2.Synthesis and phosphodiesterase type-5 inhibitory activity of sildenafil analogues possessing a guanidine group in the phenyl ring
Jing SHI ; Zheng LIU ; Zhen WANG ; Guanghui TIAN ; Xiaojun YANG ; Xuelan WANG ; Hongbin SUN ; Jingshan SHEN
Journal of China Pharmaceutical University 2010;41(2):112-117
In this study,a series of new sildenafil analogues 11-27 possessing a guanidine group were synthesized to investigate their PDE5 inhibitory activity and selectivity using[~3H]cGMP SPA kit in vitro and efficacy in the rat model of erection.Most of the compounds showed potent activity against PDE5,and more importantly,several compounds exhibited higher PDE5 selectivity over PDE6 than that of sildenafil.Structure-activity relationship of these sildenafil analogues was also discussed.Within this series of compounds,compound 15(IC_(50) =1.7 nmol/L)not only exhibited more potent PDE5 inhibitory activity than that of sildenafil (IC_(50) = 6.5 nmol/L),but also showed functional efficacy in the rat model of erection.
3.A novel method for culture and identification of primary human retinal microvascular endothelial cells
Yu-xiang, MAO ; Shao-fen, LIN ; Mei-zhen, ZENG ; Jing-yi, TIAN ; Shi-bo, TANG
Chinese Journal of Experimental Ophthalmology 2013;(1):8-12
Background To optimize the culture method of human retinal microvascular endothelial cells is very important for the study of retinal angiogenesis disease.Human retinal microvascular endothelial cells have been successfully cultured in previous studies,but further improvement of the culture method to harvest higher yields and purity cells is still needed.Objective This study was to design a modified method to isolate and purify human retinal microvascular endothelial cells much easily and quickly,and to compare the expression of specific markers of vascular endothelial cells,factor Ⅷ and CD31/CD34 in the cells.Methods The use of human donor eyeballs was approved by the Ethic Commission of Zhongshan Ophthalmic Center of Sun Yat-sen University.The retina tissue from healthy donor was isolated and digested by the two-step digestion method with 2% trypsin and 0.133% collagenase Ⅳ.Human retinal microvascular endothelial cells were collected and plated in 60 mm dishes coated by 0.1% fibronectin and cultured in endothelial cell-specialized medium supplemented with 10% fetal bovine serum,0.3 mg/L β-endothelial cell growth factor (ECGF) and 100 ng/L sodium heparin.During the culturing,the growth situation of the cells was monitored by morphological observation,and immunohistochemical staining was performed to probe vascular endothelial cell-specific membrane protein CD31,CD34 and factor Ⅷ for identification of the cell purity.Results Human retinal microvascular endothelial cells were isolated successfully from the retina by the twostep digestion method.The primary cultured cells adhered to well 72 hours later and achieved confluence with the typical cobblestone appearance 9 to 10 days after cultured.The cells exhibited the blue nuclei and reddish cytoplasm by regular haematoxylin and eosin stain and showed a strong positive response for CD31,CD34 and factor Ⅷ by immunohistochemistry.The positive dye of CD31 and CD34 was lower than Ⅷ factor in both endothelial cells.Conclusions Modified culture method of human retinal microvascular endothelial cells can improve cell culture result and purify target cells.
4.Effects of p38MAPK signaling pathway on cyclic tensile stress-induced fibroblast apoptosis
Jing QIU ; Guangyun ZHANG ; Zhen TIAN ; Yue ZHANG ; Jiangbo YU ; Xiao YUAN
Chinese Journal of Tissue Engineering Research 2011;15(20):3789-3792
BACKGROUND: When the teeth affected abnormal biting force, tooth absorption and periodontium would be greatly damaged. OBJECTIVE: To study whether periodontal membrane fibroblast affected apoptosis following cyclic tensile stress stimulation and whether p38MAPK signaling pathway participated in apoptosis. METHODS: Fibroblasts at passages from 4 to 7 were randomly assigned to control, loading and SB203580 groups after synchronization. In the loading and SB203580 groups, 12% strain was applied at a loading frequency of 6 cycles per minute, i.e. 5 seconds for tension and 5 seconds for relaxation. In the SB203580 group, cells were treated with 20 mmol/L p38MAPK inhibitor SB203580 at 1 hour before loading. At 6, 12 and 24 hours after loading, cells from each group were harvested, and cell apoptosis was detected using a flow cytometry. Expression of bax mRNA was determined using reverse transcription-polymerase chain reaction. RESULTS AND CONCLUSION: Compared with the control group, apoptotic rate of fibroblasts and bax mRNA expression were increased after loading (P < 0.05), and enhanced over time, and peaked at 12 hour following loading, and then decreased gradually. Compared with the loading group, cell apoptosis was reduced at corresponding time points in the SB203580 group (P < 0.05), and bax mRNA expression was diminished. These results indicated that cells affected apoptosis after mechanics stimulation, and mitogen activated protein kinase p38MAPK signaling pathway participates in the process of apoptosis.
