• The Korean Journal of Physiology and Pharmacology
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• 제14권5호
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• pp.305-310
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• 2010

The human $ether$-$a$-$go$-$go$-related gene ($hERG$) channel is important for repolarization in human myocardium and is a common target for drugs that prolong the QT interval. We studied the effects of two antipsychotics, tiapride and sulpiride, on hERG channels expressed in $Xenopus$ oocytes and also on delayed rectifier $K^+$ currents in guinea pig cardiomyocytes. Neither the amplitude of the hERG outward currents measured at the end of the voltage pulse, nor the amplitude of hERG tail currents, showed any concentration-dependent changes with either tiapride or sulpiride ($3{\sim}300{\mu}M$). However, our findings did show that tiapride increased the potential for half-maximal activation ($V_{1/2}$) of HERG at $10{\sim}300{\mu}M$, whereas sulpiride increased the maximum conductance ($G_{max}$) at 3, 10 and $100{\mu}M$. In guinea pig ventricular myocytes, bath applications of 100 and $500{\mu}M$ tiapride at $36^{\circ}C$ blocked rapidly activating delayed rectifier $K^+$ current ($I_{Kr}$) by 40.3% and 70.0%, respectively. Also, sulpiride at 100 and $500{\mu}M$ blocked $I_{Kr}$ by 38.9% and 76.5%, respectively. However, neither tiapride nor sulpiride significantly affected the slowly activating delayed rectifier $K^+$ current ($I_{Ks}$) at the same concentrations. Our findings suggest that the concentrations of the antipsychotics required to evoke a 50% inhibition of IKr are well above the reported therapeutic plasma concentrations of free and total compound.

• Parasites, Hosts and Diseases
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• 제49권1호
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• pp.1-8
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• 2011

The pathogenesis and pathophysiology of Acanthamoeba infections remain incompletely understood. Phospholipases are known to cleave phospholipids, suggesting their possible involvement in the host cell plasma membrane disruption leading to host cell penetration and lysis. The aims of the present study were to determine phospholipase activities in Acanthamoeba and to determine their roles in the pathogenesis of Acanthamoeba. Using an encephalitis isolate (T1 genotype), a keratitis isolate (T4 genotype), and an environmental isolate (T7 genotype), we demonstrated that Acanthamoeba exhibited phospholipase $A_2$ (PLA$_2$). and phospholipase D (PLD) activities in a spectrophotometry-based assay. Interestingly, the encephalitis isolates of Acanthamoeba exhibited higher phospholipase activities as compared with the keratitis isolates, but the environmental isolates exhibited the highest phospholipase activities. Moreover, Acanthamoeba isolates exhibited higher PLD activities compared with the PLA$_2$. Acanthamoeba exhibited optimal phospholipase activities at $37^{\circ}C$ and at neutral pH indicating their physiological relevance. The functional role of phospholipases was determined by in vitro assays using human brain microvascular endothelial cells (HBMEC), which constitute the blood-brain barrier. We observed that a PLD-specific inhibitor, i.e., compound 48/80, partially inhibited Acanthamoeba encephalitis isolate cytotoxicity of the host cells, while PLA$_2$-specific inhibitor, i.e., cytidine 5'-diphosphocholine, had no effect on parasite-mediated HBMEC cytotoxicity. Overall, the T7 exhibited higher phospholipase activities as compared to the T4. In contract, the T7 exhibited minimal binding to, or cytotoxicity of, HBMEC.

• Parasites, Hosts and Diseases
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• 제27권3호
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• pp.171-176
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• 1989

강남성모병원의 일반 내원 환자 1,019명, 내원 환자 중 천식으로 진단된 1,030명, 그리고 제주의료원에 내원 한 환자 780면 등 총 2,829명에 대하여 Toxoplasma 항체가를 측정하기 위해 간접 latex 응집반응을 실시하였다. 간접 latex 응집반응의 양성 항체가를 1 : 32로 볼 때, 강남성모병원 일반 내원 환자에서는 19명이 양성으로 1.86%(남자 550명 중 12면으로 2.18%, 여자 469명 중 7명으로 1.49%), 천식 혹은 알레르기 환자에서는 11명이 양성으로 1.07%(남자 470명 중 4명으로 0.85%, 여자 560명 중 7명으로 1.25%)이었으며, 제주의료원 내원환자 에서는 45명으로 5.77%(남자 530명 중 33명으로 6.23%, 여자 250명 중 12명으로 4.80%)이었다. 연령적 분포로는 강남성모병원 일반 환자와 제주의료원 내원 환자의 남자에서 50대에 높은 빈도를 보였고, 전체 여자에서는 일반적으로 30대, 40대 및 60대에서 높은 빈도를 보였다. 양성 항체가를 보인 75명의 항체가별 분포로는 1 32가 32명으로 42.7%, 1 : 64가 21명으로 28.0%, 1 : 128이 8명으로 10.7%, 1 256이 6명으로 8.0%, 1 : 512가 3명으로 4.0%, 그리고 1 : 2,048 혹은 그 이상의 항체가를 보유한 사람은 5명으로 6.7%였다.

