• Korean Journal of Food Science and Technology
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• v.30 no.2
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• pp.439-445
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• 1998

The antimutagenic activity of the water extract of Rehmannia glutinosa Liboschitz (RG) on the mutagenicity induced by 4-nitroquinoline 1-oxide (4-NQO), N-methyl-N'-nitro-N-nitrosoguanidine (MNNG), mitomycin C (MMC), $aflatoxin\;B_1\;(AFB_1)$ and benzo(a)pyrene [B(a)P] were studied using the SOS Chromotest with Escherichia coli PQ37. The water extract of RG was separated into methanol soluble and methanol insoluble parts. The methanol soluble part exhibited higher inhibition effects than the methanol insoluble part against the mutagenic activities of five mutagens. Step-wise fractionation of methanol soluble part was done using methanol, ethyl acetate and water. Among these fractions, water fraction had the strongest inhibitory effects against the mutagenenicity of five model mutagens, showing $4.5{\sim}29.5%$ inhibition, but the $AFB_1$ mutagenic potency was increased slightly by ethyl acetate fraction. The water fraction was further partitioned by sephadex LH-20 column chromtography, and 9 subfractions were obtained. The fraction III showed the strongest inhibitory effects with dose response against the mutagenic activities induced by all the tested chemical mutagens. The inhibition rates of fraction III at concentration of $400\;{\mu}g/assay$ were 29%, 35%, 38%, 25% and 24% against 4-NQO, MNNG, MMC, AFBl and B(a)P, respectively. The fraction III also exhibited a strong bio-an-timutagenicity against 4-NQO and $AFB_1$ by showing more than 40% inhibition.

• Archives of Pharmacal Research
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• v.28 no.3
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• pp.280-284
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• 2005

The chromatographic separation of the MeOH extract from the aerial parts of Syneilesis palmata led to the isolation of a new sesquiterpene glycoside 4, together with four known compounds. Their structures were characterized to be 4$\beta$,5$\beta$-epoxy-caryophill-8,(15)-ene (1), 3$\beta$­hydroxy-gultin-5-ene (2), 4$\alpha$,5$\beta$-dihydroxy-caryophill-8,(15)-ene (3), (-)-oplopan-4-one-10-$\alpha$-O­$\beta$-D-glucose (4) and 3-hexenyl-1-O-$\beta$-D-glucopyranose (5), based on spectroscopic and chemical methods. Compound 2 showed moderate cytotoxicity against five human tumor cell lines in vitro with its EDso values ranging from 5.90-1 0.83 $\mu$g/mL.

• Environmental Mutagens and Carcinogens
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• v.18 no.2
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• pp.98-103
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• 1998

Epigallocatechin gallate (EGCG) was reported to exert weak cytotoxicity against normal healthy cells such as C3H10T1/2 cells, but profound inhibitory effects on the initiation or promotion stage of chemical carcinogenesis in mammary gland, blood and mouse skin. This study was carried out to develop antitumor agents with weak side effects and strong antitumor activity. Human skin melanoma cells (HBT 69) and human oral epitheloid carcinoma cells (OCL 17) were cultured in RPMI-1640 media containing 10% fetal bovine serum, antibiotic, and fungizone. After incubation for 24 hrs, the cells were treated with various amounts of (EGCG) for 48 hrs. The growth inhibitory effects of EGCG in human oral epitheloid carcinoma cells were evaluated by the 3- (4,5-djmethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT), neutral red (NR), and sulforhodamine B protein (SRB) assays of colorimetric methods. The light microscopic study was also carried out to observe morphological changes of the treated cells. These results obtained were as follows; 1. Significantly inhibitory effects of EGCG against cultured human oral epithelioid carcinoma cells. 2. Significantly inhibitory effects against cultured human skin melanoma cells treated with 50 $\mu$M EGCG, but decreased inhibitory effects in 100 $\mu$M EGCG. 3. Degenerative changes against cultured human oral epitheloid carcinoma cells. 4. Degenerative changes against human skin melanoma cells treated with 50 UM EGCG, but recovered degenerative changes in 100 $\mu$M EGCG.

