• Title/Summary/Keyword: Inhibitory Activity

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Prolyl Endopeptidase Inhibitory Activity of Two Styrylpyranones from Phellinus linteus

  • Yoon, Hye-Ryeon;Han, Ah-Reum;Paik, Young-Sook
    • Journal of Applied Biological Chemistry
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    • v.56 no.3
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    • pp.183-185
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    • 2013
  • Two styrylpyranones (1 and 2) were isolated from the $CH_2Cl_2$-soluble fraction of Phellinus linteus and their structures were established by extensive Nuclear magnetic resonance (NMR) spectral data as inoscavin E and C. Both compounds showed significant prolyl endopeptidase inhibitory activity with $IC_{50}$ values of $4.26{\pm}0.14$ and $4.08{\pm}0.04{\mu}M$ and $K_i$ values of $1.50{\pm}0.02$ and $1.43{\pm}0.03{\mu}M$, respectively. They also exhibited antioxidant capacities against the ABTS radical system with $EC_{50}$ values of $6.47{\pm}0.05$ and $7.64{\pm}0.06{\mu}M$, respectively.

Prolyl Endopeptidase Inhibitory Activity of Ursolic and Oleanolic Acids from Corni Fructus

  • Park, Yoon-Seok;Jang, Hyun-Jung;Paik, Young-Sook
    • Journal of Applied Biological Chemistry
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    • v.48 no.4
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    • pp.207-212
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    • 2005
  • Prolyl endopeptidase (PEP, EC 3.4.21.26), also referred to as prolyl oligopeptidase, has been suggested to participate in learning and memory processes by cleaving peptide bonds on carboxyl side of prolyl residue within neuropeptides of less than 30 amino acids, and is abundant in brains of amnestic patients. Therefore, compounds possessing PEP inhibitory activity can be good candidate of drug against memory loss. Upon examination for PEP inhibition from traditional medicinal plants having tonic, stimulating, and anti-amnestic effects, Corni Fructus (Cornus officinallis) showed significant PEP inhibition. Ursolic and oleanolic acids, components of Corni Fructus, inhibited PEP with $IC_{50}$ values of $17.2\;{\pm}\;0.5$ and $22.5\;{\pm}\;0.7\;{\mu}M$, respectively.

Synthesis and Melanoma Inhibitory Activity of New Aminoisoquinolinylamide Derivatives (새로운 Aminoisoquinolinylamide 유도체의 합성 및 흑색종 저해 효능)

  • Yoo, Kyung-Ho;Cho, Hye-Jung
    • Journal of the Korean Applied Science and Technology
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    • v.26 no.2
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    • pp.161-170
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    • 2009
  • In this work, a novel series of aminoisoquinolinylamide derivatives 1a-c and 2a-f were synthesized via several reaction steps, starting from 2-methyl-4-nitrobenzonitrile (3) and 1-chloro-5-nitroquinoline (8). And their antiproliferative activities were screened against A375 human melanoma cell line compared to Sorafenib as a reference compound. Among them, compound 1b and 1c exhibited meaningful inhibitory activities. These results demonstrated that aminoisoquinolinylamide scaffold possesses the possibility as the treatment for melanoma.

Purification and Characterization of Trypsin Inhibitor from Alismatis Rhizoma and its Binding Protein, 10-Formyltetrahydrofolate Dehydrogenase (택사(Alismatis Rhizoma)로부터 트립신 저해제의 정제와 특성 규명 및 이와 결합하는 단백질, 10-Formyltetrahydrofolate Dehydrogenase에 관한 연구)

  • Kim, Ji-Man;Park, Jong-Ok;Shin, Young-Hee
    • YAKHAK HOEJI
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    • v.52 no.1
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    • pp.79-84
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    • 2008
  • Alismatis Rhizoma has been used as diuretics and antiphlogistics in the Chinese oriental medicine. A trypsin inhibitor was isolated from Alismatis Rhizoma using DEAE ion exchange column, trypsin affinity column, and FPLC chromatography, and its activity and characteristics were studied. The purifed Alismatis Rhizoma trypsin inhibitor (ARTI) was estimated to be about 22 kDa. The sequence determination on N-terminal amino acid residues and 84 amino acid residues has been completed, yet no homology has been found with trypsin inhibitors reported at NCBI. ARTI did not show inhibitory activities on chymotrypsin and elastase, however it exhibited a significant inhibitory activity on bovine trypsin, and formed a complex with rat liver 10-formyltetrahydrofolate dehydrogenase.

Inhibitory Activity of 8-Aminowogonin Analogues Against Prostaglandin $E_2$ Production (8-아미노우고닌 유도체의 Prostaglandin $E_2$ 생성에 대한 저해작용)

  • Jang, Jin-Hee;Sin, Kwan-Seog;Kim, Hyun-Pyo;Park, Hae-Il
    • YAKHAK HOEJI
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    • v.52 no.1
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    • pp.85-91
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    • 2008
  • 8-Acyl and 8-sulfonylamidowogonin analogues were synthesized as potential anti-inflammatory agents. Nitration of 5,7-dihydroxyflavone (chrysin) followed by methylation of phenol groups and reduction of nitro group yielded 8-aminowogonin analogues. Acylation and sufonylation of 8-aminowogonin followed by demethylation reactions gave the title compunds. The synthesized wogonin analogues showed much reduced inhibitory activity on prostaglandin $E_2\;(PGE_2)$ production.

