• 제목/요약/키워드: Selective Mechanism

검색결과 444건 처리시간 0.032초

Virulence, Resistance Genes, and Transformation Amongst Environmental Isolates of Escherichia coli and Acinetobacter spp.

  • Doughari, Hamuel James;Ndakidemi, Patrick Alois;Human, Izanne Susan;Benade, Spinney
    • Journal of Microbiology and Biotechnology
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    • 제22권1호
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    • pp.25-33
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    • 2012
  • The association of verotoxic E. coli and Acinetobacter spp. with various antibiotic-resistant, diarrhogenic, and nosocomial infections has been a cause for concern worldwide. E. coli and A. haemolyticus isolated on a number of selective media were screened for virulence factors, antibiotic resistance, and transformation of resistance genes. Out of 69 E. coli isolates obtained, 25 (35.23%), 14 (20.30%), and 28 (40.58%) were positive for Vtx1&2, Vtx1, and Vtx2, respectively, 49 (71.015%) for extendedspectrum beta-lactamases (ESBLs), 34 (49.28%) for serum resistance, 57 (82.61%) for cell surface hydrophobicity, 48 (69.57%) for gelatinase production, and 37 (53.62%) for hemolysin production. For the 14 A. haemolyticus isolates, only 2 (14.29%) in each case from all the samples investigated were positive for Vtx1, Vtx2 and Vtx1&2 respectively, 8 (57.14%) for ESBLs, 7 (50.00%) for serum resistance, 11 (78.57%) for cell surface hydrophobicity, 4 (28.57%) for gelatinase production, and 8 (57.14%) for hemolysin production. Although transformation occurred among the E. coli and Acinetobacter isolates (transformation frequency: $13.3{\times}10^{-7}-53.4^{-7}$), there was poor curing of the plasmid genes, a confirmation of the presence of stable antibiotic-resistant genes (DNA concentration between 42.7 and 123.8 ${\mu}g$) and intragenetic transfer of multidrug-resistant genes among the isolates. The isolates were potentially virulent and contained potentially transferable antibiotic resistance genes. Detection of virulence factors, antibiotic resistance genes, and transformation among these isolates is a very significant outcome that will influence approaches to proactive preventive and control measures and future investigations. However, continued surveillance for drug resistance among these bacteria and further investigation of the mechanism of action of their virulence factors are a necessity.

감초 물 추출물 및 Glycyrrhizin이 인체 간 Microsome에서 Cytochrome P450 약물대사효소에 미치는 영향 (Inhibitory Effect of Licorice Ethanol Extracts and Glycyrrhizin on Cytochrome P450 Drug-Metabolizing Enzymes in Human Liver Microsomes)

  • 박종훈;박지영;주영승
    • 대한예방한의학회지
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    • 제7권2호
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    • pp.65-74
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    • 2003
  • Objective : The aim of present study is to evaluate the inhibitory potential of licorice extract and glycyrrhizin on cytochrome P450(CYP) in human liver microsomes. Methods : Using human liver microsomes, water extract of licorice and glycyrrhizin as an inhibitor were co-incubated with each probe drug representing selective CYP isoform activity. We measured relative metabolic activity in incubation condition compared to that with no extract of licorice using HPLC system. Results : Both water extracts of licorice and glycyrrhizin showed inhibitory effect on CYP-catalyzed reactions. CYP2C19 $(IC_{50}=126.7{\mu}g/ml)$ is most potently inhibited by water extract than other tested CYP isoforms$(IC_{50}>450{\mu}g/ml)$, but glycyrrhizin exhibited potent inhibition on CYP1A2$(IC_{50}=106.9{\mu}g/ml)$ followed by CYP2C9 and CYP2D6. Conclusion: These results indicate that water extract of licorice and glycyrrhizin have inhibitory potential on CYP-catalyzed reaction in human liver microsomes. But the mechanism of inhibition was slightly different between them Water extract of licorice mainly inhibited CYP2C19, and glycyrrhizin primarily inhibited CYP1A2. The inhibition by water extract of licorice and glycyrrhizin on CYP isoforms may cause drug interaction with co-administered drug leading to toxicity or treatment failure.

