• Biodesign
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• 제7권2호
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• pp.35-37
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• 2019

Xanthomonas oryzae pv. oryzae (Xoo) is a plant pathogen, which causes a bacterial blight of rice. The bacterial blight is one of the most devastating diseases of rice in most of the rice growing countries and there is no effective pesticide against bacterial blight. The β-ketoacyl-acyl carrier protein synthase III (FabH) plays a key role in fatty acid synthesis (FAS) and is a promising drug target for the development of antibacterial agents. Xoo0878 gene, a fabH gene, from Xoo was cloned and its gene product Xoo0878 was expressed, purified and crystallized. Xoo0878 crystal diffracted to 2.1Å resolution and belonged to the triclinic space group P1, with unit-cell parameters a = 57.3Å, b = 64.7Å, c = 104.2Å and α = 81.6°, β = 84.7°, γ = 74.4°. There are four monomers in the asymmetric unit, with a corresponding crystal volume per protein weight of 2.65 ų Da^-1 and a solvent content of 53.6%. Xoo0878 structure will be useful to develop new antibacterial agents against Xoo.

• 생약학회지
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• 제20권2호
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• pp.71-75
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• 1989

A new polyyne, panaxyne, was isolated from the Korean red ginseng. The structure was determined as tetradeca-13-ene-1, 3-diyne-6, 7-diol by comparison of spectral data. The $ED_{50}\;value$ of panaxyne as cytotoxicity against L1210 cell was $11.0\;{\mu}g/ml$. The lower cytotoxic activity of the substance relative to other ginseng polyynes is presumably due to lack of the essential structural part of hept-1-en-4, 6-diyne-3-ol.

• 동의생리병리학회지
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• 제19권3호
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• pp.792-796
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• 2005

Disk assays on the compounds (10 and 12) showed both to have antifungal activity against the dermatophytic fungus Trichophyton mentagrophytes ATCC 28185, (1 and 3 mm inhibition zones at $60\;{\mu}g/disc$), but not against the Gram-positive bacterium B. subtilis or the Gram-negative bacteria Escherichia coli and Pseudomonas aeruginosa or fungi Cladosporium resinae and Candida albicans. However, the compound (13) did not show against antifungal activity. The geranyloxy compounds (10, 12, and 13) were cytotoxic to P388 murine leukaemia cells ATCC CCL 46 P388D1, ($IC_50$ >6,250 ng/mL at $7.5\;{\mu}g/disc$). These results suggest that The geranyloxy compounds possesses antimicrobial and antitumor activities.

• Bulletin of the Korean Chemical Society
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• 제28권6호
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• pp.977-982
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• 2007

For the development of novel hepatoprotective agents, C2, C3, C23 and C28 functional groups on asiatic acid were modified, and the prepared compounds were evaluated for their hepatoprotective effects. Among the prepared compounds, 9, 13 and 16 showed significant hepatoprotective activities against CCl4- and galactosamine (GaIN)-induced hepatotoxicity. Especially, compound 9 showed the most significant hepatoprotective effects against GaIN-induced hepatotoxicity (66.4% protection at 50 μM) and moderate hepatoprotective activities against CCl4-induced hepatotoxicity (20.7% protection at 50 μM).

• Archives of Pharmacal Research
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• 제29권6호
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• pp.497-502
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• 2006

A new natural C-benzylated chalcone, $2',4'-dihydroxy-3'-(2-hydroxybenzyl)-6{\c}-methoxychalcone$ (2), along with two other flavonoids, tiliroside and kaempferol 3-O-rutinoside, and an oxoaporphine alkaloid, lanuginosine were isolated from the aerial parts of Ellipeiopsis cherrevensis (Annonaceae). Two known polyoxygenated cyclohexene derivatives, ferrudiol and zeylenol, and a new analog, ellipeiopsol D, were also isolated. The chalcone 2 exhibited cytotoxic activity against human small-cell lung-cancer (NCl-H187), epidermoid carcinoma (KB) and breast cancer (BC) cell lines with $IC_{50}$ values of 1.40, 5.31 and $13.92\;{\mu}g/mL$, respectively. This compound also showed antimalarial activity against Plasmodium falciparum with an $IC_{50}$ value of $7.1\;{\mu}g/mL$ as well as antimicrobacterial activity against Mycobacterium tuberculosis with a MIC of 25 mg/mL.

• Journal of Applied Biological Chemistry
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• 제58권1호
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• pp.1-3
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• 2015

This study investigated the inhibitory activities of 2-hydroxyquinoline and its analogs against ${\alpha}$-glucosidase and ${\alpha}$-amylase. Based on the $IC_{50}$ values of 2-hydroxyquinoline analogs tested against ${\alpha}$-glucosidase and ${\alpha}$-amylase, 2-hydroxyquinoline had potent inhibitory activity (64.4 and $130.5{\mu}g/mL$, respectively), while 2-methyl-8-hydroxyquinoline showed weakly inhibitory activity (90.7 and $215.4{\mu}g/mL$, respectively). 2-Methylquinoline demonstrated no activity against ${\alpha}$-glucosidase and ${\alpha}$-amylase. In conclusion, 2-hydroxyquinoline analogs, with the existence of a methyl group and hydroxyl on quinoline, can be useful as a new diabetes treatment.

