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Jung, Kix2010,Hye,Kang, Sunx2010,Hee,Kang, Minx2010,Kyoung,Kim, Soyeon,Kim, Heex2010,Kyung,Kim, Yeounx2010,Hee,Ho Lee, Gang,Shim, Gyux2010,Bo,Jung, Jaex2010,Chang,Chang, Yongmin,Kim, Tae WILEY‐VCH Verlag 2015 European journal of inorganic chemistry Vol.2015 No.4
<P><B>Abstract</B></P><P>The synthesis of two bifunctional chelates, 1,4,7,10‐tetraazacyclododecane‐1,4,7‐triacetic acid (DO3A) conjugates of benzothiazoles (H<SUB>3</SUB>L<SUP>3a</SUP> and H<SUB>3</SUB>L<SUP>3b</SUP>), and the corresponding gadolinium complexes (GdL<SUP>3a</SUP> and GdL<SUP>3b</SUP>) was achieved. The intracellular and tumor‐specific nature of GdL<SUP>3a</SUP> and GdL<SUP>3b</SUP> were confirmed by magnetic resonance images of the cytosols and nuclei of various cell lines. The two complexes displayed antitumor activities with varying degrees of growth‐inhibition and total‐growth‐inhibition values depending on the types of tumor cells. They caused morphological changes in tumor cell lines at much lower concentrations of gadolinium ([Gd] ≥ 50 μ<SMALL>M</SMALL>) than their predecessors, DO3A–(<I>p</I>‐aniline benzothiazole) conjugates (H<SUB>3</SUB>L<SUP>1</SUP>), and its Gd<SUP>III</SUP> complex (GdL<SUP>1</SUP>) required concentrations that were almost four times as high ([Gd] ≥ 200 μ<SMALL>M</SMALL>).</P>
Capsule endoscopy in small bowel tumors: A multicenter Korean study
Cheung, Dae Young,Lee, Inx2010,Seok,Chang, Dong Kyung,Kim, Jin Oh,Cheon, Jae Hee,Jang, Byung Ik,Kim, Yongx2010,Sik,Park, Cheol Hee,Lee, Kwang Jae,Shim, Kix2010,Nam,Ryu, Jix2010,Kon,Do, Jaex2 Blackwell Publishing Asia 2010 Journal of gastroenterology and hepatology Vol.25 No.6
<P><B>Abstract</B></P><P><B>Background and Aim: </B> Capsule endoscopy (CE) has proven to be highly effective at detecting small bowel lesions in a variety of clinical conditions, but studies concerning the practical impact of CE on small bowel tumors are still scarce, especially in the Asian population. The aim of this study was to evaluate the diagnostic and therapeutic impact of CE in the field of small bowel tumors.</P><P><B>Methods: </B> CE records consecutively pooled from the beginning of use of CE in Korea, October 2001 until April 2008, in 14 centers throughout Korea were reviewed. Clinical information and CE video images of small bowel tumors were analyzed.</P><P><B>Results: </B> A total of 1332 cases undergoing CE were reviewed with all clinical indications. Small bowel tumors were diagnosed with CE in 57 (4.3%) of 1332 patients. The tumors were malignant in 33 cases, and included three adenocarcinomas, eight lymphomas, 20 gastrointestinal stromal tumors, and two metastatic cancers. The most frequent indications for CE in malignant tumors were obscure gastrointestinal bleeding, followed by abdominal pain and weight loss. Thirty of 57 tumors were identified exclusively by CE (diagnostic impact = 30/57), and they were smaller in size (mean, range: 14.3 mm, 2–35 mm) compared to the other tumors detected in radiological studies (48.7 mm, 10–110 mm). Seven patients underwent surgical resection (therapeutic impact = 7/57).</P><P><B>Conclusion: </B> CE effectively identifies small bowel tumors that are undetectable by conventional radiological studies (diagnostic impact = 52.6%) and can critically change the therapeutic course (therapeutic impact = 12.3%).</P>
Evidence of carrier‐mediated transport in the penetration of donepezil into the rat brain
Kim, Mix2010,Hwa,Maeng, Hanx2010,Joo,Yu, Kyungx2010,Ha,Lee, Kyeongx2010,Ryoon,Tsuruo, Takashi,Kim, Daex2010,Duk,Shim, Chang‐,Koo,Chung, Sukx2010,Jae Wiley Subscription Services, Inc., A Wiley Company 2010 Journal of Pharmaceutical Sciences Vol.99 No.3
<P><B>Abstract</B></P><P>The objective of this study was to characterize the mechanism that controls the transport of donepezil into the brain. The apparent brain uptake clearance (CL<SUB>app,br</SUB>) was decreased as a function of the dose of donepezil, suggesting an involvement of a saturable transport process via transporter(s) in the penetration across the blood–brain barrier (BBB). Consistent with <I>in vivo</I> results, the uptake of substrates for organic cation transporters was significantly reduced by donepezil in both MBEC4 cells (i.e., a model for BBB) and HEK 293 cells expressing the transporters found in the brain, indicative of the involvement of organic cation transporters in the transport of the drug. Furthermore, donepezil transport was enhanced (<I>p</I> < 0.01) in HEK 293 cells expressing rOCNT1, rOCTN2, or rCHT1. The CL<SUB>app,br</SUB> was reduced up to 52.8% of the control in rats that had been pretreated with choline, while the CL<SUB>app,br</SUB> was unaffected with pretreatments with organic cations other than choline, suggesting that choline and donepezil share a common transport mechanism in the penetration across the BBB <I>in vivo</I>. Taken together, these observations suggest that the transport of donepezil across the BBB is mediated by organic cation transporters such as choline transport system(s). © 2009 Wiley‐Liss, Inc. and the American Pharmacists Association J Pharm Sci 99: 1548–1566, 2010</P>
