• Title/Summary/Keyword: A-CN-K

Search Result 739, Processing Time 0.025 seconds

A Novel Suberoylanilide Hydroxamic Acid Histone Deacetylase Inhibitor Derivative, N25, Exhibiting Improved Antitumor Activity in both Human U251 and H460 Cells

  • Zhang, Song;Huang, Wei-Bin;Wu, Li;Wang, Lai-You;Ye, Lian-Bao;Feng, Bing-Hong
    • Asian Pacific Journal of Cancer Prevention
    • /
    • v.15 no.10
    • /
    • pp.4331-4338
    • /
    • 2014
  • $N^1$-(2, 5-dimethoxyphenyl)-$N^8$-hydroxyoctanediamide (N25) is a novel SAHA cap derivative of HDACi, with a patent (No. CN 103159646). This invention is a hydroxamic acid compound with a structural formula of $RNHCO(CH_2)6CONHOH$ (wherein R=2, 5dimethoxyaniline), a pharmaceutically acceptable salt which is soluble. In the present study, we investigated the effects of N25 with regard to drug distribution and molecular docking, and anti-proliferation, apoptosis, cell cycling, and $LD_{50}$. First, we designed a molecular approach for modeling selected SAHA derivatives based on available structural information regarding human HDAC8 in complex with SAHA (PDB code 1T69). N25 was found to be stabilized by direct interaction with the HDAC8. Anti-proliferative activity was observed in human glioma U251, U87, T98G cells and human lung cancer H460, A549, H1299 cells at moderate concentrations ($0.5-30{\mu}M$). Compared with SAHA, N25 displayed an increased antitumor activity in U251 and H460 cells. We further analyzed cell death mechanisms activated by N25 in U251 and H460 cells. N25 significantly increased acetylation of Histone 3 and inhibited HDAC4. On RT-PCR analysis, N25 increased the mRNA levels of p21, however, decreased the levels of p53. These resulted in promotion of apoptosis, inducing G0/G1 arrest in U251 cells and G2/M arrest in H460 cells in a time-dependent and dose-dependent manner. In addition, N25 was able to distribute to brain tissue through the blood-brain barrier of mice ($LD_{50}$: 240.840mg/kg). In conclusion, our findings demonstrate that N25 will provide an invaluable tool to investigate the molecular mechanism with potential chemotherapeutic value in several malignancies, especially human glioma.

A survey of respiratory pathogens in dogs for adoption in Gwangju metropolitan city animal shelter, South Korea (광주광역시동물보호소 입양 대상 유기견의 호흡기 질병 실태 조사)

  • Koh, Ba-Ra-Da;Kim, Han-Na;Kim, Hyo-Jung;Oh, A-Reum;Jung, Bo-Ram;Park, Jae-Sung;Lee, Jae-Gi;Na, Ho-Myoung;Kim, Yong-Hwan
    • Korean Journal of Veterinary Service
    • /
    • v.43 no.2
    • /
    • pp.67-77
    • /
    • 2020
  • Canine infectious respiratory disease (CIRD), also known as infectious tracheobronchitis or kennel cough occurs in a multiple-dog environment such as a shelter. In this study, we were collected 300 of nasal swab samples from dogs and 145 of environmental samples from a shelter to investigate respiratory pathogens of dogs in the Gwangju metropolitan city animal shelter from February to October, 2019. Bacteria cultures for isolation of Bordetella (B.) bronchiseptica and polymerase chain reaction (PCR) tests were performed for detection of eleven canine respiratory pathogens, namely Mycoplasma (M.) cynos, canine distemper virus (CDV), canine influenza virus (CIV), canine parainfluenza virus (CPIV), canine respiratory coronavirus (CRCoV), alpha-coronavirus (CCoV), canine pneumovirus (CnPnV), canine hepacivirus (CHeV), canine adenovirus type 2 (CAdV-2), canine herpesvirus-1 (CHV-1) and canine bocavirus (CBoV). Among 300 nasal swab samples, 148 samples (49.3%) were positive for at least one pathogens. CHV-1 was the most common pathogen, found in 95/300 (31.7%) samples. Subsequently, M. cynos (22.0%), B. bronchiseptica (2.3%), CPIV (2.0%), CBoV (1.7%), CCoV (0.7%) were detected. The detection rates of M. cynos and CHV-1 according to the duration of stay in the shelter were statistically significant. Among environmental samples, M. cynos, CCoV, CBoV and CHV-1 were detected in 45/145 (31.0%). These results indicated the need for disease control and prevention systems in the shelter.