• Natural Product Sciences
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• 제10권6호
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• pp.325-329
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• 2004

The composition of essential oil from O. javanica was analyzed by gas chromatography-mass spectrometry. Using the broth dilution method and disk diffusion test, anti-microbial activities of the oil fraction and its main components were evaluated against various antibiotic-susceptible and resistant strains of pathogenic microorganisms. As a result of GC-MS analysis, 57 compounds, including ${\alpha}-terpinolene$ (28.1%), dl-limonene (16.0%), ${\gamma}-terpinene$ (10.3%), ${\beta}-pinene$ (9.7%) and ${\alpha}-pinene$ (6.0%) were identified in the essential oil fraction. The essential oil fraction of O. javanica and its main components exhibited significant inhibitory activities, particularly against Candida albicans (antibiotic-susceptible strains) and Streptococcus pneumoniae (antibiotic- susceptible and resistant strains). The main components of the O. javanica oil fraction displayed different patterns of activity against the three tested Candida species as exemplified by the differential minimum inhibiting concentration (MIC) values. The disk diffusion test showed that the activities were dose dependent.

• 대한수의학회지
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• 제41권4호
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• pp.511-521
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• 2001

Microorganisms were isolated and identified from bovine 296 quarters which showed positive reaction by California Mastitis Test (CMT) in 40 farms of Jeju from September 1999 to June 2000. The organisms associated with the mastitis of bovine were 11 different bacterial species in this study. Which of them, Staphylococcus aureus was the most predominant species as 152 (51.4%) isolates. Other identified species included 49 (16.5%) coliform, 47 (15.8%) Streptococcus dysgalactiae, 15 (5.1%) Bacillus spp., 8 (2.7%) Staphylococcus epidermidis, 6 (2.1%) Streptococcus agalactiae, 5 (1.7%) Enterococcus faecalis, 5 (1.7%) Corynebacterium spp., 3 (1.0%) Streptococcus uberis, 1 (0.3%) Pseudomonas aeruginosa and 1 (0.3%) Pasteurella haemolytica. Almost of all the islolated beacterial species showed high sensitivity against kanamycin (98.6%), cephalothin (98.0%), streptomycin (94.9%), gentamicin (94.6%), ampicillin (92.2%) and polymyxin B (90.2%). On the contrary, they showed resistance against penicillin (47.0%), tetracycline (37.2%), cefazolin (26.0%), bacitracin (22.6%) and erythromycin (19.9%). Eighty-one isolates were not resistant to any antibiotics and 215 drug resistant isolates showed 89 different drug resistance patterns from single to nine multiple antibiotics resistance patterns.

• 동아시아식생활학회지
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• 제17권4호
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• pp.563-570
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• 2007

This study was performed to observe the antioxidative effects, antimutagenic capacity, and cytotoxic activity of the 70% ethanol extract, and fractions, of Agaricus blazei Murill mycelium, using DPPH free radical scavenging ability, the Ames test, and SRB assay, respectively. Among the fractions, ethyl acetate showed the most effective antioxidative capacity according to the $RC_{50}$(73.6 $\mu$g/mL) of the scavenging effect on the DPPH radical. The inhibition rate of both the aqueous fraction and 70% ethanol extract(200 $\mu$g/plate) toward the Salmonella typhimurium TA100 strain was 94.6%, and it was 89.4% against the mutagenesis induced by MNNG(0.4 $\mu$g/plate). In addition, an identical concentration of the 70% ethanol extract in the TA98 strain, and the ethyl acetate fraction in the TA100 strain, showed inhibition rates of 80.3% and 76.9%, respectively, the highest activities against the mutagenesis induced by 4NQO(0.15 $\mu$g/plate). The cytotoxic effects of the 70% ethanol extract and its fractions increased with increasing sample concentration against human cervical adenocarcinoma(HeLa), human hepatocellular carcinoma(Hep3B), human breast adenocarcinoma(MCF-7), human stomach adenocarcinoma(AGS), and human lung carcinoma (A549). A 1 mg/mL concentration of the ethyl acetate fraction showed cytotoxicities of 77%, 83.8%, 82.1%, 83.1%, and 92.6% against HeLa, Hep3B, MCF-7, AGS and A549, respectively.

• Environmental Analysis Health and Toxicology
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• 제13권3_4호
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• pp.87-94
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• 1998

The use of cisplatin is limited by severe side effects such as renal toxicity. Our platinum-base drug discovery is aimed at developing drugs capable of diminishing toxicity and improving antitumor activity. We synthesized new Pt (II) complex analogue [Pt (cis-DACH)(DPPP)]. 2NO$_3$ (PC) containing cis-1,2-diaminocyclohexane as a carrier ligand and 1,3-bis(diphenylphosphino) propane as a leaving group. Furthermore, nitrate was added to improved the solubility. In this study, its structure was determined and its antitumor activity against SKOV-3 and NIH-OVCAR-3 human ovarian adenocarcinoma, and in vitro cytotoxicity was determined against primary cultured rabbit kidney proximal tubular and renal cortical cells of human kidney using colorimetric MTT assay. PC demonstrated acceptable antitumor activity against SKOV-3 and NIH-OVCAR-3 human ovarian adenocarcinoma and significant activity as compared with that of cisplatin. The toxicity of PC was found quite less than that of cisplatin using MTT and $^3$H-thymidine uptake tests in rabbit proximal tubular cells and human kidney cortical cells. PC was used for human cortical tissue in 7 weeks hitoculture by the glucose-consumption tests. We determined that the new platinum drug has lower nephrotoxicity than cisplatin. Based on these results, this novel platinum (II) complex compound (PC) represent a valuable lead in the development of a new anticancer chemotherapeutic agent capable of improving antitumor activity and low nephrotoxicity.