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Antitumor evaluation and antimicrobial activity of geranyl phenyl ethers

  • Oh Hyun-Ju;Shin Ji-Hee;Chung Woo-Young;Han Du-Seok;Baek Seung-Hwa
    • Advances in Traditional Medicine
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    • v.2 no.1
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    • pp.52-57
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    • 2002
  • Geranyl phenyl ethers 1, 2, 3, 4 and 5, 5-fluorouracil 6 and adriamycin 7 as references were tested for their growth inhibitory effects against tumor cell lines and NIH 3T3 fibroblasts using two different assays, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) and sulforhodamine B protein (SRB) assays. These results suggest that methyl-4-[{(2E)-3,7-dimethyl-2,6-octadienyl}oxy]-3-methoxy benzoate 1 showed growth inhibition activity against tumor cell lines. The maximum activity exhibited by methyl-4-[{(2E)-3,7-dimethyl-2,6-octadienyl}oxy]-3-hydroxybenzoate 3 against Staphylococcus epidermidis (MIC, $1,000{\mu}g/ml$).

Cytotoxic Activities of some Geranylated Flavones against L1210 Cell (L1210세포에 대한 제라닐화 후라본의 세포독성)

  • Baik, Kyeong-Up;Ahn, Byung-Zun
    • YAKHAK HOEJI
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    • v.32 no.2
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    • pp.125-128
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    • 1988
  • Geranylation of some synthetic and natural flavones have yielded cytotoxic products against L1210 coll; 5,2´-dihydroxy-6,7,8-trimethoxy-6´-geranyloxyflavone 4$(8.5{\mu}g/ml)$, 5,6-dihydroxy-7-gerenyloxyflavone 9$(2.3{\mu}g/ml)$. 2 has showed the same range of cytotoxicity as the starting material, 5,2´-dihydroxy-6,7,8-trimethoxy-6´-benzyloxyflavone$(17.0{\mu}g/ml)$. The cytotoxicity of 4 was lower than its starting substance, 5,2´,6´-trihydroxy-6,7,8-trimethoxyflavone $(4.5{\mu}g/ml)$. On geranylating 5,6,7-trihydroxyflavone(baicalein, $15.0{\mu}g/ml$) the cytotoxic activity has been strongly potentiated($2.3{\mu}g/ml$ of 9). The presence of at least a free hydroxy group in B-ring of Skullkapflavone II-type flavones. was essential for a high activity. A larger RD-group than methoxy in the B-ring has weakened the activity. The cytotoxicities of baicalein series could not be correlated to their structures.

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Cytotoxicity of the Components of Albizzia julibrissin (합환피 (Albizzia julibrissin)의 성분이 종양세포에 미치는 영향)

  • Choi, Boung-Don;Ryeom, Kon
    • Biomolecules & Therapeutics
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    • v.7 no.4
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    • pp.371-376
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    • 1999
  • By cytotoxicity screening of the 65 Korean medicinal plants against leukemia L1210 and P388D$_{1}$ cell line using the MTT assay in vitro, Albizzia julibrissin was studied. This plant was extracted with MeOH and MeOH extract was solvent-fractionated with CHCl$_{3}$, EtOAc and n-BuOH in sequence. Each fraction by various solvents system was purified by column chromatography and preparative TLC, and four compounds were isolated. The structure of each compound was deduced from UV, IR, $^{1}$H-HMR, $^{13}$ C-NMR and CI-MS spectral data. The cytotoxic activity ($IC_{50}$/_ of the compounds, quercetin-3-rhamnoside, 4',5,7-trihydroxyfla-van-3-glucoside, spinasterol-3-glucoside and acacic acid lactone, were evaluated as 5 $\mu\textrm{g}$/ml, 2$\mu\textrm{g}$/ml, 1 $\mu\textrm{g}$/ml against L1210 and as 9$\mu\textrm{g}$/ml, 10$\mu\textrm{g}$/ml, 1.5 $\mu\textrm{g}$/ml, 1.5 $\mu\textrm{g}$/ml and 0.9 $\mu\textrm{g}$/ml against P388D$_{1}$, respectively.

