• Macromolecular Research
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• 제17권9호
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• pp.709-713
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• 2009

The aim of this study was to develop novel intestinal specific drug delivery systems with pH sensitive swelling and drug release properties. The carboxyl group of ibuprofen was converted to a vinyl ester group by reacting ibuprofen and vinyl acetate as an acylating agent in the presence of catalyst. The glucose-6-acrylate-1, 2, 3, 4-tetraacetate (GATA) monomer was prepared under mild conditions. Cubane-1, 4-dicarboxylic acid (CDA) linked to two 2-hydroxyethyl methacrylate (HEMA) group was used as the crosslinking agent (CA). Methacrylic-type polymeric prodrugs were synthesized by the free radical copolymerization of methacrylic acid, vinyl ester derivative of ibuprofen (VIP) and GATA in the presence of cubane cross linking agent. The structure of VIP was characterized and confirmed by FTIR, $^1H$ NMR and $^{13}C$ NMR spectroscopy. The composition of the cross-linked three-dimensional polymers was determined by FTIR spectroscopy. The hydrolysis of drug polymer conjugates was carried out in cel-lophane membrane dialysis bags, and the in vitro release profiles were established separately in enzyme-free simulated gastric and intestinal fluids (SGF, pH 1 and SIF, pH 7.4). The detection of a hydrolysis solution by UV spectroscopy at selected intervals showed that the drug can be released by hydrolysis of the ester bond between the drug and polymer backbone at a low rate. Drug release studies showed that increasing the MAA content in the copolymer enhances the rate of hydrolysis in SIP. These results suggest that these polymeric prodrugs can be useful for the release of ibuprofen in controlled release systems.

• 한국전산구조공학회논문집
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• 제24권2호
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• pp.193-200
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• 2011

본 연구를 통해 superlite라 불리는 단열 파우더를 채용한 NO96 멤브레인 타입 LNG선 단열 화물창의 만선항해 시 LNG의 BOR(Boil-Off Rate) 예측모델을 제시하였다. LNGCC(LNG Cargo Containment)의 비정상상태 열전달 FEM모델은 만선항해 시 대기 및 해수 조건을 반영하고 복잡한 화물창 단열구조에 균질화 기법을 적용하여 구축하였다. BOR은 만선항해중 LNGCC 내부로 침입하는 총 열량을 이용하여 평가되었으며, 주요 변수에 따른 BOR의 변화는 파라메트릭 열전달해석을 통하여 분석하였다. 그리고 파라메트릭 BOR 특성해석 결과를 토대로 LNG선의 탱크 크기, 단열층의 두께 그리고 superlite의 열전도율을 함수로 하는 BOR 예측모델을 유도하였다. 비선형 과도 열전달해석을 통해 직접 구한 BOR과의 비교를 통해 유도한 예측모델은 최대 1% 이내의 상대오차를 나타내었다.

• 폴리머
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• 제30권6호
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• pp.471-477
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• 2006

이온성 고분자-금속 복합체(ionic polymer metal composite, IPMC)는 낮은 구동 전압에서도 비교적 빠른 응답 속도를 갖는 전기활성고분자(electro active polymer, EAP) 재료이다. IPMC는 인간의 근육과 유사한 인성 및 변형 특성을 나타내므로 최근 인공근육용 구동체 개발을 위한 많은 연구들이 진행되어 왔으며, 또한 우주항공, 센서 및 펌프 등의 다양한 분야에서 적용가능성이 조사되고 있다. 본 연구에서는 액상 내피온을 이용하여 용액 캐스팅 방법으로 다양한 두께의 내피온 막을 제조하는 방법을 도입하였다. IPMC 제조방법은 Oguro가 제안한 방법을 기초로 하여 도금온도를 변화시켜 무전해 도금법을 이용하여 내피온 내부로의 1차 전극을 형성시켰으며, 형성된 1차 전극의 안정성과 표면전기저항을 낮추기 위하여 이온빔보조증착법(ion beam assisted deposition, IBAD)을 도입하여 금과 이리듐을 1차 전극표면 위에 증착하여 2차 전극을 형성시켰다. 1, 2차 무전해 도금한 IPMC와 2차 IBAD 코팅한 IPMC 전극의 표면과 단면 형상을 SEM으로 관찰하였으며, 전압을 인가할 때 IPMC 내부의 수분증발 및 이온전도도의 변화를 조사하였다. 또한 다양한 두께의 IPMC를 제조하여 두께변화에 따른 변위와 구동력을 측정하였다.

