1.Relationship between IP_3 and detrusor cell contraction mediated by M_3R
Gensheng LU ; Bo SONG ; Xiyu JIN
Chinese Journal of Urology 2001;0(10):-
Objective To study the relationship between IP 3 and detrusor cell contraction mediated by M 3R. Methods [3H]-IP contents of human cultured detrusor cells were detected after stimulated by carbachol,atropine,methoctramine and 4-DAMP respectively. Results [3H]-IP contents increased with carbachol concentration.On the different concentrations (10 -9、10 -8、10 -7、10 -6、10 -5、10 -4 mmol/L )of 4-DAMP,[3H]-IP contents were 3 926.57?273.29、2 780.52?211.09、2436.84?153.62、1 973.22?164.71、1 372.38?141.35 and 1 107.98?920.45 cpm respectively.On the some concertrations of Atropine,[3H]-IP contents were 3 602.69?280.17,2 891.31?207.45,1 983.97?145.74,1 269.57? 105.31,1 106.37?75.23,927.50?77.36/min,respectively.On the same concentrations of methoctramine, the [3H]-IP contents was 4 462.74?360.69、3 938.61?327.13、3 315.45?270.36、3 063.19? 246.79、2927.37?226.45 and 2 836.55?241.63 cpm.This donoted that 4-DAMP and atropine signficantly inhibited the effect of carbachol on PI decomposition(P0.05). Conclusions M 3R is much related to IP 3.
2.RELATIONSHIP BETWEEN DENSITY OF MUSCARINIC RECEPTOR SUBTYPE AND BLADDER INSTABILITY IN RATS
Gensheng LU ; Bo SONG ; Xiy JIN
Medical Journal of Chinese People's Liberation Army 1983;0(02):-
To study the relationship between the density of muscarinic receptor (MR) subtype and the occurrence of bladder instability. The rat model of unstable bladder was established, and the density of MR subtype was determined in normal and unstable bladders. The results showed that there were only m 2 RNA and m 3 RNA present in the detrusor of normal and unstable bladders, and m 1, m 2 or m 3 mRNA subtypes were not detected. In the normal bladder, the amount of m 2 RNA (1 67?0 42) was obviously greater than m 3 RNA (0 64?0 19), and the ratio of them was 2 59∶1. In the unstable bladder, the density of both m 2 and m 3 increased to (2 03?0 65) and (1 53?0 46) respectively, and the increase of m 3 was more significant ( P
3.Detection of rpsL drug-resistant gene in L-form of Mycobacterium tuberculosis by PCR-SSCP
Chinese Journal of Clinical Laboratory Science 2006;0(02):-
Objective To study the relationship between mutation of rpsL drug-resistant gene in L-forms of Mycobacterium tuberculosis and drug-resistance to streptomycin in pneumoconiosis patients.Methods A total of 52 clinical isolated strains of Mycobacterium tuberculosis L-forms were collected from 97 pneumoconiosis patients.The mutation of rpsL gene was detected by PCR-SSCP,and the drug-resistance to streptomycin was performed by routine antimicrobial susceptibility test(AST).Results The results of drug susceptibility test showed that 26 in the 52 clinical isolated strains were drug-resistant to streptomycin.The streptomycin-resistant rate was 50.00%(26/52).The gene mutation rate of rpsL detected by PCR-SSCP was 40.38%(21/52).The coincidence rate of two experimental results was 80.77%(21/26).Conclusion High detectable rate of streptomycin-resistant strains in Mycobacterium tuberculosis L-forms was found by PCR-SSCP.The application of PCR-SSCP may possess important value for guiding clinical medication of pneumoconiosis patients complicated with tuberculosis among coal workers
4.Relationship between muscarinic receptor subtype density change and unstable bladder in rats
Gensheng LU ; Bo SONG ; Enqing XIONG ; Xiyu JIN ;
Journal of Third Military Medical University 2002;0(12):-
Objective To study the relationship between muscarinic receptor(MR) subtype density changes and the producing of unstable bladder Methods The rat model of unstable bladder was established and the MR subtype density of control and unstable bladders were defermined by RT-PCR Results There were only m 2RNA and m 3RNA in the detrusor of control and unstable bladders, but no m 1, m 2 and m 3 mRNA, the amount of m 2RNA(1 67?0 42)was larger obviously than m 3RNA(0 64?0 19),the ratio was 2 59∶1 in control group, and the density of both m 2 and m 3 in unstable bladder increased to (2 03?0 65) and(1 53?0 46)respectively, and the increase of m 3 was more significant ( P