• Biomolecules & Therapeutics
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• 제16권4호
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• pp.410-415
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• 2008

Previously, we identified albumin as an inhibitory factor in serum for cell adhesion of T cells such as human Jurkat T and primary cultured human T cells. In the present study, we found that other hematopoietic cell lines including U-937 human monocytes, THP-1 human monocytes, K-562 promyelocytic leukemia cells, and HL-60 human leukemia cells, also adhere to tissue culture flasks when serum is withdrawn, and albumin exerts an inhibitory effect on cell adhesion by those cells, implying that this inhibition is a common phenomenon in hematopoietic cells. Furthermore, we found that cell adhesion is inhibited by antioxidants such as (-)-epigallocatechin- 3-gallate (EGCG), morin, and a-tocopherol. Our results suggest that albumin may inhibit basal cell adhesion of hematopoietic cells and that the oxidative balance in the plasma may be important for cell adhesion of hematopoietic cells in vivo.

• 대한의생명과학회지
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• 제18권1호
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• pp.22-28
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• 2012

The purpose of this study was to investigate the effect of soybean peptide on antioxidant enzymes, cortisol hormone and inflammatory cytokine levels. 19 high school male judo athletes participated in the experiments. They were randomly divided into two groups, one group took soybean peptide (S-peptide, n=10) 4 g a day for 4 weeks and the other group placebo (placebo group, n=9) for the same time. Blood samples were collected before intake, after 2 weeks intake and 4 weeks intake and these were analyzed for total antioxidant status (TAS), catalase (CAT), levels of cortisol hormone, tumor necrosis factor-alpha (TNF-${\alpha}$) and interleukin-6 (IL-6). As a result, the S-peptide group was significantly increased in TAS and CAT (P<0.05). The malondialdehyde (MDA) levels showed decrease after soybean peptide intake but there was no significant difference. In the levels of plasma cortisol which reflect stress status, there was significantly decreased in the S-peptide and placebo group after 4 weeks (P<0.05). There were significant decreases of TNF-${\alpha}$ and IL-6 after 4 weeks in S-peptide group (P<0.05). These results suggest that the intake of soybean peptide can activate antioxidant defenses and decrease exercise-induced oxidative stress.

• Archives of Pharmacal Research
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• 제21권5호
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• pp.503-507
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• 1998

Percutaneous absorption and model membrane variations of melationin (MT) in aqueous-based propylene glycol and $2-hydroxypropyl-{\beta}-cyclodextrin $vehicles were investigatted. the excised hairless mouse skin (HMS) and two synthetic ethylene vinyl acetate (EVA) and microporous polyethylene (MPE) were selected as a model membrane. the solubility of MT was determined by phase equilibrium study. the vertical $Franz{\circledR}$ type cell was used for diffusion study. The concentration of MT was determined using reverse phse HPLC system. The MT solubility was the highest in a mixture of PG and $2-HP{\beta}CD$. The percutaneous absorption of MT through excised HMS increased as the solubility increased. However, the permeability coefficient decreased and then slightly increased in mixture of PG and $2-HP{\beta}CD$. On the other hand, both flux and permeability coefficient through EVA membrane decreased as the solubility increased. No MT was detected over 12 h after starting diffusion through MPE membrane. The flux of MT was dependent on the type of membrane selected. Flux of MT was greatest in excised HMS followed by EBA and MPE membrane. Flux of MT through EVA membrane was 5-20 times lower when compared to excised HMS. Interestingly, volumes of donor phase when MPE membrane was used, significantly increased during the study period. the HMS might be applicable to expect plasma concentration of MT in human subjects based on flux and pharmacokinetic parameters as studied previously. the current studies may be applied to deliver MT transdermally using aqueous-based vehicles and to fabricate MT dosage forms.

• Archives of Pharmacal Research
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• 제28권4호
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• pp.488-492
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• 2005

The purpose of this study is to investigate the bioequivalence of two haloperidol 5 mg tablets, Myung In haloperidol (Myung In Pharm. Co., Ltd., test drug) and $Peridol^{R}$(Whanin Pharm. Co., Ltd., reference drug), and also to estimate the pharmacokinetic parameters of haloperidol in Korean volunteers. The bioavailability and pharmacokinetics of haloperidol tablets were examined on 24 healthy volunteers who received a single oral dose of each preparation in the fasting state in a randomized balanced 2 way crossover design. After an oral dosing, blood samples were collected for a period of 60 h. Plasma concentrations of haloperidol were determined using a liquid chromatographic electrospray mass spectrometric (LC-MS) method. The pharmacokinetic parameters were calculated with noncompartmental pharmacokinetic analysis. The geometric means of $AUC_{0-60h} and C_{max}$ between test and reference formulations were $17.21\pm8.26 ng\cdot/mL vs 17.31\pm13.24 ng\cdot/mL and 0.87\pm0.74 ng/mL vs 0.85\pm0.62 ng/mL$. respectively. The $90\%$ confidence intervals of mean difference of logarithmic transformed $AUC_{0-60h} and C_{max} were log0.9677{\sim}log1.1201 and log0.8208{\sim}log1.1981$, respectively. It shows that the bioavailability of test drug is equivalent with that of reference drug. The geometric means of other pharmacokinetic parameters ($AUC_{inf}. t_{1/2}, V_{d}/F, and CL/F$) between test drug and reference drug were $21.75\pm8.50 ng{\cdot}h/mL vs 21.77\pm15.63 ng{\cdot}h/mL, 29.87\pm8.25 h vs 29.60\pm7.56 h, 11.51\pm5.45 L vs 12.90\pm6.12 L and 0.26\pm0.09 L/h vs 0.31\pm0.17 L/h$, respectively. These observations indicate that the two formulation for haloperidol was bioequivalent and, thus, may be clinically interchangeable.

