目的:探究血清胆碱酯酶(Cholinesterase,ChE)、白细胞介素-6(Interleukin-6,IL-6)、血清尿素氮与肌酐比值(Urea-creatinine ratio,UCR)联合序贯器官衰竭(Sequential organ failure assessment,SOFA)评分预测重症肺炎患者病情与预后的价...目的:探究血清胆碱酯酶(Cholinesterase,ChE)、白细胞介素-6(Interleukin-6,IL-6)、血清尿素氮与肌酐比值(Urea-creatinine ratio,UCR)联合序贯器官衰竭(Sequential organ failure assessment,SOFA)评分预测重症肺炎患者病情与预后的价值。方法:选取2021年1月至2024年6月期间,安福县人民医院收治的60例重症肺炎患者作为研究对象(研究组),根据患者预后情况,将其分为死亡组(n=15)及存活组(n=45),取同期30例普通肺炎患者作为对照组,两组均接受常规治疗,对比分析两组患者的SOFA及血清ChE、IL-6、UCR等临床指标的差异。采用受试者工作特征(Receiver operation characteristic curve,ROC)曲线分析血清ChE、IL-6、UCR联合SOFA评分对重症肺炎患者预后的预测价值。结果:研究组患者的血清ChE水平低于对照组,IL-6、UCR水平及SOFA评分均高于对照组(P<0.05);研究组患者中,死亡组患者的血清ChE水平低于存活组,IL-6、UCR水平及SOFA评分均高于存活组(P<0.05);ROC曲线分析显示,重症肺炎血清ChE、IL-6、UCR、SOFA评分用于评估重症肺炎患者预后的曲线下面积(Area under the curve,AUC)分别为0.748、0.763、0.816、0.724,敏感度分别为66.67%、66.67%、68.89%、59.89%,特异度分别为60.00%、73.33%、73.33%、60.00%,四者联合的AUC、敏感度、特异度值分别是0.923、86.67%、60.00%。结论:血清ChE、IL-6、UCR水平与SOFA评分联合应用对重症肺炎患者病情与预后的预测能力价值较高。展开更多
AIM: To understand the correlation of serum cholinesterase (CHE) activity with gastric cancer and to assess their clinical significance.METHODS: The velocity method was adopted to detect the activity of serum CHE in p...AIM: To understand the correlation of serum cholinesterase (CHE) activity with gastric cancer and to assess their clinical significance.METHODS: The velocity method was adopted to detect the activity of serum CHE in patients with gastric cancer and in patients with non-malignant tumor as controls.RESULTS: The serum CHE activity in the treatment group was significantly lower than that in the control group with a very significant difference between the two groups (83.3:113.1,P = 0.0003). Age was significantly associated with the incidence of gastric caner.CONCLUSION: Serum CHE activity has a close relation with the incidence of gastric cancer.展开更多
To determine the predictive performance of cholinesterase compared to existing prognostic models in evaluating liver function in patients with chronic hepatitis D. METHODSIn an observational, cross-sectional and retro...To determine the predictive performance of cholinesterase compared to existing prognostic models in evaluating liver function in patients with chronic hepatitis D. METHODSIn an observational, cross-sectional and retrospective study, consecutive patients with hepatitis D cirrhosis were evaluated. Demographic, clinical and laboratory parameters were recorded. Serum cholinesterase levels were correlated with existing scoring models for chronic liver disease and Liver function tests. Receiver operating characteristic (ROC) curves were constructed to find an optimal cholinesterase level predicting ascites, Child Turcotte Pugh (CTP) score ≥ 10, model for end stage liver disease (MELD) score ≥ 15, baseline-event-anticipation (BEA) score for hepatitis D ≥ 5 and the aspartate transaminase to Platelet Ratio Index (APRI) ≥ 1.5. RESULTSThis study investigated 233 patients with chronic liver disease due to hepatitis D; 192 were male, median age 42 (16-69 years). Fifty patients had ascites and 15 had encephalopathy. One hundred and sixty-seven (71.7%) were in Child class A, 52 (22.3%) in Child class B and 14 (5.0%) in class C. A MELD score of 15 or more was seen in 24 patients. Cholinesterase levels correlated well with the INR, albumin, CTP score, MELD, MELD sodium, BEA and APRI scores (P < 0.001 each). Area under the ROC curve for ascites, CTP ≥ 10, MELD ≥ 15, BEA ≥ 5, APRI ≥ 1.5 was 0.836, 0.966, 0.913, 0.871 and 0.825 respectively (P < 0.001 each). Cut off values of cholinesterase (IU/L) for predicting ascites, CTP ≥ 10, MELD ≥ 15, BEA ≥ 5 and APRI ≥ 1.5 were < 3812, < 2853, < 2829, < 4719 and < 3954 with a sensitivity of 80%, 100%, 91.67%, 82.50%, 58.0% and specificity of 81.97%, 84.79%, 87.56%, 77.06% and 55.64% respectively. CONCLUSIONSerum cholinesterase demonstrates promising correlations with serum albumin, INR and CTP, MELD, BEA and APRI scores and is predictive of liver reserves in hepatitis D cirrhosis.展开更多
