• 제목/요약/키워드: inhibitory compound

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6-트리아졸 엑소메칠렌펜남 유도체의 베타락타마제 효소억제력과 베타락탐항생제 병용시 활성비교 ([ ${\beta}$ ]-Lactamase Inhibitory Activity and Comparative Activity of 6-Triazole Exomethylenepenam Derivatives Combined with ${\beta}$-Lactam Antibiotics)

  • 임채욱;오정석;이선혜;김경원;임철부
    • 약학회지
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    • 제49권1호
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    • pp.51-55
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    • 2005
  • In vitro ${\beta}$-lactamase inhibitory activity of 6-triazole exomethylenepenam compounds (1, 2, 3, 4, 5 and 6) was compared with clavulanic acid, sulbactam and tazobactam. The inhibitory activity of 3, 4 and 5 was stronger than those of sulbactam, clavulanic acid and tazobactam against Type IV enzymes. And, inhibitory activity of 3 and 4 was stronger than those of sulbactam, clavulanic acid and tazobactam against Type III enzymes. The in vitro antimicrobial activity of 3, 4 and 5 combined with ampicillin was better than those with sulbactam and with cefoperazone was compared with the sulbactam against ${\beta}$-lactamase producing 27 strains. The synergistic activity of (Z)-form compounds (3 and 5) was better than that of (E)-form compound (4) and sulfone compound (5) was better than sulfide compound (3).

Compound 48/80과 anti-DNP IgE로 유도되는 비만세포 활성화에 대한 복분자의 억제효과 (Inhibitory Effect of Rubus Coreanus on Compound 48/80- or Anti-DNP IgE-Induced Mast Cell Activation)

  • 이광소;채옥희;송창호
    • IMMUNE NETWORK
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    • 제4권2호
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    • pp.100-107
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    • 2004
  • Background: The fruit of Rubus coreanus (RC), a perennial herb, has been cultivated for a long time as a popular vegetable. The anti-allergy mechanism of RC is unknown. The purpose of this study is to investigate the inhibitory effect of RC on compound 48/80- or anti-DNP IgE-induced mast cell activation. Methods: For this, influences of RC on the compound 48/80-induced degranulation, histamine release, calcium influx and the change of the intracellular cAMP (cyclic adenosine-3',5' monophosphate) levels of rat peritoneal mast cells (RPMC) and on the anti-DNP IgE-induced histamine release of RPMC were observed. Results: The pretreatment of RC inhibited compound 48/80-induced degranulation, histamine release and intracelluar calcium uptake of RPMC. The anti-DNP IgE-induced histamine release of RPMC was significantly inhibited by pretreatment of RC. The RC increased the level of intracellular cAMP of RPMC, and the pretreatment of RC inhibited compound 48/80-induced decrement of intracellular cAMP of RPMC. Conclusion: These results suggest that RC contains some substances with an activity to inhibit the compound 48/80- or anti-DNP IgE-induced mast cell activitation. The inhibitory effects of RC are likely due to the stabilization of mast cells by blocking the calcium uptake and enhancing the level of intracellular cAMP.

메밀의 생리활성 물질에 대한 여러 가지 비료의 효과 (The Effect of Several Fertilizers on Physiological Active Compounds of Buckwheat(Fagopyrum esculentum Moench))

  • 박인진;황태익;김희권
    • 한국토양비료학회지
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    • 제32권4호
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    • pp.440-445
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    • 1999
  • 메밀의 지방산 및 페놀화합물 생합성과 tyrosinase 저해 활성에 대한 몇가지 비료의 영향을 조사한 결과 다음과 같다. 메밀 식물체중의 지방산 함량은 곡류중의 지방산 함량 보다 작으며 메밀 식물체와 곡류중의 지방산은 포화지방산과 불포화지방산으로 구성되어 있으며 불포화지방산이 포화지방산보다 많은 것으로 나타났다. 메밀중의 페놀화합물은 $682.6{\sim}1822.0mg\;kg^{-1}$이며 석회 시용구의 메밀중 페놀화합물이 $1822.0mg\;kg^{-1}$로 다른 비료 시용구보다 높았다. 한편 석회가 시용된 메밀 곡류중의 sediment c의 tyrosinase 저해활성은 92.8%로 같은 처리내의 sediment c의 compound A, B, C 보다 높았다. 그러나 붕사가 처리된 메밀 곡류중의 compound C의 tyrosinase의 저해활성은 80.9%로 같은 처리구 내의 sediment나 다른 compound보다 높은 것으로 나타났다.

