• 제목/요약/키워드: inhibition activities

검색결과 3,225건 처리시간 0.039초

1-(2-furyl)-3-phenylpropenone 유도체의 DNA Topoisomerase I 저해활성에 대한 parameter focusing (Parameter Focusing on the Topoisomerase I-inhibition Activities of 1-(2-furyl)-3-phenylpropenone Derivatives)

  • 명평근;최수라;성낙도
    • 약학회지
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    • 제44권4호
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    • pp.358-361
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    • 2000
  • Parameter focusing on the DNA topoisomerase-Iinhibition with X-substituted phenyl substituents in 1-(2-furyl)-3-phenylpropenone derivatives as inhibition material were analyzed. From the basis on the results the inhibition on DNA topoisomerase I suggested that the inhibition activities of X-substituted phenyl substitutents would depend largely on the net charge of $\beta$-carbon atom, LUMO energy (e.v.) and STERIMOL parameter B$_{5}$ (width) of X. Among them, non-substituent (X=H), 1 and 2,2-dichloro substituent, 4 showed the highest DNA topoisomerase-I inhibition activity.y.

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감마선을 조사한 桃仁皮(도인피)의 항산화활성 (Anti-oxidative Activities Gamma Irradiated Shell of Persicae semen)

  • 조우아
    • 대한본초학회지
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    • 제24권4호
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    • pp.95-99
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    • 2009
  • Objectives : This study were carried out to investigate the anti-oxidative activities of $\gamma$-SPE(gamma irradiated shell of Persicae semen extract with ethanol). Methods : Anti-oxidative was measured by DPPH free radical scavenging activities, nitric oxide radical scavenging activities, SOD-like activities, xanthine oxidase radical scavenging activities, nitrite scavenging activities and tyrosinase inhibition activities. Results : Effects of free radial scavenging was increased by irradiation. Tyrosinase inhibition activities was decreased by $\gamma$-SPE. Conclusions : Results suggested that $\gamma$-SPE have a potential as a new anti-oxidative material.

손바닥선인장(Opuntia ficus-indica)의 라디칼 활성, Tyrosinase 억제 활성, 항알레르기 활성 검색 (Screening of the Radical Scavenging Effects, Tyrosinase Inhibition and Anti-allergic Activities Using Opuntia ficus-indica)

  • 윤진석;이봉호;최병욱;박관하;이남호
    • 생약학회지
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    • 제31권4호
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    • pp.412-415
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    • 2000
  • We have examined radical scavenging effects, tyrosinase inhibition activities and anti-allergic activities on the methanol extracts of Opuntia ficus-indica cultivated in Cheju island. By the comparison of the four samples, methanol and 50% methanol extracts of respective fruits and stems of Opuntia, the most desirable activities were obtained in the sample of the stem's methanol extracts. Based on this analysis, further study to identify the active components in this sample is warranted.

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α-Glucosidase Inhibition Activity of the Extracts of Katsura Tree (Cercidiphyllum japonicum Sieb. Et Zucc) Leaves

  • Lee, Tae-Seong;Ryu, Wang-Gyun;Bae, Young-Soo
    • Journal of the Korean Wood Science and Technology
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    • 제43권2호
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    • pp.238-247
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    • 2015
  • Katsura tree (Cercidiphyllum japonicum Sieb. Et Zucc) leaves were collected, air-dried and extracted with 70% aqueous acetone, then concentrated and sequentially fractionated using n-hexane, $CH_2Cl_2$, EtOAc, and $H_2O$ to be freeze dried for antioxidant and ${\alpha}$-glucosidase inhibition activity tests. The antioxidant activity of the extracts was evaluated using DPPH (1,1-diphenyl 2-picrylhydrazyl) free radical scavenging assay. The test concentrations were adjusted to 500, 250, 125, 62.5, 31.25, 15.62, 7.81, 3.9, 1.95 and 0.97 ppm. The $H_2O$ and EtOAc fractions showed higher activities compared with the control, ${\alpha}$-tocopherol, at all concentrations. The crude fraction also gave better activity at the concentrations lower than 62.5 ppm. However, the nonpolar n-hexane and $CH_2Cl_2$ fractions gave prominently lower activities compared with the control at all concentrations. The $IC_{50}$ values of the crude, EtOAc, and $H_2O$ fractions exhibited 11.78, 4.29 and $9.80{\mu}g/m{\ell}$, respectively, compared with $12.08{\mu}g/m{\ell}$ of the control. But the n-hexane and $CH_2Cl_2$ fractions indicated 300 and $91.85{\mu}g/m{\ell}$ of $IC_{50}$, respectively. ${\alpha}$-Glucosidase inhibition activity was evaluated at the concentrations of 50, 25, 12.5, 6.3, 3.1, 1.6 and 0.8 ppm. The inhibition activities were increased according to as the increase of sample concentrations. However, the nonpolar n-hexane and $CH_2Cl_2$ fractions indicated very low inhibition activities compared with acarbose, a positive control. The EtOAc fraction showed very good capability as almost 100% compared with the control at the higher concentrations than 12.5 ppm and the crude fraction also indicated good potential as 95% and 100% at 25 and 50 ppm, respectively. The $H_2O$ fraction gave good inhibition value as 90% at 50 ppm although the value was lower than the control. These results showed that the polar fractions had better ${\alpha}$-glucosidase inhibition activities. The $IC_{50}$ values of the nonpolar fractions, n-hexane and $CH_2Cl_2$, showed very lower values as 468 and $103.6{\mu}g/m{\ell}$, respectively, than the control. ${\alpha}$-Glucosidase Inhibition Activity of the Extracts of Katsura Tree (Cercidiphyllum japonicum Sieb. Et Zucc) Leaves However, the polar fractions, crude, EtOAc and $H_2O$, showed 7.1, 3.7 and $13{\mu}g/m{\ell}$, respectively, indicating that these fractions can be used as natural bioresources for treating diabetes mellitus. Also ${\alpha}$-glucosidase inhibition activity had a positive correlation with antioxidant activity of the extracts.

