• Title/Summary/Keyword: Inhibitory Activity

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Inhibitory Effect of Condensed Tannins Isolated from Korean Green Tea against Xanthine Oxidase (한국산 녹차로부터 분리한 축합형 탄닌의 Xanthine Oxidase 저해효과)

  • Cho, Young-Je;Chun, Sung-Sook;Choi, Cheong
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.22 no.4
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    • pp.418-422
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    • 1993
  • For the purpose of utilizing tannins in the functional foods and crude drugs the xanthine oxidase inhibition of tannins isolated from Korean green tea was determined. Acetone extract from Korean green tea showed inhibitory effect against the xanthine oxidase. The galloyl tannins showed higher inhibitory activity against xanthine oxidase than the nongalloyl tannins. In terms of stereo isomers, (-)-epicatechins had higher inhibitory activity than the (+)-catechins. The synergistic activity was also observed. Tannins isolated from Korean green tea appeared to be incompetitive inhibitor against the xanthine oxidase.

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PTP1B Inhibitory Secondary Metabolites from Marine-Derived Fungal Strains Penicillium spp. and Eurotium sp.

  • Sohn, Jae Hak;Lee, Yu-Ri;Lee, Dong-Sung;Kim, Youn-Chul;Oh, Hyuncheol
    • Journal of Microbiology and Biotechnology
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    • v.23 no.9
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    • pp.1206-1211
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    • 2013
  • The selective inhibition of PTP1B has been widely recognized as a potential drug target for the treatment of type 2 diabetes and obesity. In the course of screening for PTP1B inhibitory fungal metabolites, the organic extracts of several fungal species isolated from marine environments were found to exhibit significant inhibitory effects, and the bioassay-guided investigation of these extracts resulted in the isolation of fructigenine A (1), cyclopenol (2), echinulin (3), flavoglaucin (4), and viridicatol (5). The structures of these compounds were determined mainly by analysis of NMR and MS data. These compounds inhibited PTP1B activity with 50% inhibitory concentration values of 10.7, 30.0, 29.4, 13.4, and 64.0 ${\mu}M$, respectively. Furthermore, the kinetic analysis of PTP1B inhibition by compounds 1 and 5 suggested that compound 1 inhibited PTP1B activity in a noncompetitive manner, whereas compound 5 inhibited PTP1B activity in a competitive manner.

Synthesis and Biological Properties of Luotonin A Derivatives

  • Rahman, A. F. M. Motiur;Kim, Dong-Hyeon;Liang, Jing-Lu;Lee, Eung-Seok;Na, Young-Hwa;Jun, Kyu-Yeon;Kwon, Young-Joo;Jahng, Yurng-Dong
    • Bulletin of the Korean Chemical Society
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    • v.29 no.10
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    • pp.1988-1992
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    • 2008
  • A series of new derivatives on the ring A of luotonin A were prepared by Friedländer condensation of 6,7,8,10- tetrahydropyrrolo[2,1-b]quinazoline-6,10-dione and suitably substituted 2-aminobenzaldehydes and 2- aminoacetophenones. Their inhibitory activities on topoisomerases and cytotoxicities against selected human cancer cell lines were evaluated. Among the compounds tested, 8-fluoroluotonin A showed similar inhibitory activity on topoisomerase I comparable to camptothecin while luotonin A and 9-hydroxyluotonin A showed 1.37 and 0.94 times stronger inhibitory activity, respectively, on topoisomerase II compared to etoposide. Some derivatives of luotonin A showed moderate cytotoxicity. The possible relationship between the inhibitory activity on Topo II and the cytotoxicity of luotonin A and its analogues, thus, cannot be ruled out.

Inhibitory Effects of Naturally Occurring Flavonoids on Rat Lens Aldose Reductase

  • Jung, Sang-Hoon;Kang, Sam-Sik;Shin, Kuk-Hyun;Kim, Yeong-Shik
    • Natural Product Sciences
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    • v.10 no.1
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    • pp.35-39
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    • 2004
  • Aldose reductase (AR), the key enzyme of the polyol pathway, is known to play important roles in the diabetic complications. The inhibitors of AR, therefore, would be potential agents for the prevention of diabetic complications. In order to clarify the structural requirements of flavonoids for aldose reductase inhibitory activity, thirty flavonoids were examined. Among the thirty flavonoids, flavonols such as quercetin (5), reyneutrin (7), quercitrin (9), isoquercitrin (11), and avicularin (14) were found to exhibit much stronger AR inhibition. Lonicerin (10), amentoflavone (27) and sophoraflavanone B (30) were also showed strong inhibitory activity. Especially, quercitrin and reyneutrin exhibited the most inhibitory potency on rat lens (RL) AR. The results suggested that flavonol having the 7-hydroxyl and/or catechol moiety at the B ring exhibit strong activity. In addition, flavonols having 3-O-monosaccharide also showed stronger inhibition than free flavonols at the 3-position. These results suggested that quercitrin and reyneutrin are attributed to be the promising compounds for the prevention and/or treatment of diabetic complications.