• Preventive Nutrition and Food Science
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• 제9권4호
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• pp.361-366
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• 2004

Defatted methanol extracts of the medicinal plants, Rubus coreanus Miq. (RC) and Atractylodes japonica Koidzumi (AJ) were added at the levels of 0.1, 0.5, or $2\%$ (w/w) to high cholesterol diets and fed to ovariectomized Sprague-Dawley female rats, weighing 212.6 $\pm$ 1.8 g for four weeks. Weight gains were lower in RC and AJ groups than the control group, but there were no changes in uterus weights. Serum levels of triglyceride decreased by 20-$27\%$ in the experimental groups fed $0.1\%$ of each extract (O.1RC and O.1AJ), compared with that of control (Ovx). Serum cholesterol levels were not changed in the RC groups but increased in the group fed $2\%$ of the AJ extract. Liver levels of cholesterol and triglyceride were reduced in both the RC and AJ groups. Microscopic observation revealed that there were no morphological alterations in liver, lung, heart, spleen and kidney tissues of the experimental groups. Plasma levels of albumin, BUN, creatinine, sodium, potassium and phosphate in the IRC and AJ groups were in normal ranges. Serum GOT and GPT activities were, however, higher in the 2.0AJ than Ovx group. These results suggest that the extracts of the Rubus coreanus Miq. and Atractylodes japonica Koidzumi at dietary levels as low as $0.1\%$ may be utilized as hypotriglyceridemic ingredients for functional foods.

• 한국환경보건학회지
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• 제31권4호
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• pp.287-293
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• 2005

Pollen has been used for Prevention or treatment of certain diseases such as diabetes, arthritis, or cancer in traditional medicine. In addition, pollen is under investigation as a host cell for a gene expression. This study was undertaken to evaluate the immunologic safety of pollen intake. BALB/c mice were administered with 500, 50,5, or 0.5 mg/kg bw of lily pollen for five times a week for four weeks through gastric intubation. Comparing the control mice administered with distilled water, no significant changes were observed in body weight gain, weight of liver, spleen, lung, and his-topathological findings of liver and kidney of the mice groups administered with the pollen. Plasma level of IgG1, IgG2a, and IgE was not different among the groups. When splenic B lymphocytes were stimulated in vitro with lipopolysaccharides for 7 days, level of IgGl and IgGwa produced in the culture supernatants was not significantly different among the groups. Furthermore, no significant alteration was observed in IL-4 and $IFN{\gamma}$ producing ability with splenic T lymphocytes stimulated in vitro with phytohemagglutinins for 48 hours between the pollen-administered and the control mice. Overall, this study suggests that the lily pollen intake is Inducing no significant modulation of humoral and cell-mediated immunity in mice.

• 한국동물생명공학회지
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• 제35권1호
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• pp.58-64
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• 2020

This present study was conducted to investigate protective effect of discontinuous Percoll gradient containing alpha-linolenic acid (ALA) before freezing process on viability, acrosome damage, mitochondrial activity, and oxidative stress of frozen-thawed boar spermatozoa. The separation of spermatozoa by discontinuous Percoll gradient was performed by different concentration of Percoll solution (45/90%) containing ALA combined with bovine serum albumin (BSA), and collected sperm in each Percoll layer was cryopreserved. To evaluate viability, acrosome damage, mitochondrial activity, and reactive oxygen species (ROS) level of frozen-thawed sperm, flow cytometry was used. Morphological abnormalities were observed under light microscope. In results, viability of sperm from 90% Percoll layer was higher than control and 45% Percoll group (p < 0.05). Separated sperm in 90% Percoll layer had lower acrosome damage and morphological abnormalities than control as well as viability, whereas 45% Percoll group was higher (p < 0.05). Similar with acrosome damage and abnormalities, mitochondrial activity was slightly enhanced and the population of live sperm with high ROS level was decreased by 90% Percoll separation, however, there was no significant difference. Supplementation of 3 ng/mL ALA into Percoll solution increased sperm viability and decreased population of live sperm with high ROS compared to control (p < 0.05). In conclusion, discontinuous Percoll gradient before freezing process could improve efficiency of cryopreservation of boar sperm through selection of sperm with high freezing resistance, and supplement of ALA during Percoll gradient might contribute suppression of ROS generation via stabilizing of plasma membrane during cryopreservation.