• 한국독성학회:학술대회논문집
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• 한국독성학회 2001년도 International Symposium on Dietary and Medicinal Antimutgens and Anticarcinogens
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• pp.195-195
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• 2001

The inhibitory potentials of TCAs (imipramine, desipramine, amitriptyline, and nortriptyline) on phenytoin p-hydroxylation and probe metabolic pathways of each CYP isoforms were evaluated from incubation studies of human liver microsomes and cDNA-expressed cytochrome P450s in vitro in order to understand the mechanism of drug interaction between TCAs and phenytoin, a substrate of CYP2C9 and CYP2C19. (omitted)

• Parasites, Hosts and Diseases
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• 제49권1호
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• pp.45-49
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• 2011

Chemotherapy of clonorchiasis with praziquantel (PZQ) is effective but about 15% of treated cases have been reported uncured. The present study investigated correlation of single nucleotide polymorphisms (SNPs) of the cytochrome P450 gene, CYP3A5 and cure of clonorchiasis. A total of 346 egg passing residents were subjected and treated by 3 doses of 25 mg/kg PZQ. Reexamination recognized 33 (9.5%) uncured and 313 cured. Numbers of eggs per gram of feces (EPGs) before treatment were significantly lower in the cured group than in the uncured group ($2,011.2{\pm}3,600.0$ vs $4,998.5{\pm}7,012.0$, P<0.001). DNAs of the subjects were screened for SNPs at 7 locations of CYP3A5 using PCR. In the uncured group, the SNP frequencies at g.-20555G > A and g.27526C > T of CYP3A5 were 15.2% and 9.1% while those were 3.8% and 1.0%, respectively, in the cured group. The cure rate was Significantly lower in the cases with SNP at g.27526C > T and EPGs ${\geq}$ 1,000. In conclusion, EPGs and SNPs of CYP3A5 are factors which influence cure of clonorchiasis by PZQ therapy. It is strongly suggested to recommend 2-day medication for individuals with high EPGs ${\geq}$ 1,000.

• 대한한의학방제학회지
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• 제30권1호
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• pp.1-9
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• 2022

Objectives : This study investigated the protective effect of Ojeok-san (OJS) on cellular damage induced by oxidative stress and whether it induces changes in CYP450 expression. Methods : To investigate the protective effect, we used cells stimulated by oxidative stress caused by the combination treatment of AA+iron. Changes in CYP450 expression were detected by immunoblotting analysis using Huh7 cells. Results : We observed that OJS altered the expression of CYP1A2, CYP3A4, CYP2C19, CYP2D6, and CYP2E1. OJS increased cell viability against AA+iron-induced oxidative stress and inhibited mitochondrial dysfunction. OJS increased phosphorylation of LKB1, phosphorylation of AMPK, and phosphorylation of ACC, which are related to the LKB1-AMPK pathway. In addition, phosphorylation of LATS1 and phosphorylation of YAP, which are related to the Hippo-YAP pathway, were increased. Conclusions : Our results show that OJS has 1) the ability to protect hepatocytes against oxidative stress, and 2) the potential to induce changes in CYP450.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.88.1-88.1
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• 2003

CJ-11668 is a new potent and selective COX-2 inhibitor (IC$\sub$50/ COX-2 65nM; COX-l/COX-2 ratio 770). The pharmacokinetic profile of CJ-11668 (20 mg/kg, p.o.) in the rat was characterized by high bioavailability (90%) and long plasma half-life (11.7 hr) with low clearance (0.4 L/hr/kg). In the dog, the PK profiles (2 mg/kg, p.o.) also showed long plasma half-life (l7.9hr) with low clearance (0.5 L/hr/kg), and the bioavalability of 60%. The inhibition of CJ-11668 infive different cytochrome P450 isozymes (1A2, 2C9, 2C19, 2D6 and 3A4) was determined in vitro and had observed no significant effect. (omitted)

• BMB Reports
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• 제40권2호
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• pp.247-260
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• 2007