조록나무 Proanthocyanidin의 ${\alpha}-Amylase$${\alpha}-Glucosidase$에 대한 저해 효과 (Inhibitory Effects of Proanthocyanidin Extracted from Distylium racemosum on ${\alpha}-Amylase$ and ${\alpha}-Glucosidase$ Activities)

  • 안진권;박영기;박소영;김용무;이해익;이위영
    • 생약학회지
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    • 제35권4호통권139호
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    • pp.271-275
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    • 2004
  • Distylium racemosum Sieb. Et Zucc contains some compounds inhibit -amylase activity in experimental conditions. The inhibitory test showed that 50% acetone extracts from the bark and leaves of the plant strongly inhibited salivary -amylase activity. Proanthocyanidin(PA) which has strong inhibitory activity was extracted from the leaves by chromatography on Sephadex LH-20. The inhibitory activities and the inhibition kinetics of the PA were studied against three kinds of enzymes: human salivary ${\alpha}-Amylase$ (SAA), pork pancreatin ${\alpha}-Amylase$ (PAA) and yeast ${\alpha}-Glucosidase$ (AG). Then the activities of PA against SAA, PAA and AG were compared with those of acarbose, a commercial agent. The inhibitory activities of PA were stronger than those of acarbose. Inhibition kinetics of the PA showed competitive inhibition for SAA and PAA, and non competitive inhibition for GA.

산채 및 해조분말을 첨가한 우리밀 밀가루 열수출물의 항돌연변이성 및 암세포 성장 억제효과 (Antimutagenicity and Cytotoxicity Effects of Woorimil Wheat Flour Extracts Added with Wild Herb and Seaweed Powder)

  • 함승시;이상영;최면;황보현주
    • 한국식품영양과학회지
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    • 제27권6호
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    • pp.1177-1182
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    • 1998
  • The antimutagenic and cancer cell growth inhibitory effects of woorimil contained herb and seaweed powders were examined. While woorimil itself showed only 40% antimutagenic effect on S. typhymurium TA98 against 4NQO(0.15 g/plate), water extracts of mountain herbs and seweeds including Comfrey, wormwood, Kale, Angelica utilis and pine leaves showed 80~90% antimutagenicity. On the other hand, these extracts along with woorimil showed 68 to 80% antimutagenic activities. Low antimutagenic activities of less than 50% were shown when these extracts were tested on TA98 against Trp P 1(0.5 g/plate), but high antimutagenic activities of 80~93.3% were shown on TA100. Water extracts of Capsella bursa pastoris and Allium grayi exhibited 60~80% of the activites in cytotoxicity tests of woorimil water extracts(0.5mg/ml) on human lung carcinoma cell. A549 showed 10% cell growth inhibitory effect. When mixed with Comfrey and Angelica utilis extracts, it showed 23~25% inhibition and other extracts showed only 12~23% inhibition. Cytotoxicity test of woorimil extracts on human liver cancer cell Hep3B revealed 20% inhibition. The additions of pine needle extracts, Angelica utilis and Comfrey showed 33%, 29% and 25% inhibition, respectively. But other extracts showed only 20% inhibition.