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Effects of Novel Potassium Channel Opener KR-30450 and its Metabolite KR-30818 on the Smooth, Muscle of the Guinea Pig

  • Jung, Yi-Sook;Moon, Chang-Hyun;Yoo, Sung-Eun;Shin, Hwa-Sup
    • Biomolecules & Therapeutics
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    • 제4권4호
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    • pp.373-377
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    • 1996
  • The effect of potassium channel openers, KR-30450, KR-30818 and lemakalim have been compared against several spasmogens in guinea pig bronchi. In guinea pig bronchi, KR-30450 had a greater relaxant effect than lemakalim and KR-30818 against tone induced by histamine $10^{-5}M$ ($EC_{50}$ $\mu$M: KR-30450, 0.108$\pm$0.077; KR-30818, 0.403$\pm$0.023; lemakalim, 0.968$\pm$0.036) and prostaglandin $F_{2\alpha} 3\times10^{-6} M$ ($EC_{50}$ $\mu$M: KR-30450, 0.018$\pm$0.001; KR-30818, 0.028$\pm$0.003; lemakalim, 0.138$\pm$0.019). Relaxant effect of KR-30450 and KR-30818 were significantly reduced by 20 min pretreatment of tissues with $10^[-6}$ M glibenclamide, a selective blocker of ATP-sensitive potassium channel. Against acetylcholine-induced tone in guinea pig bronchi, however, these compounds had little effect. In summary, KR-30450 and KR-30818 showed greater relaxant effect than lemakalim in guinea pig bronchi (KR-30450>KR-30818>lemakalim). These relaxant actions are suggested to be mediated at least in part by a mechanism which involves the opening of ATP-sensitive potassium channel.

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Inhibitory Effects of Dihydrexidine on Catecholamine Release from the Rat Adrenal Medulla

  • Lee, Jae-Hwang;Lim, Hyo-Jeong;Lim, Dong-Yoon
    • Biomolecules & Therapeutics
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    • 제17권1호
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    • pp.32-42
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    • 2009
  • The purpose of the present study was to examine the effect of dihydrexidine, a full $D_1$ receptor agonist, on the secretion of catecholamines (CA) from the perfused model of the rat adrenal gland, and to establish its mechanism of action. Dihydrexidine (10-100 ${\mu}M$), perfused into an adrenal vein for 60 min, relatively produced dose- and time-dependent inhibition in the CA secretory responses evoked by ACh (5.32 mM), high $K^+$ (56 mM), DMPP (100 ${\mu}M$) and McN-A-343 (100 ${\mu}M$). Dihydrexidine itself did fail to affect basal CA output. Also, in adrenal glands loaded with dihydrexidine (30 ${\mu}M$), the CA secretory responses evoked by Bay-K-8644 (10 ${\mu}M$), an activator of L-type $Ca^{2+}$ channels, cyclopiazonic acid (10 ${\mu}M$), an inhibitor of cytoplasmic $Ca^{2+}$-ATPase, and veratridine, an activator of voltage-dependent $Na+$ channels (10 ${\mu}M$), were also markedly inhibited, respectively. However, in the simultaneous presence of dihydrexidine (30 ${\mu}M$) and R (+)-SCH23390 (a selective antagonist of $D_1$ receptor, 3 ${\mu}M$), the CA secretory responses evoked by ACh, high K+, DMPP, McN-A-343, Bay-K-8644, cyclopiazonic acid and veratridine were considerably recovered to the extent of the corresponding control secretion compared with the inhibitory responses by dihydrexidinetreatment alone. In conclusion, these experimental results suggest that dihydrexidine significantly inhibits the CA secretion evoked by cholinergic stimulation (both nicotinic and muscarinic receptors) and membrane depolarization from the rat adrenal medulla. It seems that this inhibitory effect of dihydrexidine may be mediated by inhibiting influx of both $Ca^{2+}$ and $Na^+$ into the cytoplasm as well as by suppression of $Ca^{2+}$ release from cytoplasmic calcium store through activation of dopaminergic $D_1$ receptors located on the rat adrenomedullary chromaffin cells.

무수마레인산 생산을 위한 고정층 촉매 반응기 설계 (Design of the Fixed-Bed Catalytic Reactor for the Maleic Anhydride Production)

  • 윤영삼;구은화;박판욱
    • 공업화학
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    • 제10권3호
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    • pp.467-476
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    • 1999
  • 공기에 의한 n-butane의 산화로부터 무수마레인산을 합성하는 고정층 촉매 반응기의 거동을 조사하였다. 대류-확산-반응기구로 묘사되는 고정층 촉매반응기의 거동은 Langmuir-Hinshelwood형의 반응속도식 및 비정상상태 이차원 유사균일상 모델을 적용 조사하였다. 예측모델은 Sharma의 pilot-plant 실험 결과인 단일층 반응기의 축방향 온도 및 수율 분포에 대한 최적적합을 통한 최적매개변수 추정에 의해 구성하였다. 또한 예측모델은 단일층 반응기와 통일한 수율 및 전화율을 생성시킬 수 있도록 모사된 불균열활성의 이중층 반응기가 열점에서 $8.96^{\circ}C$ 낮은 온도 상승을 일으켰다. 단일과 이중층 반응기의 가능한 조업조건 (냉매온도, 반응물의 농도, 온도 및 유량)변화에 대한 매개변수 감응도를 조사한 결과 동일한 조업 조건하에서 이중층 반응기가 단일층 반응기에 비해 더 넓은 조업범위는 물론 전화율 및 수율이 다소 높게 나타났다.