Production of Antihypertensive Angiotensin I-Converting Enzyme Inhibitor from Malassezia pachydermatis G-14

  • Jeong, Seung-Chan;Kim, Jae-Ho;Kim, Na-Mi;Lee, Jong-Soo
    • Mycobiology
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    • v.33 no.3
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    • pp.142-146
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    • 2005
  • To produce a novel antihypertensive angiotensin I-converting enzyme (ACE) inhibitor from yeast, a yeast isolate, designated G-14 showing the highest ACE inhibitory activity was obtained and identified as Malassezia pachydermatis based on morphological, biochemical and cultural characteristics. The maximal extracellular ACE inhibitor production was obtained from M. pachydermatis G-14 when the strain was cultured in YEPD medium containing 0.5% yeast extract, 3.0% peptone and 2.0% glucose at $30^{\circ}C$ for 24 h and the final ACE inhibitory activity was 48.9% under the above condition.

Microbiological Characteristics and Physiological Functionality of New Records of Yeasts from Wild Flowers in Yokjido, Korea

  • Hyun, Se-Hee;Lee, Jong-Soo
    • Mycobiology
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    • v.42 no.2
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    • pp.198-202
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    • 2014
  • Two new yeast records, Cryptococcus adeliensis YJ19-2 and Cryptococcus uzbekistanensis YJ10-4 were screened from 60 yeasts strains that were isolated and identified from wild flowers in Yokjido, Gyeongsangnam-do, Korea. The morphological and cultural characteristics of the newly recorded yeasts and the physiological functionalities of the supernatants and cell-free extracts obtained from their cultures were investigated. The two newly recorded yeasts did not form ascospores and pseudomycelia. They also grew well in yeast extract-peptone-dextrose broth. C. uzbekistanensis YJ10-4 grew in a vitamin-free medium and was also tolerant to sugar and salt. Antihypertensive angiotensin I-converting enzyme inhibitory activity of the supernatant from C. adeliensis YJ19-2 was high (71.8%) and its cell-free extract also showed very high (81.2%) antidiabetic $\acute{a}$-glucosidase inhibitory activity.

The Inhibitory Effects of Poncirin against Nickel Induced Cytotoxicity (Poncirin의 니켈에 대한 세포독성억제효과)

  • Yang, Seung-Jin;Kwak, Dong-Keun;Han, Du-Suk
    • The Korea Journal of Herbology
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    • v.21 no.2
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    • pp.121-127
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    • 2006
  • Objectives : Nickel is a major metal used in the nickel-chromium alloys of most orthodontic appliances, partial denture and implants. This study was carried out for the examination of the cytotoxicity on nickel sulfide in cultured NIH3T3 fibroblasts, and poncirin effect on nickel-induced cytotoxicity. Methods : Cell viability for the MTT assay and cell adhesion activity for the XTT assay. Results : The $IC_{50}$ of nickel sulfide by the MTT assay was $93.7\;{\mu}M$. Poncirin was significantly increased the cell viability and cell adhesion activity. Conclusion : Nickel was highly toxic and poncirin has the inhibitory effects against nickel induced cytotoxicity.

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Composition of Methanol Extract from Hwangryeon (Coptidis rhizoma) and Antimicrobial Activity against Food Spoilage and Foodborne Disease Microorganisms

  • Lim, Mee-Kyoung;Kim, Mee-Ra
    • International Journal of Human Ecology
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    • v.7 no.1
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    • pp.145-153
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    • 2006
  • Hwangryeon (Coptidis rhizoma) was extracted by methanol and its antimicrobial activities against food spoilage and foodborne disease microorganisms were investigated by the paper-disc method. The microorganisms used in this experiment included 5 species of bacteria (Escherichia coli, Pseudomonas aeruginosa, Salmonella typhimurium, Klebsiella pneumoniae, and Staphylococcus aureus) and 3 species of fungi (Fusarium solani, Aspergillus flavus, and Penicillium citreonigrum). The Hwangryeon extract showed antimicrobial effect against P. aeruginosa, S. aureus, S. typhimurium, and K. pneumonia. The minimum inhibitory concentration on S. aureus, S. typhimurium, and K. pneumoniae was 300 mg/mL, but on P. aeruginosa it was 200 mg/mL. In the methanol extracts from Hwangryeon, 190 compounds were separated by GC/MS. The extraction yields of phenols, furans, alcohols, acids and esters, ketones, and miscellaneous compounds were 28.10%, 2.67%, 1.79%, 12.89%, and 2.35%, respectively. The phenolic compounds, generally understood to be an antimicrobial active substance, was measured at 28.10%, a relatively remarkable amount.

Anticancer Activity of Phytol and Eicosatrienoic Acid Identified from Perilla Leaves (들깻잎에서 동정된 Phytol과 Eicosatrienoic Acid의 암세포 증식억제 효과)

  • 박건영;이경임;이숙희
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.28 no.5
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    • pp.1107-1112
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    • 1999
  • We investigated the inhibitory effects of phytol and methyl 11,14,17 eicosatrienoic acid (methyl ETA, n 3, 20 : 3) separated from perilla leaves on the growth of human cancer cells. Phytol inhibited significantly the growth of HT 29 human colon cancer cells, MG 63 osteosarcoma cells and AZ 521 gastric cancer cells. Although the activity of methyl ETA was lower than that of phytol, it was also observed to have the inhibitory effect on three human cancer cell lines. Furthermore, the DNA synthesis of the MG 63 osteosarcoma cells was markedly decreased by the addition of the phytol and methyl ETA. These results suggest that phytol and methyl ETA identified from the perilla leaves may play a role on the growth inhibition of the human cancer cells.

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