• Molecules and Cells
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• 제38권11호
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• pp.1013-1021
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• 2015

Most of the axons in the vertebrate nervous system are surrounded by a lipid-rich membrane called myelin, which promotes rapid conduction of nerve impulses and protects the axon from being damaged. Multiple sclerosis (MS) is a chronic demyelinating disease of the CNS characterized by infiltration of immune cells and progressive damage to myelin and axons. One potential way to treat MS is to enhance the endogenous remyelination process, but at present there are no available treatments to promote remyelination in patients with demyelinating diseases. Sulfasalazine is an anti-inflammatory and immune-modulating drug that is used in rheumatology and inflammatory bowel disease. Its anti-inflammatory and immunomodulatory properties prompted us to test the ability of sulfasalazine to promote remyelination. In this study, we found that sulfasalazine promotes remyelination in the CNS of a transgenic zebrafish model of NTR/MTZ-induced demyelination. We also found that sulfasalazine treatment reduced the number of macrophages/microglia in the CNS of demyelinated zebrafish larvae, suggesting that the acceleration of remyelination is mediated by the immunomodulatory function of sulfasalazine. Our data suggest that temporal modulation of the immune response by sulfasalazine can be used to overcome MS by enhancing myelin repair and remyelination in the CNS.

• Journal of Pharmaceutical Investigation
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• 제19권2호
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• pp.93-98
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• 1989

The study was performed to compare the dissolution, diffusion and absorption characteristics using Sartorius dissolution and absorption simulator and in vivo bioavailability of commercially available rifampicin capsules. Both brands C and F showed similar dissolution patterns and absorption properties through artificial gastric barrier in Sartorius simulator. Diffusion rate constants through the membrane of brands C and F were $3.04\;{\times}40^{-3}$ and $2.88\;{\times}\;10^{-3}cm/min$, respectively. Rifampicin capsules were administered orally to six fasted healthy volunteers according to cross-over design. The pharmacokinetic parameters between brands C and F, maximum plasma drug concentration$(C_{max})$, the time to reach $C_{max}$, absorption rate constant and area under the curve $(AUC_{0-24hr})$, elimination rate constant, and amount of drug excreted in urine were 6.11 and $7.27\;{\mu}g/ml$, 2.71 and 1.52 hr, 0.6371 and $1.6456 hr^{-1}$, 57.84 and $57.28\;{\mu}g\;{\cdot}\;hr/ml$, 0.1891 and $0.1734 hr^{-l}$, 119.98 and 119.93 mg, respectively. On the basis of experimental results, it was concluded that the bioavailability of brand C rifampicin capsules was almost the same as that of brand F rifampicin capsules.

• The Korean Journal of Physiology and Pharmacology
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• 제7권1호
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• pp.15-23
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• 2003

Cellular redox state is known to be perturbed during ischemia and that $Ca^{2+}$ and $K^2$ channels have been shown to have functional thiol groups. In this study, the properties of thiol redox modulation of the ATP-sensitive $K^2$ ($K_{ATP}$) channel were examined in rabbit ventricular myocytes. Rabbit ventricular myocytes were isolated using a Langendorff column for coronary perfusion and collagenase. Single-channel currents were measured in excised membrane patch configuration of patch-clamp technique. The thiol oxidizing agent 5,5'-dithio-bis-(2-nitro-benzoic acid) (DTNB) inhibited the channel activity, and the inhibitory effect of DTNB was reversed by dithiothreitol (disulfide reducing agent; DTT). DTT itself did not have any effect on the channel activity. However, in the patches excised from the metabolically compromised cells, DTT increased the channel activity. DTT had no effect on the inhibitory action by ATP, showing that thiol oxidation was not involved in the blocking mechanism of ATP. There were no statistical difference in the single channel conductance for the oxidized and reduced states of the channel. Analysis of the open and closed time distributions showed that DTNB had no effect on open and closed time distributions shorter than 4 ms. On the other hand, DTNB decreased the life time of bursts and increased the interburst interval. N-ethylmaleimide (NEM), a substance that reacts with thiol groups of cystein residues in proteins, induced irreversible closure of the channel. The thiol oxidizing agents (DTNB, NEM) inhibited of the $K_{ATP}$ channel only, when added to the cytoplasmic side. The results suggested that metabolism-induced changes in the thiol redox can also modulate $K_{ATP}$ channel activity and that a modulatory site of thiol redox may be located on the cytoplasmic side of the $K_{ATP}$ channel in rabbit ventricular myocytes.

