• Title/Summary/Keyword: Inhibitory Activity

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Purification and Characterization of Angiotensin I-Converting Enzyme Inhibitors from Sinapis alba L.

  • Yuk, Jin-Su;Lim, Young-Hee;Cho, Hong-Yon
    • Preventive Nutrition and Food Science
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    • v.5 no.2
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    • pp.75-80
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    • 2000
  • To separate ACE inhibitors from edible plants, spices, and herbs, 285 extracts of 95 sources were screened for ACE inhibitory activity. The extract of Sinapis alba L. had the most potent ACE inhibitory activity. Mustard seeds were crushed homogeneously and extracted with hexane and water successively. Lyophilized water extract was fractionated with $H_2O$:butanol(1:1). The ACE inhibitor was purified from butanol fraction by methanol precipi-tation, gel filtration, HPLC, and FPLC with Superdex peptide HQ 10/30 column. The active fraction has been purified to homogeneity, which was proven by gel filtration using FPLC system. The yield was 0.02%. The com-pound has a molecular weight of about 640. The compound competitively inhibited ACE activity and the $IC_{50}$ value was 79$\mu\textrm{g}$/ml. The purified compound showed uterus contraction activity in isolated rat uterus.

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Antimicrobial Activity of Prodigiosin from Serratia sp. PDGS120915 Against Intestinal Pathogenic Bacteria

  • Ji, Keunho;Kim, Young Tae
    • Microbiology and Biotechnology Letters
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    • v.47 no.3
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    • pp.459-464
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    • 2019
  • This study aimed to identify and characterize the antimicrobial activity of prodigiosin produced by Serratia sp. $PDGS^{120915}$ isolated from stream water in Busan, Korea; the identification was performed using phonological, biochemical, and molecular techniques, including 16S rRNA sequence analysis. Prodigiosin from the bacterial culture was purified by high-performance liquid chromatography (HPLC), and its antimicrobial activity and minimum inhibitory concentrations (MICs) were evaluated against 10 intestinal pathogenic gram-positive and negative bacteria. The results revealed that the isolated prodigiosin exhibited high antimicrobial activity against Listeria monocytogenes, Bacillus cereus, Pseudomonas aeruginosa, Salmonella typhimurium, Staphylococcus aureus, and Vibrio parahaemolyticus; further, the isolated prodigiosin showed minimum inhibitory concentrations (MICs) between $3{\mu}g/ml$ and 30 mg/ml, but they were not active against Bacillus subtilis, Enterococcus faecalis, Klebsiella pneumonia, and Escherichia coli. In conclusion, prodigiosin isolated from Serratia sp. $PDGS^{120915}$ showed high antimicrobial activity against intestinal pathogenic bacteria and has potential applications in the development of new antimicrobial agents.

Anti-complement Activity of Flavonoids from Litsea japonica

  • Lee, Sun-Young;Min , Byung-Sun;Kim, Jung-Hee;Moon, Hyung-In;Lee, Joong-Ku;Kim, Tae-Jin;Kim, Young-Ho;Lee, Hyeong-Kyu
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.372.1-372.1
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    • 2002
  • AIzelin (1) and quercitrin (2) isolated from the EtOAc-soluble fraction of the leaves of Litsea japonica Jussieu (Lauraceae) showed inhibitory activity against classical pathway complement system with 50% inhibitory concentration ($IC_{50}$/) values of 112.2 and 198.2 $\mu\textrm{g}$/$m\ell$. respectively. For the structure-activity relationship of flavonoids on anti-complement system. myricitrin (3) from JUQ/ans mandshurica Maximowicz (Juglandaceae) also tested anti-complement activity. while this was devoid of any significant activity. (omitted)

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Characterization of antioxidant and anti-inflammatory activities in the grains of collected Sorghum bicolor varieties

  • Ji Won Seo;Jae Geun Lee;Bimal Kumar Ghimire;Myong Jo Kim;Chang Yeon Yu;Eun Soo Seong
    • Journal of Applied Biological Chemistry
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    • v.66
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    • pp.227-235
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    • 2023
  • The current study evaluated the presence and concentration of health-promoting phenolic antioxidants in sorghum seed accessions from seven regions in three different countries (Uzbekistan, Myanmar, and the United States). The free radical scavenging activity using the 2,2-diphenyl-1-picrylhydrazyl assay was 13.10±2.37 ㎍/mL in the Uzbekistan sorghum seed extracts, demonstrating the highest antioxidant activity. Additionally, the total phenol content was the highest in the Uzbekistan sorghum seed extracts [157.87±4.04 mg GAE/g (gallic acid equivalents per gram)]. The total flavonoid content was 12.69±0.72 mg QE/g (quercetin equivalents per gram) and represents the highest value in the Myanmar collection. The Uzbekistan collection demonstrated the greatest potential for whitening activity, with the tyrosinase inhibition rate of 79.20±4.15%. The wrinkle improvement function using elastase also showed the highest anti-aging activity of 55.85±4.78% in the same seed extract. The Uzbekistan seed extract had the highest NO production inhibitory activity of 144.35±4.55%. We conclude from these results that the Uzbekistan sorghum seed has excellent antioxidant activity, content of various functional ingredients, and anti-inflammatory activity.

