Design, synthesis and antiproliferative activity in cancer cells of novel dihydropyrazolyl and pyrazolyl artemisinin-phenyl ethers / 中国中药杂志

To explore potent anticancer agent based on artemisinin scaffold, a series of 10--phenyl ethers derivatives containing dihydropyrazolyl or pyrazolyl moiety have been designed and synthesized. Their structures were determined by LC-MS and ¹H-NMR date. Inhibitory effects of the target compounds in human breast cancer MCF-7, MCF/Adr, MDA-MB-231 cells and prostate cell line PC-3 were determined by MTT assay. Those derivatives displayed good antiproliferative activity against the tested cancer cells. Particularly, target compounds exhibited significant cytotoxicity against drug-resistance cells MCF/Adr, which was worthy for further investigation.

Updated treatments of castration-resistant prostate cancer / 中华男科学杂志

The diagnosis and treatment of prostate cancer are being improved due to the popularized screening of prostate specific antigen. Advanced prostate cancer, in spite of its response to androgen deprivation therapy, may finally develop into castration-resistant prostate cancer (CRPC) and shorten the overall survival of the patients. Many efforts have been made by worldwide researchers for new approaches to the management of CRPC, including new hormonal therapy, cytotoxic chemotherapy, immunotherapy, and bone metastasis-targeted therapy. This paper reviews the emerging agents undergoing clinical evaluation and drugs that have received approval for the treatment of CRPC in order to provide doctors and patients with more treatment options for CRPC and improve the overall survival rate and quality of life of the patients.

Indirubin inhibits the proliferation of prostate cancer PC-3 cells / 中华男科学杂志

<p><b>OBJECTIVE</b>To explore the antitumoral effect of indirubin on androgen-independent prostate cancer PC-3 cells and its possible mechanisms.</p><p><b>METHODS</b>We measured the inhibitory effect of indirubin on the proliferation of prostate cancer PC-3 cells using MTT assay, detected their cell cycles by flow cytometry, and determined the expressions of the cell cycle regulatory protein cyclin D1 and its related downstream gene c-myc by Western blot.</p><p><b>RESULTS</b>The viability of the PC-3 cells was significantly decreased by indirubin in a concentration-dependent manner, reduced to 52. 2% and 13. 6% at 5 and 10 µmol/L, respectively. The cell cycle of the PC-3 cells was markedly inhibited by indirubin at 5 µmol/L, with the cells remarkably increased in the G0 and G1 phases and decreased in the S and G2/M phases. Meanwhile, indirubin also inhibited the expressions of cyclin D1 and c-myc in the Wnt signaling pathway.</p><p><b>CONCLUSION</b>Indirubin can suppress the proliferation of androgen-independent prostate cancer PC-3 cells, which may be associated with its inhibitory effect on the cell cycle and Wnt signaling pathway.</p>

Transurethral transumbilical laparoendoscopic single-site surgery for radical prostatectomy / 中华男科学杂志

<p><b>OBJECTIVE</b>To investigate the feasibility and advantages of transurethral transumbilical laparoendoscopic single-site surgery (TU-LESS) for radical prostatectomy.</p><p><b>METHODS</b>Five patients with prostate cancer underwent TU-LESS for radical prostatectomy, with a four-channel single-port device inserted into a 2. 5 cm periumbilical incision and another placed through the urethra, followed by analysis of the perioperative data.</p><p><b>RESULTS</b>All the operations were successfully accomplished, with neither conversion to open surgery nor additional channel. The mean operation time, intraoperative blood loss, and postoperative hospital stay were 168 min, 120 ml, and 15 d, respectively. No severe perioperative complications were observed. TNM stage classification manifested T2cN0M0 in 2 cases and T2bN0M0 in the other 3. Postoperative pathology showed no negative surgical margins in any of the cases.</p><p><b>CONCLUSION</b>TU-LESS is safe and feasible for radical prostatectomy and can reduce the complication of low urinary tract surgery by single-site laparoendoscopy.</p>

Proteomic analysis of the testis and differential expression of Annexin A3 in hypospadiac rats / 中华男科学杂志

<p><b>OBJECTIVE</b>To investigate the effect of in utero exposure to di-n-butyl phthalate (DBP) on the protein expression in the penile tissue of hypospadiac rats, isolate and identify differentially expressed proteins, and determine the role of the differential expression of Annexin A3 in the development of hypospadia in the rat offspring after maternal exposure to DBP.</p><p><b>METHODS</b>Twenty pregnant SD rats were randomly assigned to an experimental group, intragastrically administered DBP at 800 mg/kg, and a control group, given soybean oil at 5 ml/kg, both for 5 days. Three days after birth, the penises of the newborn rats were removed, and the total protein extracted for 2D-electrophoretic separation and image analysis. Differentially expressed protein spots were screened and identified by mass spectrometry, and the changes in the expression of Annexin A3 detected by Western blotting and immunohistochemistry.</p><p><b>RESULTS</b>Thirty-one differentially expressed protein spots were screened, of which 17 were identified by mass spectrometry and the SwissProt database, including pyruvate kinase M2, alpha-enolase, and Annexin A3. Western blot showed that Annexin A3 was mainly located in the urethral epithelia and had a lower expression in the hypospadiac rats (1.851 +/- 0.014, n = 10) than in the controls (2.603 +/- 0.012, n = 10) (P < 0.05).</p><p><b>CONCLUSION</b>A pedigree of differentially expressed proteins in the penises of DBP-induced hypospadia and normal rats was established by the proteomic method. The differential expression of Annexin A3 may play an important role in the development of hypospadia.</p>