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1.
National Journal of Andrology ; (12): 501-505, 2013.
Article in Chinese | WPRIM | ID: wpr-350872

ABSTRACT

<p><b>OBJECTIVE</b>To study the inhibitory effect of Akt inhibitor deguelin on PC-3 human prostate cancer cell lines and its possible mechanism.</p><p><b>METHODS</b>PC-3 human prostate cancer cells were cultured in deguelin at the concentrations of 10, 100, 500 and 1 000 nmol/L for 24, 48 and 72 hours, respectively. Then the inhibitory effect of deguelin on the proliferation of the PC-3 cells was determined by MTT assay and that on the cell cycle was detected by flow cytometry. The expression levels of MDM2 and GSK3beta mRNA were measured by RT-PCR and those of MDM2 and GSK3beta proteins by Western blot.</p><p><b>RESULTS</b>At 24, 48 and 72 hours, the inhibition rates of deguelin on the proliferation of the PC-3 prostate cancer cells were (91.10 +/- 3.75), (86.39 +/- 1.16) and (79.51 +/- 2.63)% at 10 nmol/L, (82.46 +/- 3.65), (76.84 +/- 0.97) and (69.69 +/- 2.30) % at 100 nmol/L, (81.46 +/- 0.41), (75.56 +/- 1.12) and (54.07 +/- 3.21)% at 500 nmol/L, and (66.77 +/- 2.82), (58.22 +/- 0.35) and (39.34 +/- 2.40)% at 1000 nmol/L, all with statistically significant differences from the control group (P < 0.01). Deguelin at 10, 100, 500 and 1 000 nmol/L increased the cell cycles blocked in the G0/G1 phase ([62.4 +/- 2.2], [63.6 +/- 1.1 ], [65.0 +/- 0.3] and [66.5 +/- 1.9]%, P < 0.01) and reduced the percentage of the S-phase cells ([14.7 +/- 2.4], [11.1 +/- 5.2], [5.8 +/- 1.1] and [7.0 +/- 0.6]%, P < 0.01). RT-PCR and Western blot showed markedly up-regulated expressions of GSK3 P3 a3beta down-regulated expressions of MDM2 mRNA and proteins in the PC-3 cells treated with deguelin.</p><p><b>CONCLUSION</b>Akt inhibitor deguelin can inhibit the proliferation of PC-3 human prostate cancer cells by affecting the down-stream signal molecules GSK3P3 and betaDM2 in the Akt pathway.</p>


Subject(s)
Humans , Male , Cell Line, Tumor , Cell Proliferation , Glycogen Synthase Kinase 3 , Metabolism , Glycogen Synthase Kinase 3 beta , Prostatic Neoplasms , Metabolism , Proto-Oncogene Proteins c-akt , Proto-Oncogene Proteins c-mdm2 , Metabolism , Rotenone , Pharmacology
2.
China Journal of Chinese Materia Medica ; (24): 2252-2255, 2007.
Article in Chinese | WPRIM | ID: wpr-324367

ABSTRACT

<p><b>OBJECTIVE</b>To screen and optimize the extraction of Dingxiangjiangqi granules.</p><p><b>METHOD</b>The extraction route was screened by using pharmacodynamic experiment and the extraction conditions were optimized by orthogonal design and taking extract yield, content of naringin and tetrahydropalmatine as indexes.</p><p><b>RESULT</b>The pharmacodynamic result showed that aqueous extract had the best effect to cure the esophagitis of rats and the optimized extraction technique was adding 12 times water, extracting 0. 5 hour for 3 times.</p><p><b>CONCLUSION</b>The optimum extraction was simple, reasonable, stable and useful for further development.</p>


Subject(s)
Animals , Male , Rats , Berberine Alkaloids , Drug Combinations , Drugs, Chinese Herbal , Chemistry , Pharmacology , Esophagitis, Peptic , Drug Therapy , Pathology , Esophagus , Pathology , Flavanones , Phytotherapy , Plants, Medicinal , Chemistry , Random Allocation , Rats, Sprague-Dawley , Syzygium , Chemistry , Technology, Pharmaceutical , Methods
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