AIM To examine whether nizatidine stimulates duodenal HCO_3^- secretion in rats by inhibiting AChE activity. METHODS Under pentobarbital anesthesia,a proximal duodenal loop was perfused with saline,and the HCO_3 secre...AIM To examine whether nizatidine stimulates duodenal HCO_3^- secretion in rats by inhibiting AChE activity. METHODS Under pentobarbital anesthesia,a proximal duodenal loop was perfused with saline,and the HCO_3 secretion was measured at pH 7.0 using a pH-stat method and by adding 10mM HCI.Nizatidine,neostigmine,carbachol or famotidine was administered i.v.as a single injection. RESULTS Intravenous administration of nizatidine(3-30 mg/kg)dose-dependently increased duodenal HCO_3^- secretion,and the effect at 10mg/kg was equivalent to that obtained by carbachol at 0.01 mg/kg.This nizatidine action was observed at the same dose range that inhibited acid secretion and enhanced gastric motility,mimicked by i.v.injection of neostigmine(0.03 mg/kg),and significantly attenuated by bilateral vagotomy and prior s.c. administration of atropine but not by indomethacin,a cyclooxygenase inhibitor,or N^G-nitro-L-arginine methyl ester,a NO synthase inhibitor.The HCO_3^- secretory response to acetylcholine(0.001 mg/kg)was significantly potentiated by the concurrent administration of nizatidine(3mg/kg,i.v.).The IC_(50)of nizatidine for AChE of rat erythrocytes was 1.4×10^(-6)M,about 12 times higher than that of neostigmine.Neither famotidine(>10^(-3)M, 30mg/kg,i.v.)nor cisapride(> 10^(-3)M, 3mg/kg,i.v.)had any influence on AChE activity or duodenal HCO_3^- secretion.Duodenal damage induced by acid perfusion(100 mM HCI for 4 h)in the presence of indomethacin was significantly prevented by nizatidine and neostigmine,at the doses that increased the HCO_3^- secretion. CONCLUSION Nizatidine stimulates duodenal HCO_3^- secretion,in both vagal-dependent and atropine-sensitive manners,and the action is associated with the anti-AChE activity of this agent.展开更多
The results confirmed that diazepam inhibits the cholinesterase in rat serum,red cell,corpus striatum and diaphragm in vitro,that the higher the diazepam concentration,the stronger the cholinesterase inhibition,and th...The results confirmed that diazepam inhibits the cholinesterase in rat serum,red cell,corpus striatum and diaphragm in vitro,that the higher the diazepam concentration,the stronger the cholinesterase inhibition,and that diazepam is a reversible inhibitor to acetylcholinesterase and diazepam has a stabilizing action on red cell membranes.The role of these effects of diazepam in the treatment of organic phosphate poisoning is discussed展开更多
Objective:To investigate the effect of Cannabis sativa resin and/or tramadol,two commonly drugs of abuse on acetylcholinesterase and butyrylcholinesterase activities as a possible cholinergic biomarkers of neurotoxici...Objective:To investigate the effect of Cannabis sativa resin and/or tramadol,two commonly drugs of abuse on acetylcholinesterase and butyrylcholinesterase activities as a possible cholinergic biomarkers of neurotoxicity induced by these agents.Methods:rats were treated with cannabis resin(5,10 or 20 mg/kg)(equivalent to the active constituent A'-tetrahydrocannabinol),tramadol(5,10 and 20 mg/kg) or tramadol(10 mg/kg)combined with cannabis resin(5,10 and 20 mg/kg) subcutaneously daily for 6 weeks.Acetylcholinesterase(AChE) and butyrylcholinesterase(BChE) activities were measured in brain and serum.We also measured the activity of paraoxonase-1(PONl) in serum of rats treated with these agents.Results:(i) AChE activity in brain increased after 10-20 mg/kg cannabis resin(by 16.3%-36.5%).AChE activity in brain did not change after treatment with 5-20 mg/kg tramadol.The administration of both cannabis resin(5,10 