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1.
Chinese Medical Journal ; (24): 602-607, 2008.
Article in English | WPRIM | ID: wpr-287684

ABSTRACT

<p><b>BACKGROUND</b>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.</p><p><b>METHODS</b>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.</p><p><b>RESULTS</b>Lumiracoxib (15 - 240 micromol/L) has an inhibitory effect on the proliferation of A549 and NCI-H460 cell lines in concentration- and time-dependent manners with the IC50 values of 2597 micromol/L and 833 micromol/L, respectively. The synergistic effect was prominent when lumiracoxib (15 - 240 micromol/L) was combined with docetaxol (0.2 - 2 micromol/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/G1-phase cells and a decrease of S-phase cells.</p><p><b>CONCLUSIONS</b>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.</p>


Subject(s)
Humans , Apoptosis , Carcinoma, Non-Small-Cell Lung , Drug Therapy , Pathology , Cell Cycle , Cell Line, Tumor , Cell Proliferation , Cyclooxygenase 2 Inhibitors , Pharmacology , Diclofenac , Pharmacology , Lung Neoplasms , Drug Therapy , Pathology , Taxoids , Pharmacology
2.
National Journal of Andrology ; (12): 438-440, 2006.
Article in Chinese | WPRIM | ID: wpr-343602

ABSTRACT

<p><b>OBJECTIVE</b>To analyze the activity of human sperm acrosin and semen parameters in male infertile patients and discuss the effect of sperm acrosin activity on semen quality.</p><p><b>METHODS</b>Activity of human sperm acrosin, PMN-elastase, fructose, alpha-glucosidase, zinc, acid phosphatase levels and HOST of 214 male infertile patients were detected. Semen analysis was performed using WLJY-9000 WeiLi colorful semen quality analyzer. There were 111 cases of normal activity of human sperm acrosin (48.2 - 218.7 microIU/10(6) sperm), 103 cases abnormal (< 48.2 microIU/10(6) sperm). Using the group of normal activity of sperm acrosin to be the control, semen parameters was analyzed and compared with those of the group of abnormal activity of sperm acrosin.</p><p><b>RESULTS</b>There were significant difference (P < 0.001) between the 2 groups (normal and abnormal) in the areas of sperm density, motile sperm rate, percentage of grade (a + b) sperm and HOST. There were also significant difference in PMN-elastase, fructose and alpha-glucosidase (P < 0.05). There was no difference among sperm volume, zinc and acid phosphatase (P > 0.05).</p><p><b>CONCLUSION</b>There was a strong correlation between the activity of human sperm sperm acrosin and semen quality. Activity of sperm acrosin is a reliable index of semen quality.</p>


Subject(s)
Adult , Humans , Male , Middle Aged , Acrosin , Metabolism , Infertility, Male , Semen , Chemistry , Sperm Count , Sperm Motility , Spermatozoa
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