• Title/Summary/Keyword: E-MDR

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Effect of TSHAC on Human Cytochrome P450 Activity, and Transport Mediated by P-Glycoprotein

  • Im, Yelim;Kim, Yang-Weon;Song, Im-Sook;Joo, Jeongmin;Shin, Jung-Hoon;Wu, Zhexue;Lee, Hye Suk;Park, Ki Hun;Liu, Kwang-Hyeon
    • Journal of Microbiology and Biotechnology
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    • v.22 no.12
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    • pp.1659-1664
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    • 2012
  • TSAHC [4'-(p-toluenesulfonylamido)-4-hydroxychalcone] is a promising antitumorigenic chalcone compound, especially against TM4SF5 (four-transmembrane L6 family member 5)-mediated hepatocarcinoma. We evaluated the potential of TSAHC to inhibit the catalytic activities of nine cytochrome P450 isoforms and of P-glycoprotein (P-gp). The abilities of TSAHC to inhibit phenacetin O-deethylation (CYP1A2), coumarin 6-hydroxylation (CYP2A6), bupropion hydroxylation (CYP2B6), amodiaquine N-deethylation (CYP2C8), diclofenac 4-hydroxylation (CYP2C9), omeprazole 5-hydroxylation (CYP2C19), dextromethorphan O-demethylation (CYP2D6), chlorzoxazone 6-hydroxylation (CYP2E1), and midazolam 1'-hydroxylation (CYP3A) were tested using human liver microsomes. The P-gp inhibitory effect of TSAHC was assessed by [$^3H$]digoxin accumulation in the LLCPK1-MDR1 cell system. TSAHC strongly inhibited CYP2C8, CYP2C9, and CYP2C19 isoform activities with $K_i$ values of 0.81, 0.076, and $3.45{\mu}M$, respectively. It also enhanced digoxin accumulation in a dose-dependent manner in the LLCPK1-MDR1 cells. These findings indicate that TSAHC has the potential to inhibit CYP2C isoforms and P-gp activities in vitro. TSAHC might be used as a nonspecific inhibitor of CYP2C isoforms based on its negligible inhibitory effect on other P450 isoforms such as CYP1A2, CYP2A6, CYP2B6, CYP2D6, CYP2E1, and CYP3A.

Anti-CSC Effects in Human Esophageal Squamous Cell Carcinomas and Eca109/9706 Cells Induced by Nanoliposomal Quercetin Alone or Combined with CD 133 Antiserum

  • Zheng, Nai-Gang;Mo, Sai-Jun;Li, Jin-Ping;Wu, Jing-Lan
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.20
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    • pp.8679-8684
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    • 2014
  • CD133 was recently reported to be a cancer stem cell and prognostic marker. Quercetin is considered as a potential chemopreventive agent due to its involvement in suppression of oxidative stress, proliferation and metastasis. In this study, the expression of CD133/CD44 in esophageal carcinomas and Eca109/9706 cells was explored. In immunoflurorescence the locations of $CD133^+$ and multidrug resistance 1 $(MDR1)^+$ in the same E-cancer cells were coincident, mainly in cytomembranes. In esophageal squamous cell carcinomas detected by double/single immunocytochemistry, small $CD133^+$ cells were located in the basal layer of stratified squamous epithelium, determined as CSLC (cancer stem like cells); $CD44^+$ surrounding the cells appeared in diffuse pattern, and the larger $CD44^+$ (hi) cells were mainly located in the prickle cell layer of the epithelium, as progenitor cells. In E-cancer cells exposed to nanoliposomal quercetin (nLQ with cytomembrane permeability), down-regulation of NF-${\kappa}Bp65$, histone deacetylase 1 (HDAC1) and cyclin D1 and up-regulation of caspase-3 were shown by immunoblotting, and attenuated HDAC1 with nuclear translocation and promoted E-cadherin expression were demonstrated by immunocytochemistry. In particular, enhanced E-cadherin expression reflected the reversed epithelial mesenchymal transition (EMT) capacity of nLQ, acting as cancer attenuator/preventive agent. nLQ acting as an HDAC inhibitor induced apoptotic cells detected by TUNEL assay mediated via HDAC-NF-${\kappa}B$ signaling. Apoptotic effects of liposomal quercetin (LQ, with cytomembrane-philia) combined with CD133 antiserum were also detected by CD133 immunocytochemistry combined with TUNEL assay. The combination could induce greater apoptotic effects than nLQ induced alone, suggesting a novel anti-CSC treatment strategy.

