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Diary! ether: Synthesis and biological evaluation as antimitotic agents
AHN soon Kil,LEE Mi-sung,IN Jin-Kyung,YANG Jun geun,KWAK Jae-Hwan,LEE Heesoon,JUNG Jae-Kyung,BOOVANAHALLI Shanthaveerappa K .,LEE Kyeong,CHOI Nam Song,LEE sungsook,MOON Seung Kee,KIM Soo Jin 대한약학회 2006 大韓藥學會 總會 및 學術大會 Vol.2006 No.2
Lee, Young-Keun,Chang, Hwa-Hyoung,Lee, Ho-Jin,Park, Heesoon,Lee, Kyung Hee,Joe, Min-Ho Published by Elsevier/North Holland on behalf of t 2006 FEMS microbiology letters Vol.257 No.2
<P>We isolated nickel-resistant bacterium from soil in order to identify a novel nickel resistance determinant. Using 16S rRNA gene sequencing, an isolate was identified as Enterobacter sp. Ni15. This species showed a medium-level (resistant to up to 10 mM) nickel resistance in nutrient-rich media. Enterobacter sp. Ni15 has a novel plasmid, pNi15, and an increased nickel resistance to Escherichia coli DH5alphain trans. To isolate the nickel resistance gene from pNi15, the plasmid was digested with XbaI and its fragments were cloned into pBluescriptIISK(+). The clones were transferred into E. coli DH5alpha. The nickel resistance of the clones was then assayed. From these results, a pNi15100 isolate containing a 5,328 bp XbaI fragment of pNi15 was identified and sequenced. The E. coli DH5alpha harboring the pNi15100 showed a resistance to up to 7 mM nickel. Using a subcloning analysis, we were able to identify the novel nickel resistance determinant: the nrp gene encoding the putative proteins NrpA and NrpB.</P>
SYNTHESIS AND IN VITRO EVALUATION OF 3-SUBSTITUTED-1-AZAANTHRAQUINONES
Lee, Heesoon,Hong, Seoung-Soo,Kim, Young-Ho 충남대학교 약학대학 의약품개발연구소 1996 藥學論文集 Vol.12 No.-
In the course of developing novel antitumor agents, we synthesized 3-substituted-1-azaanthraquinones, incorporating the alkylating or latent alkylating substituents as potential antitum or agents. The most active comound 4 exhibited cytotoxic activity comparable to that of doxorubicin. The compounds 38 retained much of their activity against the doxorubicin-resistant cell line(MCF7/R). Copyright ⓒ 1996 Elsevier Science Ltd
Synthesis and In vitro Evaluation of 4-Substituted-1-azaanthraquinones
Lee, HeeSoon,Hong, Seoung-=Soo,Choi, Jae-Young,Cho, JungSook,Kim, Young-Ho 충남대학교 약학대학 의약품개발연구소 1998 藥學論文集 Vol.14 No.-
Doxorubicin and daunomycin are the best known members of the anthracycline antibiotics and the most commonly used intercalaing agents in the treatment of cancer(Wakelin and Waring, 1990). Doxorubicin has a broad spectrum of activity, being particularly efficacious against solid tumors. However its clinical usefulness is limited by cardiotoxicity that develop after extended therapy, and the appearance of an acquired resistance (Priebe, 1995; Surato et al 1990). Synthetic analogues, mitoxantrone and ametantrone, resulted from efforts to produce anthracycline analogues that lack cardiac toxicity. Mitoxantrone in particular currently plays an important role in the clinical management of hematological malignancies such as chronic myelogenous leukemia, acute nonlymphoblastic leukemia, and non-Hodgkin's lymphoma, as well as in combination therapy of refractory overian and breast cancers (Wakelin and Waring, 1990). Although mitoxantrone is endowed with an improved tolerability profile compared with doxorubicin and other anthracylines, this drug is not devoid of significant toxic side effects especially those associated with myelosupporession(Gandolf et al., 1995). A number of studies have identified mitoxantrone as an intercalating agent, all indications being that its biological activity is attributable to its DNA-binging properties. DNA intercalation and interference with the DNA-topoisomerase Ⅱ activity resulting in protein associated DNA strand breaks have been proposed as critical events that lead to mitoxantrone-induced cell death(Wakelin and Waring, 1990). The search for new analogues side effects of the anthracycline analogues is of extreme interest and numerous analogues have been reported(Priebe, 1995).
Synthesis and In Vitro Cytotoxicity of 3-or 4-Dialkylaminomethyl-1-azaanthraquinones
Lee, Heesoon,Choi, Jae-Young,Lee, Seung-lI,Hong, Seoung-Soo,Cho, Jungsook,Kim, Young-Ho 충남대학교 약학대학 의약품개발연구소 1999 藥學論文集 Vol.15 No.-
Six 3-dialkylaminomethyl-1-azaanthraquinones and five 4-dialkylaminomethyl-1-azaanthraquinones were synthesized and evaluated in vitro cytotoxicity against four human cancer cell lines. The compounds retained much of their cytotoxic activity against the multi-drug-resistant cell line (KB-V-1) as shown by resistance index.
Design and Synthesis of Isoindoloquinoline Derivatives as Potential Antitumor Agents
Lee, Heesoon,Jeong, Ilyeong,Yang, Sung-Il The Pharmaceutical Society of Korea 2002 Archives of Pharmacal Research Vol.25 No.4
A series of isoindoloquinoline derivatives was synthesized and evaluated in vitro cytotoxicity against four human cancer cell lines (HCT15, SK-OV-3, MDA-MB-468 and T-47D).
Effect of Insulin on the Regulation of Na/K/Cl Cotransporter (NKCC2) in HEK293 Cells
Chang, Heesoon,Lee, Jin-Ill,Shin, Dong-Min,Ohk, Seung-Ho,Lee, Syng-Ill Korean Academy of Oral Biology and the UCLA Dental 2002 International Journal of Oral Biology Vol.27 No.3
Insulin is one of the regulators involved in Na^+ reabsorption in kidney. The Na^+ channel and Na/K/2CI cotransporter (NKCC2) system are primarily considered as the possible routes for Na^+ movement into the cell. The purpose of this stud is to understand the regulation of NKCC2 as a candidate for Na^+ movement across the kidney cell in response to insulin. In order to clarify the role of the insulin in human embryonic kidney cell line, HEK293, the cells were exposed to the different circumstances (isotonic, hypertonic), and then cell volume, expression of NKCC2 mRNA, intracellular Ca^2+ and functional activity of the cotransporter using pH dye, and the intracellular Ca^2+ level were analyzed in each condition. The cell volume of HEK293 which was shrunken by hypertonic stress recovered to nearly original state by the addition of 1μM insulin. It is obvious that insulin prevented cell shrinkage by operating the regulatory volume increase (RVI) machinery of the cell. However, insulin-induced RVI was blocked by the treatment of 10μM bumetanide. Furthermore, NKCC2 mRNA was expressed remarkably in the presence of 1μM insulin. Such results might suggest that the presence of 1μM insulin. Such results might suggest that the volume regulation of HEK293 cell showed the typical change in intracellular Ca^2+ concentration in response to carbachol as seen in other normal cells. However, insulin did not induce the change of intracellular calcium level of the HEK293 cell. Taken all together, these findings suggest that the insulin stimulates the sodium transport of HEK293 cell through the upregulation of NKCC2 under the hypertonic condition.