1.Spontaneous recovery of calculation and number processing in patients with stroke: a one-year follow-up study
Yichen YIN ; Suping ZHANG ; Wanqing DENG ; Muzhen WANG
International Journal of Cerebrovascular Diseases 2013;21(7):531-535
Objective To investigate the spontaneons recovery of calculation and number processing in patients with stroke.Methods Assessment of calculation and number processing were performed in 30 stroke patients with stable conditions (21 cerebral infarction and 9 cerebral hemorrhage) within 3 weeks after stroke,and they were followed up for one year.Calculation and number processing was assessed using the Revised EC301 Calculation and Number Processing Battery in Chinese version at 3,6,and 12 months after stroke onset.Results The scores in the areas of numerical sequences,numerical understanding,numerical transcoding,numerical calculation,numerical knowledge and the total scores increased significantly with the passage of time (all P <0.001).There were significant differences between each area and total scores at 3,6,and 12 months after stroke and those at 3 weeks (all P <0.01),however,there were no significant differences among the three time points.The total scores and the scores in each area increased significantly with the passage of time in the cerebral infarction group and the hemorrhage group (all P <0.001),however,there were no significant differences in each area at the same time point between the two groups.There was significant difference in the recovery of the total scores between the cerebral hemorrhage group and the cerebral infarction group (P =0.008).Pearson correlation analysis showed that the recovery of the calculation and number processing in all patients (R =0.452,P =0.012) as well as in the cerebral infarction group (R =0.683,P=0.001) and the cerebral hemorrhage group (R =0.250,P =0.049) within one year showed a significant positive correlation with the total score of the first assessment.Conclusions The impaired calculation and number processing may partly spontaneously recover after stoke,and it shows significant improvement within 3 months after onset.The recovery in patients with cerebral hemorrhage may be better than that in those with cerebral infarction.The more serious the impairment in initial calculation and number processing,the worse the spontaneous recovery will be.
2.Observation on the effect of different types of statins combined with donepezil in the treatment of Alzheimer disease
Yichen YIN ; Wuhua XU ; Muzhen WANG ; Suping ZHANG
Chinese Journal of Primary Medicine and Pharmacy 2013;20(18):2721-2723
Objective To explore the effect of different types of statins combined with donepezil in the treatment of Alzheimer disease(AD).Methods According to the digital table,90 patients with AD were randomly divided into the statins A group(atrovstatin combined with donepezil) 31 cases,statins B group(simvastatin combined with donepezil)27 cases,and donepezil group(only with donepezil) 32 cases.All patients were treated for one year.The blood lipid level (including cholesterol (CH) and low density lipoprotein cholesterol (LDL-C),mini-mental state examination(MMSE),activity of daily living(ADL) and global deterioration scale (GDS) were detected and compared respectively among groups before and after treatment.Results The MMSE,ADL and GDS scores of the donepezil group were (17.00 ± 2.99) points,(60.44 ± 14.57) points,(4.28 ± 1.22) points,respectively,which were worse than those of the statins A group [(19.90 ± 3.07) points,(71.61 ± 18.50) points,(3.39 ± 1.15) points] (t =0.218,P < 0.05,t =2.669,P < 0.01,t =2.562,P < 0.01) and statins B group [(19.88 ± 6.66) points,(71.89 ± 19.61) points,(3.37 ±l.39)points](t=l.959,P <0.05,t=2.991,P <0.0l,t=2,265,P <0.01).Conclusion The combination of donepezil and statins can effectively improve cognitive function and daily living ability in patients with AD,and its effect is superior to single use of donepezil.