A Construction of an Ontology Server based Intelligent Retrieval using XMDR (XMDR을 이용한 지능형 검색 온톨로지 서버 구축)

  • Hwang Chi-Gon;Jung Gye-Dong
    • The Journal of Korean Institute of Communications and Information Sciences
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    • v.30 no.8B
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    • pp.549-561
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    • 2005
  • As Internet and network technologies have been developed, e-commerces are getting more complex and more various. This paper, for meta-data and data exchange between heterogeneous database systems, uses XML schema proposed in W3C, and XML schema can present meta-data and data of relational database system as XML document format which is structural. It supports various primitive data formats, so that it uses the structure which reflects adequately data formats which relational database system offered. However, current e-commerces use heterogeneous platforms, so difficulties that is mutual interchange and management exist. For the solution for these problems, a standard ontology which defines relations of product classifications and the standard of property expression and the location ontology which offers e-commerce's information about products are constructed. Applying these ontology information to search system, by offering information which customers need efficient search is performed. Combining these ontologies and product classification category information, called XMDR, this XMDR is introduced into product search system, so this paper proposes to construct ontology server method for efficient search.

A Design of Model For Interoperability in Multi-Database based XMDR on Distributed Environments (분산환경에서 XMDR 기반의 멀티데이터 베이스 상호운영 모델 설계)

  • Jung, Kye-Dong;Hwang, Chi-Gon;Choi, Young-Keun
    • Journal of the Korea Institute of Information and Communication Engineering
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    • v.11 no.9
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    • pp.1771-1780
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    • 2007
  • The necessity of Information integration has emphasized by advancement of internet and change of enterprise environment. In enterprises, it usually integrates the multi-database constructing by M&A. For this integration of information it must guarantee interpretation and integration which is stabilized with solving heterogeneous characteristic problem. In this paper, we propose the method that change the global XML query to local XML query for interpretation. It is based on XMDR(eXtended Meta-Data Registry) which expresses the connection between the standard and the local for solve the interoperability problem in heterogeneous environment. Thus, we propose the legacy model that can search and modify by one Query with creating global XML Query by XMDR. and for his, we use the 2PC technique which is the distributed transaction control technique of existing.

Functional Imaging of the Multidrug Resistance In Vivo (기능적 영상술을 이용한 다약제 내성의 체내 진단)

  • Lee, Jea-Tae
    • 대한핵의학회:학술대회논문집
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    • 2001.05a
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    • pp.66-75
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    • 2001
  • Although diverse mechanisms are involved in multidrug resistance for chemotherapeutic drugs, the development of cellular P-glycoprotein(Pgp) and multidrug-resistance associated protein (MRP) are important factors in the chemotherapy failure to cancer. Various detection assays provide information about the presence of drug efflux pumps at the mRNA and protein levels. However these methods do not yield information about dynamic function of Pgp and MRP un vivo. Single photon emission tomography (SPECT) and positron emission tomography (PET) are available for the detection of Pgp and MRP-mediated transport. $^{99m}Tc$-sestaMIBl and other $^{99m}Tc$-radiopharmaceuticals are substrates for Pgp and MRP, and have been used in clinical studies for tumor imaging, and to visualize blockade of Pgp-mediated transport after modulation of Pgp pump. Colchicine, verapamil and daunorubicin labeled with $^{11}C$ have been evaluated for the quantification of Pgp-mediated transport with PET in vivo and reported to be feasible substrates with which to image Pgp function in tumors. Leukotrienes are specific substrates for MRP and N-$[^{11}C]$acetyl-leukotriene E4 provides an opportunity to study MRP function non-invasively in vivo. Results obtained from recent publications are reviewed to confirm the feasibility of using SPECT and PET to study the functionality of MDR transporters in vivo.