Inhibitory effect of bacteriocin-producing lactic acid bacteria against histamine-forming bacteria isolated from Myeolchi-jeot

  • Lim, Eun-Seo
    • Fisheries and Aquatic Sciences
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    • v.19 no.10
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    • pp.42.1-42.10
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    • 2016
  • The objectives of this study were to identify the histamine-forming bacteria and bacteriocin- producing lactic acid bacteria (LAB) isolated from Myeolchi-jeot according to sequence analysis of the 16S rRNA gene, to evaluate the inhibitory effects of the bacteriocin on the growth and histamine accumulation of histamine-forming bacteria, and to assess the physico-chemical properties of the bacteriocin. Based on 16S rRNA gene sequences, histamine-forming bacteria were identified as Bacillus licheniformis MCH01, Serratia marcescens MCH02, Staphylococcus xylosus MCH03, Aeromonas hydrophila MCH04, and Morganella morganii MCH05. The five LAB strains identified as Pediococcus acidilactici MCL11, Leuconostoc mesenteroides MCL12, Enterococcus faecium MCL13, Lactobacillus sakei MCL14, and Lactobacillus acidophilus MCL15 were found to produce an antibacterial compound with inhibitory activity against the tested histamine-producing bacteria. The inhibitory activity of these bacteriocins obtained from the five LAB remained stable after incubation at pH 4.0-8.0 and heating for 10 min at $80^{\circ}C$; however, the bacteriocin activity was destroyed after treatment with papain, pepsin, proteinase K, ${\alpha}$-chymotrypsin, or trypsin. Meanwhile, these bacteriocins produced by the tested LAB strains also exhibited histamine-degradation ability. Therefore, these antimicrobial substances may play a role in inhibiting histamine formation in the fermented fish products and preventing seafood-related food-borne disease caused by bacterially generated histamine.

Screening and Classification of Actinomycetes Producing $\alpha$-Amylase Inhibitors and the Isolation, their Kinetic Studies of $\alpha$-Amylase Inhibitors ($\alpha$-Amylase 저해제 생산 방선균의 선별과 분류 및 $\alpha$-Amylase저해제의 분리와 Kinetics 연구)

  • 김제학;김정우;김하원;심미자;최응칠;김병각
    • Microbiology and Biotechnology Letters
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    • v.13 no.3
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    • pp.223-232
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    • 1985
  • To find microorganisms of producing $\alpha$-amylase inhibitors, actinomycetes were isolated from soil samples that were collected at different locations in Korea and screened for enzyme inhibitory activity. A strain of these microbes had a high inhibitory activity and was identified as one of the genus Streptomyces by morphological, biochemical and physiological studies according to the methods of the International Streptomyces Project (ISP). The medium used consisted of 3 % corn starch, 0.2% yeast extract and 0.8% peptone (pH 7.0). When this strain was aerobically cultured in the medium on a rotary shaker, the highest inhibitory activity was obtained after four days. This inhibitor had inhibitory activities on various $\alpha$-amylases and glucoamylase, but not on $\beta$-amylase.

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Scavenging Effects of Flavonoids on Paraquat Induced Toxicity (Paraquat 유독성에 대한 Flavonoid류의 독성경감효과)

  • 최병기;조내규
    • Environmental Analysis Health and Toxicology
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    • v.10 no.1_2
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    • pp.47-54
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    • 1995
  • To investigate and evaluated the scavenging and antioxidative effects of various flavonoids on paraquat induced toxicity, in vivo and vitro tests of eight flavonoids (catechin, epocatechin, flavone, chrysin, apigenin, quercetin, morin and biochanin A) were carried out. The generation of reactive oxygen substances(ROS) in PMS-NADH system $H_2O_2$ induced hemolysis and lipidperoxidation to blood, NADPH dependent lipidperoxidation to liver and lung microsome by paraquat were studied.The results are summerized as follows; 1) In the concentration ranges from 3.3 to 9.8$\mu$M of catechin,epicatechin, quercetin and biochanin A removed the 50% of DPPH radical scavenging effects. 2) In the concentration ranges from 0.60 to 1.86 mM of catechin, epicatechin, quercetin and biochanin A showed the inhibitory and antioxidative activity on superoxide anion which gernerated in PMA-NADH system. 3) In the concentration ranges from 0.12 to 0.49mM of catechin, epicatechin, quercetin and biochanin A showed the inhibitory and antioxidative activity on H202 which generated in PMA-NADH system. 4) In the concentration ranges from 0.6 x10$^{-5}$ to 6.3 x 10$^{-5}$mM of catechin, epicatechin, flavone, chrysin, quercetin and morin showed the inhibitory and antioxidative activity on $H_2O_2$ induced hemolysis to blood 5) All flavonoids tested exhibited inhibitory and antioxidative effects on paraquat induced liver and tung microsomal lipidperoxidation. Therefore, all flavonoids evaluated showed the useful compounds for scavenger and antioxidant on paraquat induced toxicity.