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Contrasting Correlation in the Inhibition Response of ADP-induced Platelet Aggregation and the Anti-coagulant Activities of Algal fucoidans Derived from Eisenia bicyclis and Undaria pinnatifida sporophylls (Mekabu)

  • Jeong, Eui-Sook;Yoon, Yeon-Hee;Kim, Jong-Ki
    • Fisheries and Aquatic Sciences
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    • 제12권3호
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    • pp.194-202
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    • 2009
  • Sulfated fucans are known to have both anti-thrombotic and anti-coagulant activities. In this study, the variation in platelet aggregation and anti-coagulant activities was investigated in vitro with regard to administered dose, molecular weight distribution, sulfate content, and sugar composition in two algal fucoidans from Eisenia bicyclis and Undaria pinnatifida sporophylls (Mekabu). The anti-coagulant activity largely correlated with sulfate content and with molecular weight distribution in a dose-dependent manner. However, both fucoidans demonstrated inhibitory responses to ADP-induced platelet aggregation in dose- and structure-dependent manners that contrasted with the anti-coagulant activity. Neither molecular weight distribution nor sulfate content greatly affected platelet-aggregation inhibition (PA-inhibition) by the fucoidan fractions, whereas anti-coagulant activity was sensitive to these structural factors. Interestingly, an E. bicyclis fucoidan fraction exhibited almost complete PA-inhibition at a treatment dose of 500 mg/mL while retaining weak anti-coagulant activity. In conclusion, these observations suggest that fucoidan may be a useful anti-thrombotic or anti-platelet agent in various arterial thrombotic disorders, including post-vascular intervention with controlled bleeding complications, due to its anti-coagulant modulating activity.

Antioxidant and Xanthine Oxidase Inhibition Activities of Cynomorium songaricum Extracts

  • Seo, Soo-Jung;Han, Mi-Ra;Lee, Yang-Suk
    • Preventive Nutrition and Food Science
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    • 제16권4호
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    • pp.307-312
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    • 2011
  • In this study, we evaluated the antioxidant activities and xanthine oxidase inhibition effects of water and ethanol extracts of Cynomorium songaricum. The ethanol extract of C. songaricum (EE) contained more phenolic and flavonoid compounds than the water extract (WE). The antioxidant activities of the extracts were increased as the concentration of the extract increased. The WE has better effectiveness than the EE for DPPH free radical scavenging activity and nitrite scavenging ability. The nitrite scavenging abilities of WE were 90.02% ($EC_{50}$ 653.15 ${\mu}g$/mL) at conditions of pH 1.2 and 2,000 ${\mu}g$/mL, and 84.34% ($EC_{50}$ 817.17 ${\mu}g$/mL) at pH 3.0. The EE has more effective SOD-like activity and XO inhibition than WE. The SOD-like activity of EE was 81.47% at a concentration of 2,000 ${\mu}g$/mL, $EC_{50}$ was 951.70 ${\mu}g$/mL. The xanthine oxidase inhibition of the EE, with an $EC_{50}$of 112.47 ${\mu}g$/mL, is greater than that of ascorbic acid, which was 192.50 ${\mu}g$/mL (p<0.05). These results suggest that the C. songaricum is a potentially useful antioxidant source for the development of nutraceuticals and medicines.

잔디 뿌리병 병원균인 Rhizoctonia solani의 성장을 저해하는 미생물 선발 (Screening of Potent Biofungicide for the Growth Inhibition of Soilborne Pathogenic Fungi, Rhizoctonia solani)

  • 이은열;이재화
    • 생명과학회지
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    • 제13권3호
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    • pp.355-358
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    • 2003
  • 식물 병원성 진균인 Rhizoctonia solani에 대한 길항능이 있는 Trichoderma 계열의 미생물 균주를 선별하였다. R. solani의 성장을 저해하는 능력이 우수한 균주를 선별하기 위하여 일차적으로 PDA 평판에서 inhibition zone을 측정하였고, 병원성 진균의 세포벽을 용해시킬 수 있는 세포외 효소인 glucanase 및 chitinase 활성을 분석하였다. 4∼5 mm 이상의 inhibition zone을 보여주었고, glucanase 및 chitinase 활성이 우수한 Trichoderma sp. UK-3와 T. viride 균주들을 선별할 수 있었다.

봉선화 추출물의 항균성에 관한 연구(I) -추출용매에 따른 항균성 검색- (Studies on Antimicrobial of Impatiens balsamina extract (I) -Sereening of Antimicrobial on extract solvent-)

  • 정진순;최석철
    • 한국섬유공학회:학술대회논문집
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    • 한국섬유공학회 1996년도 추계 학술발표회
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    • pp.500-506
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    • 1996
  • To study antimicrobial activities of Impatiens balsamina, its leaf and stem was extracted by methanol and water. The extracts were tested their microbial inhibition activities against several microorganisms, staphylococcus aureus KCTC 1928, Escherichia coli KCTC 1116, Klebsiella pneumoniae KCTC 2690, Trichophyton mentagrophytes KCTC 6316. The methanol extract and water extract of the leaf and stem didn't show the inhibition effect on E. coli but showed the inhibition effect against the ohter 3 species of the microorganisms tested. The extract of leaf showed higher inhibition than the extract of stem. And the methanol extract showed higher inhibition than the water extract.

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