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Isolation of Bacteria Associated with the King Oyster Mushroom, Pleurotus eryngii

  • Lim, Yun-Jung;Ryu, Jae-San;Shi, Shanliang;Noh, Won;Kim, Eon-Mi;Le, Quy Yang;Lee, Hyun-Sook;Ro, Hyeon-Su
    • Mycobiology
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    • 제36권1호
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    • pp.13-18
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    • 2008
  • Eight distinct bacteria were isolated form diseased mycelia of the edible mushroom, Pleurotus eryngii. 16S rDNA sequence analysis showed that the isolates belonged to a variety of bacterial genera including Bacillus (LBS5), Enterobacter (LBS1), Sphingomonas (LBS8 and LBS10), Staphylococcus (LBS3, LBS4 and LBS9) and Moraxella (LBS6). Among them, 4 bacterial isolates including LBS1, LBS4, LBS5, and LBS9 evidenced growth inhibitory activity on the mushroom mycelia. The inhibitory activity on the growth of the mushroom fruiting bodies was evaluated by the treatment of the bacterial culture broth or the heat-treated cell-free supernatant of the broth. The treatment of the culture broths or the cell-free supernatants of LBS4 or LBS9 completely inhibited the formation of the fruiting body, thereby suggesting that the inhibitory agent is a heat-stable compound. In the case of LBS5, only the bacterial cell-containing culture broth was capable of inhibiting the formation of the fruiting body, whereas the cell-free supernatant did not, which suggests that an inhibitory agent generated by LBS5 is a protein or a heat-labile chemical compound, potentially a fungal cell wall-degrading enzyme. The culture broth of LBS1 was not inhibitory. However, its cell-free supernatant was capable of inhibiting the formation of fruiting bodies. This indicates that LBS1 may produce an inhibitory heat-stable chemical compound which is readily degraded by its own secreted enzyme.

노각나무 잎에서 분리된 플라보노이드에 의한 대식세포에서 산화질소 생성 억제효과 (Inhibitory Effects of Flavonoids Isolated from the Leaves of Stewartia koreana on Nitric-oxide Production in LPS-stimulated RAW 264.7 Cells)

  • 이승수;방면호;박세호;정대균;양선아
    • 생명과학회지
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    • 제28권5호
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    • pp.509-516
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    • 2018
  • 노각나무(Stewartia koreana) 잎 에틸아세테이트 분획으로부터 quercetin (1), quercitrin (2), hyperin (3), quercetin-3-O-(6"-O-galloyl)-${\beta}$-D-galactopyranoside (4), kaempferol-3-o-[2",6"-di-o-(trans-p-coumaroyl)]-${\beta}$-D-glucopyranoside (5)의 5종의 플라보노이드를 분리하였으며, 이들 5종 성분의 염증 반응에 대한 활성을 분석하기 위하여 LPS를 처리한 대식세포에서 산화질소(NO) 생성 억제활성을 측정하였다. 이들 5종 성분 중 compound 4, 5는 노각나무에서 처음으로 분리된 것으로 항염증 활성에 대한 보고도 없다. 분광분석법으로 확인된 노각나무 잎 유래 성분들은 LPS 처리한 대식세포의 NO 생성을 유의적으로 저해하였으며, 특히 kaempferol-3-o-[2",6"-di-o-(transp-coumaroyl)]-${\beta}$-D-glucopyranoside (5)는 가장 강한 억제효과(17.17%, 5.0%, 3.92%, 6.32% and 63.35% inhibition of compound 1, 2, 3, 4 and 5 at $10{\mu}g/ml$)를 나타냈다. 또한, 이러한 NO 생성 억제효과는 inducible nitric oxide synthase(iNOS) 단백질 발현 억제를 통한 것으로 나타났다. 따라서, 본 연구에서 새로 분리된 플라보놀인 kaempferol-3-o-[2",6"-di-o-(trans-p-coumaroyl)]-${\beta}$-D-glucopyranoside (5)는 노각나무 잎의 항염증 활성을 나타내는 주요 물질로 사료된다.

