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Synthesis and investigation of dihydroxychalcones as calpain and cathepsin inhibitors
Baek, K.H.,Karki, R.,Lee, E.S.,Na, Y.,Kwon, Y. Academic Press ; Academic Press 2013 Bioorganic chemistry Vol.51 No.-
In order to identify potential calpain and cathepsin inhibitors we prepared 12 dihydroxychalcone analogues and tested their ability to inhibit μ-calpain, m-calpain, cathepsins B and L. In the calpain inhibition test, compound 10 exhibited the most active inhibitory activity against m-calpain with an IC<SUB>50</SUB> value of 25.25+/-0.901μM. With respect to inhibition of cathepsins B and L, compound 13 exhibited the most potent inhibitory activity on cathepsin L and moderate inhibitory activity on cathepsin B with IC<SUB>50</SUB> values of 2.80+/-0.100 and 11.47+/-0.087μM, respectively. Our results suggest the possibility of developing dual calpain and cathepsin inhibitors by properly modulating structures and/or combining the essential aspects of the functional group effective for specific calpain and cathepsin inhibition.
Upregulation and secretion of macrophage inhibitory cytokine-1 (MIC-1) in gastric cancers
Baek, K.E.,Yoon, S.R.,Kim, J.T.,Kim, K.S.,Kang, S.H.,Yang, Y.,Lim, J.S.,Choi, I.,Nam, M.S.,Yoon, M.,Lee, H.G. Elsevier Scientific Pub. Co 2009 Clinica chimica acta Vol.401 No.1
Background: Macrophage inhibitory cytokine-1 (MIC-1), a distant member of the transforming growth factor (TGF)-β superfamily, has been reported to be upregulated and secreted from several cancers. We examined MIC-1 expression and secretion in gastric cancers. Methods: MIC-1 mRNA and protein levels in cancer tissues and cell lines were analyzed by RT-PCR and Western blot. MIC-1 expression in cancer tissues and its secretion in serum were analyzed using immunohistochemistry and ELISA. Results: MIC-1 was significantly upregulated in gastric cancer tissues and cell lines. MIC-1 was secreted from gastric SNU620 cells and its levels in the serum of cancer patients were 10-fold higher than those of healthy controls. In addition, the staining of MIC-1 expression was strongly increased in metastatic gastric cancers. Conclusions: MIC-1 was obviously overexpressed in gastric cancers and MIC-1 secretion into blood may be useful for the prediction of gastric cancer progression.
Pharmacokinetics of liquiritigenin in mice, rats, rabbits, and dogs, and animal scale-up
Kang, Hee E.,Jung, Hye Y.,Cho, Yu K.,Kim, So H.,Sohn, Se I.,Baek, Seung R.,Lee, Myung G. Wiley Subscription Services, Inc., A Wiley Company 2009 Journal of Pharmaceutical Sciences Vol.98 No.11
<P>Pharmacokinetics of liquiritigenin (LQ) and its two glucuronide metabolites, M1 and M2, in mice, rats, rabbits, and dogs and animal scale-up of the pharmacokinetic parameters of LQ were evaluated. After intravenous administration of LQ, the AUC (AUC<SUB>0−t</SUB>) values of LQ, M1, and M2 were proportional to LQ doses in all animals studied. Animal scale-up of some pharmacokinetic parameters of LQ was performed based on the parameters after its intravenous administration (20 mg/kg; in the linear pharmacokinetic range) to the four species. Linear relationships were obtained (r > 0.968) between log CL (or CL/f<SUB>u</SUB>) (L/h) and log species body weight (W) (kg) [CL (or CL/f<SUB>u</SUB>) = 3.29 (34.0) W<SUP>0.723 (0.789)</SUP>] and log V<SUB>ss</SUB> (or V<SUB>ss</SUB>/f<SUB>u</SUB>) (L) and log W (kg) [V<SUB>ss</SUB> (or V<SUB>ss</SUB>/f<SUB>u</SUB>) = 0.340 (3.52) W<SUP>0.882 (0.948)</SUP>]. Interspecies scale-up of plasma concentration–time data of LQ using apolysichron (complex Dedrick plots) resulted in similar profiles, and plasma concentration–time profile of humans were predicted using the well-fitted four animal data. Our results indicate that the LQ data obtained from laboratory animals could be utilized to generate preliminary estimates of the pharmacokinetic parameters of LQ in humans. These parameters can serve as guidelines for better planning of clinical studies. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:4327–4342, 2009</P>
Kang, Hee E,Sohn, Se I,Baek, Seung R,Lee, Jee W,Lee, Myung G Pharmaceutical Society of Great Britain 2011 Journal of pharmacy and pharmacology Vol.63 No.1
<P>Liver disease and acute renal failure (ARF) are closely associated. The pharmacokinetics of liquiritigenin (LQ), a candidate therapy for inflammatory liver disease, and its metabolites M1 and M2 were evaluated in rats with ARF induced by uranyl nitrate (U-ARF rats).</P>