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| 1 | Preliminary results of integrated therapy for patients with knee osteoarthritis显示文摘 | Huang MH Yang RC Lee CL | | Arthritis and Rheumatism0,,: | 2 |
| 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 | Hyperkyphotic posture and risk of injurious falls in older persons: the Rancho Bernardo Study 显示文摘 | Kado DM Huang MH Nguyen CB | 2007 | J Gerontol A Biol Sci Med Sci2007,62,6: | 1 |
| 4 | Use of ultrasound to increase effectiveness of isokinetic exercise for knee osteoarthritis显示文摘 | Huang MH Lin YS Lee CL | 2005 | Archphys med rehabil2005,,86: | 1 |
| 5 | Hypoxia inhibits osteogenesis in human mesenchymal stem cells through direct regulation of RUNX2 by TWIST显示文摘 | Yang DC Yang MH Tsai CC Huang TF Chen YH Hung SC | | 0,,: | 1 |
| 6 | Use of ultrasound to increase effectiveness of isokinetic exercise for knee osteoarthritis 显示文摘 | Huang MH Lin YS Lee CL | 2005 | Arch Phys Med Rehabil2005,86,8: | 1 |
| 7 | Antioxidant, antinoeiceptive, and anti-inflammatory activities of Xan- thii Fructus extract 显示文摘 | Huang MH Wang BS Chiu CS | 2011 | J Ethnopharmacol2011,135,2: | 1 |
| 8 | Hyperky- photic posture predicts mortality in older community-dwell- ing men and women: a prospective study显示文摘 | Kado DM Huang MH Karlamangla AS | 2004 | J Am Geriatr Soc2004,52,10: | 1 |
| 9 | Klotho attenuates high glucose- induced fibronectin and cell hypertrophy via the ERKll2-p38 kinase signaling pathway in renal interstitial fibroblasts 显示文摘 | Huang JS Chuang CT Liu MH | 2014 | Mol Cell Endocrinol2014,390,12: | 1 |
| 10 | Can procalcitonin tests aid in identifying bacterial infections associated with influenza pneumonia?A systematic review and meta-analysis显示文摘 | Wu MH Lin CC Huang SL | 2013 | Influenza Other Respir Viruses2013,7,3: | 1 |
| 11 | Direct binding and characterization of lipase onto magnetic nanoparticles显示文摘 | HUANG SH LIAO MH CHEN DH | 2003 | Biotechnology Progress2003,19,3: | 1 |
| 12 | Multiple small-bowd intussusceptions caused by metastatic malignant melanoma显示文摘 | Huang YJ Wu MH Lin MT | 2008 | Am J Surg2008,196,3: | 1 |
| 13 | A comparision on various therapeutic exercise on funcational status of patients with knee osteoarthritis显示文摘 | Huang MH | 2003 | Semin Arthritis Rheum2003,32,: | 1 |
| 14 | A novel method to obtain modulus image of soft tissues using ultrasound water jet indentation: a phantom study显示文摘 | Lu MH Zheng YP Huang QH | 2007 | IEEE Trans Biomed Eng2007,54,1: | 1 |
| 15 | Effects of lactoferrin- containing formula in the prevention of enterovirus and rotavirus infection and impact on serum cytokine levels: a randomized trial显示文摘 | Yen MH Chiu CH Huang YC | 2011 | Chang Gung Med J2011,34,4: | 1 |
| 16 | Prevalence and risk factorsof middle cerebral artery stenosis in asymptomatic residents in Rongqi County,Guangdong显示文摘 | Huang HW Guo MH Lin RJ | | 0,,01: | 1 |
| 17 | Anatomic basis of cleft palate and velopharyngeal surgery: implications from a fresh cadaveric study显示文摘 | Huang MH Lee ST Rajendran K | 1998 | Plast Reconstr Surg1998,101,3: | 1 |
| 18 | A comparison of various thera- peutic exercises on the functional status of patients with knee osteoar- thritis 显示文摘 | Huang MH Lin YS Yang RC | 2003 | Semin Arthritis Rheum2003,,32: | 1 |
| 19 | Comparison between dobutamine and levosimendan for management of posttresuseitation myocardial dysfunetion显示文摘 | Huang L Wei MH Tang W | 2005 | Crit Care Med2005,33,: | 1 |
| 20 | Noncontact evaluation of articular cartilage degeneration using a novel ultrasound water jet indentation system显示文摘 | Lu MH Zheng YP Huang QH | 2009 | Ann Biomed Eng2009,37,1: | 1 |