3.Effect of stromal ceil-derived factor-1α on angiogenesis in focal infarct in the cerebral cortex in adult rats
Li LING ; Suping ZHANG ; Zhangge JI ; Huihong HUANG ; Muzhen WANG ; Rui HE ; Wanqing DENG
International Journal of Cerebrovascular Diseases 2014;22(7):535-540
Objective To investigate the effect of exogenous stromal cell-derived factor-1 α (SDF-1 α) on angiogenesis peri-infarct region in cerebral cortex in adult rats and its possible mechanisms.Methods Twenty-four adult male Sprague-Dawley rats were randomly divided into four groups:sham operation,solvent control,SDF-1α treatment,and SDF-1α + CXCR4 antagonist (n =6 in each group).A model of focal infarct in the cerebral cortex was induced by permanent ligation of the cortical branch of the right middle cerebral artery with temporary clip occlusion of both common carotid arteries.At 1 h after cortical branch occlusion of the right middle cerebral artery,SDF-1 α (1 μg/d) or equal volume of normal saline were injected via the lateral ventricle in the SDF-1α treatment group and solvent control group,and continued for 6 days.CXCR4 antagonist AMD3100 (1 mg/d) was injected subcutaneously before injecting SDF-1 α in the SDF-1 α + CXCR4 antagonists group,and continued for 6 days.Before all the rats were sacrificed,5-bromo-2-deoxyuridine (BrdU) was injected intraperitoneally and their newly proliferated cells were labeled.At day 7 after modeling,the rats were sacrificed after neurological scores.Immunofluorescence staining was used to detect the vascular density,the numbers of neovasculature endothelial cells and the CXCR4 + cells in the peri-infarct regions or sham operation regions.Results At 7 d after modeling,the neurological function of the SDF-1α treatment group was improved significantly compared with those of the solvent control group and the SDF-1α + CXCR4 antagonist group (all P< 0.01).The vascular densities in the peri-infarct or sham operation regions in the groups of sham operation,solvent control,SDF-1α treatment,and SDF-1α+ CXCR4 antagonist were 2.1±0.3%,7.0±0.3%,10.0 ±0.9% and 7.1 ±0.3%,respectively (F=232.469,P<0.001),and that in the sham operation was significantly lower than that in the SDF-1α group (P <0.001),SDF-1 α group significantly higher than both groups of solvent control (P =0.002) and SDF-1oα + CXCR4 antagonist (P =0.001).The numbers of BrdU+/laminin+ cells in the peri-infarct regions in the groups of sham operation,solvent control,SDF-1α treatment,and SDF-1α + CXCR4 antagonist were 21.7 ± 3.1,79.7 ± 6.0,176.0 ± 12.5 and 90.3 ± 6.9,respectively (F=391.550,P<0.001),and that in the sham operation was significantly less than that in the SDF-1 α group (P < 0.001),SDF-1 α group was significantly more than both groups of solvent control and SDF-1 oα + CXCR4 antagonist (all P <0.001).The numbers of CXCR4 + cells in the peri-infarct regions in the groups of solvent control,SDF-1α treatment,and SDF-1α+ CXCR4 antagonist were 59.3± 4.5,120.3 ± 13.9 and 62.9 ± 5.9,respectively (F =85.052,P < 0.001),and that in SDF-1α group was significantly more than those in the both groups of solvent control and SDF-1 α + CXCR4 antagonist (all P < 0.001).Conclusions SDF-1α treatment may improve the neurological function after focal infarction in the cerebral cortex in adult rats and promote angiogenesis in peri-infarct region.The SDF-1/CXCR4 signal pathway may play an important regulatory role in the process of angiogenesis after cerebral infarction.
4.The EC301-CR test of acalculia for patients with cerebral infarction
Yichen YIN ; Suping ZHANG ; Muzhen WANG ; Wanqing DENG ; Rui HE ; Ruihua LIANG
Chinese Journal of Physical Medicine and Rehabilitation 2011;33(11):823-826
Objective To investigate errors and the mechanism of acalculia in patients with left or right hemisphere cerebral infarction.Methods Fifty-six patients with single hemisphere cerebral infarction and 56 normal adults who were matched in age,sex and years of education were tested with EC301-CR.The patients were divided into a left hemisphere cerebral infarction group(n =34)and a right hemisphere cerebral infarction group(n =22).Results The scores on 30 out of 32 EC301-CR items were significantly lower among the patients than in the normal control group.Scores on 14 EC301-CR items were significantly lower in the left hemisphere group than in the right hemisphere group.In the left hemisphere group the item scores of aphasia patients were significantly lower than those of no-aphasia patients except on digit identity.Conclusion Mathematical processing and calculation were impaired in patients with single hemisphere cerebral infarction.Calculation was significantly worse among left hemisphere patients compared with right hemisphere cerebral infarction.There was a highly significant correlation between acalculia and aphasia.