5.Changes of excitability and contractility in detrusor instability
Gensheng LU ; Ci GE ; Bo SONG ; Xiyu JIN ;
Journal of Third Military Medical University 2003;0(24):-
Objectives To observe the changes of the detrusor excitability and contractility and to study the mechanism of the unstable bladder. Methods Detrusor strips were obtained from prostectomy patients with benign prostatic hyperplasia. According to the results of urodynamic examination, patients were divided into detrusor instability (DI) and detrusor stability group(DS). Test of mechanical tension and stimulations with electricity and carbachol were performed on the excitability and contractility of the detrusor strips from 8 patients selected from each of the groups in vitro . Results The minimum tension of the detrusor strips when contraction occurred in DI and DS was (0 324?0 132)g and (0 822?0 216)g, respectively. There was significant difference between DI and DS ( P
6. Optimation of infiltration process of Pericarpium Citri Reticulatae in Huoxiang Zhengqi Liquid
Chinese Traditional and Herbal Drugs 2014;45(8):1096-1101
Objective: To optimize the infiltration process of Pericarpium Citri Reticulatae (PCR) in Huoxiang Zhengqi Liquid (HZL). Methods: Using the dissolution content of hesperidin as indicator, the infiltration process parameters for PCR such as soaking time, fineness of grind, degree of compaction, infiltration rate, and medicinal infiltration or not were studied, and considering the actual production efficiency, the optimal process conditions were determined. Results: The optimal infiltration process conditions were as follows: PCR was loaded into the extraction tank without soaking (there was no difference between 24 and 48 h of soaking time), spread evenly and compacted properly; The crude medicine fineness was about 0.5 cm × 0.5 cm; The infiltration solvent was 60% ethanol; The infiltration solvent was added to the extraction tank of crude medicines, the volume of solvent can not be too much, just inundating crude medicines; Adding solvent speed and infiltration speed were basically identical; The primary infiltration speed was 1 mL/(min·kg) and the continued infiltration speed was 2 mL/(min·kg). Conclusion: The optimal PCR infiltration process conditions of HZL are determined by evaluating the dissolution content of hesperidin.
7.Advances in the study of new BCR-ABL kinase inhibitors
Wen-yu CUI ; Ruo-xi ZHAO ; Lu-lu HAN ; Wei-wei NI ; Fei LI ; Jin-song HAN
Acta Pharmaceutica Sinica 2023;58(2):258-273
The oncogenic product of BCR-ABL is an abnormal tyrosine kinase that causes chronic myeloid leukemia (CML). With further research into the pathogenesis of CML, the discovery of compounds that selectively inhibit abnormal BCR-ABL tyrosine kinases is a research focus worthy of attention. The first three generations of BCR-ABL inhibitors are orthosteric inhibitors, which competitively block the binding of ABL protein tyrosine kinase to ATP and prevent it from activating downstream signals. The fourth-generation BCR-ABL inhibitors allosterically inhibit ABL protein tyrosine kinase by binding to the myristoyl pocket, providing greater selectivity and maintaining activity against drug-resistant mutations proteins. Novel drug design strategies such as proteolytic targeting chimera (PROTAC), covalent inhibitors and dual targeting inhibitors also provide new directions for the development of BCR-ABL kinase inhibitors. This paper reviews recent research advances on BCR-ABL kinase inhibitors and discusses drug design strategies for various novel BCR-ABL inhibitors.