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A Comparison of Inhibitory Effects in Brown and White Rice ( Oryza sativa L. ) against Mutagenicity Induced by Tryptophan Pyrolysates (트립토판 열분해물 유발 변이원성에 대한 현미 및 백미의 억제 효과 비교)

  • Jo, Jeong-Sun;Yu, Jeong-Eun;Jeon, Hyang-Suk
    • Journal of the Korean Dietetic Association
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    • v.3 no.2
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    • pp.105-111
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    • 1997
  • The inhibitory effect of rice(Oryza sartiva L., illpumbyeo) against mutagenicity induced by tryptophan pyrolysates were investigated using Salmonella typhimurium reversion assay. Both methanol extracts of obtained from brown and white rice were found to possess strong activites of inhibiting the mutagenicities of 3-amino-1,4-dimethyl-5H-pyriod[4,3-b]indol(Trp-P-1) and 3-amino-1-methyl-5H-pyrido[4,3-b]indol(Trp-P-2) on Salmonella typhimurium reversion assay. As the concentration of methanol extract increased, inhibitory effect on mutagenicity increased but reached at steady state as inhibition rate of 90% when the concentration was above 10mg/plate. There was no significant difference(p>0.05) in inhibitory effect of methanol extracts between brown and white rice against tryptophan pyrolysates.

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Synergistic Action of Amphotericin B in Combination with 5-Fluorocytosine and Rifampin against Candida albicans (Candida albicans에 대한 Amphotericin B, 5-Fluorocytosine 및 Rifampin 복합처리에 의한 항균력 상승효과)

  • Koh, Choon-Myung;Park, Jeon-Han
    • The Journal of the Korean Society for Microbiology
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    • v.21 no.2
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    • pp.271-276
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    • 1986
  • Amphotericin B and rifampin or 5-fluorocytosine were tested for synergism against Candida albicans in a synthetic mdium. The test was based on viability studies in which fungicidal activity was determined during the incubation hours of drug exposure. Concentration of amphotericin B(0.2ug per ml and 0.4ug per ml) in combination with inactive concentration of rifampin(12.5ug per ml) or 5-fluorocytosine(25ug per ml) resulted in rapid decrease of colony froming unit(CFU). On the basis of these and earlier studies, it is concluded that amphotericin Band rifampin or 5-fluorocytosine are synergistic against various yeasts and yeast-like fungi under widely differing experimental conditions.

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Antifungal Effect of Chitosan against Malassezia pachydermatis Isolated from the Dog with Otitis Externa (개 외이도에서 분리된 Malassezia pachydermatis에 대한 키토산의 항진균 효과)

  • Oh, Hyun-Ho;Kim, Young-In;Seo, Jeong-A;Choe, Seong-Won;Bae, Seul-Gi;Oh, Tae-Ho
    • Journal of Veterinary Clinics
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    • v.29 no.4
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    • pp.323-327
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    • 2012
  • The effect of pH of chitosan solution (w/v) on antifungal activity against Malassezia pachydermatis isolated from a dog with otitis externa was evaluated. This study was investigated to find out the optimal pH of chitosan solution that could be able to eliminate yeast cells. For comparison of antifungal activity of chitosan solution 2% chlorhexidine that have been already proved the antifungal effect against M. pachydermatis was used as positive control. The chitosan solution at different pH (2.5, 3.0, 3.5, 4.0, 4.5, 5.0) were involved this experiment. The chitosan solutions at each pH could eliminate a number of yeast cells when they were compared to other antifungal agents. In chitosan solution's antifungal effect of varying degrees according to the pH M. pachydermatis was inhibited at pH of < 5.0. Especially it has been proved an effective antifungal effect at pH 3.5. Therefore, the pH of chitosan solution had a effect on antifungal activity and the optimal pH was 3.5 in vitro. The possibility of topical therapy with acidific solution of chitosan has a potential in skin infection against M. pachydermatis.

