1. Design, synthesis, and antifungal activity of 3-substituted triazole derivatives
Academic Journal of Second Military Medical University 2010;31(10):1114-1119
Objective: To study the in vitro antifungal activity of triazole alcohols by introduction of 1, 2, 3-triazole as the side chain. Methods: Twenty-one novel triazole alcohol compounds were designed, synthesized, and characterized by 1HNMR and MS spectra. The in vitro antifungal activities of the compounds were evaluated using eight kinds of pathogenic fungi. Results: All the synthesized compounds exhibited certain antifungal activities. The MIC 80 value of compound 7 1-(1H-1, 2, 4-triazole-1-yl)-2-(2, 4-difluorophenyl)-3-[N,N-(1-substituted-benzyl-4-methylene-1H-1,2,3-triazole)] against Candida albicans was 0.25 μg/ml, with its activity being 4 times that of fluconazole. The MIC80 value of compound VI 1-(1H-1,2,4-triazole- 1-yl)-2-(2,4-difluorophenyl)-3-(N,N-dipropargyl)-2-propanols against Candida albicans was 0.0156μg/ml, with its activity being 64 times that of fluconazole and 4 times that of itraconazole. Conclusion: The 1,2,3-triazole can be efficiently introduced by intermolecular 1,3-dipolar cycloaddition. Large side chains may be a disadvantage for improving the antifungal activity of the title compounds.
2.The value of pedicled fat and capsule-packed nerve root in operation of sacral canal cysts
Chuankun LI ; Baixiang HE ; Gang BAO ; Minxue LIAN ; Ning WANG
Journal of Xi'an Jiaotong University(Medical Sciences) 2016;(2):187-189
Objective To evaluate the value of pedicled fat and capsule-packed nerve root in operation of sacral canal cysts.Methods We collected the information of 14 cases of sacral canal cysts for operation in our department and analyzed the operation indications and skills as well as the prognosis.Results All the operations were performed with the help of the microscope and the electrophysiological monitor.The capsules were removed in 9 cases and wrapped in 6 cases,with the total resection rate of 64.3%.The clinical symptoms were improved markedly after the operation.Conclusion The operation with pedicled fat and the capsule-packed nerve root is valuable in treating sacral canal cysts because it can protect the nerve root and get lower recurrence rate.
3.The Effect of Combination Use of 1,25(OH)_2D_3 and Celecoxib on Growth and Apoptosis in Breast Cancer Cell Line Hs578T
Xueqi HE ; Yangyi BAO ; Xin SUN ; Gang MENG ; Qin WANG
Journal of Medical Research 2006;0(08):-
Objective To study the effect of combined 1,25-dihydroxyvitamin D31,25(OH)2D3 and celecoxib on growth, call cycle and apoptosis in breast cancer cell line Hs578T.Methods We compared cell numbers by using MTT method , analyzed cell cycle percentage and apoptosis with flow cytometric.Results Both with 1,25(OH)2D3 and celecoxib could inhibite tumov growth,induc apoptosis in a dose-time-dependent manner. comparing with 1,25(OH)2D3 alone,combination wse of the two drugs had a additive effect but was inferior to cececoxib alone. The combination use of 10-8mol/L1,25(OH)2D3 and celecoxib group is more effective than the combination use of 10-7mol/L1,25(OH)2D3 and celecoxib group. Conclusion 1,25(OH)2D3 and celecoxib could be a new drug for the prevention and treatment of breast cancer.
4.Relationships among Cerebral Vasospasm Following Subarachnoid Hemorrhage and Atrial Natriuretic Peptide and Hyponatremia
Chen-bao HAN ; Zhou LIU ; Yi-gang WANG ; Guanzhong HUANG
Chinese Journal of Rehabilitation Theory and Practice 2006;12(4):329-331
ObjectiveTo explore the relationships among atrial natriuretic peptide (ANP) and cerebral vasospasm (CVS) following subarachnoid hemorrhage (SAH) and hyponatremia.MethodsPlasma ANP levels and serum natrium and blood flow rate of intracal major arterial were assessed at different times (1 to 3 days, 7 days and 14 days after SAH) in 42 patients with SAH. Correlation analysis was carried out among plasma ANP, blood sodium level and blood flow rate of intracal major arterial.Results28 patients had CVS. Plasma ANP levels in CVS patients significantly elevated compared with non-CVS and control subjects (P<0.05). Hyponatremia in CVS patients also significantly elevated compared with non-CVS subjects (P<0.05). Plasma ANP level had significant negative relationship with serum natrium level at the 7th day and 14th day (r2=-0.778,r3=-0.653;P<0.01,P<0.05) in SAH patients. Plasma ANP level had significant positive correlation with middle cerebral artery mean flow velocity on the 7th day (r3=0.702,P<0.05) in SAH patients. Middle cerebral artery mean flow velocity had significant negative relationship with serum natrium level on the 7th day and 14th day (r2=-0.693,r3=-0.653 , both P<0.05) in SAH patients.ConclusionANP might cause hyponatremia following SAH and play an important role in pathogenesis of earlier period CVS.
