1.Antagonistic Effect of N-acetylcysteine on Hepatic Mitochondria Damage Induced by Cadmium in Rats
Kun GUAN ; Zhao-Fa XU ; Fang-Lin ZHANG ; Al ET ;
Journal of Environment and Health 2007;0(08):-
Objective To study the antagonistic effect of N-acetylcysteine(NAC)on the damage of hepatic mitochondria of rats induced by cadmium in vitro.Methods The mitochondria were prepared from the clean Wistar rats' whole liver by using differ ential centfifugation.The mitochondria were incubated in the assay buffer containing different concentration of CdCl_2 (10,100,1 000,10 000 ?mol/L)at 37 ℃ for 1 h.The effect of NAC(500 ?mol/L)was studied at a CdCl_2 concentration of 1 000 ?mol/L.The incubation buffer was collected and the level of GSH,cytochrome C and the activity of Mn-SOD were determined. Results Compared with the control group,the level of GSH and Mn-SOD in 100,1 000,10 000 ?mol/L CdCl_2 groups were significantly decreased,the content of cytochrome C in 1 000,10 000 ?mol/L CdCl_2 groups were significantly increased(P
2.Development of HTS model on SERT inhibitors combined biological screening model with HTVS.
Rui ZHAO ; Jian-song FANG ; Ai-lin LIU ; Guan-hua DU
Acta Pharmaceutica Sinica 2015;50(9):1116-1121
In order to improve the efficiency of drug screening on serotonin transporter (SERT) inhibitors, a high-throughput screening (HTS) model is established in RBL-2H3 cells. The RBL-2H3 cells are very similar to the serotonin genetic neuro, in modulation of post-receptor mechanisms and transduction pathway of SERT reactivated. Depending on a fluorescence substrate ASP+ used in detection method of inhibitor rates, it's convenient, quick, accurate and effective, not making the environmental biohazard compared with radioactive experiments. Furthermore, biological screening model combined with computer aided virtual screening technique describing high-throughput virtual screening (HTVS). Bayesian classification method and molecular fingerprint similarity were applied to virtual screening technique, for screening compounds in compound library. Some compounds have been found, and then validated further by biological screening model. Combination of HTS and HTVS improves the efficiency of screening SERT inhibitors.
Animals
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Bayes Theorem
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Cell Line
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Drug Evaluation, Preclinical
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High-Throughput Screening Assays
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Models, Biological
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Rats
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Serotonin Plasma Membrane Transport Proteins
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metabolism
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Serotonin Uptake Inhibitors
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pharmacology
3.Pharmacokinetics and biodistribution of 11C-HupA in the normal animal
Jin, YAN ; Yi-hui, GUAN ; Fang-ping, XUE ; Zheng-wei, ZHANG ; Ping, LIU ; Xiang-tong, LIN
Chinese Journal of Nuclear Medicine 2009;29(2):109-112
Objective HupA is one of the potential drugs which can be used to treat Alzheimer's disease(AD).The aim of this study was to explore the pharmacokinetics and biodistribution of HupA in vivo by using 11C-HupA.Methods A total of 25 SD rats were studied.They were divided into 5 groups (5 rats in each group).All had intravenous injection of 22 MBq(in0.2 ml)11C-HupA through tail vein.Dynamic im-aging Was acquired from 5 to 90 minutes after injection.Venous blood and organ activities were collected at 5,15,30,60.and 90 minutes after injection.Percentage activity of injected dose per gram of tissue(%ID/g)was calculated to characterize the biodistribution of tracer in different brain regions: frontal,apical, temporal,occipital,cerebellum,hippocampus,striatum,thalamencephalon, and brain stem, Variance analysis using SPSS 11.5 software was performed and compared among the study groups.Results 11C-HupA was character-istic for its quick clearance from blood,with half time T1/2 of (14.61±1.77) min,and clearance rate (CL)macokinetics of 11C-HupA in rats corresponded to a one-compartment model.with an activity curve(area 11C-HupA distribution in different brain regions,being greater in cerebral cortex,hippocampus,hypothala-mus and brain stem. Conclusions Pharmacokinetic study of 11C-HupA in brain was fast.convenient and showed high specificity and sensitivity.Its ability to quantitatively evaluate brain function and its character-istic distribution in mice provided some evidence for monitoring therapy in AD patients.