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Plasmid Profile and ${\beta}$-Lactamase Type of Multidrug-Resistant Salmonella typhi Isolated from Korea, 1997 (국내 분리 다제내성 장티프스균의 Plasmid 및 ${\beta}$-lactamase의 특성에 관한 연구)

  • Yoo, Jung-Sik;Shin, Young-Hack;Oh, Kyung-Soo;Lee, Jeom-Kyu;Kim, Ki-Sang
    • The Journal of the Korean Society for Microbiology
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    • v.34 no.5
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    • pp.445-452
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    • 1999
  • Eight strains of multidrug-resistant (MDR) Salmonella typhi were isolated from Kyonggi area during January-February, 1997. They were resistant to ampicillin, amoxicillin, carbenicillin, tetracycline, chloramphenicol, trimethoprim/sulfamethoxazole, trimethoprim. Eight strains had one plasmid respectively which size was approximately M.W 220 kb and showed same restriction pattern by endonuclease HindIII. The plasmid was similar to the plasmid in size that was related to multidrug resistant S. typhi isolated from southeast Asia. It were transferred by conjugation to recipient E. coli K-12 in frequency of $2.43{\times}10^4-1.73{\times}10^{-2}$ and transconjugant showed same drug-resistant pattern with donor cells. All of 8 strains produced ${\beta}$-lactamase that was assummed to TEM-l type by isoelectric focusing and PCR.

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A Design of Data Grid MiddleWare Using XMDR (XMDR을 이용한 데이터 그리드 미들웨어 설계)

  • Noh Seon-Taek;Moon S.J.;Eum Y.H.;Kook Y.G.;Jung K.D.;Choi Y.K.
    • Proceedings of the Korean Information Science Society Conference
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    • 2006.06a
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    • pp.427-429
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    • 2006
  • 데이터 그리드는 분산 데이터베이스 환경에서 상호간 데이터의 공유 및 교환을 통하여 분산 데이터를 효율적으로 사용하기 위한 기술이다. 최근에는 레거시 시스템간의 협업을 하기 위해 상호 연결의 필요성이 강조되고 있으며 많은 연구가 진행되고 있다. 독립주인 레거시 시스템을 상호 연결하기 위해서는 노드간의 회선 점유율이 증가하고, 데이터의 이질적인 문제가 발생한다. 이러한 문제점을 해결하기 위해 본 논문에서는 XMDR 기반의 데이터 그리드 시스템을 제안한다. 본 논문의 데이터 그리드 미들웨어는 ISO/IEC11179에서 제안한 정보 공유 및 교환을 위한 표준인 MDR과 정보의 효율적인 이용을 위한 온톨로지를 포함하여 확장한 개념인 XMDR(eXtended Metadata Registry)에 기반을 두었으며 분산 플랫폼으로부터 독립적이고 자유로운 이동성을 가지고 있는 이동 에이전트 기술을 사용하였다.

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Cytotoxic Polyene Antibiotics from Myxococcus stipitatus JW111 (Myxococcus stipitatus JW111이 생산하는 Polyene계 항암활성물질)

  • Ahn, Jong-Woong
    • Applied Biological Chemistry
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    • v.45 no.2
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    • pp.114-118
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    • 2002
  • Phenalamides $A_1{\sim}A_3$ were reisolated as cytotoxic substances from culture broth of Myxococcus stipitatus JW111. The producing strain was isolated from the marine sediment collected off the shore of Geomun Island, Korea. The active principles were extracted from cell mass with acetone and successively purified by silica gel column chromatography, Sephadex LH-20 column chromatography, and finally recycling prep. HPLC. These compounds demonstrated significant cytotoxicity against certain human cancer cells, having $IC_50$ values ranging from 0.23 to 0.50 ${\mu}g/ml$. Moreover, they also inhibited the growth of adriamycin-resistant HCT/ADM human cancer cell line as well as its parent sensitive cell line.