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Lignans with NADPH Oxidase 2 (NOX2)-inhibitory Activity from the Fruits of Schisandra chinensis

  • Park, Jung-Min;Pel, Pisey;Chin, Young-Won;Lee, Moo-Yeol
    • Natural Product Sciences
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    • v.24 no.1
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    • pp.59-65
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    • 2018
  • An isoform of NADPH oxidase (NOX), NOX2 is a superoxide-generating enzyme involved in diverse pathophysiological events. Although its potential as a therapeutic target has been validated, there is no clinically available inhibitor. Herein, NOX2-inhibitory activity was screened with the constituents isolated from Schisandra chinensis, which has been reported to have antioxidant and reactive oxygen species (ROS)-scavenging effects. Among the partitions prepared from crude methanolic extract, a chloroform-soluble partition showed the highest NOX2-inhibitory activity in PLB-985 cell-based NOX2 assay. A total of twenty nine compounds (1 - 29) were identified from the chloroform fraction, including two first isolated compounds; dimethyl-malate (25) and 2-(2-hydroxyacetyl) furan (27) from this plants. Of these constituents, two compounds (gomisin T, and pregomisin) exhibited an NOX2-inhibitory effect with the $IC_{50}$ of $9.4{\pm}3.6$, and $62.9{\pm}11.3{\mu}M$, respectively. They are confirmed not to be nonspecific superoxide scavengers in a counter assay using a xanthine-xanthine oxidase system. These findings suggest the potential application of gomisin T (6) and other constituents of S. chinensis to inhibit NOX2.

Inhibitory Effect of Pine Needle(Pinus densiflora S.) Extract on Potato Polyphenol Oxidase (감자 polyphenol oxidase에 대한 솔잎 추출물의 저해효과)

  • Lee, Min-Kyung
    • Journal of Life Science
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    • v.16 no.5
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    • pp.866-869
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    • 2006
  • The inhibitory effect of pine needle (Pinus densiflora S.) on potato polyphenol oxidase (PPO) was investigated. The addition of the pine needle extract exhibited a higher inhibitory effect on the potato polyphenol oxidase activity than that of the citric acid or potassium sorbate. The enzyme activity was strongly inhibited in a pH range of 7.0-8.0. When the incubation time of reaction mixture was increased, the potato polyphenol oxidase activity was markedly inhibited. The pine needle extract inhibited the potato polyphenol oxidase non-competitively. And also the pine needle extract subjected to a heat treatment at $100^{\circ}C$ for 10 min or to an acid treatment at pH 2.0, 3.0, and 4.0 for 3 hours still retained inhibitory effect on potato polyphenol oxidase.

Inhibitory Activity of Edible Plant Extracts on Proliferation of Human Umbilical Vein Endothelial Cells (HUVECs)

  • Song, Myoung-Chong;Kim, Sung-Hoon;Kwak, Ho-Young;Yang, Hye-Joung;Bang, Myun-Ho;Chung, In-Sik;Lee, Youn-Hyung;Baek, Nam-In
    • Journal of Applied Biological Chemistry
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    • v.50 no.4
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    • pp.249-253
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    • 2007
  • Thirteen edible plants previously reported to show inhibitory activities on farnesyl protein transferase (FPTase) and phosphatase of the regenerating liver-3 (PRL-3) were evaluated for inhibitory activity on the proliferation of human umbilical vein endothelial cells (HUVECs). Four plant extracts, Oenothera erythrosepala, Perilla frutescens, Panicum miliaceum, and Quercus acutissima, significantly inhibited the proliferation of HUVECs induced by the basic fibroblast growth factor (bFGF) without cytotoxicity at 100 ${\mu}g/mL$. Myristica fragrans, Rosmarinus officinalis, and Syringa patula also showed inhibitory activity on the proliferation with only mild cytotoxicity.