or 20 mg/kg) and tramadol(10 mg/kg) resulted in decreased brain AChE activity by 14.1%,12.9%and 13.6%,respectively;(ii) BChE activity in serum was markedly and dose-dependenlly inhibited by cannabis resin(by 60.9%-76.9%).BChE activity also decreased by 17.6%-36.5%by 10-20mg/kg tramadol and by 57.2%-63.9%by the cannabis resin/tramadol combined treatment;(iii)Cannabis resin at dose of 20 mg/kg increased serum PONl activity by 25.7%.In contrast,tramadol given at 5,10 and 20 mg/kg resulted in a dose-dependent decrease in serum PON1 activity by 19%,36.7%,and 46.1%,respectively.Meanwhile,treatment with cannabis resin plus tramadol resulted in 40.2%,35.8%,30.7%inhibition of PONl activity compared to the saline group.Conclusions:these data suggest that cannabis resin exerts different effects on AChE and BChE activities which could contribute to the memory problems and the decline in cognitive function in chronic users.展开更多
The density functional theory at the B3LYP/6-311G（d, p） level was applied to exploring the inhibition mechanism of cholinesterases by carbamate. The results indicate that the inhibition reactions with or without the...The density functional theory at the B3LYP/6-311G（d, p） level was applied to exploring the inhibition mechanism of cholinesterases by carbamate. The results indicate that the inhibition reactions with or without the catalytic effect of the catalytic triad in eholinesterases underwent a two-step addition-elimination mechanism, which is in good agreement with the proposed mechanism. The solvent has a strong effect on the inhibition reactions and the reaction with the catalytic triad in the solvent phase is close to the real reaction under biological condition.展开更多
Objective:To explore cholinesterase inhibitory and antioxidant effect of six coniferous trees(Abies bornmulleriana,Picea pungens,Juniperus communis,Cedrus libani,Taxus baccata,and Cupressus sempervirens var.horizantal...Objective:To explore cholinesterase inhibitory and antioxidant effect of six coniferous trees(Abies bornmulleriana,Picea pungens,Juniperus communis,Cedrus libani,Taxus baccata,and Cupressus sempervirens var.horizantalis).Methods:Acetone(Ace),ethyl acetate(EtOAc),and ethanol(EtOH)extracts prepared from the needles and shoots of the six coniferous trees were screened for their acetylcholinesterase(AChE)and butyrylcholinesterasc(BChE)inhibitory activity at 100μg/mL.Antioxidant activity of the extracts was tested using 2,2-diphenyl-1-picrylhydrazyl(DPPH)and N,N-dimethyl-p-phenylendiamine(DMPD)radical scavenging,nietal-chelation capacity,ferric-(FRAP)and phosphomolibdenum-reducing antioxidant power(PRAP)assays.All of the assays were performed in ELISA microplate reader.Total phenol and flavonoid amounts in the extracts were determined spectrophotometrically.Results:Among thirty-six extracts in total,the shoot-Ace extract of Cupressus sempervirens var.horizantalis exerted the highest inhibition against AChE[(54.84±2.51)%],while the needle-Ace extract of Cedrus libani was the most effective in inhibiting BChE[(67.54±0.30)%].The highest DPPH radical scavenging effect,FRAP and PRAP was observed in the shoot-Ace and EtOAc extracts from Taxus baccata.whereas all the extracts showed a variable degree of scavenging effect against DPMD radical.The shoot-EtOAc extract of Cedrus libani had the highest metalchelation capacity[(58.04±0.70)%].The shoot extracts of Taxus baccata were determined to have the richest total phenol content,which may contribute to its marked antioxidant activity.Conclusions:The conifer species screened in this study may contain cholinesterase-inhibiting and antioxidant properties,which might be useful against Alzheimer's disease.展开更多