Retention Behavior and Separation of Phenol Derivatives through Cyclodextrin Complexes in Reversed-Phase Liquid Chromatography (역상 액체 크로마토그래피에서 씨클로덱스트린 착물을 이용한 페놀유도체들의 머무름 거동 및 분리)

  • Moon, Young-Ja;Kang, Sam-Woo
    • Analytical Science and Technology
    • /
    • v.11 no.3
    • /
    • pp.179-188
    • /
    • 1998
  • The capacity factor of fifteen phenol derivatives was determined with respect to the concentration of ${\alpha}$- or ${\beta}$-cyclodextrin [CD], the type as well as the content of organic solvent in the mobile phase, and the temperature. The effect of the inclusion complex formation between solutes and ${\alpha}$- or ${\beta}$-cyclodextrin on their retention and selectivity has been investigated. The inclusion effect of ${\beta}$-cyclodextrin was the most effective in aqueous methanol, whereas only a poor effect was observed in aqueous tetrahydrofuran and aqueous acetonitrile. A plot of the reciprocal of the capacity factor against $[CD]_T$ gives a straight line and the dissociation constant, $K_D$ of the inclusion complex can be calculated from the slope. It was possible to estimate the $k_D$ values in 100% water from a linear plot of $pK_D$ vs. water content in the solution by extrapolation. The separation factor, ${\alpha}$, of two compounds has been found to be affected not only by the $[CD]_T$ but also by their $K_D$ values. Under optimum conditions, some mixtures of phenol derivatives were able to separate successfully.

  • PDF

Geochemical Study of the Cretaceous Granitic Rocks in Southwestern Part of the Korean Peninsula (한반도 남서부지역에 분포하는 백악기 화강암류에 대한 지화학적 연구)

  • Wee Soo Meen;Park Se Mi;Choi Seon Cyu;Ryu In Chang
    • Economic and Environmental Geology
    • /
    • v.38 no.2 s.171
    • /
    • pp.113-127
    • /
    • 2005
  • Cretaceous intrusive and extrusive rocks are widely distributed in the southwestern part of the Korean peninsula, possibly the result of intensive magmatism which occurred in response to subduction of the western proto-Pacific plate beneath the north-eastern part of the Eurasian plate. Geochemical and petrological study on the Cretaceous granitic rocks were carried out in order to constrain the petrogenesis of the granitic magma and to establish the paleotectonic environment of the area. Whole rock chemical data of the granitic rocks from the study area indicate that the all the rocks have characteristics of calc-alkaline series in the subalkaline field. The overall geochemical features show systematic variations in each granitic body, but the source materials of each granitic body are thought to have been different in their chemical composition. Higher values of $Fe_2O_3/FeO$ of the granitic rocks in the western area suggest that the granitoids had been solidified under highly oxidizing environment. The granitic bodies in the eastern area also show higher contents of Li, Ni, Co, Sr, Cr, Sc and lower Rb and Nb compared to the those of the western area. Chondrite normalized REE patterns show generally enriched LREE and strong negative Eu anomalies in the western wet while slight to flat Eu anomalies in the east-ern area. The REE and $(La/Lu)_{CN}$ of the granites are $60{\~}499ppm$ and $8.9{\~}66$ correspond to the range of the continental margin granite. On the ANK vs. ACNK and tectonic discrimination diagrams, parental magma type of the granites corresponds to I-type, VAG and syn-collision granite. Interpretations of the chemical characteristics of the granitic rocks favor their emplacement in a compressional tectonic regime at continental margin during the subduction of proto-Pacific plate.

Conformations, Chemical Reactivities and Spectroscopic Characteristics of Some Di-substituted Ketenes: An ab initio Study

  • Gupta, V.P.;Sharma, Archna;Agrawal, S.G.
    • Bulletin of the Korean Chemical Society
    • /
    • v.27 no.9
    • /
    • pp.1297-1304
    • /
    • 2006
  • A systematic study of the structure, energetics and spectral characteristics of substituted aminoketenes $R(NH_2)$C=C=O (R = H, $CH_3$, $NH_2$, OH, $OCH_3$, CH=$CH_2$, C$\equiv$CH, CN, CHO, NO, $NO_2$) which are highly reactive and transient intermediates in synthesis has been conducted by ab initio calculations at the MP2/6- 31G*//MP2/6-31G* level. Twenty four stable isomers of the eleven substituted aminoketenes having dihedral angles $\phi NH_2\sim120{^{\circ}}$ and $60^{\circ}$ have been identified and their optimized geometries and energies obtained. Electrostatic and steric effects on the molecular geometries have been analyzed. While the $\pi$-acceptor groups lead to planar conformations, the electron-donor groups give rise to non-planar conformations. Isodesmic substituent stabilization energies relative to alkenes have been calculated and correlation with group electronegativities established. Role of induction effect by the substituent groups and resonance effects in charge distribution in the molecules has been analyzed. An analysis of the asymmetric stretching frequencies and intensities of the C=C=O group shows that affect of non-$\pi$ acceptor substituents on the frequency is determined by the field effect (F) and resonance effect (R) parameters, the calculated intensities I (km/mol.) are correlated to group electronegativities $x$ of the substituents by the relationship I = 640.2–100.1 $x$ (r = 0.92). The $\pi$-acceptor substituents increase the intensity which may be explained in terms of their delocalizing effect on the negative charge at the $C_{\beta}$ atom.