6.Effects of vertebral height restoration of vertebroplasty for osteoporotic vertebra compression fractures.
Hai-Peng LI ; Tian-Sheng SUN ; Fang LI ; Kai GUAN ; Guang-Min ZHAO ; Jian-Lin SHAN ; Zhi-Cheng ZHANG
China Journal of Orthopaedics and Traumatology 2012;25(8):667-669
OBJECTIVETo evaluate the effect of vertebral height restoration of vertebroplasty for osteoporotic vertebra compression fractures (VCFs).
METHODSFrom October 2004 to June 2007, a total of 37 patients with 40 VCFs were treated by vertebroplasty. There were 12 males and 25 females with a mean age of (72.4 +/- 12.7) years (ranged, 48 to 87). Pain easement state was evaluated by visual analog scale (VAS) before and after operation, as well as in followed-up. Preoperative and postoperative vertebral height, kyphosis angle at fractured levels were measured on X-rays.
RESULTSAll of patients were followed-up for 12 to 47 months (averaged, 35.8 +/- 9.6). The VAS score was 8.4 +/- 1.6 before operative, 2.1 +/- 1.2 at the 2nd day after operative, there were significant difference between pre-and postoperative (P < 0.05); the average follow-up VAS was 1.6 +/- 0.9, there were significant difference as compared with the preoperative (P < 0.05). Lateral X-ray showed that the preoperative degree of vertebral height in the of anterior and middle vertebral were (72.0 +/- 10.6)% and (68.0 +/- 15.6)%, and postoperative were (76.0 +/- 8.6)% and (73.0 +/-6.1)%, respectively. There were no significant difference in vertebral height between preoperative and postoperative. The vertebral kyphosis angle was corrected from preoperative (7.8 +/- 2.7) degree to postoperative (8.1 +/- 2.3) degree.
CONCLUSIONVertebroplasty is a safe and effective method for treatment of osteoporotic VCFs, it can relieve the pain effectively. Failure to restore vertebaral height does not seem to interfere with the excellent pain management.
Aged ; Aged, 80 and over ; Female ; Fractures, Compression ; complications ; diagnostic imaging ; surgery ; Humans ; Male ; Middle Aged ; Osteoporosis ; complications ; Radiography ; Spinal Fractures ; complications ; diagnostic imaging ; surgery ; Spine ; diagnostic imaging ; pathology ; surgery ; Treatment Outcome ; Vertebroplasty ; methods
7.Research advance in the drug target prediction based on chemoinformatics.
Jian-song FANG ; Ai-lin LIU ; Guan-hua DU
Acta Pharmaceutica Sinica 2014;49(10):1357-1364
The emerging of network pharmacology and polypharmacology forces the scientists to recognize and explore new mechanisms of existing drugs. The drug target prediction can play a key significance on the elucidation of the molecular mechanism of drugs and drug reposition. In this paper, we systematically review the existing approaches to the prediction of biological targets of small molecule based on chemoinformatics, including ligand-based prediction, receptor-based prediction and data mining-based prediction. We also depict the strength of these methods as well as their applications, and put forward their developing direction.
Computational Biology
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Data Mining
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Drug Delivery Systems
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Drug Design
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Ligands
8.Application and nursing of Icare rebound tonometer
Min WANG ; Haiyan QIAN ; Fang-Li LIN ; Ye GUAN ; Xiuyun CHEN
Chinese Journal of Modern Nursing 2011;17(16):1901-1902
Objective To observe the clinical application and nursing of Icare rebound tonometer.Methods Intraocular pressure (IOP) measurements were performed on 112 cases (112 eyes) with ICARE rebound tonometer, measure on central cornea 2mm distance to temporal and nasal limbus corneae respectively.Results The results of intraocular pressure measurement on central cornea, 2mm distance to temporal and nasal limbus corneae are (15.4±3.4),(15.8±3.6),(15.6±3.4)mm Hg. There were no significant difference among them(F=0.325,P>0.05), but they have a good consistency.Conclusions There was good consistency on three different position on IOP measurements. The nursing is important for correct measurement.