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Influence of 5′-(N′-Ethylcarboxanlido) Adenosine on Catecholarnine Secretion Evoked by Cholinergic Stimulation and Membrane Depolarization in the Rat Adrenal Gland

  • Lim, Dong-Yoon;Oh, Hyeong-Geun;Woo, Seong-Chang
    • Biomolecules & Therapeutics
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    • 제8권4호
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    • pp.338-348
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    • 2000
  • The present study was attempted to determine the effect of 5'-(N'-ethylcarboxamido) adenosine (NECA), which is an potent $A_2$-adenosine receptor agonist, on catecholamine (CA) secretion evoked by cholinergic stimulation, membrane depolarization and calcium mobilization from the isolated perfused rat adrenal gland. NECA (20 nM) perfused into the adrenal vein for 60 min produced a time-related inhibition in CA secretion evoked by ACh (5.32x10$^{-3}$ M), high $K^{+}$(5.6x10$^{-2}$ M), DMPP (10$^{-4}$ M for 2 min), McN-A-343 (10$^{-4}$ M for 2 min), cyclopiazonic acid (10$^{-5}$ M for 4 min) and Bay-K-8644 (10$^{-5}$ M for 4 min). Also, in the presence of $\beta$,${\gamma}$-methylene adenosine-5'-triphosphate (MATP), which is also known to be a selective $P_{2x}$-purinergic receptor agonist, showed a similar inhibition elf CA release evoked by ACh, high potassium, DMPP, McN-A-343, Bay-K-8644 and cyclopiazonic acid. However, in adrenal glands preloaded with 20$\mu$M NECA for 20 min under the presence of 20$\mu$M 3-isobutyl-1-methyl-xanthine (IBMX), an adenosine receptors antagonist, CA secretory responses evoked by ACh, high potassium, DMPP, McN-A-343, Bay-K-8644 and cyclopiazonic acid were much recovered in comparison to the case of NECA-treatment only. Taken together, these results indicate that NECA causes the marked inhibition of CA secretion evoked by stimulation of cholinergic (both nicotinic and muscarinic) receptors as well as by membrane depolarization. This inhibitory effect may be mediated by inhibiting influx of extracellular calcium and release in intracellular calcium in the rat adrenomedullary chromaffin cells through the adenosine receptor stimulation. Therefore, it is suggested that the inhibitory mechanism of adenosine receptor stimulation may play a modulatory role in regulating CA secretion.n.n.

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β-ketohexanal에 의한 Cu(II)의 추출 특성 (Characteristics of Cu(II) Extraction by β-ketohexanal)

  • 신정호;이상훈;정갑섭;박경기;전상우
    • 공업화학
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    • 제7권6호
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    • pp.1053-1060
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    • 1996
  • Sodium amide에 의한 methyl propyl ketone과 ethyl formate의 반응으로 킬레이트 추출제의 하나인 $\beta$-ketohexanal(이하 KHA)를 합성하고, KHA-클로로포름에 의한 구리의 추출평형 실험을 통하여 추출특성을 고찰하였다. 흡광도를 측정하여 추출제 KHA의 상간 분배계수와 해리상수, KHA와 구리간 킬레이트의 안정도 상수와 분배계수 및 총괄 추출 평형상수등을 구하고, 추출기구를 구명하였다 합성한 추출제에 의한 구리의 추출율은 pH 5 이상에서 거의 100%이었고, Cu-Zn-Cd 혼합 금속으로부터 구리의 선택적 추출이 가능하였다. KHA-클로로포름에 의한 구리의 추출 화학종은 $CuR_2$였으며 추출 평형 식은 $Cu^{2+}+2{\overline{HR}}{\rightarrow}{\overline{CuR{_2}}}+2H^+$로 표시되었다.

