ exhibited potent antimicrobial activity against antibiotic-resistant bacterial strains, methicillin-resistant Staphylococcus aureus (MRSA) isolated from patients, and human pathogenic fungi without having any hemolytic effect on human erythrocytes. In particular, compound 1 induced the accumulation of intracellular trehalose on C. albicans as stress response to the drug, and disrupted the dimorphic transition that forms pseudo-hyphae caused by the pathogenesis. This indicates that $(+)-Lyoniresinol-3{\alpha}-O-\beta-D-glucopyranoside$ has excellent potential as a lead compound for the development of antibiotic agents.

• Archives of Pharmacal Research
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• v.27 no.5
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• pp.471-477
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• 2004

In this study, a series of 4-amino-5-cyano-3-substituted-2,3-dihydrothiazol-2-thiones (1a-c), as well as their triazolo and triazinopyrimidine derivatives such as 8-substituted-3-benzyl-5-meth-ylthiazolo[5,4-e][1,2,4] triazolo[1,5-c]pyrimidin-2-thiones (4-6, 10) and 3-benzyl-5-methyl thiazolo[5,4-e]pyrimidino[3,4-b][1,2,4]triazin-2-thiones (7a-b) were prepared as potential antimicrobial and antitumor agents. Some of the tested compounds showed promising antimicrobial activity and non of them showed any appreciable antitumor activity.