2.SYNTHESIS AND BIOLOGICAL ACTIVITIES OF NEW 5-HT2A SELECTIVE LIGANDSN-SUBSTITUTED-PIPERIDINYL4-PHENYLTHIOETHER AND SULFONE DERIVATIVES
Hao WANG ; Ren WEN ; Lei HUANG ; B.innis ROBERT ; Pingzhong TAN
Acta Pharmaceutica Sinica 2001;36(4):274-277
AIM A series of 4-piperidinylthioether and sulfone derivatives of 4-[1-hydroxy-1-(2,3-dimethoxyphenyl) methyl]-N-2-(4-fluorophenylethyl) piperidine (MDL 100907) were synthesized in order to find new 5-HT2A selective ligands. METHODS Title compounds 2a-2c were synthesized from 2,3-dimethoxythiophenol and tested for their affinities to 5-HT2A, 5-HT2C, 5-HT6 and 5-HT7 receptors and some other nervous transmitter receptors in vitro. RESULTS Compounds 2a-2c are new compounds. The results of the binding assay demonstrated that they have relatively high selectivity for 5-HT2A receptor in vitro. CONCLUSION Some sulfur containing analogues of MDL 100907 showed selective affinity to 5-HT2A receptor and are worth further study.
3.EFFECT OF wt-P53 PROTEIN ON TELOMERASE ACTIVITY IN KELOID FIBROBLASTS
Zhibo XIAO ; Lijun HAO ; Lihong REN ; Wen TENG
Chinese Journal of Reparative and Reconstructive Surgery 2007;21(7):702-706
Objective To evaluated the role of wt-P53 protein in telomerase regulation in keloid fibroblasts(KFBs). Methods The fibroblasts were derived from human keloid tissue which was proved by pathological diagnosis. KFBs were divided into 2 groups, the transfection group and the untransfection group. wt-p53 gene was transfected into the fibroblasts by adenovirus vectors in the transfection group. The KFBs untransfected with wt-p53 gene served as control (untransfection group). After 48 hours of transfection, the expression of wt-P53 protein was analyzed by both Western blotting and immunofluorescence method, respectively. The telomerase activity was evaluated by TRAP-ELISA after 1-7 days of transfection.Results All the KFBs from 2 groups expressed wt-P53 protein. But the expression level of wt-P53 protein in the transfection group was significantly higher than that in the untransfection group. At the same time of high expression of wt-P53 protein, the telomerase activity of KFBs in transfection group was significantly lower than that in the untransfection group( P<0.05). Conclusion High level expression of wt-P53 protein can transiently inhibit the telomerase activity of KFBs.
4.Influence of Wt-p53 gene by adenovirus vector on proliferation of keloid fibroblasts
Zhibo XIAO ; Lijun HAO ; Lihong REN ; Wen TENG
Chinese Journal of Medical Aesthetics and Cosmetology 2001;0(04):-
Objective To study wt-p53 gene's influence on the proliferation of keloid fibroblasts in vitro. Methods wt-p53 gene was transfected into keloid fibroblasts by adenovirus vector. wt-p53 mRNA was analyzed by RT-PCR; wt-p53 protein was evaluated by indirectiy immunofluorescence; The ability of proliferation of keloid fibroblasts was analyzed by cell growing curves; The cell cycle of KFB was checked by FCAS. Results The expression of wt-p53 mRNA and protein was obviously higher in the fibroblasts of the experimental group than those of control group; the rate of G_0~G_1 in cell cycle was higher in the fibroblasts of the experimental group than those of control group; at the same time, the rate of G_2~M was lower in fibroblasts of the experimental group than those of control group (P
5.Effects of Salidroside on Tic Behavior of Tourette Syndrome Model Rats.
Hui XIE ; Zhen WANG ; Yan JI ; Jing YIN ; Wen-hao YANG ; Li-min REN
Chinese Journal of Integrated Traditional and Western Medicine 2016;36(1):90-93
OBJECTIVETo observe the effect of salidroside on tic behavior and in vivo dopamine DA) and serotonin (5-HT) levels in Tourette syndrome (TS) model rats.