5.The influence of economic and cultural differences on the psychological characteristics of the recruits
Shen HUANG ; Muzhen GUAN ; Wei XIAO ; Wei WANG ; Jianzhang CHEN ; Dianmin MIAO
Chinese Journal of Behavioral Medicine and Brain Science 2011;20(3):270-272
Objective In the two division methods which are GDP per capita gathering and administrative level division of the state, which method can more reflect regional economy on teenagers psychological characteristics influence. Methods 10684 recruited youths were tested by Chinese enrollment psychological test system,and the division method of GDP per capita gathering and administrative level division of the state was adopted.Results By the method of GDP gathering, the percent of pass from digital operation was higher in second class region to first class region(P< 0.05 ). The percent of pass from digital search was higher in first and second class of region compared to third class of region(P <0.05). For the Net dimension, the average value of third class region (52.28 ±10. 53 ) was obviously higher than that of first class region (50. 64 ±- 10. 17)and second class region (51.53 ± 10.28 ) (P<0. 05 ). For the Dit dimension, the average value of third class region (52.83 ± 11.03 ) was obviously higher than that of first class region (50. 56 ± 10. 56 ) and second class region (51.80 ± 10. 81 ) (P <0.05 ). The average value of Set dimension of second class region (51.81 ± 10.72)and third class region (52.44±- 10.94) was evidently higher than that of first class region (49.90 ± 10.76 ) (P < 0. 05 ). While through the administrative level division of the state, the percent of pass was apparently higher in city than in country for digital searching and words reasoning; Set dimension was distinctly higher in country ( 52.30± 10. 85 ) than in city (51.07 ±10.90)(P<0.05). Conclusion The GDP per capita clustering method can better reflect the regional economy on teenagers psychological characteristics influence.
6.Protective effect of blood-activating and stasis-resolving medicines against cerebral ischemia-reperfusion injury in rats: A controlled trial to verify the time-effect and dose-effect relation
Suping ZHANG ; Rui HE ; Muzhen WANG ; Wanqing DENG ; Ruihua LIANG ; Jinghua LIN
Chinese Journal of Tissue Engineering Research 2005;9(25):226-229
BACKGROUND: The injury of blood-brain barrier following cerebral ischemia reperfusion is a considerate pathological basis for injury caused by cerebral ischemia and reperfusion.OBJECTIVE: To investigate the effects of four most basic Chinese medicinal herbs, or safflower, peach seed, ligusticum and red peony with actions of activating blood and resolving the stasis on the contents of nitric oxide, immunoglobulins, C-reactive protein (CRP) and complements (immunological indices) of serum and cerebral homogenate, as well as the morphological and structural changes of cerebral tissue cells in rats with ischemia and reperfusion to vertify relationship between time effectiveness and quantitative effectiveness.DESIGN: A randomized controlled study, and evaluation by single blind.MATERIALS: The experiment was completed in the Laboratory of Traumatology Institute of Guangzhou Red Cross Hospital from January 2001 to De cember 2002. Safflower, peach seed, szechwan lovge rhizome and red peony are concentrated granules of single decocting pieces, the blood activating and stasis resolving decoction was prepared at 2.5 g/L according to 1:1:1:2 ratio.Totally 138 adult female SD rats were selected for the experiment,weighing 280-300 g, provided by Animal Center of Guangzhou University of TCM.INTERVENTIONS:The models rats with middle cerebral artery occlusion were set up by thread ligation(24 hours reperfusion after 2 hours middle cerebral artery occlusion).All 138 rats were randomly divided into 6 groups with 23 in each group.Sham operation group:The vessels were ligated but the middle cerebral artery was not occluded.No.1 medicated group: The BASR was by gavage given in a dose of 2 g/kg 30 minutes before operation. No. 2 medicated group: The BASR was by garage given in a dose of 2.5 g/kg 30 minutes before operation. No. 3 medicated group: The BASR was by garage given in a dose of 2 g/kg for consecutive 7 days be fore operation. No. 4 medicated group: The BASR was by gavage given in a dose of 2.5 g/kg for consecutive 7 days before operation.Control group:the same volume of saline was by gavage given for consecutive 7 days before operation. ① Scoring of dysneuria (5-score system: 0-1 score meant mild dysneuria, 2-4 scores meant severe dysneuria) for all rats were performed after consciousness following 2 hours ischemia and 24 hours reperfusion.