1.Effects of dalteparin and unfractionated heparin on plasma anti-Xa activity and activated clotting time during elective percutaneous coronary intervention or coronary angiography
Qianyi WANG ; Wei CUI ; Jingchao LU
Chinese Journal of Interventional Cardiology 1993;0(02):-
Objective To evaluate the safety and efficacy of intravenous dalteparin compared with unfractionated heparin in patients underwent coronary angiogram with or without percutaneous coronary intervention(PCI).Methods A total of 87 patients who underwent one-stage elective PCI were randomized to intravenously unfractionated heparin(UFH,10 000 IU) group or dalteparin group.The dalteparin group was further divided into low dose dalteparin(5 000 IU) group or high dose dalteparin(10 000 IU) group according to whether the patients underwent PCI procedure.Blood samples for anti-Xa levels and ACTs were assayed at baseline and at 10 min,20 min,1 hour,2 hours and 4 hours after all dalteparin or UFH doses were administered.Results Baseline characteristics were similar across the three groups.In all groups,ACTs reached the maximum at 10 min after the total doses given,with the highest value in the UFH group and lowest in the low dose dalteparin group(524.68 ?278.32 s vs 191.26?39.35 s vs 304.20?42.71 s,P0.05).Conclusion Both 5 000 IU and 10 000 IU dalteparin injected through sheath before PCI or coronary angiography could reach an anti-Xa levels similar to that achieved by 10 000 IU UFH.
2.Effect of Supercritical Fluid Carbon Dioxide Extracts from Pericarpium Zanthoxyli on in- Vitro Activity of Guinea Pig Trachea
Yuxiang ZHANG ; Xiaohui ZENG ; Ruiling ZHOU ; Yuxing CHENG ; Jingchao CUI
Traditional Chinese Drug Research & Clinical Pharmacology 1993;0(01):-
Objective To investigate the effect of Pericarpium Zanthoxyli (HJ) on guinea pigs trachea in vitro and its therapeutic mechanism. Methods The actions of HJ on the contraction of normal trachea and on the spasm of spasmodic tracheas caused by acetylcholine (Ach) and histamine phosphate (HIS), as well as the actions on intracellular Ca2+ - dependent contraction and extracellular Ca2+ - dependent contraction induced by HIS were observed. Results HJ could inhibit the guinea pigs trachea contraction , antagonize the contraction of trachea spasm induced by Ach and HIS , restrain the extracellular Ca2+ - dependent contraction induced by HIS in a dose- dependent manner. Conclusion HJ has an antiasthma effect.
3.Pharmacological Studies on Liniao Capsules
Yuxing CHEN ; Ruiling ZHOU ; Lan SUN ; Jingchao CUI ;
Chinese Traditional Patent Medicine 1992;0(02):-
Objective:To observe the diuretic action of Liniao Capsules (LC). Methods: The urinary effects of LC were studied in the loading rats with water.Results: LC could significantly increase the urinary output, shorten the latent period of emiction, and reduce the contents of TP in urine and BUN in blood serum. Conclusion: LC exerted the significant diuretic effect in rats.
4.Effects of aldosterone on the expression of endothelin in rat cardiac fibroblasts
Yuzhou WU ; Wei CUI ; Shuqin LI ; Lei ZHANG ; Jingchao LU ; Jidong ZHANG ; Jun DU
Basic & Clinical Medicine 2006;0(01):-
Objective To investigate the effects of aldosterone on the expression of endothelin(ET)in cultured neonatal rat cardiac fibroblasts(CFs).Methods CFs were isolated by trypsin digestion.ET concentration in conditioned medium was measured by radioimmunoassay,intracellular ET-1 level was evaluated by immunofluorescence assay,and the expression of preproendothelin-1(ppET-1)was detected using reverse transcriptase-polymerase chain reaction(RT-PCR)method.Results Aldosterone(10-9,10-8,10-7 mol/L)induced a dose-dependent changes in ppET-1 mRNA expression,as well as ET-1 synthesis and secretion in CFs.Meanwhile,aldosterone(10-7 mol/L)time-related induced ppET-1 mRNA expression in CFs,which began to increase in 2 h and reached the highest level in 4 h,thereafter decreased.The effects of aldosterone(10-7 mol/L)were significantly inhibited by the pre-incubation with spironolactone(10-6 mol/L).Conclusion Aldosterone increases the expression of ppET-1 mRNA,ET-1 synthesis and secretion via mineralocorticoid receptor.
5.Effect of 1,3-O,N spiroheterocyclic inhibitors of heparanase on the growth of HeLa cells
Hongjie QU ; Bin HU ; Cheng WANG ; Jingchao TAO ; Yunxiao ZHANG ; Jinquan CUI
Chinese Journal of Obstetrics and Gynecology 2015;(7):529-536
Objective To provide the theoretical supportting for targeted heparanase (HPA) inhibition of cervical cancer through observing the anti-proliferative effect of the HPA inhibitor on HeLa cell line of cervical cancer. Methods The two series of 13 kinds of novel HPA inhibitors were synthesized and optimized. Heparan degrading enzyme assay kit was used to test the effect of the inhibitors on the inhibition of HPA enzyme activity. Methyl thiazolyl tetrazolium (MTT) method and scratch test were used to observe the anti-proliferative and the migration effect of the inhibitors on HeLa cells. Flow cytometry was performed to determine the cell cycles and apoptosis. The expression of HPA was evaluated by reverse transcription (RT)-PCR, western blot and immunocytochemistry. Results All tested inhibitors could inhibit the activity of HPA enzyme [the range of 50% inhibiting concentration (IC50) values from 4.47 to 47.19 μmol/L] and the growth of HeLa cells (the range of IC50 values from 48.16 to 96.64μmol/L). Among them, No.16 compound exhibits the strongest inhibition against the growth of HeLa, which could arrest the cell into G0/G1 and G2/M phases. The rate of cell apoptosis in the group treated with 50μmol/L No.16 for 48 hours [(11.9±1.2)%] was significantly higher than that [(6.6 ± 1.8)%] in untreated group (P=0.013). Real time PCR and western blot showed that expression levels of HPA mRNA (1.23±0.46) and protein (0.46±0.31) significantly decreased in the treated group as compared with the levels of HPA mRNA (3.43 ± 0.45) and protein (1.30 ± 0.58) in the untreated group (both P<0.05). Immunocytochemistry also showed that the treatment of No.16 significantly reduced the average optical density (0.39 ± 0.04) of HPA immuostaining signal compared with that in the control group (0.50 ± 0.09; P=0.026). Conclusion Novel 1,3-O,N spiroheterocyclic HPA inhibitors could inhibit the proliferation of HeLa cells,inhibit the HPA enzyme activity in different degree, and down-regulate the expression of HPA protein.