• Biomolecules & Therapeutics
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• 제12권2호
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• pp.114-121
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• 2004

This study was undertaken to evaluate the general pharmacological properties of CJ-11828, an amlodipine adipate, in experimental animals and in vitro system. CJ-11828 had no effects on general behavior, motor coordination, writhing syndromes, pentetrazol-induced chemoshock and electric shock in mice at dose levels of 3,10, anti 30 mg/kg, po. But there were decrease of body temperature, prolongation of sleeping time, and inhibition of intestinal activity in mice treated with CJ-11828 at doses of 10 and 30 mg/kg, po. CJ-11828 decreased the blood pressure in coscuous fog at the dose level of 2mg/kg, po, but it was expected as a result of pharmacological activity of CJ-11828. Any effect on respiratory system was not observed in conscious rat at doses of 3,10, and 30 mg/kg, po. The slight decrease in spontaneous motor activity was observed in mice treated with CJ-11828 at high dose, 30 mg/kg. In vitro experiments, CJ-11828 had no effect on agonists-induced contraction of isolated guinea pig ileum at 0.1, 1, and 10 ${\mu}$M. Based on these results, it was concluded that CJ-11828 had no pharmacological effect ill these studies even up to the 36-fold anticipated clinical dose, 3 mg/kg.

• 생약학회지
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• 제36권4호통권143호
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• pp.273-277
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• 2005

In mammalian melanocytes, melanin synthesis is controlled by tyrosinase, the key enzyme in the pigment synthesis. In this study, to develop a new whitening agent, we have investigated the antioxidant and the inhibitory effect of Artemisia anomala extract on tyrosinase activity and melanigenesis in the B16/F1 melanoma cells. The inhibition ratio of tyrosinase activity of butanol fraction from A. anomala was higher than that of arbutin ($97.5{\pm}0.5%$ at the concentration of 2 mg/ml). The butanol fraction was shown scavenging activities of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals and superoxide anion radicals in a dose dependent manner. The highest inhibitory activity of melanogenesis was also butanol fraction ($25.0{\pm}3%$ at the concentration of $200\;{\mu}g/ml$). From these results, we suggest that the A. anomala extract might be used to be a potential agent for skin whitening.

• 약학회지
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• 제42권1호
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• pp.89-94
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• 1998

Propionibacterium acnes is the pharmacological target site of antiacne drugs. We have examined the antiacne activity of ninety seven natural products which have been used as Korean traditional medicines in various skin disorders. The antibacterial activity of extracts from the natural products were evaluated against P. acnes ATCC 9616 by disc method. Twelve natural products showed the potent antibacterial activity against P. acnes, and were, selected for the minimal inhibitory concentration(MC) against P. acnes. MICs of nine extracts were below 0.3% (w/v) and Sophora flavescens showed the most potent activity with a MIC of less than 0.008%(w/v) against P. acnes. Thus, the results suggest that nine natural products including S. flavescens can be developed as sources of promising potent antiacne agents.

• 대한화장품학회지
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• 제39권4호
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• pp.329-335
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• 2013

본 연구에서는 기질 화합물로써 일련의 4-hydroxybenzyl alchol (4-HBA) 유도체들의 치환기($R_1$ 및 $R_2$) 변화에 따른 tyrosinase 활성저해에 관한 3차원적인 구조-활성 상관관계(3D-QSARs) 모델을 유도하고 정량적으로 검토하였다. 그 결과, 입체장(S), 정전기장(E), 소수성장(Hy), 수소결합 받게장(HA) 및 수소결합 주게장(HD)의 조합조건에서 통계적으로 양호한 CoMSIA FF 모델(상관성; $r^2$ = 0.858 및 예측성; $q^2$ = 0.951)을 유도하였다. 등고도 분석결과에 의하면 기질분자의 $R_2$-치환기는 입체적으로 작고 음전하를 띄며, 소수성이면서 수소결합 주게장을 선호하지 않는 치환기가 올수록 tyrosinase 활성저해 작용이 용이하다. 그리고 $R_1$-치환기는 수소결합 주게장을 선호하는 치환기 이어서 $R_1$-치환체가 용이하게 탈 양성자화가 일어나야 tyrosinase 활성저해 작용을 용이하게 할 것이라고 예상되며, 이를 위해서는 $R_1$-치환기가 비 치환체(H)이어야 될 것으로 예상되었다.