Inhibitory Effects of Poturaca oleracea L. Extract on the Mutagenicity of Various Mutagen (각종 변이원에 대한 쇠비름 추출물의 돌연변이 억제 효과)

  • 최근표;정성원;김은정;함승시
    • Journal of the East Asian Society of Dietary Life
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    • v.7 no.4
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    • pp.527-537
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    • 1997
  • This study was performed to determine the effects of antimutagenicity of Porturaca oleracea L. in Korea. In Ames test, the ethanol extract of Poturaca oleracea L. inhibited mutagenic activity of N-methyl-N'-nitro-N-nitrosoguanidine(MNNG), , 4-nitroquinoline-1-oxide(4NQO), benzo($\alpha$)pyrene (B($\alpha$)P) and 3-amino-1,4-dimethyl-5H-pyrido-(4,3-b)indole (Trp-P-1) in Salmonella typhimurium TA98 and TA100. But hot-water extract Poturaca oleracea L. only Inhibited mutagenic activity of MNNG in Salmonella typhimurium TA100, On 4NQO, the ethanol extract 100-1,600$\mu\textrm{g}$/plate of Porturaca oleracea L. showed a slight inhibitory effect of 13-48%, 4-47% in TA98 and TA100, respectively, but on MNNG, it showed higher inhibitory effect of 6-86% in TA100, And the treatment of 1,600$\mu\textrm{g}$/plate of ethanol extract of Porturacea L. had strong antimutagenicity with 74-87% inhibition against TA98 and TA100 induced by B(a)P and with 85-93% inhibition against TA98 and TA100 induced by Trp-P-1. The ethanol extract was fractionated with ether. chloroform, ethylacetate, butanol and water. Among them, most of the fraction except water fraction showed strong antimutagenicity effects against mutation induced by 4-NQO, MNNG, B(a)P and Trp-P-1. Chloroform fraction had strong antimutagenicity with 91% inhibition against TA100 induced by MNNG, diethyl etherfraction had strong antimutagenicity with 92%, 98% inhibition against TA98 and TA100 induced by 4NQO, Chloroform fraction had strong antimutagenicity with 97% inhibition against TA100 induced by B (a)P and diethyl etherfraction had strong antimutagenicity with 98% inhibition against both strain Induced by Trp-P-1, respectively.

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Syntheses and Central Nervous Depressant Activities of Piperine Derivatives (V) (피페린 유도체의 합성 및 중추 억제작용에 관한 연구(V) -Methylenedioxyphenylalkenoic Acid Amide 유도체-)

  • 도경삼;임중기;우경식;이은방
    • YAKHAK HOEJI
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    • v.30 no.4
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    • pp.163-168
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    • 1986
  • Thirteen compounds were synthesized by condensing the N-heterocyclic amines (piperidine, pyrrolidine, morpholine) and secondary aliphatic amines (dimethylamine, diethylamine) with 3,4-methylenedioxyphenylalkenoic acid chlorides for developing CNS depressants. Among them, N, N-diethyl-3,4-methylenedioxycinnamamide (IX) and N, N-dimethyl-5-(3,4-methylenedioxyphenyl)-2, 4-pentadienoic acid amicle (XII) exhibited strong activity in antagonism against pentylenetetrazole-induced convulsion, strychnine-induced convulsion and maximal electroshock seizure. N, N-Dimethyl-3, 4-methylenedioxycinnamide (VIII) showed more potent activity in antagonism against strychnine-induced convulsion and maximal electroshock seizure and in the prolongation of hexobarbital sleeping time.

