Lumiracoxib是一种选择性COX-2抑制剂，于2004年在澳大利亚注册，用于骨关节炎患者的症状缓解（每日200mg），还用于治疗由于痛经引起的急性疼痛和疼痛（每天400mg，连续用药5天）。在2006年7月份被列入PBS（Schedule of Pharmaceutical...Lumiracoxib是一种选择性COX-2抑制剂，于2004年在澳大利亚注册，用于骨关节炎患者的症状缓解（每日200mg），还用于治疗由于痛经引起的急性疼痛和疼痛（每天400mg，连续用药5天）。在2006年7月份被列入PBS（Schedule of Pharmaceutical Benefits）药物名单之前，lumiracoxib并没有被广泛使用。展开更多
Background Lumiracoxib is a highly selective cyclooxygenase-2 （COX-2） inhibitor with antiinflammatory, analgesic and antipyretic activities comparable with class specific drugs, but with much improved gastrointestin...Background Lumiracoxib is a highly selective cyclooxygenase-2 （COX-2） inhibitor with antiinflammatory, analgesic and antipyretic activities comparable with class specific drugs, but with much improved gastrointestinal safety. No studies have examined lumiracoxib for antitumorigenic activity on human nonsmall cell lung cancer cell lines in vitro or its possible molecular mechanisms. Methods The antiproliferative effect of lumiracoxib alone or combined with docetaxol on A549 and NCI-H460 lines was assessed by 3-（4, 5-dimethylthiazol-2-yl）-2, 5-diphenyltetrazolium bromide （MTT） assay. Drug-drug interactions were analyzed using the coefficient of drug interaction （CDI） to characterize the interactions as synergism, additivity or antagonism. Morphological changes were observed by acridine orange fluorescent staining. Extent of apoptosis was determined by flow cytometry. Results Lumiracoxib （15-240 pmol/L） has an inhibitory effect on the proliferation of A549 and NCI-H460 cell lines in concentration- and time-dependent manners with the ICso values of 2597 pmol/L and 833 pmol/L, respectively. The synergistic effect was prominent when lumiracoxib （15-240 pmoVL） was combined with docetaxol （0.2-2 pmol/L） （CDI 〈1）. Fluorescent staining showed that lumiracoxib could induce apoptosis in A549 and NCI-H460 cells. Lumiracoxib treatment also caused an increase of the sub-G1 fraction in each cell line and resulted in an increase of G0/Gl-phase cells and a decrease of S-phase cells. Conclusions Lumiracoxib had antiproliferative effect on the human nonsmall cell lung cancer cell lines A549 and NCI-H460 and had a significant synergy with docetaxol, which may be related to apoptotic induction and cell cycle arrest.展开更多
文摘Lumiracoxib是一种选择性COX-2抑制剂，于2004年在澳大利亚注册，用于骨关节炎患者的症状缓解（每日200mg），还用于治疗由于痛经引起的急性疼痛和疼痛（每天400mg，连续用药5天）。在2006年7月份被列入PBS（Schedule of Pharmaceutical Benefits）药物名单之前，lumiracoxib并没有被广泛使用。
基金This work was supported by grants from the Natural Science Foundation of Anhui Province （No. 07021008） and the General Project of the Natural Science Foundation of the Department of Education, Anhui Province （No. KJ2007B142）.
文摘Background Lumiracoxib is a highly selective cyclooxygenase-2 （COX-2） inhibitor with antiinflammatory, analgesic and antipyretic activities comparable with class specific drugs, but with much improved gastrointestinal safety. No studies have examined lumiracoxib for antitumorigenic activity on human nonsmall cell lung cancer cell lines in vitro or its possible molecular mechanisms. Methods The antiproliferative effect of lumiracoxib alone or combined with docetaxol on A549 and NCI-H460 lines was assessed by 3-（4, 5-dimethylthiazol-2-yl）-2, 5-diphenyltetrazolium bromide （MTT） assay. Drug-drug interactions were analyzed using the coefficient of drug interaction （CDI） to characterize the interactions as synergism, additivity or antagonism. Morphological changes were observed by acridine orange fluorescent staining. Extent of apoptosis was determined by flow cytometry. Results Lumiracoxib （15-240 pmol/L） has an inhibitory effect on the proliferation of A549 and NCI-H460 cell lines in concentration- and time-dependent manners with the ICso values of 2597 pmol/L and 833 pmol/L, respectively. The synergistic effect was prominent when lumiracoxib （15-240 pmoVL） was combined with docetaxol （0.2-2 pmol/L） （CDI 〈1）. Fluorescent staining showed that lumiracoxib could induce apoptosis in A549 and NCI-H460 cells. Lumiracoxib treatment also caused an increase of the sub-G1 fraction in each cell line and resulted in an increase of G0/Gl-phase cells and a decrease of S-phase cells. Conclusions Lumiracoxib had antiproliferative effect on the human nonsmall cell lung cancer cell lines A549 and NCI-H460 and had a significant synergy with docetaxol, which may be related to apoptotic induction and cell cycle arrest.