Inhibition of Klebsiella pneumoniae ATCC 13883 Cells by Hexane Extract of Halimeda discoidea (Decaisne) and the Identification of Its Potential Bioactive Compounds

  • Supardy, Nor Afifah;Ibrahim, Darah;Sulaiman, Shaida Fariza;Zakaria, Nurul Aili
    • Journal of Microbiology and Biotechnology
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    • 제22권6호
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    • pp.872-881
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    • 2012
  • The inhibitory effect of the Klebsiella pneumoniae ATCC 13883 strain caused by the hexane extract of Halimeda discoidea (Nor Afifah et al., 2010) was further evaluated by means of the microscopy view and its growth curves. The morphological changes of the K. pneumoniae ATCC 13883 cells were observed under the scanning electron microscope (SEM) and transmission electron microscope (TEM) after they were treated at minimum inhibitory concentration (MIC; 0.50 mg/ml) (Nor Afifah et al., 2010) for 12, 24, and 36 h. The results showed the severity of the morphological deteriorations experienced by the treated cells. The killing curve assay was performed for 48 h at three different extract concentrations (1/2 MIC, MIC, and 2 MIC). An increase in the extract concentration of up to 2 MIC value did significantly reduce the number of cells by approximately 1.9 $log_{10}$, as compared with the control. Identification of the potential compounds of the extract responsible for the antibacterial activity was carried out through the gas chromatography-mass spectrum (GC-MS) analysis of the active subfraction, and the compound E-15-heptadecenal was identified and suggested as the most potential antibacterial compound of this extract. The subsequent cellular degenerations showed by the data might well explain the inhibitory mechanisms of the suggested antibacterial compound. All of these inhibitory effects have further proven the presence of an antibacterial compound within H. discoidea that can inhibit the growth of K. pneumoniae ATCC 13883.

Compound 48/80 유도 즉시형 과민반응에 대한 뱀차즈기의 억제효과 (Inhibitory Effect of Salvia plebeia on Compound 48/80-Induced Immediate Hypersensitivity Reaction)

  • 최용길;김상현;임종필;김대근;엄동옥;이경보;김상용;신태용
    • 생약학회지
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    • 제32권4호통권127호
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    • pp.297-301
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    • 2001
  • We studied the inhibitory effect of the aqueous extract of Salvia plebeia (SPAE) on immediate hypersensitivity reactions. SPAE inhibited immediate hypersensitivity reaction induced by compound 48/80 in mice. When SPAE was employed in an immediate hypersensitivity reaction test, the plasma histamine levels were reduced in a dose-dependent manner. SPAE also inhibited the histamine release from rat peritoneal mast cells (RPMC) by compound 48/80. The level of cAMP in RPMC, when SPAE was added, significantly increased compared with that of a normal control. These results indicate that SPAE may be beneficial in the treatment of immediate hypersensitivity reactions.