• Food Science and Biotechnology
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• v.15 no.5
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• pp.817-819
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• 2006

8-Quinolinol and other quinolinol derivatives were evaluated with regard to their growth-inhibitory effects against intestinal bacteria, using the paper disk-agar diffusion method. The observed growth responses varied according to the chemicals and dosages used, as well as the bacterial species tested. 8-Quinolinol showed a significant inhibitory effect against Clostridium difficile, C. perfringens, and Escherichia coli, at 5, 2, 1, and 0.5 mg/disk, and also exhibited a very strong inhibitory effect at 0.25 mg/disk. At low concentrations, 8-quinolinol had strong inhibitory effects against C. perfringens at 0.1 and 0.05 mg/disk; 8-quinolinol also manifested a moderate inhibitory effect against C. perfringens at 0.025 mg/disk. Furthermore, 8-quinolinol revealed moderate and weak growth inhibition against C. difficile and E. coli at concentrations of 0.1 and 0.05 mg/disk, respectively, but 2-quinolinol, 4-quinolinol, and 6-quinolinol evidenced no growth inhibition against B. bifidum, B. longum, C. difficile, C. perfringens, E. coli, or L. casei. The inhibitory effects of 8-quinolinol against C. difficile, C. perfringens, and E. coli lead to its consideration as a possible therapeutic modality for the treatment of diseases associated with harmful intestinal bacteria.

• Archives of Pharmacal Research
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• v.26 no.1
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• pp.9-14
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• 2003

For probing the importance of planarity of imidazolidinone motif of 4-phenyl-1-(benzenesulfonyl)imidazolidinones 1 for their cytotoxicity, 4-phenyl-2-(benzoyl)[1,2,5]thiadiazolidine-1,1-dioxide (2a), 4-phenyl-2-(p-toluoyl)[1,2,5]thiadiazolidine-1,1-dioxide (2b), 4-phenyl-2-(phenylcarbamoyl)[1,2,5]thiadiazolidine-1,1-dioxide (3a), and 4-phenyl-2-(p-tolylcarbamoyl)[1,2,5]thiadiazolidine-1,1-dioxide (3b) were prepared along with their regioisomers (5a, 5b, 9a, 9b) and their cytotoxicity were measured against human lung carcinoma (A549), human colon carcinoma (COLO205), human ovarian cancer (SK-OV-3), human leukemic cancer (K562), and murine colon adenocarcinoma (Colon26) cell lines in vitro. All compounds prepared do not show any activity against all five cancer cell lines unlike 1. Compounds 1 possess planarity of imidazolidinone, especially in sulfonylurea moiety ($-SO_2$NHCONH-). However compounds 2 and 3 have nonplanar 5-membered ring, [1,2,5]thiadiazolidine-1,1-dioxides. Such structural differentiation might result in the loss of activity. Therefore the inactivity of 2 and 3 could also be an indication for the necessity of planarity of imidazolidinone ring of 1 for their cytotoxic activity.

• Archives of Pharmacal Research
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• v.24 no.4
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• pp.263-269
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• 2001

Diazepamoxadiazoles 4,5,6,12,14 and 22 were prepared with the binary form system. Diazepamthiadiazoles 15,20 and Diazepamtriazoles 7,8,9,17,18,19 and 21 were also shapely synthesized. Some of these compounds were screened to test their antibacterial activity against E. coli and B. subtilis compounds 15 and 20 show potent activity against these bacteria.