② After 24 hours reperfusion,10 rats in each group were at random selected for assay of levels of CRP, complement 3 (C3) and complement 4 (C4) (rate nephelometry), and concentration of nitric oxide (nitrate reductase method)in both cerebral homogenate and serum.③ After 24hours reperfusion, 10 rats in each group were at random selected, and after anesthesia was completed, the brain was quickly collected through decapitation, put into a 110 ℃ drying oven till its constant weight, then the water content in brain was calculated.④ The cerebral cytomorphology in every group was observed under light microscope. ⑤ After reperfusion, 3 rats in each group were randomly selected for preparation of coronal section of cerebral tissue,the cerebral ultrastructure in each group was observed under transmission electronic microscope.MAIN OUTCOME MEASURES: ① The results of dysneuria scoring in each group. ② The levels of CRP, C3 and C4, and concentration of nitric oxide in both cerebral homogenate and serum.③ The water content in brain. ④ The cerebral cytomorphology and the cerebral ultrastructure. RESULTS: All 138 rats entered into the result analysis. ① Comparison of the extents of dysneuria of rats in each group: The ratio of severe dysneuria after 24 hours ischemic reperfusion in all medicated groups was obviously lower than that in control group(P < 0.01),and the ratio in No.4 medicated group was lower than that in No.2 medicated group(P < 0.05).② Comparison of water contents in brain of rats in each group:The water contents in sham operation group and all medicated groups were obviously lower than that in control group (P < 0.05). ③ Comparison of the nitric oxide concentration in cerebral homogenate of rats in each group: The concentration in sham operation group and all medicated groups were obviously lower than that in control group (P < 0.01). The concentration in No. 3medicated group was obviously lower than that in No. 1 medicated group (P < 0.05).The concentration in No.4 medicated group was obviously lower than that in No. 2 medicated group (P < 0.01). ④ Comparison of the nitric oxide concentration in serum of rats in each group:The concentrations in sham operation group and all medicated groups were obviously lower than that in control group(P < 0.01).The concentration in No.3 medicated group was higher than that in No. 1 medicated group (P < 0.05). The concentration in No. 4 medicated group was higher than those in No. 2 and in No. 3 medicated groups (P < 0.05). ⑤ Comparison of the levels of CRP in cerebral homogenate and serum of rats in each group: The levels in sham operation group and all medicated groups were lower than that in control group(P < 0.05-0.01).The level in No.3 medicated group was lower than that in No. 1 medicated group (P < 0.01). The level in No. 4 medicated group was lower than those in No. 2 and in No. 3 medicated groups (P <0.05-0.01).⑥ Comparison of the levels of C3 in cerebral homogenate and serum of rats in each group:The levels in sham operation group and all medicated groups were lower than that in control group (P < 0.05-0.01). The level in No.3 medicated group was lower than that in No.1 medicated group (P < 0.05). The level in No. 4 medicated group was lower than those in No. 2 and in No. 3 medicated groups (P < 0.01). ⑦ Comparison of the levels of C 4 in cerebral homogenate and serum of rats in each group:The levels in sham operation group and all medicated groups were lower than that in control group (P < 0.05-0.01). The level in No. 3 medicated group was lower than that in No. 1 medicated group (P < 0.05). The level in No.4 medicated group was lower than those in No. 2 and in No. 3 medicated groups (P < 0.01). ⑧ Comparison of the condition of cerebral edema of rats in each group:In control group there was obvious cerebral congestive edema,indicating an obvious infection;while in medicated groups the extent of cerebral edema was milder than that in control group.