http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
Phylogeny of the Korean Erwinia Species as Determined by Comparison of 16S rDNA Sequences
( Thapa,S. P. ),( H. R. Park ),( C. K. Lim ),( J. H. Hur ) 강원대학교 농업생명과학연구원(구 농업과학연구소) 2011 강원 농업생명환경연구 Vol.23 No.4
The complete 16S rRNA sequences of the genus Erwinia species isolated from diverse geographical area from Korea were determined following isolation and cloning of the amplified genes. These sequences along with the sequences of other Erwinia species obtained from the GenBank were aligned and phylogenetic trees were inferred by VectorNTI and neighbor-joining method. The levels of sequence similarity between different type strains broadly ranged from 90-100%. Erw. rhapontici and Erw. persicinus showed a distinct seperate cluster from that of amylovora group. The Korean Erw. carotovora subsp. carotovora strains were closer to Asian strains (strains from Japan, China more closer to Chinese strains) than to the European and American strains.
Thapa, Prakash,Thapa, Ritu,Choi, Du Hyung,Jeong, Seong Hoon Elsevier 2018 Powder technology Vol.339 No.-
<P><B>Abstract</B></P> <P>The main purpose of this study was to investigate the influence of ethylcellulose (EC) coating and curing conditions on the quality attributes of pharmaceutical pellets prepared using a quality by design (QbD) approach. The drug release rate of methimazole, a freely soluble model drug, was evaluated extensively together with the mechanical strength and true density of the coated pellets. Moreover, the thermal and spectroscopic properties, as well as the surface characteristics were studied using differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), Raman spectroscopy, scanning electron microscopy (SEM), and atomic force microscopy (AFM). Drug layering and EC coating of the pellets were performed in a fluid bed granulator. The results of thermal and infrared analyses showed the absence of significant interactions between the drug and the EC. The regression model was developed to predict the dependent variables (drug release at time 1 h, 4 h, 8 h, and 12 h, hardness of coated pellet, and true density). The results showed that the degree of coating and curing had the most significant effects on all response variables. The design space was built in accordance with the drug release rate following failure probability analysis using Monte Carlo simulations. Robustness and accuracy were also successfully validated and the control variables were optimized. The results highlighted the importance of the optimization in process parameters using the QbD strategy to achieve consistent quality of the pharmaceutical coating process.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Quality by design for process optimization in ethylcellulose coated pellets </LI> <LI> Design space and simulation performed to achieve consistent coating quality. </LI> <LI> Effects of coating and curing on drug release and hardness were confirmed. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Thapa, P.,Kadayat, T.M.,Park, S.,Shin, S.,Thapa Magar, T.B.,Bist, G.,Shrestha, A.,Na, Y.,Kwon, Y.,Lee, E.S. Academic Press ; Academic Press 2016 Bioorganic chemistry Vol.66 No.-
<P>A new series of 2-phenol-4-chlorophenyl-6-aryl pyridines were designed, synthesized, and evaluated for topoisomerase (topo) I and II inhibitory activities as well as cytotoxic activity against four different human cancer cell lines such as HCT15, T47D, DU145, and Hela. Most of the tested compounds exhibited stronger topo II inhibitory activity at 100 mu M as compared to etoposide. All the compounds, except 39, did not show topo I inhibitory activity. Interestingly, compounds that showed better topo II inhibition than etoposide have ortho-or para-chlorophenyl at 4-position of central pyridine, and none of the compounds possess meta-chlorophenyl. SAR study revealed the importance of ortho-or para-chlorophenyl at 4-position of the central pyridine for selective topo II inhibitory activity. Similarly, all compounds possessing meta-or para-hydroxyphenyl moieties showed moderate to significant cytotoxic effects. Particularly, compounds 27-37, and 39 which showed excellent cytotoxicity (IC50 = 0.68-1.25 mu M) against T47D breast cancer cells suggest the importance of meta-or para-hydroxyphenyl moiety at 2-position of the central pyridine for the design of anticancer agents with related scaffolds. (C) 2016 Elsevier Inc. All rights reserved.</P>
( Pritam Thapa ),( Tara Man Kadayat ),( Seojeong Park ),( Somin Shin ),( Til Bahadur Thapa Magar ),( Ganesh Bist ),( Aarajana Shrestha ),( Younghwa Na ),( Youngjoo Kwon ),( Eung Seok Lee ) 영남대학교 약품개발연구소 2016 영남대학교 약품개발연구소 연구업적집 Vol.26 No.-
A new series of 2-phenol-4-chlorophenyl-6-aryl pyridines were designed, synthesized, and evaluated for topoisomerase (topo) I and II inhibitory activities as well as cytotoxic activity against four different human cancer cell lines such as HCT15, T47D, DU145, and Hela. Most of the tested compounds exhibited stronger topo II inhibitory activity at 100 μM as compared to etoposide. All the compounds, except 39, did not show topo I inhibitory activity. Interestingly, compounds that showed better topo II inhibition than etoposide have ortho- or para-chlorophenyl at 4-position of central pyridine, and none of the com-pounds possess meta-chlorophenyl. SAR study revealed the importance of ortha- or para-chlorophenyl at 4-position of the central pyridine for selective tapa II inhibitory activity. Similarly, all compounds possessing mere- or para-hydroxyphenyl moieties shawed moderate to significant cytotoxic effects. Particularly, compounds 27-37, and 39 which showed excellent cytotoxicity (IC<sub>50</sub> = 0.68-1.25 μM) against T47D breast cancer cells suggest the importance of meta- or para-hydroxyphenyl moiety at 2-position of the central pyridine for the design of anticancer agents with related scaffolds.
( Pritam Thapa ),( Kyu Yeon Jun ),( Tara Man Kadayat ),( Chanmi Park ),( Zhi Zheng ),( Til Bahadur Thapa Magar ),( Ganesh Bist ),( Aarajana Shrestha ),( Younghwa Na ),( Youngjoo Kwon ),( Eung Seok Lee 영남대학교 약품개발연구소 2016 영남대학교 약품개발연구소 연구업적집 Vol.26 No.-
To develop novel selective topoisomerase II inhibitors, we designed and synthesized a series of conforma-tionally constrained hydroxylated 4-phenyl-2-aryl chromenopyridines and evaluated their to poi so-merase inhibitory activity and cytotoxicity against three human cancer cell lines (DU145, HCn5, and T47D) and a normal cell line (MCF10A). All of the prepared compounds displayed stronger or similar topoisomerase II inhibitory activity as well as cytotoxicity against three human cancer cell lines com-pared to etoposide. Compounds 10., 109, 11., 11f, 11g, 12., 12f, and 12g especially showed stronger topoisornerase II inhibitory activity as compared to etoposide at both 100 μM and 20 μM. A structure-ac-tivity relationship study revealed that hydroxyphenyl moiety at 4-position of pyridine and ortho-hydrox-yphenyl or thienyl moiety at 2-position of pyridine has an important role in displaying selective topoisomerase II inhibition. The compound 12b with para-hydroxyphenyl and meta-hydroxyphenyl at 4- and 2-position of pyridine. respectively, showed the most significant cytotoxicity against all three can-cer cell lines, whereas less cytotoxicity to a normal cell line as compared to adriamycin.