• Journal of Integrative Natural Science
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• v.10 no.3
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• pp.141-147
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• 2017

Vascular endothelial growth factor (VEGF) is an important signaling protein involved in angiogenesis, which is the formation of new blood vessels from pre-existing vessels. Consequently, blocking of the vascular endothelial growth factor receptor (VEGFR-2) by small molecule inhibitors leads to the inhibition of cancer induced angiogenesis. In this study, we performed a two dimensional quantitative structure activity relationship (2D-QSAR) study of 38 N-Phenyl-N'-{4-(4-quinolyloxy) phenyl} urea derivatives as VEGFR-2 inhibitors based on hologram quantitative structure-activity (HQSAR). The model developed showed reasonable $q^2=0.521$ and $r^2=0.932$ values indicating good predictive ability and reliability. The atomic contribution map analysis of most active compound (compound 7) indicates that hydrogen and oxygen atoms in the side chain of ring A and oxygen atom in side chain of ring C contributes positively to the activity of the compounds. The HQSAR model developed and the atomic contribution map can serve as a guideline in designing new compounds for VEGFR-2 inhibition.

• Journal of the East Asian Society of Dietary Life
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• v.15 no.2
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• pp.182-187
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• 2005

This study was performed to investigate the antimicrobial effect of the Viscum album var. coloratum extracts against food-borne pathogens. First, the Viscum album var. coloratum was extracted with methanol at room temperature and the fractionation of the methanol extracts was carried out by using petroleum ether, chloroform, and ethyl acetate, and methanol, respectively. The antimicrobial activity of the Viscum album var. coloratum extracts was determined by using a paper disc method against food-borne pathogens and food spoilage bacteria. The petroleum ether extracts of Viscum album var. coloratum showed the highest antimicrobial activity against Bacillus cereus and Shigella dysenteriae. Synergistic effect in inhibition was observed when Viscum album var. coloratum extract was mixed with Perillae folium extract as compared with each extract alone. Finally, the growth inhibition curves were determined by using petroleum ether extracts of Viscum album var. coloratum against Bacillus cereus and Shigella dysenteriae. The petroleum ether extract of Viscum album var. coloratum had strong antimicrobial activity against Bacillus cereus at the concentration of 5,000 ppm. At this concentration, the growth of Bacillus cereus was retarded more than 24 hours and up to 12 hours for Shigella dysenteriae. In conclusion, the petroleum ether extracts of Viscum album var. coloratum inhibit efficiently Bacillus cereus and Shigella dysenteriae.

• Biomedical Science Letters
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• v.15 no.2
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• pp.105-112
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• 2009

The screening of the anti-cancer activity of the chemical library provided 2-thio-4-aminopyrimidine as the initial hit. The confirmation of structure and biological effect of hit was performed by synthesis and biological evaluation. The optimization of hit was performed by derivatization of substituents while keeping the core structure. The evaluation of growth inhibitory activity was carried out using SRB assay against 6 human cancer cell lines and human fibroblast. The growth inhibitory activity of compounds showed substituent dependency and more than 5 compounds showed complete growth inhibition of cancer cell lines at 10 ${\mu}M$ concentration. Chemical library screening followed by synthetic modification provided possibility that 2-thio-4-aminopyrimidine can be used as a new scaffold for the development of anti-cancer agent.

• Korean Journal of Weed Science
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• v.15 no.4
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• pp.247-253
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• 1995

The herbicide butachlor [N-(butoxymethyl)-2-chloro-N-(2,6-di-methylphenyl) acetamide] is widely used by farmers as a tool for weed management of transplanted rice(Oryza sativa L.) in Taiwan. The herbicide did not stop germination of rice and weed seeds, but strongly inhibited the subsequent growth of young shoots and roots. The inhibition was also strong on established seedlings. However, they could recover to normal growth after the herbicide effect disappeared. Butachlor greatly decreased the endogenous indole-3-acetic acid (IAA) but increased the endogenous abscisic acid (ABA) contents of rice seedlings. Addition of lAA into growth medium (Hoagland's solution) partly relieved growth inhibition. Pretreatment of both gibberellic acid ($GA_3$) and IAA 24 hours before butachlor treatment almost completely alleviated the butachlor-interfere with GA and/or IAA metabolism or their action resulting in the growth inhibition of rice. Butachlor was readily absorbed by rice roots. During 24 hours of uptake experiment, 32% of the applied herbicide was absorbed. Pretreatment of the herbicide for 2 days did ncx affect the absorption. Of the absorbed herbicide, 80% remained in roots, only 20% transported into shoots, and more than 50% was metabolized to water soluble substances. Thin-layer chromatographic (TLC) analysis indicated that the Rf value of the most abundant metabolite was butachlor-glutathione conjugate. Rice, barnyardgrass (Echinochloa crus-galli (L.) Beauv.), and monochoria (Monochoria vaginalis Presl) seedlings contained relatively high level of non-protein thiols, while the glutathione S-transferase (GST) activity was found highest in rice, barnyardgrass the next, monochoria the lowest. The difference in GST activity among these species might be related to their sensitivity to butachlor.

