• Title/Summary/Keyword: Inhibitory Activity

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Synthesis and $\beta$-lactamase inhibitory activity of 6-exomethylene penamsulfone derivatives-III (In vitro $\beta$-lactamase inhibitory activity and comparative susceptibility test of 6-exomethylene penamsulfone derivatives)

  • Park, Hee-Suk;Yoon, Sang-Bae;Chaeuk Im;Yim, Chul-Bu
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1997.04a
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    • pp.72-72
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    • 1997
  • 합성한 5종의 6-Exomethylene penamsulfone 유도체의 Type I, Type II, Type III, TypeIV, TEM 효소에 대한 $\beta$-lactamase저해효과를 spectrophotometric assay방법으로 측정하였다. 또한 여기서 우수한 효소억제활성을 보여준 3종의 화합물을 가지고 In vitro antibacterial activity를 Agar dilution method법으로 27종의 $\beta$-lactamase생성균주에 대하여, Sulbactam, Ampicillin 및 Cefoperazone과 병용투여하여 MIC를 측정하였다.

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Influence of Garlic and Red Pepper on the Microflora of Kajami Shik-hae

  • MoussaSouane;Lee, Cherl-Ho
    • Proceedings of the Korean Society for Applied Microbiology Conference
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    • 1986.12a
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    • pp.516.1-516
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    • 1986
  • Kajami Shik-hae processing consists of the fermentation of low salted Kajami (6% NaCl maximum) coated with a vegetable mixture, composed with cooked millet, red pepper, garlic and ginger. Lactic bacteria are the main component of the microflora. In order to determine their eventual selective role on the microflora the antimicrobial activity of garlic and red pepper was tested with some strain of bacteria and molds isolated from Shik-hae and Shik-hae raw materials. And the influence of their concentration in Kajami Shik-hae on the microflora was also checked. At the concentration of 10% garlic have no inhibitory activity against lactic bacteria but on strains of Bacillus, Micrococcus and Aspergillus niger. At the concentration of 20% red pepper showed a slight inhibitory activity on two strains of Bacillus. These results shows that red pepper and garlic are not only flavoring ingredients but they might play an important role in the control of the microflora growth and composition during Kajami Shik-hae fermentation.

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Tyrosinase Inhibitor from the Flowers of Impatiens balsamina

  • Lim, Young-Hee;Kim, In-Hwan;Seo, Jung-Ju;Kim, Jeong-Keun
    • Journal of Microbiology and Biotechnology
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    • v.16 no.12
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    • pp.1977-1983
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    • 2006
  • Kaempferol was isolated and identified from the methanol extract of the flowers of Impatiens balsamina. Kaempferol showed inhibitory activity against mushroom tyrosinase with an $ID_{50}$ of 0.042 mM. Inhibition kinetics, as determined using a Lineweaver-Burk plot, showed kaempferol to be a competitive inhibitor of mushroom tyrosinase with a $K_i$ value of 0.011 mM. The lag phase of tyrosine hydroxylation catalyzed by mushroom tyrosinase clearly increased on increasing the concentration of kaempferol. In addition to its tyrosinase inhibiting activity, kaempferol strongly inhibited melanin production by Streptomyces bikiniensis, in a dose-dependent manner, without inhibiting cell growth. For comparative purposes, the tyrosinase inhibitory activity of kaempferol was also assayed versus quercetin, a positive standard.

Antioxidant and Anti-inflammatory Activities of Allium victorialis subsp. platyphyllum Extracts

  • Lee, Je-Hyuk;Choi, Soo-Im;Lee, Yong-Soo;Kim, Gun-Hee
    • Food Science and Biotechnology
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    • v.16 no.5
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    • pp.796-801
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    • 2007
  • This study was conducted to investigate antioxidant activity and anti-immunological inflammatory effect of Allium victorialis subsp. platyphyllum extracts (AVPEs). Antioxidant activities of AVPEs were determined by free radical scavenging assay and reducing power test. Leaf-part extract had comparatively better antioxidant activity than other-part extracts. Antioxidant activity of extracts had protective effect for human umbilical vein endothelial cells (HUVECs) against superoxide anions secreted from activated neutrophils. Also, we observed AVPEs had inhibitory effects on the adherence of monocytic THP-1 to HUVEC monolayer to the basal level. Inhibitory effect on cell adhesion was caused by suppression of tumor necrosis factor-${\alpha}\;(TNF-{\alpha})-upregulated$ expression of vascular cellular adhesion molecule-1 (VCAM-1) and E-selectin in HUVECs. From these results, we expect to support the evidence of anti-immunological inflammatory effects of Allium victorialis subsp. platyphyllum (AVP) as a Korean traditional pharmaceutical.

Isolation of 6,6'-Bieckol from Grateloupia elliptica and its Antioxidative and Anti-Cholinesterase Activity

  • Lee, Bong Ho;Choi, Byoung Wook;Lee, Soo Young
    • Ocean and Polar Research
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    • v.39 no.1
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    • pp.45-49
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    • 2017
  • During the search for anticholinesterase compounds from marine organisms, we were able to isolate 6,6'-bieckol from a red alga, Grateloupia elliptica. This compound showed moderate acetylcholinesterase (AChE) inhibitory activity in a micromole range ($IC_{50}$ $44.5{\mu}M$). However, for butyrylcholinesterase (BuChE), a new target for the treatment of Alzheimer's disease (AD), it showed particularly potent inhibitory activity ($IC_{50}$ $27.4{\mu}M$), which is more potent compared to AChE. It also inhibits BACE-1, a new target for reducing the generation of ${\beta}-amyloid$.

