• Title/Summary/Keyword: binding agents

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Bradykinin Antagonistic Activities of Antihistamine Agents Containing Piperazine Moiety (피페라진계 항히스타민제들의 브라디키닌 길항작용)

  • 정성현;이소영;윤혜숙
    • YAKHAK HOEJI
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    • v.37 no.6
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    • pp.625-630
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    • 1993
  • Among the six antihistamine agents tested in this study, homochlorcyclizine showed the highest bradykinin antagonistic activity in the receptor binding assay as well as the isolated rat ileum assay. Schild plot analysis of bradykinin-induced ileal contraction in the presence of three different concentrations of homochlorcyclizine revealed a pA$_{2}$=6.26, and a correlation coefficient of 0.984. Homochlorcyclizine of (100 $\mu{M}$ final concentration) also showed 25% antagonistic activity in the receptor binding assay.

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Sorption Behavior of 1-Methylcyclopropene on Adsorbing Agents for Use in Extending the Freshness of Postharvest Food Products

  • Lee, Youn-Suk;Shin, Han-Seung
    • Food Science and Biotechnology
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    • v.15 no.4
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    • pp.572-577
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    • 2006
  • The physiochemical interactions of 1-methylcyclopropene (1-MCP) and adsorbing agents can be described using a very powerful tool, inverse gas chromatography (IGC). Sorption behavior of 1-MCP on various adsorbing agents was assessed using the profile peaks of 1-MCP at an infinite dilution concentration using the IGC technique. Chromatogram peaks of 1-MCP adsorption were not observed for the adsorbing agent activated carbon. The forms of sorption isotherms followed Henry's law, and behaved according to the binding site theory. Specific retention volume and distribution coefficients for 1-MCP on the adsorbing agents were determined at 50, 60, 70, and $80^{\circ}C$, respectively. Silica gel had a much higher number of binding sites for 1-MCP compared to Tenax-TA and activated clay agents. Meanwhile, activated carbon proved to be a very strong binding agent for 1-MCP based on 1-MCP efficiency experiments on the selected adsorbing agents. However, as a proper means of delivering 1-MCP molecules to fresh food products, activated carbon is not fit for the binding and release of 1-MCP gas under dry or high humidity conditions because activated carbon has a strong affinity for 1-MCP, even when treated with distilled water.

Preparation of Porous SiC Ceramics Using Polycarbosilane Derivatives as Binding Agents (폴리카보실란계 바인더를 이용한 다공성 SiC 세라믹스의 제조)

  • Park, Jihye;Kim, Younghee;Jung, Miewon
    • Journal of the Korean Ceramic Society
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    • v.49 no.5
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    • pp.412-416
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    • 2012
  • Porous SiC ceramics were prepared by using recycled SiC sludge, which is an industrial waste generated from solar cell industry. Polycarbosilane derivatives, such as polycarbosilane (PCS), polyphenylcarbosilane (PPCS) and hydridopolycarbosilane (HPCS) were used as binding agents for the fabrication of porous SiC ceramics at $1800^{\circ}C$ under Ar atmosphere. The effects of the various binding agents having different C/Si ratios were discussed on the sintering and porosity of the SiC ceramics. The prepared porous SiC ceramics were characterized by X-ray Diffraction (XRD) and Field-Emission Scanning Electron Microscope (FE-SEM). Thermal conductivity and porosity of SiC ceramics were measured at room temperature, and they were 56.7W/mK and 29.8%, respectively.

Construction of Chimeric Human Epidermal Growth Factor Containing Short Collagen-Binding Domain Moieties for Use as a Wound Tissue Healing Agent