Acetylcholine is an essential neurotransmitter found throughout the nervous system. Its action on postsynaptic receptors is regulated through hydrolysis by various carboxylesterases, especially cholinesterases (ChEs)....Acetylcholine is an essential neurotransmitter found throughout the nervous system. Its action on postsynaptic receptors is regulated through hydrolysis by various carboxylesterases, especially cholinesterases (ChEs). The acute toxicity of organophosphate (OP) compounds is directly linked to their action as inhibitors of ChE. One widely used assay for evaluating ChE activity is a spectrophotometric method developed by Ellman et al. When the enzyme source is from tissues or, in particular, blood, hemoglobin displays a spectrophotometric peak at the same wave-length used to analyze cholinergic activity. This creates a substantial background that interferes with the Ellman’s assay and must be overcome in order to accurately monitor cholinesterase activity. Herein, we directly compare blood processing methods: classical method (1.67 ± 0.30 U/mL) and HemogloBindTM treatment (1.51 ± 0.17 U/mL), and clearly demonstrate that pretreatment of blood samples with HemoglobindTM is both a sufficient and rapid sample preparation method for the assessment of ChE activity using the Ellman’s method.展开更多
Cholinergic dysfunction is common to Alzheimer’s dementia and Schizophrenia. The objective of this study is to undertake a systematic review and meta-analysis of the literature on the cognitive and clinical effects o...Cholinergic dysfunction is common to Alzheimer’s dementia and Schizophrenia. The objective of this study is to undertake a systematic review and meta-analysis of the literature on the cognitive and clinical effects of cholinesterase inhibitors administered to patients with schizophrenia and co-morbid Alzheimer’s disease dementia. A literature search of the MEDLINE, CINAHL, PubMed, PsycINFO, EMBASE, AMED, BNI, HMIC and Health Business Elite databases has been performed (up to January 2013) to investigate the use of cholinesterase inhibitors in patients with schizophrenia and dementia. The terms “schizophrenia”, “dementia”, “rivastigmine”, “donepezil”, “galantamine” and “cognitive deficit” have been searched, with a restriction for English language. Five published studies including 1 RCT have been included for the qualitative review. Treatments include Donepezil 5 mg and 10 mg as well as Rivastigmine 9 mg. The numbers of participants vary from 2 incase report to20 inthe RCT. Only 1 study qualifies for meta-analysis. There is a very limited evidence on the efficacy and safety of using acetylcholinesterase inhibitors in the management of dementia co-morbid with schizophrenia. The only randomised controlled study shows lack of evidence in terms of efficacy in using cholinesterase inhibitors in the management of dementia with schizophrenia. Future research projects will have to look at an adequate sample size to explore treatment on various cognitive and noncognitive domains and the sample should be selected by using definitive and internationally acceptable diagnostic criteria.展开更多
Introduction: Dementia is frequently associated with Parkinson’s disease, especially in later stages. Efficacy of cholinesterase inhibitors (ChI) in Alzheimer’s dementia is well established. However, treatment with ...Introduction: Dementia is frequently associated with Parkinson’s disease, especially in later stages. Efficacy of cholinesterase inhibitors (ChI) in Alzheimer’s dementia is well established. However, treatment with ChI in Parkinson’s disease dementia (PDD) remains controversial. The objective of this systematic review and meta-analysis was to assess the effects of ChI in PDD. Methods: A comprehensive literature search was performed in MEDLINE, EMBASE and Cochrane library up to March 2014 using the descriptors “Parkinson’s disease”, “dementia in Parkinson’s disease”, “cognition”, “acetylcholinesterase inhibitors”, “cholinesterase inhibitors”, “anticholinesterase agents”, “rivastigmine”, “donepezil” and “galantamine” (Pubmed search strategy). All randomized, doubleblinded, placebo-controlled trials that met the eligibility criteria and assessed the effects of ChI in PDD were considered for analysis. There were no restrictions regarding paper language. Summary effect-sizes were presented as standardized mean differences (SMD) and the pooled analysis was performed with a fixed-effects model. Outcomes considered for analysis were the Mini Mental Status Exam (MMSE) score and the cognition scale for evaluation of dementia ADAS-Cog. The degree of heterogeneity between included studies was assessed through the I2 test. Results: After a comprehensive search, 175 references were retrieved. From these, five randomized trials involving 946PDD subjects were included in the review. Four studies used donepezil and only one study used rivastigmine. The pooled analysis of five studies that assessed the effects of ChI in MMSE total score showed a SMD of 0.24 (CI 95% 0.11 - 0.38). Three studies considered the effects of ChI on Adas-Cog and the pooled results showed a SMD of 0.21 (CI 95% 0.07 - 0.35). There was no significant heterogeneity between the studies. Conclusions: The results of this systematic review and meta- analysis suggest that ChI improves cognitive impairment in PDD subjects. Despite statistically significant, the translation of these results into relevant clinical improvement should be taken with caution, as the studies did not address what would be considered a clinically significant result.展开更多
Two novel naphthol derivatives（1 and 2） were synthesized and characterized via IR,~1H NMR,and HRMS.The structure of compound 2 was verified by single-crystal X-ray crystallography.It crystallizes in monoclinic,space...Two novel naphthol derivatives（1 and 2） were synthesized and characterized via IR,~1H NMR,and HRMS.The structure of compound 2 was verified by single-crystal X-ray crystallography.It crystallizes in monoclinic,space group C2/c with a = 21.6725（9）,b = 6.0127（3）,c = 25.5405（14） A,β = 94.716（5）o,V = 3316.9（3） A^3,Z = 8,F（000） = 1384,D_c = 1.511 Mg/m^3,M_r = 377.22 and μ = 2.487 mm^-1.In addition,their cholinesterase inhibitory activities in vitro toward Electrophorus electricus acetylcholinesterase（eel ACh E） and horse serum butyrylcholinesterase（eq BCh E） were further determined.The results showed that compound 1 as a new acetylcholinesterase（ACh E） inhibitor displayed higher ACh E inhibitory activity（IC_（50） = 1.4 μM）,which could be considered for Alzheimer＇s disease therapeutics.展开更多
<strong>Objective:</strong> To evaluate early prediction value of IPS<span> </span><span><span style="font-family:Verdana;">combined with SchE and D-dimer detection for in...<strong>Objective:</strong> To evaluate early prediction value of IPS<span> </span><span><span style="font-family:Verdana;">combined with SchE and D-dimer detection for infection and survival in critically ill patients. </span><b><span style="font-family:Verdana;">Methods:</span></b></span><b><span> </span></b><span style="font-family:Verdana;">199 critically ill patients admitted to the emergency intensive care unit (EICU) of our hospital from December 2018 to December 2019 were retrospectively analyzed, including 110 infection patients (infection group) and 89 non-infection</span><span> </span><span style="font-family:Verdana;">patients (non-infection group).