⑨ Changes of cerebral ultrastructure of rats in each group:The ultrastructure in sham group was normal. In control group, there obvious edema of cells, capillaries and sheaths in the marginal zone of cortex necrosis,and reduction of organelles of neuron. As well. In No. 3 and No. 4 medicated groups, the limits of cell membranes were clear, the structure was integral, the chondriosomes were rich and even in size,the medullated fibers were morphologically normal.And in No.1 and No.2 medicated groups the changes were between the twoCONCLUSION:① The scoring of dysneuria in rats was decreased after the blood-activating and stasis-resolving medicine was given,and it was lower in rats that were given a longer period of medication,indicating that the improved extent for dysneuria is related to prolonged medication.②The nitric oxide concentration of cerebral tissue in rats that recevied the blood-activating and stasis-resolving medicine was decreased, and the nitric oxide concentration of serum in the rats was increased,indicating that the blood-activating and stasis-resolving medicine can reverse the anomalies of nitric concentration in different tissues after ischemic reperfusion so as to reduce cerebralinjury.③ The levels of C3 and C4 of cerebral tissue and serum in rats that received the blood-activating andstasis-resolving medicine were obviously decreased,indicating that the medicine may reduce the cerebral injury through triggering complement system;and the CRP was also get decreased,further suggesting that the medicine can inhibiting infective reaction.④ The longer the period of medication,the milder the cerebral injury, and the dose of 2.5 g/L was better in effect.
7.Graded and time effects of huoxue huayu tang on anti-injury of cerebral ischemic reperfusion in rats
Rui HE ; Suping ZHANG ; Muzhen WANG ; Wanqing DENG ; Ruihua LIANG ; Jinghua LIN
Chinese Journal of Tissue Engineering Research 2005;9(25):196-199
BACKGROUND: It has been known that re-recovery of blood flow after cerebral ischema may aggravate brain injury. It has been verified in some researches that the components for activating blood circulation and removing stasis in Chinese herbs can resist cerebral ischemic reperfusion injury.OBJECTIVE: To observe 4 most basic Chinese herbs for activating blood circulation and resolving stasis [honghua (Flos Carthami), taoren (Semen Persicase), chuanxiong (Rhizoma ligustici Chuanxiong) and chishao (Radix Paeoniae Rubra)] as the exertive factors on their influences on immune index changes in IgG, C-reactive protein (CRP) and complements of serum and homogenate in brain tissue so as to verify their graded and time effects.DESIGN: Randomized control experiment and single blind method.SETTING: Guangzhou Red Cross Hospital and Department of Neurology of the Fourth Hospital Affiliated to Jina University.MATERIALS: The experiment was performed from January 2001 to Decemb er 2002 in Experimental Room of Traumatic Institute of Guangzhou Red Cross Hospital. Totally 138 SD female adult rats were employed, mass weighted varied from 280 to 300 g, provided from Experimental Animal Center of Guangzhou University of Chinese Medicine. Honghua (Flos Carthami), taoren (Semen Persicase), chuanxiong (Rhizoma ligustici Chuanxiong)and chishao (Radix Paeoniae Rubra)] were the concentrated granules individually. At the ratio of 1:1:1:2, they were prepared into 2.5 g/mL raw herbal decoction (huoxue huayu tang).INTERVENTIONS: Thread embolic method was used to prepare cerebral medium sized artery obstruction model in rats (reperfusion for 24 hours after cerebral medium sized artery obstruction for 2 hours). Totally 138 rats were randomized into 6 groups, 23 rats in each. Sham operation group: ligature was done in each vessel without blocking medium sized artery of cerebrum.First perfusion group: 30 minutes before operation, gastric peffusion was done with 2 g/kg huoxue huayu tang. Second peffusion group: 30 minutes before operation, gastric perfusion was done with 2.5 g/kg huoxue huayu tang. Third perfusion group: before operation, gastric perfusion was done with 2 g/kg huoxue huayu tang continuously for 7 days. Fourth perfusion group: before operation, gastric perfusion was done with 2.5 g/kg huoxue huayu tang continuously for 7 days. In the control, physiological saline of all of the groups, when rats woke up, after 24 hours reperfusion and 2 hours ischemia, neural functional deficits were evaluated (5-score system, 