• The Korean Journal of Pesticide Science
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• v.10 no.4
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• pp.249-261
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• 2006

Fifty compounds such as ester, sulfonyl ester, carbamate, ether and phosphoyl ester derivatives of 4-isopropyl-3-methylphenol(I) and 5-isopropyl-3-methylphenol(II) were synthesized. These derivatives were identified by IR, GC/MS and $^1H$-NMR spectra. Their in vitro antifungal activities were tested against 10 plant pathogenic fungi. Among them, several compounds showed potent in vitro antifungal activity. The selected compounds showing potent in vitro antifungal activity were tested for their in vivo antifungal activities against 5 plant diseases such as rice blast, rice sheath blast, cucumber anthracnose, cucumber gray mold and tomato late blight. As a result, 4-isopropyl-3-methylphenyl(2-amino-thiazole-4-yl)methoxyiminoacetate(I-7a) showed a potent in vivo antifungal activity against rice blast. Both methyl (4-isopropyl-3-methylphenoxy)acetate(I-4d) and methyl (5-isopropyl-3-methylphenoxy)acetate(II-4d) effectively inhibited the development of cucumber gray mold.

• YAKHAK HOEJI
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• v.37 no.2
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• pp.136-142
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• 1993

To a suspension of 1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-{3,7-diazabicyclo[3.3.0]oct-1(5)-en-3-yl}-4-oxo-3-quinoline carboxylic acid(C1) in sodium hydroxide solution and water is added dropwise with stirring carbon disulfide. [6R-[6$\alpha$, 7$\beta$(Z)]]-7-[[[2-Amino-4-thiazoly)methoxyimino]-acetyl]amino]-3-[[[[7-( 3-carboxy-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-7-guinolonyl)-3,7-diazabicyclo[3.3.0]oct-1(5)-en-3-yl]thioxomethyl]thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-2-carboxylic acid (DACD) was synthesized from 1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-[7-(mercapto) thioxomethyl-[3,7-dia zabicyclo[3.3.0]oct-1(5)-en-3-yl}]-4-oxo-3-quinoline carboxylic acid disodium salt(C2) and cefotaxime. The invitro activity of novel dual-action cephalosporin, DACD, was compared with the in vitro activities of CENO(cefotaxime 3'-norfloxacin dithiocarbamate), cefotaxime, and norfloxacin against a variety of bacterial species. In vitro activity of DACD was superior to that of norfloxacin against Streptococcus pyogenes. Against Gram-positive and Gram-negative bacteria, its activity was almost equal to that of CENO.

• Advances in Traditional Medicine
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• v.6 no.4
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• pp.306-311
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• 2006

This communication emphasized upon the sensitivity of the crude extracts of clerodendrum inerme against some of the human pathogenic bacteria. Five plant extracts (Petrol, Benzene, Methanol, Ethly acetate and Aqueous) under six different concentrations(500 ${\mu}g/ml$, 1 mg/ml, 2 mg/ml, 5 mg/ml, 10 mg/ml and 15 mg/ml) were tested by disk diffusion method. Methanol, Ethyl acetate and Aqueous extracts of the plant showed significant inhibition against fifteen of the eighteen bacteria tested. No earlier report on antibacterial activity of this taxon could be found in literature.

• Applied Biological Chemistry
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• v.48 no.1
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• pp.40-47
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• 2005

In order to develop a multi-microbial biofungicide against several important plant pathogenic fungi, strains were isolated from the phtophthora blight suppressive red-pepper field soil of Gyeongsangbuk-do, Korea. Strains AY1, AY6, AB1, BB2 and F4, which had strong antagonistic ability against Phytophthota capsici and Fusarium oxysporum, were selected for their involvement with strains of biocontrol fungicide. There were no antagonism among the selected strains and were compatible for making the biofungicide. Their antagonistic mechanisms, except for strain BB2, were an antibiosis by the production of antibiotic, while BB2 produced not only an antibiotic but also cellulase as an antagonistic mechanism against blight causing P. capsici. They were identified as Halobacterium sp. AB1, Xenorhadus sp. AY1, Bacillus sp. AY6, Bacillus sp. BB2, Zymomonas sp. F4 by various cultural, biochemical test and $Biolog^{TM}$ System 4.0. The highest levels of antifungal antibiotic could be produced after 48 hrs of incubation under the optimal medium which were 0.1% galactose, 0.1% $NaNO_2$, 5 mM $Na_2{\cdot}HPO_4$ (pH 5.5). The cultured multi-microbial biofungicide showed strong biocontrol activity against bacterial wilt disease and fusarium wilt disease in cucumber and tomato fields.