Antioxidative and Nitric Oxide Production Inhibitory Activities of Lespedeza bicolor Stem Extracts Depending on Solvents (싸리나무 줄기 추출물의 추출 용매에 따른 항산화활성과 Nitric Oxide 생성 억제 활성)

  • Lee, Kyoung-In;Yang, Sun-Ah;Kim, Sun-Min
    • Korean Journal of Medicinal Crop Science
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    • v.19 no.5
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    • pp.368-372
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    • 2011
  • In this study, we investigated on antioxidative activity and nitric oxide production inhibitory activity of various solvent extracts of Lespedeza bicolor. The total polyphenol content of the methanol extract was 192.6 mg/g and flavonoid content of the acetone extract was 40.6 mg/g, as the highest content. In DPPH radical scavenging ability, $SC_{50}$ values of the ethanol and methanol extract were exhibited $0.69mg/m{\ell}$ and $0.89mg/m{\ell}$, respectively. However, in nitric oxide(NO) scavenging ability, $SC_{50}$ values of the acetone was exhibited $0.72mg/m{\ell}$ as the highest activity. Moreover, the acetone extract showed strong NO production inhibitory effect in lipopolysaccharide(LPS)-stimulated Raw 264.7 cell. In the cytotoxicity measurement by MTT assay, the extracts were exhibited Raw 264.7 cell viabilities of 92.57~129.04% as nontoxic result in concentration of $65{\sim}650{\mu}g/m{\ell}$. As a result, the acetone extract of L. bicolor could be applicable to functional materials for anti-inflammatory related fields.

Production of Antihypertensive Angiotensin I-Converting Enzyme Inhibitor-Enriched Edible Yeast Using Gugija (Lycium chinesis Mill)

  • Kim, Ran;Jang, Jeong-Hoon;Park, Won-Jong;Kim, Ha-Kun;Kwak, Hahn-Shik;Lee, Jong-Soo
    • Mycobiology
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    • v.38 no.3
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    • pp.206-209
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    • 2010
  • To produce bioactive compound enriched yeast using medicinal Gugiga (Lycium chinensis Mill), several edible Saccharomyces species were cultured in Gugija extracts added yeast extract, peptone and dextrose medium (GE - YEPD medium) at $30^{\circ}C$ for 24 hr, and their growth were determined. Growth of Saccharomyces cerevisiae K-7 and Sacchromyces cerevisiae ACTC 7904 were better than those of the other yeasts. Two yeasts were selected and then determined their some physiological functionalities after cultivated the yeasts in the GE - YEPD medium and compared those grown on YEPD medium. Antihypertensive angiotensin I-converting enzyme (ACE) inhibitory activity of S. cerevisiae K-7 grown on GE - YEPD medium was about 20% higher than that grown on YEPD medium. Superoxide dismutase-like activity of S. cerevisiae ACTC 7904 was also about 12% more high. However, the other physiological functionalities were almost same or lower. Optimal addition concentration of Gugija extract was 10%, and maximally growth and ACE inhibitory activity of S. cerevisiae K-7 were shown when the strain was cultured in 10% Gugija extracts containing YEPD medium at $30^{\circ}C$ for 12 hr.

Studies on $Na^+,\;K^+-ATPase$ Activity of the Constituents of Adonis amurensis in Korea (한국산(韓國産) 복수초성분(福壽草成分)의 $Na^+,\;K^+-ATPase$활성(活性)에 대한 연구(硏究))

  • Ro, Jai-Seup;Lee, Kyong-Soon;Park, Woong-Yang;Oh, Kap-Jin;Ahn, Beung-Tae;Eo, Kyong-Chun;Jeong, Do-Rae;Nambara, Toshio
    • Korean Journal of Pharmacognosy
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    • v.21 no.2
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    • pp.130-136
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    • 1990
  • Four known cardiotonic steroids were isolated from roots of Adonis amurensis Regel et Radde and identified as digitoxigenin, cymarin, K-strophanthin and convallatoxin by chromatography on Amberlite XAD-2 resin and silica gel, high performance liquid chromatography and gel chromatography on Sephadex LH-20. In order to clarify the structure-activity relationship, thirteen related compounds of digitoxigenin were tested for the inhibitory activities for $Na^+,\;K^+$-adenosine triphosphatase from guinea pig heart. The inhibitory activities of related compounds of digitoxigenin were dependent upon the dicarboxylic acid and amino acid components. The compound having both the arginine and suberic acid moiety showed the higher inhibitory activity. The sulfate and glucuronide of digitoxigenin exhibited much less potency than the parent genin.