Inhibitory Effects of Plant Extracts on Adjuvant-induced Arthritis

  • Kim, Sung-Yong;Son, Kun-Ho;Chang, Hyun-Wook;Kang, Sam-Sik;Kim, Hyung-Pyo
    • Archives of Pharmacal Research
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    • v.20 no.4
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    • pp.313-317
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    • 1997
  • Twenty seven plant extracts were selected on the basis of ancient literature search for rheurnatoid arthritis or similar syndrome. Methanol extract of each plant was prepared and administered orally to rats everyday at a dose of 200 mg/kg/day. Experimental arthritis was induced by subplantar injection of heat-killed Mycobacterium butyricum to right hind paw of rats. This treatment provoked swelling of the treated paw in two phases, acute primary swelling and secondary arthritic swelling. An inhibition of secondary swelling was considered to be antiarthritic activity. Several plant methanol extracts such as Akebia quinata (caulis), Ephedla sinica (herba) and 5ophorae subprostratd (radix) were found to show significant inhibitory activity against secondary swelling at the dose tested. Our results strongly suggested an antiarthritic potential of these plant extracts.

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Inhibition of Nitric Oxide Production by the Extracts of Hibiscus manihot (황촉규 추출물의 Nitric Oxide 생성 저해활성)

  • Park, Eun-Young;Yang, Ki-Sook
    • YAKHAK HOEJI
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    • v.52 no.4
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    • pp.259-263
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    • 2008
  • Anti-inflammatory activity of the extracts of Hibiscus manihot was investigated through the evaluation of its inhibitory effect on the production of inflammatory biomarkers (i-NOS, COX-2) in RAW264.7 murine macrophage cells. Among the sequential solvent fractions (hexane, dichloromethane, ethyl acetate, n-butanol and water), the fractions of dichloromethane (1 ${\mu}g/ml$) and ethyl acetate (5 ${\mu}g/ml$) showed potential inhibitory activities on i-NOS and COX-2 activity in RAW264.7 cells. These results suggest that Hibiscus manihot might have an anti-inflammatory activity through the suppression of inflammatory markers.

Inhibition of Aromatic L-Amino Acid Decarboxylase (AADC) by Some Phenolic Compounds from Medicinal Plants (천연 페놀성 화합물들의 방향족 아미노산 탈탄산효소 저해작용)

  • Ryu, Shi-Yong;Han, Yong-Nam;Han, Byung-Hoon
    • YAKHAK HOEJI
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    • v.38 no.6
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    • pp.791-794
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    • 1994
  • Sixteen kinds of naturally occurring phenolic compounds including 5 stilbenes, 7 flavonoids and 4 anthraquinones were examined in the inhibitory activity against rat liver AADC(aromatic L-amino acid decarboxylase) in vitro, using 5-hydroxytryptophan as a substrate. Three hydroxystilbenes, resveratrol 1, rhapontigenin 3 and piceatanol 5, which were known to be monoamine oxidase A inhibitors, exhibited a significant inhibition against AADC($IC_{50}$=20, 8 and $5\;{\mu}M$, respectively). By the comparison of the activity of each phenolic compound, it was suggested that the 3',4'-dihydroxyphenyl group of stilbenes or flavones was the best pharmacophore for the AADC inhibitory activity.

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Physico-chemical Characteristics and Antiviral Activity of ASA, an Antibiotic Produced by Actinomycetes B25 (방선균 B25 균주가 생산하는 항생물질 ASA의 물리.화학적 특성 및 항바이러스 활성)

  • 여운형;김영호;박은경;김상석
    • Korean Journal Plant Pathology
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    • v.13 no.1
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    • pp.63-68
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    • 1997
  • In the screening of antiviral materials produced by actinomycetes, an isolate named B25 was fond to produce an antibiotic substance ASA, which showed a strong inhibitory activity against tobacco mosaic virus (TMV) infection. ASA was purified from culture broth of B25 by silica gel column chromatography, preparative TLC, and reversed phase HPLC. Also MS, IR, UV spectrum, and melting point of ASA were determined and analysed. ASA was white powder soluble in dimethyl sulfoxide, chloroform, and ethyl acetate, having absorption peaks at 223 and 328 nm in UV-VIS spectrum, and had a molecular weight of 548. ASA showed strong inhibitory effect on TMV infection when it was applied as a mixture of TMV to the upper surface of leaves of a local lesion host (Nicotiana tabacum c. Xanthi-nc). It also showed antimicrobial effect against yeast and some phytopathogenic fungi.

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Boron Trifluoride Etherate on Silica-A Modified Lewis Acid Reagent (VII). Antitumor Activity of Cannabigerol Against Human Oral Epitheloid Carcinoma Cells

  • Baek, Seung-Hwa;Kim, Young-Ok;Kwag, Jung-Suk;Choi, Kyw-Eun;Jung, Woo-Young;Han, Du-Seok
    • Archives of Pharmacal Research
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    • v.21 no.3
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    • pp.353-356
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    • 1998
  • Geraniol (1), olivetol (2), cannabinoids (3 and 4) and 5-fluorouracil (5) were tested for their growth inhibitory effects against human oral epitheloid carcinoma cell lines (KB) and NIH 3T3 fibrobalsts using two different 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay and sulforhodamine B protein (SRB) assay. Cannabigerol (3) exhibited the highest growth-inhibitory activity against the cancer cell lines.

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