Cinnamate 4-hydroxylase (C4H) is a key enzyme of phenylpropanoid pathway, which synthesizes numerous secondary metabolites to participate in development and adaption. Two C4H isoforms, the 2192-bp BnC4H-1 and 2108-bp BnC4H-2, were cloned from oilseed rape (Brassica napus). They both have two introns and a 1518-bp open reading frame encoding a 505-amino-acid polypeptide. BnC4H-1 is 57.73 kDa with an isoelectric point of 9.11, while 57.75 kDa and 9.13 for BnC4H-2. They share only 80.6% identities on nucleotide level but 96.6% identities and 98.4% positives on protein level. Showing highest homologies to Arabidopsis thaliana C4H, they possess a conserved p450 domain and all P450-featured motifs, and are identical to typical C4Hs at substrate-recognition sites and active site residues. They are most probably associated with endoplasmic reticulum by one or both of the N- and C-terminal transmembrane helices. Phosphorylation may be a necessary post-translational modification. Their secondary structures are dominated by alpha helices and random coils. Most helices locate in the central region, while extended strands mainly distribute before and after this region. Southern blot indicated about 9 or more C4H paralogs in B. napus. In hypocotyl, cotyledon, stem, flower, bud, young- and middle-stage seed, they are co-dominantly expressed. In root and old seed, BnC4H-2 is dominant over BnC4H-1, with a reverse trend in leaf and pericarp. Paralogous C4H numbers in Brassicaceae genomes and possible roles of conserved motifs in 5' UTR and the 2nd intron are discussed.

• Biomolecules & Therapeutics
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• 제25권3호
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• pp.288-295
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• 2017

The incidence of polypharmacy-which can result in drug-drug interactions-has increased in recent years. Drug-metabolizing enzymes and drug transporters are important polypharmacy modulators. In this study, the effects of bosentan and rifampin on the expression and activities of organic anion-transporting peptide (OATP) and cytochrome P450 (CYP450) 2C9 and CYP3A4 were investigated in vitro. HEK293 cells and primary human hepatocytes overexpressing the target genes were treated with bosentan and various concentrations of rifampin, which decreased the uptake activities of OATP transporters in a dose-dependent manner. In primary human hepatocytes, CYP2C9 and CYP3A4 gene expression and activities decreased upon treatment with $20{\mu}M$ $bosentan+200{\mu}M$ rifampin. Rifampin also reduced gene expression of OATP1B1, OATP1B3, and OATP2B1 transporter, and inhibited bosentan influx in human hepatocytes at increasing concentrations. These results confirm rifampin- and bosentan-induced interactions between OATP transporters and CYP450.

• 한국어류학회지
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• 제18권3호
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• pp.202-208
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• 2006

점농어 치어의 수온과 염분에 따른 대사율 변화를 조사하기 위해 평균 무게 $5.5{\pm}0.3g$인 개체를 대상으로 수온 (15, 20, $25^{\circ}C$)과 염분 (0, 15, 30 psu)에 따른 산소 소비율을 측정하였다. 9가지 실험 조합의 산소 소비율은 유수식 형태의 호흡실을 이용하여 24시간 동안, 3반복 측정하였다. 수온은 점농어 치어의 산소 소비율에 유의한 영향을 미쳤지만(p<0.001), 염분과 수온 염분의 상호작용은 영향을 미치지 않았다(p>0.05). 각 염분 조건에서 수온 상승에 따라 산소 소비율은 유의적으로 증가하였다(p<0.001). 15, 20 그리고 $25^{\circ}C$에서의 시간당 평균 산소 소비율은 각각 328.8~342.3, 433.9~441.0 그리고 $651.5{\sim}659.9mg\;O_2\;kg^{-1}\;h^{-1}$이었다. $Q_{10}$ 값은 염분의 영향은 받지 않았으며, 수온에 따라 변하였다. 15~20, $20{\sim}25^{\circ}C$ 그리고 전 수온 범위에서의 $Q_{10}$ 값은 각각 1.63~1.75, 2.24~2.26 그리고 1.92~1.98이었다. 대사에 의한 에너지 손실은 수온의 증가에 따라 유의하게 증가하였다(p<0.001). 15, 20 그리고 $25^{\circ}C$에서의 호흡 대사로 인한 일간 평균 에너지 손실은 각각 224.6~233.8, 296.3~301.2 그리고 $444.9{\sim}450.7kJ\;kg^{-1}\;d^{-1}$이었다. 이 실험 결과는 점농어 치어를 염분 적응 후 염분 차이에 의한 에너지 손실 없이 해수뿐만 아니라 담수에서 사육이 가능하다는 것을 나타내며, 사육관리 및 성장을 위한 생체역학 모델 결정에 활용할 수 있다.