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Inhibitory Activity of Chinese Medicinal Plants on Nitric Oxide Synthesis in Lipopolysaccharide -Activated Macrophages

  • Ryu, Jae-Ha;Ahn, Han-Na;Lee, Hwa-Jin;Feng, Li;Qun, Wen-He;Han, Yong-Nam;Han, Byung-Hoon
    • Biomolecules & Therapeutics
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    • v.9 no.3
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    • pp.183-187
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    • 2001
  • Nitric oxide (NO) produced in large amounts by the inducible nitric oxide synthase (iNOS) is known to be responsible for the vasodilation and hypotension observed in septic shock and inflammation. The inhibitors of iNOS, thus, may be useful candidate for the treatment of inflammatory diseases accompanied by the overproduction of NO. We prepared alcoholic extracts of Chinese medicinal plants and screened their inhibitory activity against NO production in lipopolysaccharide (LPS)-activated macrophages. Among the 80 kinds of extracts of herbal drugs, 15 extracts showed potent inhibitory activity of NO production above 80% at the concentration o$50\mu\textrm{g}/ml$. These potent extracts showed dose dependent inhibition of NO production of LPS-activated macrophages at the concentration of 50, 30,$10\mu\textrm{g}/ml$. Especially, Rhus chinensis, Senecio scandens and Wikstroemia indica showed most potent inhibition above 50% at the concentration of $10\mu\textrm{g}/ml$. These plants are promising candidates for the study of the activity-guided purification of active compounds and would be useful for the treatment of inflammatory diseases and endotoxemia accompanying the overproduction of NO.

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Biological Characterization of Periconicins, Bioactive Secondary Metabolites, Produced by Periconia sp. OBW-15

  • SHIN, DONG-SUN;OH, MI-NA;YANG, HYEONG-CHEOL;OH, KI-BONG
    • Journal of Microbiology and Biotechnology
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    • v.15 no.1
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    • pp.216-220
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    • 2005
  • Periconicin A and B, two new fusicoccane diterpenes originally isolated from the cultures of endophytic fungus Periconia sp. OBW-15, were tested by several biological assays. Periconicin A was consistently more active than periconicin B. In an antifungal activity assay, periconicin A showed potent inhibitory activity against the agents of human mycoses, including Candida albicans, Trichophyton mentagrophytes, and T. rubrum, with minimum inhibitory concentration (MIC) in the range of 3.12- 6.25 $\mug$ /ml. In a plant growth regulatory activity assay, periconicins inhibited hypocotyl elongation and root growth of Brassica campestris L. and Raphanus sativus L. At concentrations below 1 μg/ml, however, both compounds accelerated root growth by 110- 135%. From these results, it is apparent that a methyl group positioned in a cyclopentane ring may play an important role in plant and fungal growth inhibitory activity.

Synthesis and Akt1 Kinase Inhibitory Activity of 1,3,4-Thiadiazole Derivatives (1,3,4-Thiadiazole 유도체의 합성 및 Akt1 카이네이즈 저해 활성)

  • Yoo, Kyung-Ho;Kim, Se-Young;Ryu, Jae-Chun
    • Journal of the Korean Applied Science and Technology
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    • v.25 no.3
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    • pp.370-379
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    • 2008
  • Akt, a serine/threonine protein kinase as a viral oncogene, is a critical regulator of PI3K-mediated cell proliferation and survival. On translocation, Akt is phosphorylated and activated, ultimately resulting in stimulation of cell growth and survival. As a part of our program toward the novel Akt1 inhibitors with potent activity over PI3K signaling pathway, we found primary hit compound 2 with an $IC_{50}$ value of $620\mu}M$ from protein kinase focused library. Based on the structural features of 2, new 1,3,4-thiadiazole derivatives were designed by the introduction of aromatic and heteroaromatic moieties onto thiadiazole nucleus. In this work, a series of 1,3,4-thiadiazole derivatives 1a-1 were synthesized and evaluated for Akt1 inhibitory activity.