• 한국경영과학회:학술대회논문집
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• 한국경영과학회/대한산업공학회 2003년도 춘계공동학술대회
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• pp.683-690
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• 2003

This purpose of this research is an attempt to measure and comparatively analyze the efficiencies and RTS(Returns to Scale) using panel data of OECD countries including Korea. In order to achieve this purpose, at first this study used efficient production frontier estimation combined with DEA for obtaining parameter estimates of a efficient production frontier. secondly using estimated results, measured R&D productivity and RTS(Returns to Scale) on all of the OECD countries. thirdly using time-series data related to R&D activity of korea, measured R&D productivity and RTS(Returns to Scale). Finally based on the results of R&D productivity and RTS(Returns to Scale) using efficient production frontier, some policy implications for enhancing the R&D competitiveness and the technological capabilities are discussed.

• The Plant Pathology Journal
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• 제24권2호
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• pp.164-170
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• 2008

Carbon utilization by Chryseobacterium strain KJ1R5 was studied to enhance its biocontrol activity against Phytophthora capsid. Chryseobacterium strain KJ1R5 has previously been shown to control Phytophthora blight of pepper (Capsicum annuum L.). Strain KJ1R5 could utilize carbon sources such as L-arabinose, D-cellobiose, ${\beta}-lactose$ and D-galactose well. P. capsici could utilize D-glucose well, showing the absorbencies ranged from 0.577 to 0.767 at 600nm. When 2% L-arabinose, which could only be utilized by the bio-control strain KJ1R5, was amended into the bacterial suspension, the efficacy of biological control increased. Among the amendments of various carbon sources into bacterial suspension, L-arabinose and D-(+)-glucose significantly enhanced biological control activity, resulting in a reduction of disease incidence to 6.9%, compared to 21.9% for the strain KJ1R5 alone and 81.3% for P. capsici inoculation alone, indicating that amendment with specific carbon sources could increase the biological control activity.

• 산업경영시스템학회지
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• 제35권1호
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• pp.87-92
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• 2012

This study examines the relationship between R&D investment and subsequent outputs of the research activity. Usually, there is some time difference between the production of research outputs, such as academic papers and application or registration of patents, and the investment of R&D expenditure. The time lag for producing this kind of research outputs should be considered to evaluate the performance of research activity exactly. The purpose of this study is to identify time lag effect between the times of input and output of a R&D activity and to derive the degree of time lag using the data set of a long term R&D program supported by Korean government. A modified Almon model is suggested to identify the time lag effect between input and output of research activities performed by this program. Time-series cross-section data from 16 research centers between 2001 and 2009 are used to find time lag effect.

• 한국생물공학회:학술대회논문집
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• 한국생물공학회 2005년도 생물공학의 동향(XVI)
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• pp.35-35
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• 2005

Recombinant human $interferon-{\beta}-1a(rIFN-{\beta})$ is a single glycosylated protein (at N80, 1N) with anti-viral activity. However, present drugs have a relatively short serum half-life of $rIFN-{\beta}$, thus patients suffer from frequent $infections.^{1)}$ To improve its half-life, eight glycosylation analogs were prepared, which have additional N-linked glycosylation consensus sequences (N-X-T/S) within the $IFN-{\beta}$ molecule and/or at C-terminal. Each $rIFN-{\beta}$ analog was examined for the presence of additional N-linked glycosylation and the maintenance of anti-viral activity in CHO cells. The molecular weights of five analogs were not changed. However, two analogs, R27T within $rIFN-{\beta}$ (27 kDa, 2N) and GNITVNITV at C-terminal (29kDa, 2N), showed a clear increase in molecular weights, compared to native $rIFN-{\beta}$ (23 kDa, 1N). And another combined analog of R27T+GNITVNITV showed increased molecular weight (33 kDa, 3N). It was confimed that the molecular weight increment of analogs was caued by the N-linked glycosylation with the treatment of N-glycansae. In the case of anti-viral activity, the analog GNITVNITV showed a reduction in activity compared to native $IFN-{\beta}$, whereas the analogs R27T and R27T+GNITVNITV were found to have distinctly increased activities. Pharmacokinetic study in rats also disclosed that the analogs R27T and R27T+GNITVNITV had 2 3 fold increased serum half-life, respectively. In conclusion, the addition of N-linked glycosylation in $rIFN-{\beta}$ increased serum half-life, thereby its less frequent administration will be expected.