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Synergistic Antibacterial Activity of an Active Compound Derived from Sedum takesimense against Methicillin-Resistant Staphylococcus aureus and Its Clinical Isolates

  • Jeong, Eun-Tak;Park, Seul-Ki;Jo, Du-Min;Khan, Fazlurrahman;Choi, Tae Ho;Yoon, Tae-Mi;Kim, Young-Mog
    • Journal of Microbiology and Biotechnology
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    • 제31권9호
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    • pp.1288-1294
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    • 2021
  • There are a growing number of reports of hospital-acquired infections caused by pathogenic bacteria, especially methicillin-resistant Staphylococcus aureus (MRSA). Many plant products are now being used as a natural means of exploring antimicrobial agents against different types of human pathogenic bacteria. In this research, we sought to isolate and identify an active molecule from Sedum takesimense that has possible antibacterial activity against various clinical isolates of MRSA. NMR analysis revealed that the structure of the HPLC-purified compound was 1,2,4,6-tetra-O-galloyl-glucose. The minimum inhibitory concentration (MIC) of different extract fractions against numerous pathogenic bacteria was determined, and the actively purified compound has potent antibacterial activity against multidrug-resistant pathogenic bacteria, i.e., MRSA and its clinical isolates. In addition, the combination of the active compound and β-lactam antibiotics (e.g., oxacillin) demonstrated synergistic action against MRSA, with a fractional inhibitory concentration (FIC) index of 0.281. The current research revealed an alternative approach to combating pathogenesis caused by multi-drug resistant bacteria using plant materials. Furthermore, using a combination approach in which the active plant-derived compound is combined with antibiotics has proved to be a successful way of destroying pathogens synergistically.

현호색의 Acetylcholinesterase 활성 저해 성분 및 그 작용기전 (An Acetylcholinesterase Inhibitor Isolated from Corydalis Tuber and Its Mode of Action)

  • 황세영;장영표;변순정;전미희;김영중
    • 생약학회지
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    • 제27권2호
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    • pp.91-95
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    • 1996
  • In the course of searching for acetylcholinesterase inhibitors from crude drugs, it was found that total MeOH extract of Corydalis Tuber showed significant inhibitory effect on acetylcholinesterase. To isolate acetylcholinesterase inhibitors from Corydalis Tuber, total MeOH extract of the the crude drug was subjected to activity guided fractionation. The MeOH extract was suspended in water and fractionated with methylene chloride and subjected to acid-base fractionation. Silica gel column chromatography of the basic fraction which showed significant inhibitory effect on acetylcholinesterase was carried out and 5 subfractions (1-5) were obtained. From subtraction 4, compound I was isolated. The structure of isolated compound I was identified by spectroscopic parameters of $^1H-NMR$, $^{13}C-NMR$, EI-MS and FAB-MS. The compound I was identified as berberine. It was found from the Lineweaver-Burk plot that berberine was a reversible and specific inhibitor of acetylcholinesterase having 90% inhibitory effect at the concentration of $2.5{\mu}M$.

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Production of a Phytotoxic Compound, 3-Phenylpropionic Acid by a Bacterial Endophyte, Arthrobacter humicola YC6002 Isolated from the Root of Zoysia japonica

  • Chung, Eu-Jin;Park, Joo-Hwang;Park, Tae-Soon;Ahn, Jong-Woong;Chung, Young-Ryun
    • The Plant Pathology Journal
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    • 제26권3호
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    • pp.245-252
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    • 2010
  • An endophytic bacterial strain, Arthrobacter humicola YC6002, was isolated from a surface sterilized root of Korean turf grass (Zoysia japonica) collected from Jinju, Korea. This strain showed inhibitory effect on germination and shoot growth of radish. The inhibition of germination and shoot growth of radish seeds varied depending on the age of culture and the temperature at which it was incubated. The culture filtrate of 1/10-strength Tryptic Soy Broth medium, incubated for 48 hours at $30^{\circ}C$, showed the highest inhibitory effect on radish seed germination and shoot growth (92% inhibition as compared to control). The active compound with seed germination and shoot growth inhibition was purified and identified as 3-phenylpropionic acid. The purified compound had 53% and 93% inhibitory effect on seed germination and shoot growth of radish for 500 and 1000 ppm solutions, respectively.