3.EFFECT OF KB-R7943 ON Na+-Ca2+ EXCHANGE CURRENT IN GUINEA PIG VENTRICULAR MYOCYTES
Jing LU ; Xianghua XU ; Xiaoliang WANG
Acta Pharmaceutica Sinica 2001;36(1):25-28
AIM To study whether KB-R7943 has selective inhibitory effect on the inward and outward Na+-Ca2+ exchange current (INa-Ca) in guinea pig ventricular myocytes. METHODS Through setting up the model of intracellular Na+-overload during myocardial ischemia and reperfusion, the current-voltage relationship of INa-Ca was recorded using whole-cell patch clamp technique under bi-directional ionic conditions. RESULTS Currents were elicited by a declining ramp pulse depolarized immediately from holding potential of -40 mV to +60 mV, then repolarized to -100 mV at a speed of 80 mV*s-1 and returned to the holding potential under bi-directional ionic conditions, while the [Na+] was 25 mmol*L-1 in the pipette solution. The currents increased time-dependently and voltage-dependently which reached from (2.51±0.15) pA*pF-1 to (5.94±0.13) pA*pF-1 at +50 mV and from (-1.92±0.13) pA*pF-1 to (-3.17±0.16) pA*pF-1 at -80 mV (n=12) after 3 min and there is no significant run-down of the current. KB-R7943 10-6 mol*L-1 was found to decrease the current to (4.62±0.05) pA*pF-1 by 29.4% at +50 mV and to (-2.30±0.18) pA*pF-1 by 22.1% at -80 mV (n=5) after 5 min. While 10-5 mol*L-1 KB-R7943 was shown to decrease the current to (3.13±0.03) pA*pF-1 by 61.7% at +50 mV and to (-1.62±0.03) pA*pF-1 by 56.9% at -80 mV (n=7). CONCLUSION KB-R7943 can block INa-Ca in guinea pig ventricular myocytes. But, it did not show selective inhibition effect on inward and outward currents.
4.Anterior cingulated cortex modulating the nociception of spinal in CCI rats
Jing XU ; Yugang LU ; Weifeng YU
The Journal of Clinical Anesthesiology 2016;32(4):393-397
Objective To observe how the ACC transmits nociceptive information and how it regulates spinal noceciption.Methods A total of 32 male SD rats were randomly divided into four groups:Sham group,CCI group,ACC group,and AP-5 group.After light-dark transition test, forced swimming test (FST),paw withdrawal mechanical threshold (PWMT),paw withdrawal ther-mal latency (PWTL)had been measured,the rats were finally anesthetized,then ACC and the spinal cord was rapidly removed,the expression of cAMP-response element binding protein (pCREB)and extracellular regulated protein kinases (pERK)were measured by Western blot.Results Compared with the sham group,the PWMT of the CCI rats were significantly decreased,rats spent less time in the light compartment and number of transition were decreased (P <0.01 ).The immobility time in FST were also significantly prolonged (P <0.01).After AP-5 injected in bilateral ACC 13 days after CCI operation,the PWMT of the CCI rats were significantly increased,rats spent more time in the light compartment and number of transition were increased (P <0.01).The immobility time in FST were also significantly shortened (P <0.01).Compared with sham group,the expression of pCREB, pERK increased significantly in ACC in CCI group (P <0.01).The expression of pCREB,pERK in spinal cord was increased in CCI group and decreased in AP-5 group (P <0.01 ).Conclusion ACC facilitate the spinal nociception in a descending mode.
5.Determination of ginsenoside R_e and R_(g1) in Compound Jiangtang Oral Liquid by HPLC
Chinese Traditional Patent Medicine 1992;0(02):-
AIM: To establish the determination of ginsenoside R e and R g1 in Compound Jiangtang Oral Liquid(Radix Ginseng, Fructus Schisandrae Chinensis, Radix Rehmannia, Radix Asparagi, etc.) by HPLC. METHODS: C 18 ODS was used as a stationary phase, acetonitrile-0.05% phosphoric acid (96∶400) as a mobile phase and detection wavelength at 203nm. RESULTS: The linear range of ginsenoside R e concentration was from 0.66 to 3.29?g?mL -1 and correlation coefficient was 0.9991, the linear range of ginsenoside R g1 concentration was from 1.05 to 5.27?g?mL -1 and correlation coefficient was 0.9998. The average recovery of sample was 98.2% and RSD 2.2% ( n =5), respectively. CONCLUSION: The method is simple and convenient, accurate with a good reproducibility and can be used for determination of ginsenoside R e and R g1 in Compound Jiangtang Oral Liquid.