6.CT guided percutaneous drainage in treatment of solitary retroperitoneai abscess
Cheng-Wei SHAO ; Jian-Ming TIAN ; Chang-Jing ZUO ; Tao-Zhen LV ;
Journal of Interventional Radiology 2006;0(12):-
Objective To evaluate the therapeutic efficacy of percutaneous drainage of solitary retroperitoneal abscess under CT guidance.Methods A retrospective analysis was made for percutaneous drainage of solitary retroperitoneal abscess with CT guidance in 13 patients including 4 at the tail of pancreas, 3 nearby the head of pancreas,3 in perirenal space,2 in posterior renal space and 1 case was by the side of psoas muscle.The maximum diameters of retroperitoneal abscess were between 3.5cm and 8cm.Results Out of 13 patients,8 with one time drainage,3 with twice drainages and 2 with thrice drainages.The mean duration of drainage was 16 days with no recurrence or residual lesions during clinical follow up.Conclusion CT guided percutaneous drainage of solitary retroperitoneal abscess is effective and minimally invasive.(J Intervent Radiol,2007,16:828-830)
7.Clinical value of multislice CT in diagnosis and preoperative TNM-staging of gastric carcinoma
Li-Juan DU ; Jian-Ming TIAN ; Tao-Zhen LV ; Chang-Jing ZUO ;
Academic Journal of Second Military Medical University 2000;0(07):-
Objective: To evaluate the clinical value of multislice CT (MSCT) in the diagnosis and preoperative TNM staging of gastric carcinoma. Methods: Fifty patients with advanced gastric carcinoma were examined by MSCT, gastrointestinal series (GI), fiberoptic gastroscopy (FG) and transabdominal ultrasonography (US). The results of the 4 methods were compared with postoperative pathological results. Forty patients, who were diagnosed as having advanced gastric carcinoma by both MSCT and US, had their TNM staging evaluated and the results were compared with postoperative pathological TNM evaluation. Results: The detection rates of MSCT, FG, GI and US for advanced gastric carcinoma were 98%, 100%, 88% and 80%, respectively. The detection rate of MSCT was not significantly different with that of FG, but was obviously higher than that of GI (P=0.027) and US (P=0.004). The accuracy of MSCT in preoperative TNM staging was significantly higher than that of US(92.5% vs 72.5%). Conclusion: MSCT, with two-phase thin slice incremental scanning image, multiplaner reformats (MPR) and three-dimension (3D) image, is more advantaged in detecting the gross type, size, location, invasion and metastasis of advanced gastric carcinoma, thus greatly improving the detection rate and preoperative TNM staging of advanced gastric carcinoma.
8.Evaluation of brain metastases with dynamic susceptibility-contrast MR imaging
Hao ZHANG ; Tian-Zhen SHEN ; Xing-Rong CHEN ; Jing-Tao MIAO ; Xue-Qian XIE ;
Chinese Journal of Radiology 2001;0(09):-
Objective To study the characteristics of dynamic susceptibility-contrast(DSC)MR perfusion curves,color images and perfusion values in pre-operative brain metastasis.Methods Twenty- eight brain metastases underwent DSC MR perfusion imaging by using a first-pass T_2~* echo-planar sequence. The patients' data were transferred to on-line workstation.Time-signal intensity curves,color perfusion maps and rCBV,rMTT values in both tumor parenchyma and peri-tumor edema were analyzed,and independent t- test was used and P0.05).Conclusion Different originated brain metastases have nearly same characteristics in DSC MR perfusion imaging.
9.Clinical application of CT-guided curve-needle percutaneous ethanol injection for celiac plexus block analgesia
Cheng-Wei SHAO ; Chang-Jing ZUO ; Jian-Ming TIAN ; Qi ZHAO ; Tao-Zhen LV ;
Academic Journal of Second Military Medical University 1999;0(12):-
Objective:To validate the clinical value of CT-guided curve-needle percutaneous ethanol injection (CNPEI) for celiac plexus block analgesia. Methods: Thirty-two patients with end-stage cancer, including 13 complicated with extensive retroperitoneal lymph node enlargement and fusion, were enrolled in this study. All patients complained of refractory upper abdominal pain and had received narcotic analgesics and radiotherapy, but the analgesic effect was not good. CT-guided CNPEI was therefore prescribed. Results: The effective rates of CT-guided CNPEI were 100%, 100%, 96.9%, 90.6%, 87.5%, and 84.4% immediately,and at 2 weeks, 4 weeks, 8 weeks, 12 weeks, and 16 weeks after treatment, respectively. All enlarged lymph nodes had obvious necrosis and became shrunk. Conclusion: Combined application of bilateral anterior and posterior diaphragmatic crura block and trans-lymph node block can produce good analgesic effects, and curve-needle puncture make the above technique simpler.
10.CT-guided percutaneous ethanol injection in treatment of metastatic adrenal tumors
Chang-Jing ZUO ; Cheng-Wei SHAO ; Jian-Ming TIAN ; Qi ZHAO ; Tao-Zhen LV ;
Academic Journal of Second Military Medical University 1999;0(12):-
Objective:To validate the therapeutic value of CT-guided percutaneous ethanol injection (PEI) in the treatment of metastatic adrenal tumors. Methods: Thirty-one foci (diameter ranging from 1.5 cm to 7.2 cm) in 25 patients with metastatic adrenal tumors were treated with CT-guided PEI for more than twice. Plain and enhanced CT scans were performed 1-2 months after PEI to observe the size and necrosis of the tumors. Results: Post-PEI enhanced CT scan showed that 18 of the 20 foci with diameters less than 3 cm completely necrotized; 11 foci with diameters between 3 cm and 7.2 cm necrotized partially, and 2 foci completely necrotized after another 2-3 courses of PEI treatment. Conclusion: CT-guided PEI is a simple and minimally invasive means for treatment of metastatic adrenal tumors, and the therapeutic effect is satisfactory.