0-1:After 24 hours reperfusion, 10 rats were randomized from each group for determination of the contents of CRP in homogenate and serum, complehours reperfusion, 10 rats were randomized from each group. After anesthetized, they were sacrificed rapidly to collect brains. Dried over heat in oven at 110℃ till constant weight, the water content of brain tissue was domized from each group to observe ultrastructure of brain tissue under transmission electron microscope (TEM) of rats in each group.and homogenate, complement C3 and C4 as well as serum IgG in rats of of severe neural functional deficits after 24 hours ischemic reperfusion in rats of each peffusion group was lower remarkably than the control (P < 0.01),in which, that in fourth peffusion group was lower than second group (13%,group and each perfusion group was lower than the control (P < 0.05), in which, that in third peffusion group was lower than first group (P < 0.01).ment C3: That in sham operation group and each perfusion group was lower sham operation group and each perfusion group was lower than the control ( P < 0.01), in which, that in third perfusion group was lower than first group (P < 0.01); That in fourth perfusion group was lower than second and group and each perfusion group was lower than the control (P < 0.01), in which, that in fourth perfusion group was lower than second group(P < 0.05).each perfusion group was lower than the control (t=5.626-17.929, P < 0.01),in which, that in third perfusion group was lower than first group (P < 0.01),complement C3 in brain homogenate: That in sham operation group and each perfusion group was lower than the control (P < 0.05-0.01), in which, third perfusion group was lower than first group (P < 0.01), that in fourth group brain homogenate: That in sham operation group and each perfusion group was lower than the control ( P< 0.05-0.01), in which, that in third perfusion group was lower than first group (P < 0.01), that in fourth group was lower tissue: The inflammatory reaction in the control was obvious. Brain edema and pathological damage in perfusion groups were milder than the control.Ulztrastructure was normal in sham operation group. The edema was obvious in cells, capillaries and myelin sheath in cortical necrosis margin area and neuronal cell organs were decreased in the control. In third and fourth peffusion groups, cellular membrane was clear in boundary line,integrative in structure, rich in mitochondria and even in size and the morphology of medullated fibers was normal. The situation of first and second perfusion was between two of them.deficits in the evaluation of rats and the score with long medication was lower, suggesting that long medication can even better improve neural funcplement C3 and C4 in brain bomogenate and serum and decreases serum IgG content, explaining that the medicine alleviates brain tissue injury by startup complement system. The remarkable decrease of C-reactive protein further suggests the inhibition of such medicine on inflammatory reaction.jury is, and the better result is achieved at dosage of 2.5 g/L.
8.SYNTHESIS OF TRIPHENYLETHYLENE WITH ALIPHATIC CYCLIC MOIETY AND ITS ANTAGONISM ON ESTROGEN RECEPTOR
Bailing XU ; Zongru GUO ; Xiaotian LIANG ; Fengming CHU ; Naigong WANG ; Muzhen GUAN
Acta Pharmaceutica Sinica 2001;36(3):179-184
AIM In order to improve the biological activity and reduce the side effects and toxicity, a series of novel estrogen receptor antagonists were designed. METHODS The key triphenylethylene intermediates were obtained by the McMurry reaction. The target compounds were prepared by etherification. The binding affinities of the target compounds for the estrogen receptor in rat uterine cytosol were measured by a competitive binding assay and their estrogen agonistic/antagonistic properties were investigated in the 3-day uterine weight assay in the immature rats. RESULTS Thirty-five new compounds have been synthesized and their geometric configuration were determined by X-ray crystallography and 1HNMR spectral data. CONCLUSION All of the test compounds showed affinity for the estrogen receptor (IC50<10-6 mol.L-1), especially compound 35 with IC50 1.07×10-8 mol.L-1. Some compounds are antagonists, inhibiting uterus growth; others are agonists, promoting uterus growth. Compounds 14 and 27 are superior antagonists to tamoxifen.
