• YAKHAK HOEJI
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• v.40 no.3
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• pp.357-368
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• 1996

The in vitro antibacterial activity of a novel fluoroquinolone, DWP20373(1-Cyclopropyl-6-fluoro-8-methoxy-7-(2,7-diazabicyclo[3,3,0]oct-4-ene-7-yl)-1,4-dihydro-4 oxoquino line-3carboxylic acid) was compared with those of ciprofloxacin (CPFX), sparfloxacin (SPFX) and ofloxacin (OFLX). DWP20373 was more active than SPFX and OFLX but was less potent than CPFX against gram-negative bacteria. DWP20373 showed an excellent activity against L-MRSA and H-MRSA ($MlC_{90}=0.781{\sim}1.563{\mu}g/ml$).The activity of DWP20373 decreased moderately in the presence of 5mM $Mg^{2+}$. However, pH and serum had no effect on the activity of DWP20373. DWP20373 possessed a rapid bactericidal activity against gram-positive and gram-negative strains.

• Applied Biological Chemistry
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• v.45 no.4
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• pp.195-202
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• 2002

The cytotoxic, mutagenic and antimutagenic activities against chemical direct mutagens such as mitomycin C, 4-nitroquinoline-N-oxide, 2,4,7-trinitro-9-fluorenone of the 70% ethanol extracts of 29 colored rice varieties and chuchung as a control were examined. The results obtained using authentic alkaline phosphatase activity as a growth representative of the indicator cell E. coli PQ 37 demonstrated that the extracts of 13 kinds of colored rice varieties including Jumlalocal and Jumlalocal-1 showed strong toxic effect on the cell growth. However the extracts of DK 1, SC-5, LK 1A-2-12-1-1 and wx 139-3-64-20-3-1 seemed to have stimulatory effects on the cell growth. The mutagenicity and antimutagenicity of the colored rice varieties were screened using SOS chromotest. The mutagenic activity was detected from Jumalocal-1, IR 17491-5-4-3-3 and Jumlalocal. On the contrary, 7 samples including LK 1-3-6-12-1-1, Parnkhari 203, Jumlalocal, wx 139-3-64-20-3-1, Muthumanikam, HP 883-1-1-1-B-1-1 and Jumlalocal-1 were shown to have antimutagenic acitivities against the chemical direct mutagens used in this study.

• Archives of Pharmacal Research
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• v.29 no.12
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• pp.1102-1108
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• 2006

An in vitro bioassay-guide revealed that the methanol (MeOH) extract of the stem bark of Populus davidiana showed considerable inhibitory activity against cyclooxygenase (COX-1, COX-2). Continuous phytochemical study of the MeOH extract of this plant led to the isolation of ten flavonoids; sakuranetin (1), rhamnocitrin (2), 7-O-methylaromadendrin (3), naringenin (4), eriodictyol (5), aromadendrin (6), kaempferol (7), neosakuranin (8), sakuranin (9) and sakurenetin-5,4'-di-${\beta}$-D-glucopyranoside (10). Their structures were identified on the basis of their physicochemical and spectroscopic analyses. The isolated compounds, 1-10, were tested for their inhibitory activities against COX-1 and COX-2. Compound 7 was found to have potent inhibitory effect on COX-1 and a moderate effect on COX-2, meanwhile, compounds 1-6 showed moderate inhibition against COX-1 only. Moreover, compounds 5-8 exhibited suppressive effects on xanthine oxidase (XO). These results may explain, in part, the traditional uses of P. davidiana in ethnomedicine.

• Mycobiology
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• v.28 no.3
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• pp.123-126
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• 2000

Sodium hypochlorite alkaline was tested against Pseudomonas tolaasii causing bacterial blotch on cultivated oyster mushroom (Pleurotus ostreatus). The minimum inhibitory concentration of sodium hypochlorite against P. tolaasii contained active chlorine (AC) at 1.4 mg/l on plate assay. The highest cultivation yield was obtained from the treatment of AC 5.7 mg/l. Treatment of sodium hypochlorite at the rate of higher than AC 11.4 mg/l resulted in reduced yields at the harvest. However, the population of total bacteria on the bed surface treated with AC 5.7 mg/l of sodium hypochlorite was maintained to some extent. Inhibitory concentration against total bacteria on the bed surface was over AC 22.8 mg/l. Mushroom mycelium was damaged and its growth strongly inhibited at the concentration of AC 200 mg/l. Mushroom caps showed yellowish symptom by chemical injury by treatments of AC 74.1 mg/l or higher. Sporocarps infected by P. tolaasii were irrevocable at any concentration of sodium hypochlorite. Routine watering with AC 5.7 mg/l from mushroom initiation to the end of picking resulted in reduced bacterial blotch incidence of 40% and 86% at two mushroom farms. The treatment resulted in higher quality mushroom production compared to that conventionally watered with tap water alone.