METHODSForty rats were randomly divided into the blank control group, the TS model group, the haloperidol-treated group (0.5 mg/kg x d(-1)), and the salidroside-treated group (50 mg/kg x d(-1)), 10 in each group. TS rat model was induced by imino-dipropio-nitrile (IDPN). Peritoneal injection of haloperidol and salidroside was started from the 4th day of modeling in the haloperidol-treated group and the salidroside-treated group respectively. Normal saline was peritoneally injected to rats in the blank control group and the TS model group respectively. Stereotyped behavior was scored, and changes of DA and 5-HT levels in blood and striatum were measured before modeling, after modeling, and after intervention.
RESULTSCompared with the blank control group, the score of the tic behavior was elevated (P < 0.01) , levels of DA and 5-HT in plasma and striatum were reduced in the model group (P < 0.01, P < 0.05). Compared with the same group after modeling, the tic behavior score decreased and plasma DA levels increased in the two treated groups after intervention (P < 0.01). 5-HT content increased in the salidroside-treated group (P < 0.01). Compared with the model group after intervention, the tic behavior score was significantly reduced (P < 0.01), and DA levels in plasma and striatum were elevated (P < 0.01, P < 0.05) in the salidroside-treated group and the haloperidol-treated group. Compared with the haloperidol-treated group, the tic behavior score increased (P < 0.01), DA levels in plasma and striatum were lowered (P < 0.01, P < 0.05), the 5-HT level increased in plasma and striatum (P < 0.01, P < 0.05) in the salidroside-treated group.
CONCLUSIONSIn the salidroside-treated group, the tic behavior was significantly reduced, and DA levels in plasma and striatum were elevated. Its mechanism might be related to regulating activities of dopamine neurons in striatum.
Animals ; Corpus Striatum ; Dopamine ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Glucosides ; pharmacology ; therapeutic use ; Haloperidol ; Phenols ; pharmacology ; therapeutic use ; Rats ; Serotonin ; Stereotyped Behavior ; Tics ; drug therapy ; Tourette Syndrome ; drug therapy
6.Rapid isolation and culture of pig airway epithelial cells.
Wen-shu CHEN ; Tian-ling HAO ; Xi WANG ; Dan TIAN ; Ren-liang WU
Chinese Journal of Pathology 2005;34(10):685-687
7.Dynamic observation on the serum level of vascular endothelial growth factor in experimental rats with hepatic alveolar echinococcosis after hepatic arterial infusion of bevacizumab treatment
Zejie SANG ; Diwen ZHU ; Weizheng JI ; Junpeng GU ; Haixiao ZHANG ; Weixin REN ; Hao WEN
Journal of Interventional Radiology 2014;(6):516-519
Objective To investigate the changes in the serum level of vascular endothelial growth factor (VEGF) in experimental Wistar rats with hepatic alveolar echinococcosis (HAE) after hepatic arterial infusion (HAI) of bevacizumab treatment, and to discuss the efficacy of HAI of bevacizumab for hepatic alveolar echinococcosis. Methods Forty Wistar rats with successfully established HAE were randomly and equally divided into two groups with 20 rats in each group: the control group and the study group. Hepatic arterial infusion of saline was performed in the rats of the control group , while hepatic arterial infusion of bevacizumab was carried out in the rats of the study group. Before and 7, 14, 21 and 28 days after the treatment peripheral blood samples were collected from the tail vein, and the serum levels of VEGF, apartate aminotransferase (AST) and alanine aminotransferase (ALT) were determined by the quantitative sandwich enzyme-linked immunosorbent assay (ELISA). All the rats were sacrificed 28 days after the treatment. HAE samples were examined to evaluate the effect of bevacizumab on HAE lesions. Results Seven days after hepatic arterial infusion of bevacizumab, serum VEGF expression level in the study group became gradually decreased, and the difference was statistically significant when compared with the preoperative level or with that in the control group (P = 0.019). Fourteen days after the treatment, the serum VEGF expression level kept going down to its lowest point, and the difference in serum VEGF expression level was statistically significant when compared with the preoperative level (P < 0.01). Twenty-one days after the treatment, serum VEGF expression level started to rise and it returned to normal level in 28 days after the treatment. In the control group no significant changes in serum VEGF expression levels was observed after hepatic arterial injection of saline (P > 0.05). Conclusion In treating hepatic alveolar echinococcosis, hepatic arterial infusion of bevacizumab has certain inhibitory effect on angiogenesis. This therapy is safe and effective.