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The production of monoclonal antibodies against canine distemper virus (Canine Distemper Virus에 대한 단클론성 항체의 생산)

  • Kim, Tae-jong;Kim, Se-young
    • Korean Journal of Veterinary Research
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    • v.37 no.2
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    • pp.375-381
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    • 1997
  • The purpose of the production of monoclonal antibodies aganist the Canine distemper virus(CDV) were perfect diagnosis and a new approach to treat canine distemper because the diagnosis and treatment of canine distemper were difficult. Canine distemper virus(CDV) was purified using saturated ammonium sulfate, and injected into hind footpads of BALB/c mouse. 12-15 days later, popliteal lymph node(PN) cells were harvested and fused with SP2/O myeloma cells. Characteristics of monoclonal antibodies were analysed. 1. 9 hybridomas produce the specific antibody against CDV. 2. 6 monoclonal antibodies are against intranuclear and cytoplasmic component of CDV, and 3 monoclonal antibodies are against cytoplasmic inclusions. 3. All monoclonal antibodies did not react with other 5 different viruses (CAV-I, CAV-II, CCV, CPV and CPIV) and react with another CDV-FXNO strain. 4. 3 monoclonal antibodies have neutralizing activity against CDV. 5. Antigenic difference was observed between CDV by IFA.

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Study of Measles, Mumps and Rubella Antibodies by Enzyme Immunoassay in Infants and Children in Korea (효소 면역측정법에 의한 한국 영아 소아의 홍역 볼거리 및 풍진 항체에 관한 연구)

  • Park, Hae-Kyung;Kee, Bock-Keun
    • The Journal of the Korean Society for Microbiology
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    • v.22 no.4
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    • pp.473-483
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    • 1987
  • Present study was undertaken to find when is right time for vaccination against Measles, Mumps and Rubella and what is the seropositive conversion rate after those vacinations. For this purpose, sera from 106 infants and children adimitted in Prediatric Department of Won Kwang University Hospital, Iri, Chonbuk, Korea were divided into 3 groups, such as (1) Vaccination group with definite information when it was given, (2) Unknown group whether vaccination was given or not, (3) Not vaccinated group. They were tested of IgG and IgM antibodies against Measles, Mumps and Rubella using Enzyme Immunoassay method and the following results were obtained. 1. Infants below 6 month of age showed to have IgG antibodies which seemed to have been transferred from mother in 87.8%(29/33) for Measles, 78.8%(26/33) for Mumps and 39.4%(13/13) for Rubella. And they showed IgM antibodies which are thought to have been produced by recent infection in 24.2%(8/33) for Measles, 48.5%(16/33) for Mumps and 9.1%(3/33) for Rubella. 2. Positivity of antibody IgG against Rubella was observed remarkably lower than it is against Measles and Mumps being only 39.4%(13/33) in $0{\sim}5$ month, 30.8%(8/26) in $6{\sim}11$ months, 30%(3/10) in $12{\sim}14$ months and 62.9%(22/35) in $18{\sim}36$ months of age. 3. ${\Delta}OD's$ of IgG and IgM antibodies against Measles were observed increasing with age being 0.444, 0.220 in $0{\sim}5$ months, 0.326, 0.134 in $6{\sim}11$ months, 0.581, 0.140 in $12{\sim}14$ months, 0.512, 0.000 in $15{\sim}17$ months and 0.887, 0.278 in $18{\sim}36$ months of age, respectively. 4. ${\Delta}OD's$ of IgG and IgM antibodies against Mumps were observed increasing with age being 0.427, 0.340 in $0{\sim}5$ months, 0.400, 0.249 in $6{\sim}11$ months, 0.694, 0.314 in $12{\sim}14$ months, 0.539, 0.165 in $15{\sim}17$ months and 0.854, 0.350 in $18{\sim}36$ months of age, respectively. 5. Vaccination for Measles, Mumps and Rubella is generally to start at 15 months of age in Korea, by which age their antibodies are found to exsist in more than 80% of tested samples. So, it seems to be very reasonable to start the vaccination schedule at earlier age than it does currently. 6. From the present study, it seems to have been clearly confirmed that Enzyme Immunoassay method is a reliable method with good reproducibility for mass survey of IgG and IgM antibodies against Measles, Mumps and Rubella in infants and children.

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