• Archives of Pharmacal Research
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• v.21 no.5
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• pp.599-609
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• 1998

In search for new antitumor agents, twelve 6-aziridinylbenzimidazole derivatives were synthesized and their cytotoxicities were tested against three cancer cell lines (mouse lymphocytic leukemia P388 and B16, and human gastric carcinoma SNU-16). From 4-amino-3-nitrotoluene as the starting material, 2-(acetoxymethyl)benzimidazoles (5a-d) were obtained by Phillips reaction. These benzimidazoles were then reacted with Fremy's salt to give a mixture of three 2-(acetoxymethyl) (8a-c) and four 2-(hydroxymethyl)benzimidazole-4,7-diones (9a-d). Addition of these quinones with aziridine afforded 6-aziridinyl-2-(acetoxymethyl) (10a-c) and 6-aziridinyl-2-(hydroxymethyl)benzimidazole-4,7-diones (11a-d). Utilizing 2-(hydroxymethyl)benzimidazole-4,7-diones (9b,d), esters 10d and 13e-h were prepared by the sequential reactions of esterification and addition. The synthesized compounds show potent cytotoxicity against all of three cell lines tested. The cytotoxicities of 10a-d or 11a-d against SNU-16 were wuperior to those of 13e-h, and were equal to or slightly higher than that of mitomycin C. compounds 11a-d were slightly more cytotoxic than 10a-d in all cell lines tested.

• YAKHAK HOEJI
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• v.50 no.4
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• pp.278-286
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• 2006

Classical dihydropyrrole[3,4-f]quinazoline antifolates 7,8 and 9, in which the tricyclic ring is structurally similar to the pteridine ring of $CH_2-THF(1)$, the cofactor of thymidylate synthase (TS), were synthesized, and their in vitro antitumor activity was evaluated by measuring the cell growth inhibitory activity against cancer cell lines. The target compounds were cytotoxic against CCRF-CEM, human T-cell acute lymphoblastic leukemia, with the cell growth inhibitory activity $(IC_{50})$ of $0.8{\sim}8.3\;{\mu}M$. Among the three compounds, 3-amino analog 7 was 10- and 3.5-fold more cytotoxic compared to the 3-methyl analogs 8 and 9, and its cytotoxicity was similar to that of the reference compound with the $IC_{50}$ value of $0.83\;{\mu}M$. This result was supposed as the consequence of the fact that dihydropyrroloquinazolinone ring with amino group was able to bind well in the active site of TS. In the case of 3-methyl analogs, analog 9, which has two-carbon bridge between the dihydropyrroloquinazolinone ring and benzoyl-L-glutamic acid, was 3-times more potent in cytotoxicity than analog 8 which has one-carbon bridge, and this result indicates that the distance and conformational orientation of the benzoyl-L-glutamic acid moiety with respect to the tricyclic ring may also be a crucial determinant of cell growth inhibitory activity.

• Korean Journal of Food Science and Technology
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• v.41 no.6
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• pp.694-699
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• 2009

The antimutagenic activities of ethanol extracts of Korean and American propolis were tested using Salmonella Typhimurium TA98 with two indirect mutagens of 3-amino-1,4-dimethyl-5H-pyrido [4,3-b]indole (Trp-P-1) and 2-aminoanthracene (2-AA) with S9 mix. Additionally, their antimicrobial activities against acne-related pathogenic strains of Propionibacterium acnes, Staphylococcus Epidermidis, Staphylococcus aureus and Pseudomonas aeruginosa were evaluated using both paper disk method and agar dilution method. Ethanol extracts of Korean and American propolis showed strong inhibitory effects, in a dose dependant manner, against the mutagenicities induced by Trp-P-1 and 2-AA. The antimutagenic effect of ethanol extracts of Korean propolis showed significantly higher protective activity than that of American propolis against the Trp-P-1 induced mutagenicity of S. Typhimurium TA98 at the lower concentration ($1-10\;{\mu}g$), but significantly lower protective activity at the higher concentration ($50-200\;{\mu}g$). The antimutagenic effect of ethanol extract of Korean propolis showed significantly higher protective activity than that of American propolis against the 2-AA induced mutagenicity at the concentration of $1\;{\mu}g$, but significantly lower protective activity than that of the American at the higher concentration ($50-200\;{\mu}g$). Both extracts showed strong antimicrobial activities against all the acne-related pathogens tested, with minimal inhibitory concentration (MIC) values in the range $1,500-5,000\;{\mu}g/mL$.