• 생명과학회지
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• 제9권3호
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• pp.268-275
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• 1999

고저화된 Rp.palustris균을 이용한 양식장 폐수주으이 질산염 제거를 위하여 Rp.palustris균의 고정화를 위한 담체를 조사하였는데, 탈질능력과 내구성을 실험한 결과 agar,k-carrageenan,그리고 PVA 3종의 담체주우 3% agar가 가장 적합한 담체이었다.Agar bead 내부로의 기질 이동 및 sheer stress를 고려해볼 때 최적 bead 크기는 직경 4mm 였고,접종되는 세포의 양은 25mg dry $cells/cm^2$gel 이었다. 탄소원으로 ethanol이 가장 적합하였고,최적 C:N ratio는 1.5이며,온도와 pH는 각각$31^{\circ}C$,PH 6 이었다. 이러한 조건에서의 최대 탈질율은 인공합성폐수의 경우 $345{\MU}{\ell};N_2/Cm^3 gel{\cdot}hr;이었으며,;modifed MYC 배지의; 경우는; 450{\MU}{\ell}};N_2/Cm^3 gel{\cdot}hr $이었다.

• 한국결정성장학회지
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• 제9권6호
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• pp.542-546
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• 1999

InP single crystal, III-V binary compound semiconductor, was grown by VGF(vertical gradient freeze) method using quartz ampoule and its electrical optical properties were investigated. Phosphorous powders were put in the bottom of quartz ampoule and Indium metal charged in conical quartz crucible what was attached at the upper side position inside the quartz ampoule. It was vacuous under the pressure of $10^5$Torr and sealed up. Indium metal was melted at $1070^{\circ}C$ and InP composition was formed by diffusion of phosphorous sublimated at $450^{\circ}C$ into Indium melt. By cooling the InP composition melt ($2^{\circ}C$~$5^{\circ}C$/hr of cooling rate) in range of $1070^{\circ}C$~$900^{\circ}C$, InP crystal was grown. The grown InP single crystals were investigated by X-ray analysis and polarized optical microscopy. Electrical properties were measured by Van der Pauw method. At the cooling method. At the cooling rate of $2^{\circ}C$/hr, growth direction of ingot was [111] and the quality of ingot was better at the upper side of ingot than the lower side. It was found that the InP crystals were n-type semiconductor and the carrier concentration, electron mobility and relative resistivity were $10^{15}$~$10^{16}/\textrm{cm}^3$ , $2\times 10^3$~$3\times 10^4{\textrm}{cm}^2$/Vsec and$2\times 10^{-1}$~$2\times 10^{-3}$/ Wcm in the range of 150K~300K, respectively.

• Biomolecules & Therapeutics
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• 제17권3호
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• pp.311-317
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• 2009

Ginkgo biloba (G. biloba) extract is a widely used phytomedicine for the oral treatment of peripheral vascular disease. Cilostazol is a synthetic antiplatelet and vasodilating agent for the treatment of intermittent claudication resulting from peripheral arterial disease. It is likely to use concomitantly G. biloba extract and cilostazol for the treatment of peripheral arterial disease, which raises a concern of increasing their adverse effects of herbal-drug interactions. To clarify any possible herbal-drug interaction between G. biloba extract and cilostazol, the effect of the G. biloba extract on the pharmacokinetics of cilostazol was investigated. As cilostazol is known to be eliminated mainly by cytochrome P450 (CYP)-mediated metabolism, we investigated the effects of G. biloba extract on the human CYP enzyme activities and the effect of G. biloba extract on the pharmacokinetics of cilostazol after co-administration of the two agents to male beagle dogs. The G. biloba extract inhibited more or less CYP2C8, CYP2C9, and CYP2C19 enzyme activities in the in vitro microsomal study with $IC_{50}$ values of 30.8, 60.5, and $25.2{\mu}g/ml$, respectively. In the pharmacokinetic study, co-administration with the G. biloba extract had no significant effect on the pharmacokinetics of cilostazol in dogs, although CYP2C has been reported to be responsible for the metabolism of cilostazol. In conclusion, these results suggest that there may not be a pharmacokinetic interaction between G. biloba extract and cilostazol.