9.Synthesis and profiling of [3H]trantinterol excretion following oral administration of rats
Tianhong ZHANG ; Cheng ZHANG ; Cuiping YANG ; Xiaoying WANG ; Sha LIAO ; Muzhen SUN ; Jinglai LI ; Zhenqing ZHANG
Chinese Journal of Pharmacology and Toxicology 2015;(5):785-792
OBJECTIVE To synthesize[3H]labelled trantinterol and determine the mass balance in rats and the profile of trantinterol and its metabolites in excreta. METHODS [3H]Trantinterol was synthesised from the intermediate1-(4-amino-3-chloro-5-trifluoromethyl-phenyl)-2-bromo-ethanone through reduction by sodium borotritide and aminolysis by t-butylamine. Following an oral dose of[3H] trantinterol(45.5 MBq·kg-1)to bile duct cannulated(BDC)rats and normal rats. Bile,urine and faeces were collected individually before and after dosing at different times. Liquid scintillation counter(LSC) was used to detect total radioactivity recovery and HPLC/radio-detector for metabolite profiling in urine and bile. RESULTS The majority(73.6%)of the administered radioactivity was recovered in the first 24 h postdose with 48.3%in urine and 25.4%in faeces. It was cumulated to(84.7±6.8)%till 168 h. In BDC rats,29.3%of the dose was recovered in the bile 3 d post-dose. According to the peak area ratio determined by HPLC/radio-detector,only 4.7%and 9.5%of the radioactive dose were excreted as the parent drug in urine and bile,respectively,while the majority of the remaining radioactivity was excreted in the form of various metabolites. CONCLUSION Following oral administration in rats,trantinterol is completely absorbed,extensively metabolized and rapidly excreted mainly in urine as various metabolites.
10.PGE1 alleviates cognitive impairment and upregulates the VEGF and BDNF expression in VD rats
Boliu HUI ; Zhang SUPING ; Ling LI ; Xiong XIFENG ; Wang MUZHEN ; He RUI ; Deng WANQING
Chinese Journal of Nervous and Mental Diseases 2015;(8):471-476
Objective To explore the effect of PGE1 on the cognitive impairment and the expression of VEGF and BDNF in the hippocampus after bilateral common carotid artery occlusion in adult rats. Methods Forty-eight rats were randomly divided into PGE1 group (10μg·kg-1·d-1, iv), PGE1+VEGFR antagonist group (PGE1, 10μg·kg-1·d-1, iv;SU5416, 25 mg·kg-1·d-1, ip), saline group and sham group (n=12 each). Morris Water Maze test (MWM) was used to examine cognitive function in rats. Drugs and saline were given to VD rats at 24 d for 7 consecutive days following opera?tion. Half of the rats in each group were sacrificed for Western Blot at 6 days after MWM test. Western Blot was conduct?ed to examine the relative expression levels of VEGF and BDNF in the hippocampus. Results Compared to saline and PGE1+VEGFR antagonist groups, the escape latency in PGE1 group was shorter (P<0.05), and the times that rats swam across the platform location and time percentage in previous platform quadrant in PGE1 group was longer (5.77±0.83 vs.2.88 ± 0.47 vs. 2.63 ± 0.44, P<0.01;32.28%± 4.56%vs. 20.42%± 5.50%, 23.08%± 5.06%, P<0.05). Compared with saline group and sham group, PGE1 group had higher levels of VEGF (0.057±0.005 vs. 0.038±0.002 vs. 0.027±0.002, P<0.05) and BDNF (0.481±0.049 vs. 0.339±0.021 vs. 0.224±0.04, P<0.05). but the increase in VEGF expression in PGE1 group was no significant (0.057±0.005 vs. 0.053±0.003, P>0.05) compared with PGE1+VEGFR antagonist group, while the aug?ment of BDNF in PGE1 group was remarkable (0.481±0.049 vs. 0.373±0.034, P<0.05). Conclusions PGE1 can upregu?late VEGF and BDNF expression and modify cognitive impairment in VD rats, while the effects of PGE1 on cognitive function and BDNF expression can be partially blocked by VEGFR antagonist SU5416.