2.Design, synthesis and cholinesterase inhibitory activity of quinoline-polyamine conjugates.
Wen LUO ; Kai HUANG ; Zhen ZHANG ; Chen HONG ; Chaojie WANG
Acta Pharmaceutica Sinica 2013;48(2):269-75
A series of quinoline-polyamine conjugates (8a-8n) were designed, synthesized and evaluated as inhibitors of cholinesterases (ChEs). Some of these compounds had potent ChEs inhibitory activity with IC50 values at micromolar range. Compound 8n exhibited the strongest inhibition on acetylcholinesterase (AChE) with an IC50 value of 8.78 micromol x L(-1), and compound 8i showed the most potent inhibition on butyrylcholinesterase (BChE) with IC50 value of 1.60 micromol x L(-1) which was slightly better than rivastigmine. The structure-activity relationship revealed that the chain length of polyamine and linker played important roles for inhibitory activity. Molecular modeling studies showed that 8i targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of cholinesterases.
3.The relationship between symptoms and signs of temporomandibular disorders and the patients' quality of life.
Hui-min CHEN ; Kai-yuan FU ; Zhen-kang ZHANG
Chinese Journal of Stomatology 2007;42(3):173-175
OBJECTIVETo analyze the relationship between symptoms and signs of temporomandibular disorders (TMD) and the patients' quality of life (QOL).
METHODSA total of 492 TMD patients were included in this study. The clinical examination results were recorded using Fricton index of temporomandibular joint function. "Visual analog scale (VAS) evaluation of QOL disturbance" was designed to quantitate patients' QOL, to evaluate the degree that the patients QOL was affected.
RESULTSChewing, daily life and emotion among all 8 items of QOL were frequently affected by TMD, and joint clicking had the least influence on QOL. Intermittent closed lock had more severe interference with QOL than joint clicking only. Severe and moderate pain or limited mouth opening affected the QOL more severely than mild pain or mild limited mouth opening. The simple linear relationship between Fricton index and patients' QOL was poor (r < 0.4).
CONCLUSIONSPain is the most frequently seen symptom in TMD. TMD could affect patients' QOL, including both physical and social-psychological functions. The results suggest that the patients' QOL as well as TMD symptoms and signs should be considered in the management of TMD.
Adult ; Facial Pain ; etiology ; Female ; Humans ; Male ; Quality of Life ; Temporomandibular Joint Disorders ; complications
4.A comparative study of opening the pterygopalatine arteries improved preparation of autologous blood clots in cerebral infarction model
Zhen ZHOU ; Xueyan WANG ; Kun WANG ; Kai WANG ; Yulian ZHANG
Chinese Journal of Comparative Medicine 2014;(9):62-65
Objective To open pterygopalatine artery using autologous blood clot clogged the middle cerebral artery, resulting in cerebral infarction model of middle cerebral artery in the distal blood supply area.Methods Open PPA, ligation of ECA, embolus through CCA blood flow, rushed into the MCA distal embolus, cause infarction model. According to Bederson rating score the neural function.TTC staining to determine the infarction volume.Results Comparison of two operation models, scores were increased, and white infarcted area appears.There is no significant differences detected by statistical analysis.Conclusion Open PPA manufacturing cerebral infarction model rats of autologous blood clots could shorten the operation time, reduce the mortality rate.