  • Kim, Dong-Gyun;Kim, Eun-Young;Kim, Yu-Ri;Kong, In-Soo
    • Journal of Microbiology and Biotechnology
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    • v.25 no.1
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    • pp.119-126
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    • 2015
  • Among the various human growth factors, epidermal growth factor (hEGF, consisting of 53 amino acids) has various effects on cell regeneration, stimulation of proliferation, migration of keratinocytes, formation of granulation tissues, and stimulation of fibroblast motility, which are important for wound healing. Owing to their multiple activities, EGFs are used as pharmaceutical and cosmetic agents. However, their low productivity, limited target specificity, and short half-life inhibit their application as therapeutic agents. To overcome these obstacles, we fused the collagen-binding domain (CBD) of Vibrio mimicus metalloprotease to EGF protein. About 18 or 12 amino acids (aa) (of the 33 total amino acids), which were essential for collagen-binding activity, were combined with the N- and C-termini of EGF. We constructed, expressed, and purified EGF (53 aa)-CBD (18 aa), EGF (53 aa)-CBD (12 aa), CBD (18 aa)-EGF (53 aa), and CBD (12 aa)-EGF (53 aa). These purified recombinant proteins increased the numbers of cells in treated specimens compared with non-treated specimens and control hEGF samples. The collagen-binding activities were also evaluated. Furthermore, CBD-hybridized hEGF induced phosphorylation of the EGF receptor. These results suggested that these fusion proteins could be applicable as small therapeutic agents in wound tissue healing.

Effects of Drying Condition and Binding Agent on the Quality Characteristics of Ground Dried-Pork Meat Products

  • Choi, Yun-Sang;Ku, Su-Kyung;Park, Jong-Dae;Kim, Hee-Ju;Jang, Aera;Kim, Young-Boong
    • Food Science of Animal Resources
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    • v.35 no.5
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    • pp.597-603
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    • 2015
  • The purpose of this study was to investigate the influence of processing conditions (temperature and time) and binding agent types (glutinous rice flour, potato starch, bean flour, and acorn flour) on the physicochemical and sensory characteristics of ground dried-pork meat product. For this purpose, ground dried-pork meat product was produced by adding several binding agents at different drying temperatures and times. The drying time affected moisture content and water activity in all drying temperature. However, under the similar drying conditions, the extent of drying varied depending on the type of binding agents. The results of sensory evaluation for texture degree and overall acceptability indicated the following: overall, higher drying temperatures and longer drying time heightened the degree of texture, and the overall acceptability varied depending on binding agent type. Physicochemical and sensory characteristics were analyzed to determine any possible correlation. The results revealed a high correlation between moisture content, water activity, shear forces, and sensory evaluation (p<0.01). However, there was no correlation with respect to overall acceptability.

Chemometric Studies on Brain-uptake of PET Agents via VolSurf Analysis

  • Lee, Hyo-Seon;Kim, Mi-Kyoung;Lee, Chae-Woon;Kim, Jin-Young;Choo, Il-Han;Woo, Jong-Inn;Chong, You-Hoon
    • Bulletin of the Korean Chemical Society
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    • v.29 no.1
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    • pp.61-68
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    • 2008
  • High initial (2 minutes after iv injection) brain-uptake of PET agents is required to deliver the agent to binding sites in brain tissue but, for quantification of the specific binding, relatively rapid washout of free and non-specifically bound PET agents from the brain (30 minutes after injection) also is required. In order to compare the physicochemical properties of the PET agents which are responsible for early brain-uptake and rapid washout, respectively, chemometric analysis on brain-uptake of PET agents was performed via a classical VolSurf approach. According to the PCA and PLS results, high 2-30 min brain-uptake ratio seems to be related to the large hydrophobic regions in the PET agents which are not confined to a particular surface.

Studies on the Binding Affinity of Aminoglycoside Antibiotics to the HIV-l Rev Responsive Element for Designing Potential Antiviral Agents

  • Kwon, Young-Joo
    • Journal of Microbiology and Biotechnology
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    • v.16 no.1
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    • pp.109-117
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    • 2006
  • The Rev binding to Rev Responsive Element (RRE) of HIV-1 mRNA plays an important role in the HIV-I viral replication cycle. The disruption of the Rev-RRE interaction has been studied extensively in order to develop a potential antiviral drug. In order to provide the basis for a more promising approach to develop a Rev-RRE binding inhibitor against HIV-I infection, it is necessary to understand the binding modes of the aminoglycoside antibiotics to RRE. In the present study, the binding mode of a modified antibiotic, a neamine conjugated with pyrene and arginine (NCPA), to RRE has been studied by the methods of $T_m$ measurement and spectroscopic analysis of RRE with or without antibiotics. The results confirmed that NCPA competes with Rev in binding to RRE.

