• Title/Summary/Keyword: Inhibitory Activity

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Inhibitory effects of Korean plant resources on human immunodeficiency virus type 1 protease activity

  • Park, Jong-Cheol
    • Advances in Traditional Medicine
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    • v.3 no.1
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    • pp.1-7
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    • 2003
  • Some Korean plants were found to inhibit HIV-1 protease activity. The extracts of Acanthopanax koreanum (stem bark), Berchemia berchemiaefolia (stem), Berchemia berchemiaefolia (bark), Distylium racemosum (leaves), Distylium racemosum (stem), Lindera erythrocarpa (leaves), Physalis alkekengi var. francheti (root), Platycarya strobilacea (stem), Rodiola rosea (root), Rosa davurica (stem), Syringa dilatata (leaves), Viburnum awabuki (stem) and Viburnum awabuki (leaves) showed significant inhibitory effect against HIV-1 protease. Camelliatannin H from Camellia japonica and uvaol from Cratagus pinatrifida were potent active inhibitors of HIV-1 protease with $IC_{50}$ values of $0.9\;{\mu}M$ and $5.5\;{\mu}M$, respectively. The cure and prevention of AIDS have been a global challenge since it was discovered in the ealy 1980s. However, the development of anti-HIV agent that can effectively treat or prevent this disease are still demanded.

Protein Tyrosine Phosphatase 1B Inhibitors: Heterocyclic Carboxylic Acids

  • Cho, Sung-Yun;Ahn, Jin-Hee;Ha, Jae-Du;Kang, Seung-Kyu;Baek, Ji-Yoen;Han, Sang-Sub;Shin, Eun-Young;Kim, Sung-Soo;Kim, Kwang-Rok;Cheon, Hyae-Gyeong;Choi, Joong-Kwon
    • Bulletin of the Korean Chemical Society
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    • v.24 no.10
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    • pp.1455-1464
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    • 2003
  • Several series of compounds (benzoic acids, pyrazolecarboxylic acids, phenoxyacetic acids, and quinolinoxyacetic acids) were prepared and evaluated for their inhibitory activity against PTP-1B. Several compounds showed submicromolar inhibitory activity.

Antimicrobial activities in the Korean Traditional Leaf Mustard, Brassica juncea Coss.

  • Kang Seong-Koo
    • Plant Resources
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    • v.8 no.2
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    • pp.96-102
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    • 2005
  • As part of developing natural food preservatives, the antimicrobial effect of ethanol and water extracts from the Cruciferous vegetable was examined Korean traditional Brassica juncea Coss. was used widely as an ingredient of Kimchi, a natural flavoring and spice for a long time. Antimicrobial activities were examined against 15 microorganisms which were food-born pathogens and/or food poisioning microorganisms and food-related bacteria and yeasts. Ethanol extract from leaf mustard showed an antimicrobial effect in most of the strains used in the present study. The lowest minimum inhibitory concentration (MIC) were seen in Bacillus subtilis and Bacillus natto at 10 mg/ml. MIC of water extract was 40-60 mg/ml for bacteria and yeast. Antimicrobial activity of the ethanol extract was not disappeared by the heating at $121^{\circ}C$ for 15 min and not affected by pH.

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Effect of Ginseng Saponin on Adrenaline-Induced Hyperglycemia and Hyperlipidemia (인삼사포닌이 Adrenaline에 의한 고혈당 및 고지방혈증에 미치는 영향)

  • 이동권;임창진;박은희;홍순근
    • YAKHAK HOEJI
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    • v.25 no.2
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    • pp.49-55
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    • 1981
  • To elucidate the effect of ginseng saponin on adrenaline-induced hyperglycemia and hyperlipidemia, ginseng saponin was administered before and after administration of adrenaline, and concentration of glucose, triglyceride(TG), and free fatty acid (FFA) as well as lipase activity in plasma was determined. 1) Glucose concentration was slightly increased by administration of ginseng saponin at 1 hour before and 10 minutes after adrenaline administration, but decreased by administration of ginseng saponin at 7 and 4 hours before adrenaline administration. TG and FFA concentration was also greatly inhibited by administration of ginseng saponin in advance. 2) When gineseng saponin 3, 10, 30mg/kg were administered 7 hours before adrenaline administration, glucose and TG concentration as well as lipase activity were inhibited in proportion to the dose of ginseng saponin, but FFA concentration was slightly inhibited. 3) It was suggested that protopanaxatriol group have potentiating effect on adrenaline induced hyperglycemia but protopanaxadiol group have inhibitory effect. And ginseng saponin seems to have strong inhibitory action on TG mobilization into blood and stimulatory effect on esterification of FFA in liver and adipose tissue.