6.Study of left ventricular systolic volume and synchrony in patients with premature ventricular complexes from the right ventricular outflow tract by instantaneous full-volume imaging
Jing YAO ; Di XU ; Fengxiang LU ; Yonghong YONG ; Hongping WU ; Meijuan LU ; Jian HONG ; Liang XU
Chinese Journal of Ultrasonography 2011;20(5):369-373
Objective To assess alternations in left ventricular volume and systolic synchrony in patients with frequent premature ventricular complexes(PVCs) from the right ventricular outflow tract(RVOT).Methods Twenty-nine patients with frequent isolated PVCs from RVOT were included and 30 healthy subjects as control.Instantaneous full-volume imaging(IFI) was performed to evaluate left ventricle volumetric parameters,including end-systolic volume (ESV),end-diastolic volume (EDV),stroke volume (SV),ejection fraction (EF),and systolic synchrony parameters,including systolic dyssynchrony index (SDI),dispersion end-systole (DISPES),mean end-systolic time (MES),pre-contraction time volume (PreContr) and post-contraction time volume (PostContr).Contraction front mapping was performed to visualize volumetric contraction sequence.All values of patients with PVCs were recorded during sinus beats (PVC-S) and premature ventricular beats (PVC-V) respectively.Results Significant differences were observed in left ventricular systolic volumetric and synchrony parameters between PVC-V and control subjects (P<0.01),as well as in MES and PreContr between PVC-S and control subjects (P<0.01).Conclusions Left ventricular systolic dysynchrony was demonstrated in patients with PVCs from RVOT.IFI was a novel tool to analyze left ventricular global and regional volumetric alternations.
7.Preliminary study on the correlation between regulation of Cox-2 gene expression and radiosensitivity of esophageal cancer
Xiaoxu LU ; Hui WU ; Jing XU ; Yanling WANG ; Rong HUANG
Chinese Journal of Radiological Medicine and Protection 2015;35(7):496-500
Objective To investigate the mechanism of the radiosensitivity effect of Cox-2 gene in esophageal cancer.Methods Cox-2 specific siRNA was constructed and transfected to EC9706 cells to downregulate intracellular Cox-2 expression.The expressions of MMP-2,Bcl-2 mRNA,AKT and phosphorylated AKT proteins were assayed after radiation.Colony formation,cell proliferation,apoptosis and cell invasion in vitro were examined as well.One-way ANOVA method was used to analyze the data.Results Affter 2 and 4 Gy irradiation,a significant increase in the mRNA expression of Bcl-2 was observed in the Cox-2 up-regulation group (F =3.36,4.32,P < 0.05).In the group of Cox-2 downregulation,the expression of MMP-2 mRNA was significantly reduced(F =3.86,8.09,P < 0.05).Affter irradiation,a significant decreaseof Bcl-2 mRNA (F =3.73,5.64,P < 0.05) as well as an increase of Bax(F =7.03,7.42,P < 0.05) was detected,and the levels of total and phosphorylated AKT proteins had the highest level in the Cox-2 upregulation group and had the lowest level in the Cox-2 downregulation group.In the Cox-2 downregulation group,the apoptosis induction obviously increased with dose (F =317.40,P < 0.05),and the proportion of cells in Go-G1 phase gradually increased but the proportion of cells in S and G2-M phases decreased,concomitant with the obvious suppression of cell proliferation,in addition,cell invasion was decreased.Conclusions Downregulation of intracellular Cox-2 mRNA expression,concomitant with subsequent downregulation of MMP-2 and Bcl-2 and upregulation of Bax,resulted in reduction of the invasion and metastatic capabilities of tumor cells,and induction of Go-G1 phase arrest and apoptosis.Downregulation of AKT and phosphorylated AKT (pAKT) protein expression might also interfere with the capability of the PI3K/Akt signal transduction pathway to resist radiotherapy.