</span><span> </span><span><span style="font-family:Verdana;">According to the survival, the infection group was divided into death group (68 cases) and survival group (42 cases). The IPS, APACHE II, SOFA and SchE, D-dimer expression levels were detected and compared;Univariate and logistic regression analysis were used to evaluate the independent prognostic factors. </span><b><span style="font-family:Verdana;">Results: </span></b><span style="font-family:Verdana;">The IPS and APACHE II of patients in the infected group were higher than those in the non-infected group, the level of SchE was lower than that in the non-infected group, and the level of D-dimer was higher than that in the non-infected group (</span><i><span style="font-family:Verdana;">P</span></i></span><i><span> </span></i><span style="font-family:Verdana;"><</span><span> </span><span style="font-family:Verdana;">0.001). IPS, SOFA, APACHE</span><span style="font-family:Verdana;"> II</span><span style="font-family:Verdana;">, SchE, D-dimer, invasive mechanical ventilation, septic shock, and ICU length</span><span style="font-family:Verdana;"> of stay had significant influence on the prognosis of critically ill patients</span><span> </span><span><span style="font-family:Verdana;">(</span><i><span style="font-family:Verdana;">P</span></i></span><i><span> </span></i><span style="font-family:Verdana;"><</span><span> </span><span><span style="font-family:Verdana;">0.001). Logistic regression analysis showed that IPS (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 2.821, </span><span><span style="font-family:Verdana;">95%</span><i><span style="font-family:Verdana;"> CI</span></i></span><span style="font-family:Verdana;"> 1.501</span></span><span style="font-family:Verdana;"> - </span><span><span style="font-family:Verdana;">5.227), SOFA (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 5.078, </span><span><span style="font-family:Verdana;">95% </span><i><span style="font-family:Verdana;">CI</span></i></span><span style="font-family:Verdana;"> 3.327 </span></span><span style="font-family:Verdana;">-</span><span><span style="font-family:Verdana;"> 7.690), APACHE II (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 14.308, </span><span><span style="font-family:Verdana;">95% </span><i><span style="font-family:Verdana;">CI</span></i></span><span style="font-family:Verdana;"> 8.901 </span></span><span style="font-family:Verdana;">-</span><span><span style="font-family:Verdana;"> 21.893), SchE (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 0.223, </span><span><span style="font-family:Verdana;">95%</span><i><span style="font-family:Verdana;"> CI</span></i></span><span style="font-family:Verdana;"> 0.165 </span></span><span style="font-family:Verdana;">-</span><span style="font-family:Verdana;"> 0.291), D-dimer</span><span style="font-family:Verdana;"> (</span><i><span style="font-family:Verdana;">OR</span></i><i><span> </span></i><span style="font-family:Verdana;">=</span><span> </span><span style="font-family:Verdana;">2.10</span><span style="font-family:Verdana;">, </span><span style="font-family:Verdana;">95%</span><i><span> </span></i><i><span style="font-family:Verdana;">CI</span></i><i><span> </span></i><span style="font-family:Verdana;">1.55</span><span style="font-family:Verdana;"> - </span><span style="font-family:Verdana;">2.85</span><span style="font-family:Verdana;">)</span><span><span style="font-family:Verdana;">, septic shock (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 9.948,</span></span><span> </span><span style="font-family:Verdana;">95%</span><span> </span><i><span style="font-family:Verdana;">CI</span></i><span style="font-family:Verdana;"> 7.012</span><span style="font-family:Verdana;"> - </span><span style="font-family:Verdana;">17.012)</span><span> </span><span style="font-family:Verdana;">were independent factors affecting the prognosis of critically ill patients with infection</span><span style="font-family:Verdana;"> (</span><i><span style="font-family:Verdana;">P</span></i><span> </span><span style="font-family:Verdana;"><</span><span> </span><span style="font-family:Verdana;">0.001</span><span style="font-family:Verdana;">)</span><span style="font-family:Verdana;">.</span><span> </span><b><span style="font-family:Verdana;">Conclusion:</span></b><b><span> </span></b><span style="font-family:Verdana;">IPS and D-dimer expression level in infected patients were increased and SchE decreased significantly compared with those in non-infected patients, and they significantly correlated with</span><span> </span><span style="font-family:Verdana;">disease severity of infected</span><span> </span><span style="font-family:Verdana;">patients</span><span> </span><span style="font-family:Verdana;">and could be early prediction</span><span> </span><span style="font-family:Verdana;">for prognosis.</span>展开更多