8.Procedure of seed quality testing and seed grading standard of Prunus humilis.
Hao WEN ; Guang-Xi REN ; Ya GAO ; Jun LUO ; Chun-Sheng LIU ; Wei-Dong LI
China Journal of Chinese Materia Medica 2014;39(21):4191-4196
So far there exists no corresponding quality test procedures and grading standards for the seed of Prunus humilis, which is one of the important source of base of semen pruni. Therefor we set up test procedures that are adapt to characteristics of the P. humilis seed through the study of the test of sampling, seed purity, thousand-grain weight, seed moisture, seed viability and germination percentage. 50 cases of seed specimens of P. humilis tested. The related data were analyzed by cluster analysis. Through this research, the seed quality test procedure was developed, and the seed quality grading standard was formulated. The seed quality of each grade should meet the following requirements: for first grade seeds, germination percentage ≥ 68%, thousand-grain weight 383 g, purity ≥ 93%, seed moisture ≤ 5%; for second grade seeds, germination percentage ≥ 26%, thousand-grain weight ≥ 266 g, purity ≥ 73%, seed moisture ≤9%; for third grade seeds, germination percentage ≥ 10%, purity ≥ 50%, thousand-grain weight ≥ 08 g, seed moisture ≤ 13%.
Cluster Analysis
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Germination
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Prunus
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growth & development
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Seeds
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physiology
9.The prognostic factors in 32 patients with metastatic pancreatic tumor
Peng JIN ; He REN ; Wei SUN ; Wen XIN ; Yong TANG ; Jihui HAO
Chinese Journal of Hepatobiliary Surgery 2013;(4):263-266
Objective To study the clinicopathological characteristics and the prognostic factors in metastatic pancreatic tumor.Methods The clinical data of 32 patients with metastatic pancreatic tumors were retrospectively analyzed.The survival of the patients were evaluated with the KaplanMeier method.Univariate analysis was done by log-rank test.Results The primary foei of these32 patients included:9 lung cancer,6 renal cell carcinoma,5 gastric cancer,12 others.The median survival was 15.5 months in the radical surgery group (n 8),18 months in the cryosurgery group(n=3),8 months in the group with palliative bypass operation (n=9),6 months in the group with local radiotherapy (n=3),and 5 months in the group without treatment (n=9).Univariable analysis revealed the type of primary tumor,treatment of the primary tumor,interval between diagnosis of primary tumor and pancreatic metastases,localized pancreatic metastasis,and treatment of the metastatic pancreatic tumor were associated with prognosis.Conclusions Metastatic pancreatic tumors are rare.Long term survival can be achieved with pancreatic resection in a highly selected subset of patients according to the type of primary tumor.Therapeutic cryosurgery as a new minimally invasive,targeted and immunologic method needs to be further evaluated.
10.Mucinous cystic neoplasms of pancreas: an analysis of 42 patients
Peng JIN ; He REN ; Wei SUN ; Wen XIN ; Yong TANG ; Jihui HAO
Chinese Journal of Hepatobiliary Surgery 2013;(5):352-355
Objective To study the clinicopathological characteristics,diagnosis and treatment of patients with mucinous cystic neoplasms (MCNs) of the pancreas.Methods The clinical data of 42 patients with mucinous cystic neoplasms of pancreas were retrospectively analyzed.Chi-square test and independent sample t-test were used for statistical analysis.Results The mean age of the patients was 53.1 yeas (ranged from 29 to 78 y).There were 32 female (76.2%).The patients were divided into two groups according to symptoms (the symptomatic group and the asymptomatic group).There were significant differences in tumor size,tumor location,operation type,operation time and adhesions with the surrounding tissues between the 2 groups of patients.The patients were then divided into three groups according to pathological type.There were significant differences in age,tumor marker,tumor location,operation type,operation time,adhesions with the surrounding tissues,operative blood loss,and postoperative hospital stay among the 3 groups of patients.There was no tumour recurrence in the patients with cystadenoma.Patients with cystadenocarcinoma developed tumor recurrence at a mean of 16.4 months (range,0-50) and died of tumor recurrence even after radical surgery at a mean of 22.9 months (range,3-58).Conclusion MCNs were seen most commonly in middleaged women.The presence of symptoms was a sign of malignancy.Resection of the tumor in the early stage is the key in dealing with MCNs.