• Journal of Microbiology and Biotechnology
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• 제18권11호
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• pp.1862-1867
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• 2008

Streptochlorin is a small molecule isolated from marine Streptomyces sp. that is known to have antiangiogenic and anticancer properties. In this study, we examined the effects of this compound on reactive oxygen species (ROS) production and the association of these effects with apoptotic tumor cell death, using a human hepatocarcinoma Hep3B cell line. The results of this study demonstrated that streptochlorin mediates ROS production, and that this mediation is followed by a decrease in the mitochondrial membrane potential (MMP, ${\Delta}{\Psi}_m$), activation of caspase-3, and downregulation of antiapoptotic Bcl-2 protein. The quenching of ROS generation by N-acetyl-L-cysteine administration, a scavenger of ROS, reversed the streptochlorin-induced apoptosis effects via inhibition of ROS production, MMP collapse, and the subsequent activation of caspase-3. These observations clearly indicate that ROS are involved in the early molecular events in the streptochlorin-induced apoptotic pathway. Taken together, our data imply that streptochlorin-induced ROS is a key mediator of MMP collapse, which leads to the caspase-3 activation, culminating in apoptosis.

• 한국생물물리학회:학술대회논문집
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• 한국생물물리학회 2003년도 정기총회 및 학술발표회
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• pp.47-47
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• 2003

The presenilin 1 (PS1) or PS2 is an essential component of the ${\gamma}$-secretase complex, which mediates the intramembrane proteolysis of selected type-I membrane, including the ${\beta}$-amyloid precursor protein (APP) to yield A${\beta}$. Familial Alzheimer's disease (FAD)-associated mutations in presenilins give rise to an increased production of a highly amyloidogenic A${\beta}$42. In addition to their well-documented proteolytic function, the presenilins play a role in calcium signaling. We have previously reported that presenilin FAD mutations cause highly consistent alterations in intracellular calcium signaling pathways, which include deficits in capacitative calcium entry (CCE), the refilling mechanism for depleted internal calcium stores. However, molecular basis for the presenilin-mediated modulation of CCE remains to be elucidated. In the present study, whole-cell patch clamp method was used to identify a specific calcium-permeable ion channel current(s) that is responsible for the CCE deficits associated with FAD-linked PS1 mutants. Unexpectedly, both voltage-activated and conventional store depletion-activated calcium currents I(CRAC), were absent in HEK293 cells, which were stably transfected either with wild-type or FAD mutant (L286V, M146L, and delta E9) forms of PS1. Recently, magnesium-nucleotide-regulated metal cation current, or I(MagNum), has been described and appears to share many common properties with I(CRAC) including calcium permeability and inhibitor sensitivity (e.g. 2-APB). We have detected I(MagNum) in all 293 cells tested. Interestingly, FAD mutant 293 cells developed only about half of currents compared to PS1 wild type cells.

• 폴리머
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• 제38권3호
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• pp.293-298
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• 2014

본 연구에서는 방사선을 이용하여 다공성 polytetrafluoroethylene(PTFE) 지지체에 acrylonitrile(AN)과 친수성 작용기를 가진 sodium allylsulfonate(SAS)를 접목시켜 복합 연료전지막의 지지체로 사용되는 친수화 다공성 지지체를 제조하였다. SAS/AN의 몰비율, 단량체 농도, 방사선의 조사선량에 변화를 주어 제조된 지지체의 물성을 평가하였다. 제조된 지지체의 FTIR 분석을 통하여 각 단량체들이 다공성 PTFE 지지체에 성공적으로 그래프팅되었음을 확인하였다. 또한 FE-SEM과 gurley number 측정을 이용하여 그래프트율이 증가할수록 지지체 표면의 기공이 감소하는 것을 관찰하였고, 그래프트율, 접촉각, TBO(toluidine blue O) uptake 분석을 통해 그래프트율이 증가됨에 따라 제조된 지지체의 친수화도가 증가하는 것을 확인하였다.

• 한국수소및신에너지학회논문집
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• 제22권5호
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• pp.579-584
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• 2011

Sulfonated poly (ether sulfone)s containing BFBN were prepared from 2,3-bis(4-fluorophenyl)-2-butenedinitrile , 4,4-sulfonyldiphenol and sulfonated 4,4'-difluorodiphenylsulfone sodium salt using potassium carbonate, and followed acidification reaction with 1M $H_2SO_4$. BFBN was prepared from 4-fluorobenzylcyanide, $CCl_4$, NaOH using trimethylbenzylammoniumchloride . Sulfonated poly(ether sulfone)s containing BFBN were studied by FT-IR, $^1H$-NMR spectroscopy, and thermo gravimetric analysis (TGA). The water uptake of synthesized S-PBFBN membranes exhibit 31~62% compared with 28% of Nafion 211. The S-PBFBN membranes exhibit proton conductivities ($80^{\circ}C$, RH 100) of 53.8~117.4 mS/cm compared with 137.4 mS/cm of Nafion 211.