Design and Implementation of a Reusable and Extensible HL7 Encoding/Decoding Framework (재사용성과 확장성 있는 HL7 인코딩/디코딩 프레임워크의 설계 및 구현)

  • Kim, Jung-Sun;Park, Seung-Hun;Nah, Yun-Mook
    • Journal of KIISE:Computing Practices and Letters
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    • v.8 no.1
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    • pp.96-106
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    • 2002
  • this paper, we propose a flexible, reusable, and extensible HL7 encoding and decoding framework using a Message Object Model (MOM) and Message Definition Repository (MDR). The MOM provides an abstract HL7 message form represented by a group of objects and their relationships. It reflects logical relationships among the standard HL7 message elements such as segments, fields, and components, while enforcing the key structural constraints imposed by the standard. Since the MOM completely eliminates the dependency of the HL7 encoder and decoder on platform-specific data formats, it makes it possible to build the encoder and decoder as reusable standalone software components, enabling the interconnection of arbitrary heterogeneous hospital information systems(HISs) with little effort. Moreover, the MDR, an external database of key definitions for HL7 messages, helps make the encoder and decoder as resilient as possible to future modifications of the standard HL7 message formats. It is also used by the encoder and decoder to perform a well formedness check for their respective inputs (i. e., HL7 message objects expressed in the MOM and encoded HL7 message strings). Although we implemented a prototype version of the encoder and decoder using JAVA, they can be easily packaged and delivered as standalone components using the standard component frameworks like ActiveX, JAVABEAN, or CORBA component.

Serotype and antimicrobial susceptibility of Salmonella spp. isolated from pigs and cattle (소와 돼지유래 Salmonella속 균의 혈청형 및 약제감수성)

  • Lee, Woo-Won;Jung, Byeong-Yeal;Lee, Gang-Rok;Lee, Dong-Soo;Kim, Yong-Hwan
    • Korean Journal of Veterinary Service
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    • v.32 no.1
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    • pp.49-59
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    • 2009
  • At the present study, it was aimed to explore the states of antimicrobial resistant Salmonella spp. isolates from 3,850 pigs (2,732 ileocecocolic lymphnodes and 1,118 cecal contents) and 1,764 cattle (965 cecal lymphnodes and 799 cecal contents) slaughtered in Busan province from December 2000 to November 2001. Among 5,614 samples, 457 of Salmonella spp. were isolated from pig lymphnodes (13.5%), pig cecal contents (4.4%), cattle lymphnodes (3.5%) and cattle cecal contents (0.5%). Salmonella spp. were showed different isolation ratio, that was 10.8% in summer, 9.0% in autumn, 8.4% in spring and 5.0% in winter. As a result of serotyping, B group (65.4%) were identified as the most common in pigs and cattle, in order of $C_1$ (14.0%), $D_1$ (5.5%), $C_2$ (4.2%), $E_1$ (4.2%) and L (3.5%). 34 serotypes were found, among them, Salmonella Typhimurium (S. Typhimurium) (21.0%) was the most common serotype from pigs and cattle. The major serotypes were in order of S. Derby (15.3%), S. Schwarzengrund (14.7%), S. Typhimurium var Copenhagen (9.2%), S. Mbandaka (5.7%), S. Enteritidis (5.5%) and S. Ruiru (3.5%). The most common serotype was S. Typhimurium in pigs, and S. Ruiru in cattle. S. Ruiru was firstly isolated from pigs and cattle in Korea. In antimicrobial susceptibility test, all the isolates were demonstrated susceptibility to norfloxacin and ofloxacin. But the isolates were showed resistance other antibiotics in order of doxycycline (68.3%), tetracycline (67.8%), penicillin (54.5%) and streptomycin (52.5%). S. Typhimurium were exhibited resistance to ampicillin (34.8%), chloramphenicol (36.2%), streptomycin (94.9%), sulfamethoxazole/trimethoprim (34.8%) and tetracycline (97.8%). There were 53 strains (38.4%) which had multi drug resistant (MDR) isolates, resistant to more than 6 antimicrobial agents. The most common resistance patterns of MDR isolates were ampicillin, chloramphenicol, carbenicillin, doxycycline, nalidixic acid, penicillin, streptomycin, sulfamethoxazole/trimethoprim and tetracycline (ACCbDNaPSSuT).