Spatial Analysis of Nonpoint Source Pollutant Loading from the Imha dam Watershed using L-THIA (L-THIA를 이용한 낙동강수계 임하댐유역 비점오염원의 공간적 분포해석)

  • Jeon, Ji-Hong;Cha, Daniel K.;Choi, Donghyuk;Kim, Tae-Dong
    • Journal of The Korean Society of Agricultural Engineers
    • /
    • v.55 no.1
    • /
    • pp.17-29
    • /
    • 2013
  • Long-Term Hydrologic Impact Assessment (L-THIA) model which is a distributed watershed model was applied to analyze the spatial distribution of surface runoff and nonpoint source pollutant loading from Imha watershed during 2001~2010. L-THIA CN Calibration Tool linked with SCE-UA was developed to calibrate surface runoff automatically. Calibration (2001~2005) and validation (2006~2010) of monthly surface runoff were represented as 'very good' model performance showing 0.91 for calibration and 0.89 for validation as Nash-Sutcliffe (NS) values. Average annual surface runoff from Imha watershed was 218.4 mm and Banbyun subwatershed was much more than other watersheds due to poor hydrologic condition. Average annual nonpoint source pollutant loading from Imha wateshed were 2,295 ton/year for $BOD_5$, 14,752 ton/year for SS, 358 ton/year for T-N, and 79 ton/year for T-P. Amount of pollutant loading and pollutant loading rates from Banbyun watershed were much higher than other watersheds. As results of analysis of loading rate from grid size ($30m{\times}30m$), most of high 10 % of loading rate were generated from upland. Therefore, major hot spot area to manage nonpoint source pollution in Imha watershed is the combination of upland and Banbyun subwatershed. L-THIA model is easy to use and prepare input file and useful tool to manage nonpoint source pollution at screening level.

Nano-Ruthenium Oxide Polymeric Composite pH Electrodes (나노 Ruthenium Oxide 고분자 복합재료 pH전극)

  • Park, Jongman
    • Journal of the Korean Chemical Society
    • /
    • v.62 no.4
    • /
    • pp.269-274
    • /
    • 2018
  • Surface renewable nano-$RuO_2$/poly(methyl methacrylate) polymeric composite pH electrodes were prepared. The composite electrode with 53 wt% of nano-$RuO_2$ showed similar good response characteristics to nano-$IrO_2$ composite electrode reported earlier. It showed response slope of -58.7 mV/pH, response time of <1 s, surface renewability of $-57.0{\pm}0.3mV/pH$ (n=5) and long time stability for a month as well as low interferences but high interferences by electrochemically active species like $I^-$ and $Fe(CN){_6}^{3-}$. However, the response slope and time became worse at higher pH than 9 compared to those of nano-$IrO_2$ composite electrodes possibly due to the difference of physical properties resulting from higher content of nano-$RuO_2$ in polymeric composite matrix.

Spectrophotometric Determination of Bisphenol A by Complexation with Ferricyanide and Ferric chloride solution (Ferricyanide와 ferric chloride 혼합액을 사용한 Bisphenol A의 비색 정량법 개발)

  • Kum, Eun-Joo;Ryu, Hee-Young;Kwon, Gi-Seok;Sohn, Ho-Yong
    • Journal of Life Science
    • /
    • v.17 no.2 s.82
    • /
    • pp.266-271
    • /
    • 2007
  • Bisphenol A (BPA) has been widely used as a monomer for production of epoxy resins and polycarbonate plastics. The annual production of BPA exceeds 640,000 metric tons in worldwide. BPA, a suspected phenolic endocrine disrupter, is moderately soluble and frequently detected in industrial wastewater. To date, HPLC and GC has been used for BPA analysis. However, HPLC and GC-analysis need high operation lost, experts, and an elaborate pre-treatment of samples, and is difficult to apply on-time and mass analysis. Therefore, simple, mass and rapid detection of BPA in environments is necessary. In the present study, spectrophotometric method of BPA quantification was developed. Based on blue-color product formation with BPA and ferric chloride/ferricyanide under the optimized conditions, the standard curve was acquired $({\lambda}_{750}=0.061\;BPA\;[{\mu}M]+0.07155,\;R^2=0.992)$. Using an established method, the BPA contents in the soil extract, and different water samples and living products, including disposable syringe, cup and plastic tube, were analyzed. The results suggested that the method is useful for BPA determination from different massive samples. Since the BPA metabolites, nontoxic 4-hydroxyacetophenone or 4-hydroxybenzaldehyde, did not form blue-color product, this method is also useful to screen a microorganism for BPA bioremediation.