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구강암세포주에서의 Tamoxifen의 항암효과 (ANTICANCER EFFECT OF TAMOXIFEN IN ORAL CANCER CELL)

  • 정재화;윤필영;명훈;신재일;이종호;김명진
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • 제29권6호
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    • pp.365-373
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    • 2003
  • Tamoxifen is an selective estrogen receptor antagonist widely used in the management of patients with breast cancer for more than 30 years. It was thought to act primarily through occupying the estrogen receptor sites in ER positive breast cancer cells and directly on cancer cell proper. These inhibitory effects, which have been shown to be independent of the ER, highlight new mechanism of therapeutic action of tamoxifen. The purposes of this study were to identify ER in oral carcinoma cell lines and to evaluate ER independent cytotoxic effect of tamoxifen. KB(SCC), HSC-3(SCC) and A253(ACC) cell line were used and capacity of cell proliferation, apoptosis, in vitro invasion and gelatin zymography were tested. ER expression of each cell line were detected by RT-PCR and immunocytochemistry. Dose dependent inhibition of cell proliferation and inhibition of gelatinolytic activity were observed in all oral carcinoma cell lines and significant difference of apoptotic index were observed in A253 and KB. Tamoxifen inhibited in vitro invasion in all experimental groups. ER expression was detected in KB and A253. These data suggest that tamoxifen may play a role in management of oral carcinoma by independent cytotoxic effect and more advanced research must processed confirming ER-dependent cytotoxicity.

3D Architectures of LaVO4:Eu3+ Microcrystals via an EG-assisted Hydrothermal Method: Phase Selective Synthesis, Growth Mechanism and Luminescent Properties

  • Ding, Yi;Zhang, Bo;Ren, Qifang;Zhang, Qicai;Zha, Weiwei;Li, Xin;Chen, Shaohua;Oh, Won-Chun
    • 한국세라믹학회지
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    • 제54권2호
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    • pp.96-101
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    • 2017
  • In this article, pure $m-LaVO_4:Eu^{3+}$ and $t-LaVO_4:Eu^{3+}$ nanocrystals were prepared by an EG-assisted hydrothermal method with regular shapes. A series of controlled experiments showed that the pH value of a mixed solution, the volume ratio of $EG/H_2O$ and the dosage of the doped $Eu^{3+}$ all had an important effect on the sizes and shapes of the final products. Furthermore, the constitutional unit of the products changed from 0D to 2D with an increase in the EG dosage. The PL results showed that $t-LaVO_4$ doped with $Eu^{3+}$ ions had better luminescence properties than $m-LaVO_4$ due to its special structure. All of these results not only expand our understanding of the luminescence properties of lanthanide orthovanadates, but they also elucidate the principles of the crystal growth.

6-Hydroxydopamine으로 유도된 질소적 세포 사멸에 대한 고려홍삼 추출물의 보호효과 (Protective Effect of Korean Red Ginseng against 6-Hydroxydopamine-induced Nitrosative Cell Death via Fortifying Cellular Defense System)

  • 이찬;장정희;박규환
    • 약학회지
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    • 제60권2호
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    • pp.92-99
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    • 2016
  • Parkinson's disease (PD) is one of the representative neurodegenerative movement disorders with the selective loss of dopaminergic neurons in the substantia nigra. 6-Hydroxydopamine (6-OHDA) is widely used as an experimental model system to mimic PD and has been reported to cause neuronal cell death via oxidative and/or nitrosative stress. Therefore, daily intake of dietary or medicinal plants which fortifies cellular antioxidant capacity can exert neuroprotective effects in PD. In the present study, we have investigated the protective effect of Korean red ginseng (KRG) against 6-OHDA-induced nitrosative death in C6 glioma cells. Treatment of C6 cells with 6-OHDA decreased cell viability and increased expression of inducible nitric oxide synthase, production of nitric oxide as well as peroxynitrite, and formation of nitrotyrosine. 6-OHDA led to apoptotic cell death as determined by decreased Bcl-2/Bax, phosphorylation of JNK, activation of caspase-3, and cleavage of PARP. Conversely, pretreatment of C6 cells with KRG attenuated 6-ODHA-induced cytotoxicity, apoptosis, and nitrosative damages. To further elucidate the molecular mechanism of KRG protection against 6-OHDA-induced nitrosative cell death, we have focused on the cellular self-defense molecules against exogenous noxious stimuli. KRG treatment up-regulated heme oxygenase-1 (HO-1), a key antioxidant enzyme essential for cellular defense against oxidative and/or nitrosative stress via activation of Nrf2. Taken together, these findings suggest KRG may have preventive and/or therapeutic potentials for the management of PD.