5.Experimental study of antitumor immunity of DC/C6 fusion vaccine
Donghai WANG ; Xingang LI ; Ying WANG ; Xun QU ; Gang LI ; Songfeng GONG ; Quanmeng LIU ; Xiufeng BAO
Chinese Journal of Pathophysiology 1986;0(02):-
AIM:To study the anti-tumor effect and mechanism of fusion vaccine on DCs and C6 glioma cells.METHODS: PEG was used to fuse DCs with C6 glioma cells.Immunofluorescence with GFAP-FITC was used to identify the DC/C6 fusion cells.Rat brain glioma models were made by stereotactic technique.After 5 days of inoculation of C6,107 fusion cells were injected through tail vein in group A.The same number of DCs and the same volume of PBS were used in group B and group C.The survival time of rats in these three groups was analyzed by Log-rank survival analysis.Tumor samples were checked by HE staining and immunohistochemical staining with CD8Mcab.RESULTS: Positive result of GFAP-FITC immunofluorescence was observed in DC/C6 fusion cells.The Log-rank survival analysis showed that statistically significant difference in group A was observed compared to that in group B and group C(P
8.Radiosynthesis and preliminary evaluation of 5-(11Cmethyloxy)-L-tryptophan as PET tumor imaging.
Shan-zhen HE ; Shu-xia WANG ; Kong-zhen HU ; Bao-guo YAO ; Gang-hua TANG
Acta Pharmaceutica Sinica 2015;50(5):565-568
The PET tracer 5-([11C]methyloxy)-L-tryptophan (5-(11)CMTP) was prepared by nucleophilic fluorination and alkylation reaction via a two-step procedure in order to develop specific tumor probe. The biodistribution and microPET imaging of 5-(11)CMTP were executed. The results unveiled that the overall radiochemical yield with no decay correction was (14.6 ±7.2) %, the radiochemical purity was more than 95% and high uptake and long retention time of 5-(11)CMTP in liver, kidney and blood were observed but low uptake in brain and muscle were found, furthermore, high uptake of 5-(11)CMTP in tumor tissue was observed. It seems that 5-(11)CMTP will be a potential amino acid tracer for tumors imaging with PET.
Amino Acids
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Animals
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Neoplasms
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diagnostic imaging
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Positron-Emission Tomography
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Radioactive Tracers
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Tissue Distribution
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Tryptophan
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analogs & derivatives
9.Relationships between induction of apoptosis by Taxol in Hela cells and apoptosis-related proteins
Xiangyang HU ; Gang MENG ; Yangyi BAO ; Xiaomei ZHU ; Yuan WANG ; Qin ZHOU
Chinese Pharmacological Bulletin 2003;0(09):-
Aim To investigate the effects of taxol on apoptosis in Hela cell and the mechanism of apoptosis. The apoptotic cells were detected by TUNEL, HE, eletronic micrpscopy and flow cytometry method. The expressions and activity of apoptosis associated proteins such as PCNA and caspase-3 were examined using S-P and enzyme histochemistric method.The results followed as: HeLa cells exposed to Taxol undergo cell death, presenting morphological and biochemical characteristics typical of apoptosis and the apoptotic cells increased with time and concentration. In contrast to untreated Hela cells, which express low PCNA, Ones treated with Taxol expressed high amounts of PCNA. Conclusion Taxol may induced apoptosis in Hela cell. The apoptosis induced by taxol is related to the increase of PCNA protein and activity of caspase-3.
10.Application of intraoperative nerve electrophysiological monitoring inlumbosacral spinal cord tumor resection
Haiping LIAN ; Zhijin LI ; Baixiang HE ; Xiaofang LIU ; Gang BAO ; Wei WANG ; Minxue LIAN ; Chuankun LI
Journal of Xi'an Jiaotong University(Medical Sciences) 2016;(2):178-182
Objective To study intraoperative neural electrophysiological monitoring applied in lumbosacral spinal cord tumor resection.Methods We retrospectively reviewed the clinical data of 212 patients undergoing lumbosacral spinal cord tumor resection with or without intraoperative neural electrophysiological monitoring in our hospital.The patients were divided into two groups:124 patients in the monitored group received intraoperative neural electrophysiological monitoring while 88 ones in the control group did not.The monitoring was performed by recording the cortical somatosensory evoked potential (CSEP),dermatomal somatosensory evoked potential (DSEP) and electromyography (EMG).The patients were followed up for 3-6 months and their postoperative outcome was analyzed.Results There were significant differences in the outcome (P <0.05),but no difference was found in the incidence of complications between the monitored group and the control group.The sensitivity of CSEP +DSEP+EMG was 100%,and the specificity was 55.9% in the former group.Conclusion Combined monitoring with CSEP,DSEP and EMG during lumbosacral spinal cord tumor resection is valuable in protecting the spinal nerve roots and ensuring better operation safety.