Molecular and Epidemiological Characterization of Enteroviruses Isolated in Chungnam, Korea from 2005 to 2006

  • Baek, Kyung-Ah;Park, Kwi-Sung;Jung, Eun-Hye;Chung, Eun-Hee;Park, Joon-Soo;Choi, Hwa-Jung;Baek, Seung-Hwa;Jee, Young-Mee;Cheon, Doo-Sung;Ahn, Gwang-Sook
    • Journal of Microbiology and Biotechnology
    • /
    • v.19 no.9
    • /
    • pp.1055-1064
    • /
    • 2009
  • Enteroviruses were identified and characterized from patients with aseptic meningitis and other enterovirus-related diseases in Chungnam, Korea from 2005 to 2006. Enteroviruses were isolated from 79 of 519 cases (15.2%) in 2005, and 37 of 386 cases (9.6%) in 2006. Based on partial VP1 sequencing, a total of 116 enterovirus isolates were resolved into 13 types. Prevalent among the Chungnam isolates were echovirus 18 and coxsackievirus B5 in 2005, and echoviruses 5 and 25 in 2006. This is the first time echoviruses 5 and 18 have been identified in Korea since enterovirus surveillance began there in 1993. The temporal distribution of enterovirus epidemics in Chungnam showed a remarkable seasonal pattern, with cases occurring during most of the three months of the summer from June to August. The highest rate of enterovirus-positive cases occurred in patients less than 1 year of age. The ratio of male to female enterovirus-positive patients was approximately 1.8:1. Comparison of the VP1 amino acid sequences of the 15 coxsackievirus B5 isolates with reference strains revealed that all Chungnam isolates are substituted at positions 23 (V231), 19 (S19G), 75 (Y75F), and 95 (N95S). Upon comparing the nine ECV5 isolates with foreign strains, it was found that only the Chungnam isolates, with the exception of Kor06-ECV5-239cn, have P at position 153 and F at position 146. The three ECV9 isolates from 2006 show alterations at amino acids 36, 148, and 154 outside of the BC-loop and at position 84 in the BC-loop, whereas the seven isolates from 2005 and the other ECV9 strains in the database only show the alteration at position 84 (D, I, N, S). The five ECV25 isolates have an S residue at position 134, whereas most of the foreign strains have an N residue.

A Geochemical Study on Pyrophyllite Deposits and Andesitic Wall-Rocks in the Milyang Area, Kyeongnam Province (경남 밀양지역 납석광상과 안산암질 모암의 지구화학적 연구)

  • Oh, Dae-Gyun;Chon, Hyo-Taek;Min, Kyoung-Won
    • Economic and Environmental Geology
    • /
    • v.25 no.1
    • /
    • pp.27-39
    • /
    • 1992
  • Several pyrophyllite deposits occur around the Milyang area where Cretaceous andesitic rocks and spatially related granitic rocks are widely distributed. Pyrophyllite ores consist mainly of pyrophyllite, and quartz with small amount of sericite, pyrite, dumortierite, and diaspore. The andesitic rocks and spatially related granitic rocks in this area suggest that they could be formed from the same series of a calc-alkaline magma series. The contents of $SiO_2$, $Al_2O_3$, LOI(loss on ignition) are enriched, and $K_2O$, $Na_2O$, CaO, MgO, $Fe_2O_3$ are depleted in altered andesitic rocks and ores. Enrichment of As, Cr, Sr, V, Sb and depletion of Ba, Cs, Ni, Rb, U, Y, Co, Sc, Zn are characteristic during mineralization. The pyrophyllite ores can be discriminated from the altered-and unaltered wall-rocks by an increasing of $(La/Lu)_{cn}$ from 4.18~22.13 to 8.98~55.05. In R-mode cluster analysis, Yb-Lu-Y, La-Ce-Hf-Th-U-Zr, $TiO_2-V-Al_2O_3$, Sm-Eu, $CaO-Na_2O-MnO$, Cu-Zn-Ag, $K_2O-Rb$ are closely correlated. In the discriminant analysis of multi-element data, $P_2O_5$, As, Cr and $Fe_2O_3$, Sr are helpful to identify the ores from the unaltered-and altered wall-rocks. In the factor analysis, the factors of alteration of andesitic rocks and ore mineralization were extracted. In the change of ions per unit volume, $SiO_2$, $Al^{3+}$ and LOI are enriched and $Na^+$, $K^+$, $Ca^{2+}$, $Mg^{2+}$, $Mn^{2+}$ and $Fe^{3+}$ are depleted during the alteration processes. The Milyang and the Sungjin pyrophyllite deposits could be mineralized by hydrothermal alteration in a geochemical condition of low activity ratio of alkaline ions to hydrogen ion with reference to spatially related granitic rocks.

  • PDF