• Journal of Nutrition and Health
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• v.35 no.9
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• pp.926-931
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• 2002

The antimicrobial properties of extracts of Prunus mume were tested on Salmonella paratyphimurium and S. typhimurium. First, the Prumus mume was extracted with methanol at several temperatures, and then fractionation of the methanol extracts from Prunus mume was carried out by using petroleum ether, chloroform, ethyl acetate or butanol. Secondly, absorption column chromatoraphy (using a Diaion HP 20) was conducted to eliminate some water soluble materials that might inhibit the antimicrobial activity of some extracts. The antimicrobial activitry of each of the Prunus mume extracts was determined using a paper disc method against several food-borne pathogens, The growth inhibition curve was determine using butanol extracts of Prunus mume against Salmonella typhimurium. The extraction temperature did not have any significant effect on the yield of the extract or on the level of antimicrobial activity. The butanol extract of Prunus mume showed strong antimicrobial activity against Salmonella paratyphimurium and S. typhimurium; a 1,000 ppm of butanol extract of Prunus mume retared the growth of S. typhimurium up to 36 hours. (Korean J Nutrition 35(9) : 926~931, 2002)

• Journal of Applied Biological Chemistry
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• v.48 no.2
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• pp.79-83
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• 2005

While screening for nematicidal activity of bacterial origins, various pseudomonads strains were inhabited in tomato rhizosphere. One isolate designated as $PE_{10}$ was selected for studies on nematicidal properties and plant growth-promoting (PGP) activity and was identified as Pseudomonas aeruginosa based on morphological features, biochemical and physiological tests, and carbohydrate utilization. To investigate nematicidal activity, Meloidogyne incognita juvenile mortality was determined using $PE_{10}$ culture filtrate. Inhibition of strain $PE_{10}$ against Fusarium oxysporum was observed using dual culture technique. Strain $PE_{10}$ showed good siderophore activity, HCN and IAA production abilities, and growth and development enhancement of tomato.

• Journal of Nutrition and Health
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• v.36 no.2
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• pp.147-153
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• 2003

In this study, Artemisia capillaries, which has been used as a folk remedy, was investigated for its antimicrobial activity. First, the Aremisia capillaris was extracted with methanol at room temperature, and fractionation of the methanol extracts from Artemisia capillaris was carried out using petroleum ether, chloroform, and ethyl acetate. Second, the antimicrobial activity of the Artemisia capillaris extracts was determined using a paper disc method and minimum inhibitory concentration of ethyl acetate extracts from Artemisia capillaris against food-borne pathogens and food spoilage bacteria was measured. Finally, the growth inhibition curve was determined using ethyl acetate extracts of Artemisia capillaris against Staphylococcus aureus and Salmonella typhimurium. The ethyl acetate extract of Artemisia capillaris showed strong antimicrobial activity against S. typhimurium at a concentration of 1,000 ppm. The 3,000 ppm of ethyl acetate extract from Artemisia capillaris retarded the growth of S. aureus and S. typhimurium for up to 6 hours.

• Journal of the East Asian Society of Dietary Life
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• v.14 no.5
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• pp.472-478
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• 2004

In this study, Perilla frutescens wh~ch has been used as a folk remedy was investigated its antimicrobial activity. First, the Perilla frutescens was extracted with methanol at room temperatures, and fractionation of the methanol extracts from Perilla frutescens was carried out by using petroleum ether, chloroform, and ethyl acetate, respectively. The antimicrobial activity. of the. Perilla frutescens extracts was determined using a paper disc method and the growth inhibition curve was determined using methanol extracts of Perilla frutescens against Salmonella enteritidis and Bacillus cereus. The methanol extract of Perilla frutescens showed strong antimicrobial activity against Bacillus cereus at the concentration of 1.000 ppm. The 4,000 ppm of methanol extract from Perilla frutescens. retarded the growth of S. enteritidis and Bacillus cereus up to 72 hours.

• The Korean Journal of Food And Nutrition
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• v.19 no.4
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• pp.526-531
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• 2006

Minimum inhibition concentration(MIC), growth inhibition activity, and colony forming inhibitory activity of grapefruit seed extract against Bacillus cereus, Bacillus subtilis, Listeria monocytogenes, Escherichia coli, Salmonella enterifidis and Serratia marcescens were tested. MIC of grapefruit seed extract against Bacillus cereus, Bacillus subtilis, Listeria monocytogenes, Escherichia coli, Salmonella enteritidis and Serratia marcescens was 12.5, 12.5, 12.5, 50, 50, 100ppm, respectively. Growth inhibition concentration of grapefruit seed extract against Bacillus cereus, Bacillus subtilis, Listeria monocytogenes, Escherichia coli, Salmonella enteritidis and Serratia marcescens was below 1.0, 6.25, below 1.0, 6.25, 25, 25ppm, respectively. Colony forming inhibitory activity of grapefruit seed extract against Bacillus cereus, Bacillus subtilis, Listeria monocytogenes, Escherichia coli, Salmonella enteritidis and Serratia marcescens was 93.9, 94.0, 99.9, 4.4, 82.7, 86.4%, respectively. Colony forming inhibitory activities of grapefruit seed extract against Gram positive bacteria were higher than that against Gram negative bacteria.

• Bulletin of the Korean Chemical Society
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• v.25 no.12
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• pp.1898-1906
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• 2004

Nonclassical quinazolinone analogs I, II, and III, in which the glutamic acid moiety of the classical antifolates is substituted by phenylglycine, phenylalanine or aminobenzoic acid and their methyl esters, were synthesized and evaluated as lipophilic inhibitors of thymidylate synthase (TS). The target compounds were generally potent inhibitors of L. casei and human TS with $IC_{50}$ values within the narrow range of 0.2-10 ${\mu}$M and 0.003-0.03 ${\mu}$M, respectively. Further, most of the target compounds showed cytotoxicity against tumor cell lines of murine and human origin with $IC_{50}$ values of as low as 0.050 ${\mu}$M. Substitution of another hydroxyl or carboxylic acid/ester group at the phenyl ring further increased the potency of TS inhibition and cell growth inhibition. Most effective were compounds If and Ic in which extra carboxylic acid/ester was present at the phenyl ring with nanomolar $IC_{50}$ values of 0.0044 and 0.0093 ${\mu}$M against human TS and submicromolar cytotoxic growth inhibition against all four tumor cell lines.