Assessment of Lipopolysaccharide-binding Activity of Bifidobacterium and Its Relationship with Cell Surface Hydrophobicity, Autoaggregation, and Inhibition of Interleukin-8 Production

  • Park, Myeong-Soo;Kim, Min-Jeong;Ji, Geun-Eog
    • Journal of Microbiology and Biotechnology
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    • v.17 no.7
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    • pp.1120-1126
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    • 2007
  • This study was performed to screen probiotic bifidobacteria for their ability to bind and neutralize lipopolysaccharides (LPS) from Escherichia coli and to verify the relationship between LPS-binding ability, cell surface hydrophobicity (CSH), and inhibition of LPS-induced interleukin-8 (IL-8) secretion by HT-29 cells of the various bifidobacterial strains. Ninety bifidobacteria isolates from human feces were assessed for their ability to bind fluorescein isothiocyanate (FITC)-labeled LPS from E. coli. Isolates showing 30-60% binding were designated LPS-high binding (LPS-H) and those with less than 15% binding were designated LPS-low binding (LPS-L). The CSH, autoaggregation (AA), and inhibition of LPS-induced IL-8 release from HT-29 cells of the LPS-H and LPS-L groups were evaluated. Five bifidobacteria strains showed high levels of LPS binding, CSH, AA, and inhibition of IL-8 release. However, statistically significant correlations between LPS binding, CSH, AA, and reduction of IL-8 release were not found. Although we could isolate bifidobacteria with high LPS-binding ability, CSH, AA, and inhibition of IL-8 release, each characteristic should be considered as strain dependent. Bifidobacteria with high LPS binding and inhibition of IL-8 release may be good agents for preventing inflammation by neutralizing Gram-negative endotoxins and improving intestinal health.

Preparation and characterization of Ga-68-deferoxamine to test the feasibility as a bifunctional chelating agent or a renal imaging radiopharmaceutical

  • Kim, Young Ju;Lee, Yun-Sang;Jeong, Jae Min
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.1 no.1
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    • pp.31-37
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    • 2015
  • Chelating agents 1,4,7-triazacyclononanetriacetic acid (NOTA), 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) and 30-amino-3,14,25-trihydroxy-3,9,14,20,25-penta-azatriacontane-2,10,13,21,24-pentaone (desferrioxamine, DFO) were labeled with $^{68}Ga$ and tested in vitro properties to check the feasibility of using DFO as a bifunctional chelating agent or renal imaging agent. The chelating agents of concentration $2{\mu}M$ were labeled with $^{68}Ga$ in 0.1 M HCl at pH 1.7-10.3 at room temperature and $80^{\circ}C$ and the optimal pH for labeling each chelating agent was found. And then, the chelating agents were labeled with $^{68}Ga$ in various concentration of chelating agents at optimal pH. The labeled chelating agents were subject to stability test in human serum and to binding studies to human red blood cell (RBC) and plasma protein. The optimal pH's of NOTA, DOTA and DFO for $^{68}Ga$-labeling were 4.4, 3.6 and 5.6, respectively. DFO ($10{\mu}M$) showed high labeling efficiency (>97%) at pH 5.6. All the labeled chelating agents showed high stability in human serum. $^{68}Ga$-DFO showed low RBC binding but significant amount was bound to plasma protein. The results demonstrated that $^{68}Ga$-DFO can be used as a bifunctional chelating agent but not as a renal imaging agent.

Developing a Protein-chip for Depigmenting Agents Screening (미백제 스크리닝용 단백질칩의 개발)

  • Kim, Eun-Ki;Kwak, Eun-Young;Han, Jung-Sun;Lee, Hyang-Bok;Shin, Jung-Hyun
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.31 no.1 s.49
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    • pp.13-16
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    • 2005
  • For the high-throughput-screening system (HTS) of depigmenting agents using a protein chip, effects of oligonucleotide-inhibitor sequence on the binding of Mitf protein to E box of MC1R was investigated. The sequence of oligonucletide-inhibitor affected the binding of the target DNA to Mitf, depending on the location of the sequence variation in the inhibitor nucleotide. The oligonucletide-inhibitor that changed the CATGTG sequence didn't show enough inhibition of the target DNA to Mitf, whereas significant inhibition was observed when the sequence outside the CATGTG was changed. This result indicated that CATCTG is crucial sequence for the binding of Mitf to I-box which initiates the transcription of pigmenting genes.