9.Long-term therapeutic effect of liver transplantation in patients with hepatic myelopathy
Guosheng DU ; Hong LU ; Bingyi SHI ; Jiyong SONG ; Hailong JIN ; Ming CAI ; Yeyong QIAN ; Zhidong ZHU
Chinese Journal of Tissue Engineering Research 2010;14(18):3397-3400
BACKGROUND: Hepatic myelopathy results from liver disease, which lacks of effective cure method. Liver transplantation has attempted to cure this disease; however, the long-term therapeutic effect is rarely reported. OBJECTIVE: To explore the long-term therapeutic effect of liver transplantation in patients with hepatic myelopathy. METHODS: The clinical data of 2 patients with hepatic myelopathy, who underwent orthotopic liver transplantation, in August 2002 and November 2004, at the 309 Hospital of Chinese PLA, were analyzed retrospectively. The time of follow-up was 18 and 43 months, respectively. The muscle strength of double lower limbs in 2 patients was assessed prior to and after operation. RESULTS AND CONCLUSION: Two patients recovered well at 4 weeks after transplantation, the clinical symptom and physical signs of patients were improved obviously, the blood routine examination and other biochemical index were normal,and the function of transplanted kidney was normal. Two patients discharged at 6 weeks after transplantation. Patient 1 could stand for a long time at months 6 after transplantation, walked slowly with the supporter after 12 months and without the supporter at 43 months. The muscular strength of two lower limbs was grade 4. And the liver function was normal. Patients 2 could move his lower limbs in bed at months 6 after transplantation, walked with the supporter at 18 months. The muscular strength of two lower limbs was grade 3. The liver function was normal. It demonstrated that liver transplantation is beneficial to control hepatic myelopathy and recover muscular strength of two lower limbs. It is a newly developed, effective curing method for treating hepatic myelopathy. However, the numbers were small with short time observation, thus, the long-term therapeutic effect still need to be explored.
10.Effect of propofol on brain injury in children undergoing open heart surgery under cardiopulmonary bypass
Dandan SONG ; Tiezheng ZHANG ; Yingjie SUN ; Jin ZHOU ; Yuping LU ; Xiaojiang LIU
Chinese Journal of Anesthesiology 2010;30(8):928-930
Objective To investigate the effect of propofol on the brain injury in children undergoing open heart surgery under cardiopulmonary bypass (CPB).Methods Thirty children aged 4-10 yr undergoing repair of ventricular septal defect or atrial septal defect under CPB were randomly divided into 2 groups ( n = 15 each):control group (group C) and propofol group (group P). Anesthesia was induced with iv injection of sufentanil 1 μg/kg, propofol 2.5 mg/kg (midazolam 0.2 mg/kg in group C) and pipecuronium 0.1 mg/kg in group P. Anesthesia was maintained with iv infusion of 1% propofol 6 mg·kg-1 ·h-1 (0.05% midazolam 0.2 mg·kg-1 ·h-1 in group C) until the end of operation. Isoflurane ( 1%-2% ) were inhaled during the operation in all patients. Sufentanil 1 μg/kg and pipecuronium 0. 1 mg/kg were injected intravenously after the start of CPB. A catheter was inserted into right internal jugular vein and advanced cephalad until jugular bulb for blood sampling before CPB, at 30 min of CPB, at the end of CPB, at 30 min after termination of CPB, at the end of operation, and at 24 h after termination of CPB to detect the plasma concentrations of 8-iso-PGF2 and S-100β by ELISA. Arterial and jugular bulb venous blood samples were collected for determination of SjvO2 before CPB, when naso-pharyngeal temperature was reduced to 30 ℃, when naso-pharyngeal temperature returned to 36 ℃ and at the end of CPB. Cerebral arterial venous oxygen content differences ( Da-jvO2 ) and cerebral oxygen extraction rate of oxygen ( CEO2 ) were calculated. Results Plasma concentrations of 8-iso-PGF2α and S-100β were significantly lower, SjvO2 was significantly higher, Da-jvO2 and CEO2 were significantly lower in group P than in group C (P < 0.05=. ConclusionPropofol can reduce the brain injury in children undergoing open heart surgery during CPB and the mechanism is related to decrease in cerebral oxygen metabolic rate and lipid peroxidation.