文摘目的:探究血清胆碱酯酶(Cholinesterase,ChE)、白细胞介素-6(Interleukin-6,IL-6)、血清尿素氮与肌酐比值(Urea-creatinine ratio,UCR)联合序贯器官衰竭(Sequential organ failure assessment,SOFA)评分预测重症肺炎患者病情与预后的价值。方法:选取2021年1月至2024年6月期间,安福县人民医院收治的60例重症肺炎患者作为研究对象(研究组),根据患者预后情况,将其分为死亡组(n=15)及存活组(n=45),取同期30例普通肺炎患者作为对照组,两组均接受常规治疗,对比分析两组患者的SOFA及血清ChE、IL-6、UCR等临床指标的差异。采用受试者工作特征(Receiver operation characteristic curve,ROC)曲线分析血清ChE、IL-6、UCR联合SOFA评分对重症肺炎患者预后的预测价值。结果:研究组患者的血清ChE水平低于对照组,IL-6、UCR水平及SOFA评分均高于对照组(P<0.05);研究组患者中,死亡组患者的血清ChE水平低于存活组,IL-6、UCR水平及SOFA评分均高于存活组(P<0.05);ROC曲线分析显示,重症肺炎血清ChE、IL-6、UCR、SOFA评分用于评估重症肺炎患者预后的曲线下面积(Area under the curve,AUC)分别为0.748、0.763、0.816、0.724,敏感度分别为66.67%、66.67%、68.89%、59.89%,特异度分别为60.00%、73.33%、73.33%、60.00%,四者联合的AUC、敏感度、特异度值分别是0.923、86.67%、60.00%。结论:血清ChE、IL-6、UCR水平与SOFA评分联合应用对重症肺炎患者病情与预后的预测能力价值较高。
文摘AIM: To understand the correlation of serum cholinesterase (CHE) activity with gastric cancer and to assess their clinical significance.METHODS: The velocity method was adopted to detect the activity of serum CHE in patients with gastric cancer and in patients with non-malignant tumor as controls.RESULTS: The serum CHE activity in the treatment group was significantly lower than that in the control group with a very significant difference between the two groups (83.3:113.1,P = 0.0003). Age was significantly associated with the incidence of gastric caner.CONCLUSION: Serum CHE activity has a close relation with the incidence of gastric cancer.
文摘To determine the predictive performance of cholinesterase compared to existing prognostic models in evaluating liver function in patients with chronic hepatitis D. METHODSIn an observational, cross-sectional and retrospective study, consecutive patients with hepatitis D cirrhosis were evaluated. Demographic, clinical and laboratory parameters were recorded. Serum cholinesterase levels were correlated with existing scoring models for chronic liver disease and Liver function tests. Receiver operating characteristic (ROC) curves were constructed to find an optimal cholinesterase level predicting ascites, Child Turcotte Pugh (CTP) score ≥ 10, model for end stage liver disease (MELD) score ≥ 15, baseline-event-anticipation (BEA) score for hepatitis D ≥ 5 and the aspartate transaminase to Platelet Ratio Index (APRI) ≥ 1.5. RESULTSThis study investigated 233 patients with chronic liver disease due to hepatitis D; 192 were male, median age 42 (16-69 years). Fifty patients had ascites and 15 had encephalopathy. One hundred and sixty-seven (71.7%) were in Child class A, 52 (22.3%) in Child class B and 14 (5.0%) in class C. A MELD score of 15 or more was seen in 24 patients. Cholinesterase levels correlated well with the INR, albumin, CTP score, MELD, MELD sodium, BEA and APRI scores (P < 0.001 each). Area under the ROC curve for ascites, CTP ≥ 10, MELD ≥ 15, BEA ≥ 5, APRI ≥ 1.5 was 0.836, 0.966, 0.913, 0.871 and 0.825 respectively (P < 0.001 each). Cut off values of cholinesterase (IU/L) for predicting ascites, CTP ≥ 10, MELD ≥ 15, BEA ≥ 5 and APRI ≥ 1.5 were < 3812, < 2853, < 2829, < 4719 and < 3954 with a sensitivity of 80%, 100%, 91.67%, 82.50%, 58.0% and specificity of 81.97%, 84.79%, 87.56%, 77.06% and 55.64% respectively. CONCLUSIONSerum cholinesterase demonstrates promising correlations with serum albumin, INR and CTP, MELD, BEA and APRI scores and is predictive of liver reserves in hepatitis D cirrhosis.