5.Effects of oleanolic acid on learning and memory, synaptic morphology and the expression of CREB in the hippocampus and cereberal cortex of SAMP8 mice
Kun WANG ; Yulian ZHANG ; Zhen ZHOU ; Linlin ZHANG ; Wanshan SONG ; Xueyan WANG ; Kai WANG
Chinese Journal of Behavioral Medicine and Brain Science 2015;24(6):493-496
Objective To observe the influence of oleanolic acid on the ethology of 9-month-old mice,the completeness of synapsis structure and the expression of cAMP-response element binding protein (CREB) in cortex and hippocampus.Methods Thirty 9-month-old healthy male SMAP8 mice were randomly divided into model group,oleanolic acid group and aricept group,and with 10 rats in each group,while 10 healthy male mice of the same age and species as normal group.Oleanolic acid group and aricept group were given intragastric administration with corresponding drugs,while the normal group and model group were given the same amount of physiological saline.4 weeks later,the ethology changes were observed by Morris water maze and morphology changes of hippocampus neurons were viewed by electron microscope and the expression of CREB was detected by Western Blot.Results (1)Morris water maze results suggested that compared with the normal group,the latency time in the model group mice was longer,which were ((83.33±4.96) s,(75.13±6.01) s,(71.75±7.77) s,(63.40± 8.93) s,(60.97±8.38) s),while compared with the model group,the latency time in the oleanolic acid group and the aricept group was remarkably shorter (P< 0.05),which were (75.97± 4.49) s,(64.98± 4.93) s,(64.16± 6.23) s,(53.47±5.99) s,(47.91±7.64) s and (71.30±7.65) s,(63.32±7.57) s,(59.82±4.69) s,(52.28±5.90) s,(46.22±7.27) s respectively.In the spatial probe trial,compared with tbe normal group,the crossing times of the model was less,while compared with the model one,the crossing times of the oleanolic acid group and the aricept group was more(P<0.05).(2)Compared with the normal group,the number of synapses in the model group was smaller,in which the synaptic cleft was mixed with the front of synapses severely swollen,uninform synaptic vesicles and few clear outlines of mitochondrias.While the oleanolic acid group and the aricept group had clear synapses outlines with the front of synapses slightly swollen,intensive and uniform synaptic vesicles and clear mitochondrias with their cristae not easy to be seen.(3) The Western Blot showed that compared with the normal group,there was a decline in the CREB expression both in the cortex and hippocampus in the model group,while compared with the model group,there was a rise in the oleanolic acid group as well as the aricept group(P<0.05).Conclusion Oleanolic acid can improve the learning and memorizing of model rats,which is possibly related to the increased expression of CREB protein to protect the synapses structure of model mice.
6.Progress of Engineered Saccharomyces cerevisiae of Xylose Metabolism and Fermentation for Ethanol Production
Jin-Xin ZHANG ; Shen TIAN ; Ji-Kai LIU ; Ya-Zhen ZHANG ; Xiu-Shan YANG ;
Microbiology 1992;0(04):-
With the constant rise of energy price,it has a great practical meaning of using lignocellulose to produce ethanol.Xylose is a kind of monosaccharide whose content is only less than glucose in most lignocellulosic hydrolysates.There is some difficulty of producing ethanol from lignocellulose by the traditional ethanol production strain Saccharomyces cerevisiae,because it cannot metabolize xylose.People have tried to use genetic engineering technology and cell fusion method to modify Saccharomyces cerevisiae to make it metabolize xylose and produce ethanol for many years.This review indroduced the progress in this field.
7.Preparation of rivastigmine liposome and its pharmacokinetics in rats after intranasal administration.
Zhen-Zhen YANG ; Zhan-Zhang WANG ; Kai WU ; Xian-Rong QI
Acta Pharmaceutica Sinica 2011;46(7):859-863
To prepare rivastigmine liposome, rivastigmine was loaded into liposome via ammonium sulfate gradient method. Its pharmacokinetic profile in rats was evaluated after intranasal administration. The size, zeta potential, entrapped efficiency and release of rivastigmine from the liposome in vitro were determined. Plasma concentration of rivastigmine was determined by high performance liquid chromatography-tandem mass spectrometry (HPLC/MS) using antipyrine as internal standard. The pharmacokinetic parameters were calculated by DAS 2.0. The entrapped efficiency of rivastigmine liposome was (33.41 +/- 6.58) %, with the mean diameter of 154-236 nm and zeta potential of (-10.47 +/- 2.41) mV. The release behavior of rivastigmine was fitting the first order equation in vitro. The pharmacokinetic studies indicated that the C(max), T(max) and AUC(0-infinity), of rivastigmine liposome were (1.50 +/- 0.15) mg x L(-1), 15 min and (89.06 +/- 8.30) mg x L(-') x min, respectively. Rivastimine liposome was absorbed rapidly, and could reach a certain concentration in rat plasma after intranasal delivery.