8.Charlson index combined with agestratification used to assess the tolerance of elderly patients with esophageal carcinoma to chemoradiotherapy
Xiaoxu LU ; Hui WU ; Hao CHENG ; Jianhua WANG ; Jing XU
Chinese Journal of Geriatrics 2014;33(10):1093-1096
Objective To assess the tolerance of elderly patients with esophageal carcinoma to chemoradiotherapy through.Methods A retrospective analysis of 596 elderly patients with esophageal carcinoma receiving chemoradiotherapy was conducted.Patients were divided into radiachemotherapy group and radiotherapy group,and according to age,patients were divided into four age groups (aged 70-74,75-79,80 80 and 85years and over).The tolerance to treatment was assessed by Charlson index.Results 185 patients completed chemoradiotherapy,113 patients reduced the dose of chemotherapy (reduction group),81 patients unfinished chemoradiotherapy (unfinished CRT group),160 patients completed radical radiotherapy alone (unfinished RT group),and 57 patients incompleted radiotherapy.Further analysis found that the tolerance to treatment in reduction group had significant differences between patients aged ≥ 75 years and < 75 years (x2 =6.815,P=0.009),and between WIC ≥ 1 and < 1(x2 =10.636,P=0.001); the tolerance to treatment in unfinished CRT group had significantly differences between aged ≥ 80 years and <80 years (x2 =63.842,P=0.000),and between WIC =0,1 and ≥ 2 (x2 =21.153,P=0.000).Conclusions Further age re-grouping and WIC assessment is necessary before treating esophageal cancer patients.Reduction of therapy dosage is more beneficial for patients aged ≥ 75 years and WIC≥1,and greater caution is required in chemotherapy for patients aged ≥ 80 years and WIC>1.
9.Prognostic analysis of thoracic esophageal carcinoma treated with postoperative prophylactic radiotherapy
Jing XU ; Hui WU ; Xiaoxu LU ; Yanling WANG ; Jianhua WANG
Chinese Journal of Radiation Oncology 2015;24(1):33-35
Objective To investigate the effect of the extent of postoperative prophylactic radiotherapy after radical surgery on the long-term survival in patients with thoracic esophageal carcinoma.Methods A retrospective analysis was performed on the clinical data of 201 patients with thoracic esophageal cancer who received postoperative prophylactic radiotherapy after radical surgery from 2000 to 2007.The effect of the extent of radiotherapy on survival was evaluated,and the possible prognostic factors were subjected to multivariate Cox regression analysis.The Kaplan-Meier method was used to calculate overall survival (OS) rates,and the log-rank test was used for survival difference analysis.Results The 5-year follow-up rate was 97.0%.The OS rates for patients who received radiotherapy to the whole mediastinum,whole mediastinum + lymph nodes along the left gastric artery,whole mediastinum + bilateral supraclavicular regions,upper and middle mediastinum + bilateral supraclavicular regions,and whole mediastinum + bilateral supraclavicular regions + lymph nodes along the left gastric artery were 21.7%,37.1%,38.7%,34.8%,and 19.8%,respectively (P =0.406).Multivariate analysis showed that postoperative N stage was the independent prognostic factor (P =0.009).After prophylactic irradiation,metastases to the supraclavicular lymph nodes,lymph nodes in the upper and middle mediastinum,and abdominal lymph nodes were observed in 11,34,and 10 patients,respectively.Conclusions The extent of postoperative prophylactic radiotherapy after radical surgery for thoracic esophageal carcinoma only includes upper and middle mediastinum and bilateral supraclavicular regions.
10.DPP-4 Inhibitor for the Treatment of Type 2 Diabetes and Intellectual Property Analysis
Xu YONG ; Huang LU ; Yang JING ; Liu QUAN ; He WEN
China Pharmacist 2015;(2):301-306
DPP-4 inhibitors are new oral hypoglycemic drugs and hot spots developed and launched in recent years, and they pro-vide new choices for the clinical treatment of type 2 diabetes. In China, DPP-4 inhibitors that are approved to use in the treatment of type 2 diabetes are all imported products currently. In the paper, the current intellectual property situation of DPP-4 inhibitors that are developed and approved at home and abroad is researched and analyzed. Reasonable use of the patent information of DPP-4 inhibitors that is about to expire or have failed can provide good guidance for the subsequent development of DPP-4 inhibitors in domestic with promising curative effect and good market prospects, and can generate new patents in order to enhance the market competitiveness.