• Molecules and Cells
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• 제42권11호
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• pp.755-762
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• 2019

Despite decades of research into colorectal cancer (CRC), there is an ongoing need for treatments that are more effective and safer than those currently available. Lactic acid bacteria (LAB) show beneficial effects in the context of several diseases, including CRC, and are generally regarded as safe. Here, we isolated a Lactobacillus rhamnosus (LR)-derived therapeutic protein, p8, which suppressed CRC proliferation. We found that p8 translocated specifically to the cytosol of DLD-1 cells. Moreover, p8 down-regulated expression of Cyclin B1 and Cdk1, both of which are required for cell cycle progression. We confirmed that p8 exerted strong anti-proliferative activity in a mouse CRC xenograft model. Intraperitoneal injection of recombinant p8 (r-p8) led to a significant reduction (up to 59%) in tumor mass when compared with controls. In recent years, bacterial drug delivery systems (DDSs) have proven to be effective therapeutic agents for acute colitis. Therefore, we aimed to use such systems, particularly LAB, to generate the valuable therapeutic proteins to treat CRC. To this end, we developed a gene expression cassette capable of inducing secretion of large amounts of p8 protein from Pediococcus pentosaceus SL4 (PP). We then confirmed that this protein (PP-p8) exerted anti-proliferative activity in a mouse CRC xenograft model. Oral administration of PP-p8 DDS led to a marked reduction in tumor mass (up to 64%) compared with controls. The PP-p8 DDS using LAB described herein has advantages over other therapeutics; these advantages include improved safety (the protein is a probiotic), cost-free purification, and specific targeting of CRC cells.

• The Korean Journal of Physiology and Pharmacology
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• 제19권2호
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• pp.89-97
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• 2015

The aim of this study was to investigate the involvement of dopaminergic receptors (DR) in behavioral sensitization, as measured by locomotor activity, and the over-expression of cocaine- and amphetamine-regulated transcript (CART) peptides after repeated administration of cocaine in mice. Repeated administrations of cocaine induced behavioral sensitization and CART over-expression in mice. The levels of striatal CART mRNA were significantly increased on the $3^{rd}$ day. CART peptides were over-expressed on the $5^{th}$ day in the striata of behaviorally sensitized mice. A higher proportion of $CART^+$ cells in the cocaine-treated mice were present in the nucleus accumbens (NAc) shell than in the dorsolateral (DL) part of caudate putamen (CP). The concomitant administration of both $D_1R$ and $D_2R$ antagonists, SCH 23390 ($D_1R$ selective) and raclopride ($D_2R$ selective), blocked cocaine induced-behavioral sensitization, CART over-expression, and cyclic adenosine 5'-monophosphate (cAMP)/ protein kinase A (PKA)/phospho-cAMP response element-binding protein (pCREB) signal pathways. SCH 23390 more predominantly inhibited the locomotor activity, CART over-expression, pCREB and PKA activity than raclopride. Cocaine induced-behavioral sensitization was also attenuated in the both $D_1R$ and $D_2R$ knockout (KO) mice, respectively. CART over-expression and activated cAMP/PKA/pCREB signal pathways were inhibited in the $D_1R$-KO mice, but not in the $D_2R$-KO mice. It is suggested that behavioral sensitization, CART over-expression and activated cAMP/PKA/pCREB signal pathways induced by repeated administration of cocaine could be more predominantly mediated by $D_1R$.