Administration, Intranasal
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Animals
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Area Under Curve
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Chromatography, Liquid
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Drug Carriers
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Drug Compounding
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Liposomes
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Male
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Neuroprotective Agents
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administration & dosage
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blood
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chemistry
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pharmacokinetics
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Particle Size
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Phenylcarbamates
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administration & dosage
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blood
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chemistry
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pharmacokinetics
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Rats
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Rats, Sprague-Dawley
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Rivastigmine
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Tandem Mass Spectrometry
9.Mechanism and process optimization of ultrafiltration of residual DNA in rabies vaccine
Ziwei LIU ; Wei ZHAO ; Huan XIONG ; Kai WANG ; Ju GUO ; Zhen LIU ; Heng ZHANG
Military Medical Sciences 2014;(12):968-971
Objective To control residual DNA by optimizing methodology during the production of rabies vaccine using Vero cells as a vector .Methods The antigen recovery rate was assessed by linked immunosorbent assay-sandwich technique while the residual DNA was detected by DNA probe hybridization method .Antigen recovery and removal of DNA were the main indexes for evaluateing ultrafiltration , the vital part of rabies vaccine production .Three key factors in ultrafiltration were assessed: selection of membrane packages , ultrafiltration pressure and the concentration ratio .Then protamine was used to pretreat ultrafiltrates .Based on the two indicators mentioned above , the effect of protamine pretreat-ment on the ultrafiltrate was evaluated .Results and Conclusion The optimum condition of ultrafiltration was obtained on the basis of the general antigen recovery rate , DNA removal rate and actual production .The primary parameters of ultrafil-tration were as follows:7.5 ×105 ultrafiltration membrane packages, 20 times concentrated, 15 psi ultrafiltration pressure. After pretreatment with protamine , ultrafiltration has proved to be a molecular sieve in intercepting DNA ,while protamine can tangle the fragmented DNA and form a larger molecular segment , which is believed to be more conducive to ultrafiltra-tion interception .
10.Comparison of the Work Before and After the JCI Clinical Care Program Certification-Acute Myocardial Infarction
Yulai WANG ; Jin YU ; Zhen LU ; Yongbo WU ; Kai ZHANG ; Xiaoyun WENG
Herald of Medicine 2017;36(7):813-817
Objective To analyze the effect of clinical pharmacists involving in JCI clinical care program certification-AMI(CCPC-AMI) on the compliance rates of clinical drug treatment guideline and the awareness rates of patient medication health education in cardiovascular.Methods Selected cases of acute myocardial infarction(AMI) from March to August in 2015 was as the former group,from September 2015 to March 2016 as the latter group in their hospital,then comparative analysis of two groups was done by statistical method.Results After clinical pharmacists involved in CCPC-AMI,the compliance rates of AMI clinical drug treatment guidelines (after the AMI diagnosis, the 10min was given aspirin, intensified statin therapy and dose selection, the use of ACEI/ARB before discharge and the use of beta blocker before discharge) were increased from 92.7% 67.9%,60.7%,51.8% to 98.1%,85.2%,94.4%,90.7%.The awareness rates of patient medication health education (awareness of safe medication, awareness of self-management, awareness of follow-up knowledge) were all increased to 100% from 75.0%,57.1%,82.1% before participation.Conclusion Clinical pharmacists who carried out pharmaceutical care,has played a critical role in quality control of AMI single disease through the preparing of CCPC-AMI evaluation.