9.Effect of two tonometers on measuring normal intraocular pressure
Min WANG ; Fang-Li LIN ; Hai-Yan QIAN ; Ye GUAN ; Xiu-Yun CHEN
Chinese Journal of Modern Nursing 2011;17(34):4131-4133
Objective To discuss the clinical performance of ICARE rebound tonometer.Methods Intraocular pressure measurements were performed on 112 cases(224 eyes)with non-contact tonometer and ICARE rebound tonometer respectively.Results The intraocular pressure of right eyes which measured by ICARE rebound tonometer was(15.4 ±3.4)mm Hg,and the left eyes' was(15.6 ±3.2)mm Hg on average,but they were(13.5 ±2.7)mm Hg and(13.6 ±2.6)mm Hg respectively measured by non-contact tonometer There was significant difference between the two tonometer(t =4.384,4.535;P <0.01).Conclusions lOP measured by ICARE rebound tonometer is higher than that of non-contact tonometer when IOP is in the normal range.ICARE rebound and non-contact tonometer have a good consistency.
10.Effect of Zishen Huoxue Recipe on Pathomorphology in Coronary Heart Disease Rats with Shen Deficiency Blood Stasis Syndrome.
Sheng-fang ZHOU ; Ru-xiu LIU ; He-wei LUO ; Hui LI ; Xuan-ke GUAN ; Lin-lin YIN ; Li LI ; Dong-peng HU
Chinese Journal of Integrated Traditional and Western Medicine 2016;36(1):85-89
OBJECTIVETo observe the effect of Zishen Huoxue Recipe (ZHR) on pathomorphology in coronary heart disease (CHD) rats with Shen deficiency blood stasis syndrome (SDBSS).
METHODSTotally 60 healthy Wistar rats were divided into the blank control group, the model group, high, middle, and low dose ZHR groups according to random digit table, 12 in each group. Myocardial ischemia SDBSS rat model was prepared by ligating the left anterior descending coronary artery and injecting hydrocortisone. ZHR physic liquor was administered to rats in high, middle, and low dose ZHR groups at the daily dose of 21.6, 10.8, 5.4 g/kg by gastrogavage for 7 successive days, equal volume of pure water was administered to rats in the blank control group and the model group by gastrogavage for 7 successive days. Rat heart was collected for pathomorphological observation under light microscope.
RESULTSIn the model group the heart muscle fiber was swollen and deformed with widened space, loose and dropsy tissues. Blood vessels in myocardial mesenchymal were dilated, infiltrated with more inflammatory cells. Myocardial cells were markedly swollen, degenerated, or necrotic, with caryolysis or disappearance of partial nuclear. A large amount of collagen fibrous tissue became hyperplasia. Endocardial blood vessels were swollen and degenerated with infiltration of few inflammatory cells. Epicardium tissue and structure were destroyed and got hyperplasia. Swollen, degenerated, or necrotic vessels could be seen, with infiltration of more inflammatory cells and collagen deposition. Pathomorphological injuries were alleviated in each ZHR group. The higher ZHR concentration, the milder the injury degree of myocardial tissue, the more limited range of damage.
CONCLUSIONZHR could attenuate pathomorphological injuries of myocardial ischemia rats with SDBSS and regulate myocardial function, thus improving myocardial ischemia in CHD rats with SDBSS.
Animals ; Coronary Artery Disease ; drug therapy ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Medicine, Chinese Traditional ; Myocardial Ischemia ; Myocardium ; Rats ; Rats, Wistar