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Inhibitory Effects of of Tacrine Derivatives on Activity of Prostanoids Biosynthesis Prostaglandin Biosynthesis: A Potential Use for Degenerative Brain Disease Treatment (퇴행성 뇌질환 치료제 Tacrine 유도체의 프로스타글란딘 생합성 억제효과)

  • Shin Hea Soon
    • YAKHAK HOEJI
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    • v.49 no.1
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    • pp.103-108
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    • 2005
  • Tacrine analogues for degenerative brain disease treatments have been designed. A series of diazaanthrine derivatives as novel analogues of tacrine has been prepared through the alkyl substitution and the ring expansion. They were expected to retain anti-inflammatory activity by inhibition of prostaglandin production with reduction of side effect as the selective prostaglandin synthase inhibitor. Prostaglandin synthase expression is associated with the deposition of beta-amyloid protein in neuritic plaques in brain inflammation. Therefore selective prostaglandin synthase blockade is important for the prevention and treatment of alzheimer's disease. To evaluate inhibitory effect of prostaglandin synthase, synthetic tacrine derivatives were screened with accumulation of prostaglandin biosynthesis by lipopolysaccharide in aspirin-treated murine macrophage cell. Most of synthetic compounds have shown significant prostaglandin synthase activities in vitro screening with $84.3{\sim}33.6\%$ inhibition of the prostaglandin $E_2$ production at $10\;{\mu}g/ml$.

Inhibitory Mechanism of a New Antitumor Agent DA125 on DNA Replication (새로운 항암제 DA-125의 유전자 복제 억제 기작)

  • 이상광;김도진;오유택;이상득;우은란;신차균
    • YAKHAK HOEJI
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    • v.43 no.5
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    • pp.623-628
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    • 1999
  • DA-125, a new antitumor agent, was compared with adriamycin, a known DNA intercalator, in terms of inhibitory mechanism of DNA replication by using replicating simian virus 40 (SV40) genome in vivo. In analyzing the SV40 DNA replication intermediates present in cells treated with DA-125, it was not observed to accumulate B-dimers of SV40 DNA which are prominent in adriamycin-treated cells. However, treatment with DA-125 induced dose-dependent formation of DNA-topoisomerase complex which is characteristic of topoisomerase poisons. In addition, DA-125 showed more efficient in inhibiting SV40 DNA replication than adriamycin. Therefore, on the basis of this observation, we suggest that DA-125, a derivative of adriamycin, inhibits DNA replication by blocking topoisomerase activity as a toposomerase poison although adriamycin blocks topoisomerase activity as a DNA intercalator.

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Structure-Activity Relationship of Chroman-2-carboxylic Acid N-Arylalkylamide Derivatives (크로만-2-카르복실산 N-아릴알킬아마이드 유도체의 구조-활성관계)

  • Yi, Wonhui;Hwang, Yeong-Sik;Han, Sang-Bae;Kim, Youngsoo;Jung, Jae-Kyung;Lee, Heesoon
    • YAKHAK HOEJI
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    • v.57 no.6
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    • pp.426-431
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    • 2013
  • In our previous studies, 6-hydroxy-7-methoxychroman-2-carboxylic acid N-phenylamide (KL-1156) was identified as a good inhibitor of nuclear factor-${\kappa}B$ (NF-${\kappa}B$) activation. In continuation of our study, we describe the structure-activity relationship of chroman derivatives containing N-arylalkyl groups and their NF-${\kappa}B$ inhibitory activities. In addition, inhibitory effects of cell proliferation are evaluated against human cancer cell lines (NCI-H23 and PC-3). The most active compounds 3i and 3j contained diphenylethyl and diphenylpropyl side chain on amide nitrogen.

Isolation of Lactobacillus plantarum from Kimchi and Its Inhibitory Activity on the Adherence and Growth of Helicobacter pylori

  • Lee, Hak-Mee;Lee, Yeon-Hee
    • Journal of Microbiology and Biotechnology
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    • v.16 no.10
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    • pp.1513-1517
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    • 2006
  • One single lactic acid producing bacterium, isolated from kimchi, inhibited the growth and adherence of Helicobacter pylori to the human gastric epithelial cell line MKN-45. This isolate was identified as Lactobacillus plantarum and termed L. plantarum strain PL9011. The adherence of H pylori, in the presence of live or nonviable L. plantarum strain PL9011 (10-fold CFU), decreased to 14-20%. The spent culture supernatant of L. plantarum strain PL9011 resulted in the eradication of H pylori. This activity remained stable following neutralization and heat treatment, but not following pepsin treatment, thereby suggesting small peptides as the inhibitory factor. L. plantarum strain PL9011 did not produce any harmful metabolites or enzymes. The results obtained in this study suggest that the L. plantarum strain PL9011 may be a potential novel probiotic for the stomach.

Isolation of a Halotolerant Yeast and the Production of Extracellular Protease (내염성 효모의 분리 및 세포외 Protease의 생산)

  • 정승찬;현광욱;김재호;이종수
    • KSBB Journal
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    • v.16 no.2
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    • pp.158-162
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    • 2001
  • A halotolerant and extracellular protease-producing yeast was isolated from traditional Meju and identified as a strain of Hansenular polymorpha by investigating its microbiological characteristics. The optimum pH, temperature and NaCl concentration reauired for the growth of Hansenular polymorpha S-9 were found to be pH 6.0, 30$^{\circ}C$ and 0.5 M, respectively. Extracellular protease was produced maximally at 10 U ml(sup)-1 when Hansenular polymorpha S-9 was grown on the medium containing 1.0% beef extract and 0.1 M NaCl for 12 hr at 30$^{\circ}C$. About 13% of the angiotensin-converting enzyme (ACE) inhibitory activity was shown in the hydrolysates which were obtained from the digestion of soybean protein (6 mg) for 6 hr at 30$^{\circ}C$ by the crude enzyme (1 U).

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