|
|
|
题名
|
作者
|
年代
|
出处
|
被引量
|
| 1 | Analysis of bacterial communities on aging flue-cured tobacco leaves by 16S rDNA PCR-DGGE technology显示文摘 | Zhao MQ Wang BX Li FX Qiu LY Li FF Wang SM Cui JK | 2007 | 中国生物学文摘2007,21,9: | 23 |
| 2 | Design,synthesis,and anti-inflammatory evaluation of a series of novel amino acid-binding 1,5-diarylpyrazole derivatives显示文摘Aim: To design and synthesize a series of novel amino acid-binding 1,5-diarylpyrazole derivatives, which are intended to act as prodrugs with better aqueous solubility than celecoxib, and which will exert potent anti-inflammatory activi-ties after being converted to their parent compounds in vivo. Methods: To introduce an amino acid, celecoxib analogs containing amino or methylamino group were synthesized first through multi-step chemical reactions. All the synthesized compounds were screened in an intact cell-based assay in vitro and in carrageenan-induced mouse paw edema in vivo. Some active compounds were selected for further evaluation in a carrageenan-induced rat paw edema model. The preliminary pharmacokinetics experiments were conducted using high performance liquid chromatography/mass spectrometry (HPLC/MS). Results: Celecoxib, 6 of the 1,5-diarylpyrazole class of celecoxib analogs, and their amino acid derivatives (hydrochloride salts) were synthesized. In vitro screening, the hydrochloride salts showed decreased inhibitory effects on cyclooxygenase (COX)- 1 and COX-2 compared with their parent compounds, but some exhibited potent anti-inflammatory activity in vivo. Compound 4a was selected for further evaluation, and its anti-inflammatory effect was equivalent to that of celecoxib after oral administration in the carrageenan-induced rat paw edema model. At three doses (25 mg/kg, 50 mg/kg, and 100 mg/kg) the percentage inhibition on edema was 20.7%, 52.6%, and 62.6% (for compound 4a) and 27.8%, 38.4%, and 40.1% (for celecoxib), respectively. Preliminary pharmacokinetic evaluations support the hypothesis that compound 4a was actually converted to its parent compound, compound 4. Conclusion: The compound bound with amino acid acts like prodrug, which can exert anti-inflammatory effect similar to celecoxib after being converted to its parent compound. This finding will be of great benefit in carrying out structural modifications of prodrug-like selective COX-2 inhibitors. | Li MH Yin LL Cai MJ Zhang WY Huang Y Wang X Zhu XZ Shen JK | 2005 | Acta Pharmacologica Sinica2005,26,7: | 2 |
| 3 | Reconstruction of damaged corneas by transplantation of autologous limbal epithelial cells显示文摘 | Tsai RJ Li LM Chen JK | 2000 | N Eng J Med2000,343,2: | 1 |
| 4 | Gaps remain in China’s ability to detect emerging infectious diseases despite advances since the onset of SARS and avian flu显示文摘 | Feng ZJ Li WK Varma JK | 2010 | Health Affairs2010,30,1: | 1 |
| 5 | Targeted delivery of paclitaxel using folate-conjugated heparin-poly (β-benzyl-l-aspartate) self- assembled nanoparticles 显示文摘 | Li L Kim JK Huh KM | 2012 | Carbohydr Polymers2012,87,3: | 1 |
| 6 | Resolving postoperative neuroinflammation and cognitive decline 显示文摘 | Terrando N Eriksson LI Ryu JK | 2011 | Ann Neurol2011,70,6: | 1 |
| 7 | Dysregulation of the Hedgehog pathway in human hepatocarcinogenesis显示文摘 | Sicklick JK Li YX Jayaraman A | 2006 | Carcinogenesis2006,27,4: | 1 |
| 8 | Physical validation of a patient - specific contact finite element model of the ankle 显示文摘 | Anderson DD Goldsworthy JK Li W | 2007 | J Biomech2007,40,8: | 1 |
| 9 | Protein oxidation: key to bacterial desiccation resistance?显示文摘 | Fredrickson JK Li SM Gaidamakova EK | 2008 | The ISME Journal2008,2,4: | 1 |
| 10 | Matrilysin(matrix metalloproteinase- 7) mediates E-cadherin ectodomain shedding in injured lung ep- ithelium显示文摘 | McGuire JK Li Q Parks WC | 2003 | Am J Patho12003,162,: | 1 |
| 11 | Probucol alleviates atherosclerosis and improves high density lipoprotein function显示文摘 | Zhong JK Guo ZG Li C | 2011 | Lipids Health Dis2011,10,1: | 1 |
| 12 | Spread and development of lapa- roscopie surgery for gastric tumors in mainland China: initial expe- riences 显示文摘 | Chen XZ Li YY Hn JK | 2012 | Hepatogastroenterology2012,59,114: | 1 |
| 13 | Enhancement of tendon graft osteointegration using mesenchymal stem cells in a rabbit model of anteriorcruciate ligament reconstruction显示文摘 | Lim JK Hui J Li L | | 0,,: | 1 |
| 14 | Effect of time factors on the mortality in brittle hip fracture 显示文摘 | Li YZ Lin JK Wang PW | 2014 | J Orthop Surg Res2014,9,: | 1 |
| 15 | Comparison of ultrasound and electromagnetic field effects on osteoblast growth 显示文摘 | Li JK Lin JC Liu HC | 2006 | Ultrasound Med Biol2006,32,: | 1 |
| 16 | Nicotine, body weight and potential implications in the treatment of obesity显示文摘 | LI MD Kane JK Konu O | 2003 | Curr Top Med Chem2003,3,8: | 1 |
| 17 | Unique sequence, ski, in Slnan-Kettering avian retroviruses with properties of a new cell- derived oncngene 显示文摘 | Li Y Turek CM Teumer JK et ol | 1986 | J Virol1986,57,3: | 1 |
| 18 | Application of identified QTL marker associations in rice quality improvement through a design-breeding approach显示文摘 | WANG JK WAN XY LI HH | 2007 | Theor Appl Genet2007,115,: | 1 |
| 19 | Physical vali- dation of a patient-specific contact finite element model of the ankle 显示文摘 | Anderson DD Goldsworthy JK Li W | 2007 | J Biomech2007,40,8: | 1 |
| 20 | Prognostic significance of elevated hemostatic markers in patients with acute myocardial infarction显示文摘 | Teng JK Tsai WC | 1999 | J Am Coll Cardiol1999,33,6: | 1 |