Chae, Yoonx2010,Jee,Lee, Kyeongx2010,Ryoon,Noh, Chix2010,Kyung,Chong, Saeho,Kim, Daex2010,Duk,Shim, Chang‐,Koo,Chung, Sukx2010,Jae Wiley Subscription Services, Inc., A Wiley Company 2012 Journal of Pharmaceutical Sciences Vol.101 No.3
<P><B>Abstract</B></P><P>The objectives of this study were to investigate the allele frequencies and linkage disequilibrium (LD) in the organic anion transporting polypeptide 1B3 (OATP1B3) in the Korean population and to examine the functional consequences. Using samples from 48 Koreans, direct sequencing was carried out to determine the allele frequencies and LD of OATP1B3 in a representative Korean population. Thirty‐six genetic variations in the transporter were found in Koreans; among them, five undocumented variations (i.e.,−6436G>C in the 5′‐upstream region, 26A>C and 586A>G in the protein coding region, and IVS6‐72A>T and IVS12‐80A>T in intron regions) were identified. In the upstream region, −5035G>A was found to have lowered gene expression, as determined by a reporter gene assay, suggesting that this variation reduces the expression of OATP1B3 in humans. The functional relevance of the genetic variations in the protein coding region was determined by an uptake study involving representative substrates in human embryonic kidney 293 cells expressing wild type or variant forms. Variations involving 699G>A showed a reduced uptake activity for testosterone, but not for estradiol 17β‐<SMALL>d</SMALL>‐glucuronide or methotrexate, indicating that the functional impact of the variations is substrate specific. Considering the kinetic relevance of OATP1B3, the functionally affected variations may be therapeutically important. © 2011 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 101:1302–1313, 2012</P>
Public attitudes toward cancer and cancer patients: a national survey in Korea
Cho, Juhee,Smith, Katherine,Choi, Eunx2010,Kyung,Kim, Imx2010,Ryung,Chang, Yoonx2010,Jung,Park, Hyunx2010,Young,Guallar, Eliseo,Shim, Young Mog John Wiley Sons, Ltd 2013 PSYCHOONCOLOGY Vol.22 No.3
<P><B>Abstract</B></P><P><B>Background</B></P><P>Regardless of improved survival rate, negative images and myths about cancer still abound. Cancer stigma may reduce patients' life opportunities resulting in social isolation, decreased level of emotional well‐being, and poor health outcomes. This study was aimed to evaluate public attitudes toward cancer and cancer patients and people's willingness to disclose cancer diagnosis in South Korea.</P><P><B>Methods</B></P><P>A cross‐sectional survey was conducted in August and September 2009. A nationally representative sample of 1011 men and women with no history of cancer was recruited. A set of 12 questions grouped into three domains (impossibility of recovery, cancer stereotypes, and discrimination) was used to assess public attitudes toward cancer.</P><P><B>Results</B></P><P>It was found 58.5% of study participants agreed that it is impossible to treat cancer regardless of highly developed medical science, 71.8% agreed that cancer patients would not be able to make contributions to society, and 23.5% agreed that they would avoid working with persons who have cancer. The proportions of people who said that that they would not disclose a cancer diagnosis to family, friends or neighbors, or coworkers were 30.2%, 47.0%, and 50.7%, respectively. Negative attitudes toward cancer were strongly associated with lower willingness to disclose a cancer diagnosis.</P><P><B>Conclusions</B></P><P>Negative attitudes, stereotypes, and discriminating attitudes toward cancer and people affected by the disease were very common in spite of clinical progress and improved survivorship.</P><P><B>Impact</B></P><P>Our findings emphasize the need for health policy and social changes to provide a more supportive environment for cancer survivors. Copyright © 2012 John Wiley & Sons, Ltd.</P>