• Journal of Society of Preventive Korean Medicine
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• v.5 no.1
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• pp.144-150
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• 2001

The cytotoxic activity of Cratalariae sessiliflorae on cultured NIH 3T3 fibroblasts and human oral epithelioid carcinoma cells (KB) were evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide (MTT) colorimetric method These fractions of methanol extract of Cratalariae sessiliflorae showed inhibitory effect in vitro in the milligram range against KB cell lines. In general, the antitumor activities of these fractions were does-dependent over the milligram range. The comparison of IC50 values of these fractions in tumor cell lines showed that their susceptibility to these fractions decrease in the following order: Fr. 4> Fr. 6> Fr. 10> Fr. 2> Fr. 11> Fr. 3> Fr. 8> Fr. 7> Fr. 9> Fr. 1> Fr. 5 by the MTT assay. These fractions were tested for their cytotoxic effects on NIH 3T3 fibroblasts using MTT assay. They exhibited potent cytotoxic activities in vitro in the milligram range against NIH 3T3 fibroblasts. In general, the cytotoxic activities of these fractions were does-dependent over the milligram range. The comparison of CD50 values of these fractions in NIH 313 fibroblasts shows that their susceptibility to these fractions in decrease the following order: Fr. 10> Fr. 9> Fr. 2 = Fr. 4> Fr. 8> Fr. 11> Fr. 1 = Fr. 7> Fr. 3> Fr. 5 = Fr. 6 by the MTT assay. These results suggests that fraction 5 has the most growth - inhibitory activity against KB cell lines.

• Journal of Integrative Natural Science
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• v.7 no.3
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• pp.159-165
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• 2014

Pyrazole, hydroxyimino, aldehyde and isoxazole derivatives exhibit a broad spectrum of biological activities such as antimicrobial, anti-inflammatory and antitumor activities. With growing application on their synthesis and bioactivity, chemists and biologists in recent years have considerable attention on the research of these derivatives. In the view of potential importance of these derivatives, we have crystallized few of the derivatives and its report has been published. The present study focuses on docking studies of these derivatives against Phospholipases $A_2$ enzyme. This enzymes has implicated as potential targets for anti-inflammatory drug design. co-crystal structure (PDB ID: 1POE) of $PLA_2$ deposited in Protein Data Bank has been retrieved for docking analysis. Docking studies using Schrodinger's GLIDE reveals that these derivatives shows better binding energy and score in the defined active site. These results may provide a guiding role to design a lead molecule which may reduce inflamation.

• YAKHAK HOEJI
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• v.44 no.1
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• pp.87-94
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• 2000

In order to investigate the hepatoprotective constituents, Melonis Pedicellus was systematically extracted and fractionated with n-hexane, ethyl acetate, butanol and water Treatment of rats with ethyl acetate fraction reduced hepatic injuries induced by $\alpha$-naphthylisothiocyanate or D-galactosamine, whereas the components in water fraction showed protective effect only against D-galactosamine-induced hepatitis in rats. Two cucurbitacins and three sterols were isolated from ethylacetate fraction and their chemical structures were identified as cucurbitacin B, isocucurbitacin B, $\alpha$-spinasterol, stigmast-7-en-3-ol and stigmast-7-en-3-ol-0-$\beta$-D-glucopyranoside. Cucurbitacin B at the dose of 1 mg/kg (p.o.) signifcantly increased in bile flow in rats with ANIT-induced cholestasis. Isocucurbitacin B at 5 mg/hg (p.o.) showed signilicant protective effects against ANIT-induced cholestasis. These results showed that cucurbitacin B and isocucurbitacin B from Melonis Pedicellus may have hepatoprotective effect in rats with experimental cholestasis.