文摘AIM To examine whether nizatidine stimulates duodenal HCO_3^- secretion in rats by inhibiting AChE activity. METHODS Under pentobarbital anesthesia,a proximal duodenal loop was perfused with saline,and the HCO_3 secretion was measured at pH 7.0 using a pH-stat method and by adding 10mM HCI.Nizatidine,neostigmine,carbachol or famotidine was administered i.v.as a single injection. RESULTS Intravenous administration of nizatidine(3-30 mg/kg)dose-dependently increased duodenal HCO_3^- secretion,and the effect at 10mg/kg was equivalent to that obtained by carbachol at 0.01 mg/kg.This nizatidine action was observed at the same dose range that inhibited acid secretion and enhanced gastric motility,mimicked by i.v.injection of neostigmine(0.03 mg/kg),and significantly attenuated by bilateral vagotomy and prior s.c. administration of atropine but not by indomethacin,a cyclooxygenase inhibitor,or N^G-nitro-L-arginine methyl ester,a NO synthase inhibitor.The HCO_3^- secretory response to acetylcholine(0.001 mg/kg)was significantly potentiated by the concurrent administration of nizatidine(3mg/kg,i.v.).The IC_(50)of nizatidine for AChE of rat erythrocytes was 1.4×10^(-6)M,about 12 times higher than that of neostigmine.Neither famotidine(>10^(-3)M, 30mg/kg,i.v.)nor cisapride(> 10^(-3)M, 3mg/kg,i.v.)had any influence on AChE activity or duodenal HCO_3^- secretion.Duodenal damage induced by acid perfusion(100 mM HCI for 4 h)in the presence of indomethacin was significantly prevented by nizatidine and neostigmine,at the doses that increased the HCO_3^- secretion. CONCLUSION Nizatidine stimulates duodenal HCO_3^- secretion,in both vagal-dependent and atropine-sensitive manners,and the action is associated with the anti-AChE activity of this agent.
文摘The results confirmed that diazepam inhibits the cholinesterase in rat serum,red cell,corpus striatum and diaphragm in vitro,that the higher the diazepam concentration,the stronger the cholinesterase inhibition,and that diazepam is a reversible inhibitor to acetylcholinesterase and diazepam has a stabilizing action on red cell membranes.The role of these effects of diazepam in the treatment of organic phosphate poisoning is discussed
文摘Objective:To investigate the effect of Cannabis sativa resin and/or tramadol,two commonly drugs of abuse on acetylcholinesterase and butyrylcholinesterase activities as a possible cholinergic biomarkers of neurotoxicity induced by these agents.Methods:rats were treated with cannabis resin(5,10 or 20 mg/kg)(equivalent to the active constituent A'-tetrahydrocannabinol),tramadol(5,10 and 20 mg/kg) or tramadol(10 mg/kg)combined with cannabis resin(5,10 and 20 mg/kg) subcutaneously daily for 6 weeks.Acetylcholinesterase(AChE) and butyrylcholinesterase(BChE) activities were measured in brain and serum.We also measured the activity of paraoxonase-1(PONl) in serum of rats treated with these agents.Results:(i) AChE activity in brain increased after 10-20 mg/kg cannabis resin(by 16.3%-36.5%).AChE activity in brain did not change after treatment with 5-20 mg/kg tramadol.The administration of both cannabis resin(5,10 or 20 mg/kg) and tramadol(10 mg/kg) resulted in decreased brain AChE activity by 14.1%,12.9%and 13.6%,respectively;(ii) BChE activity in serum was markedly and dose-dependenlly inhibited by cannabis resin(by 60.9%-76.9%).BChE activity also decreased by 17.6%-36.5%by 10-20mg/kg tramadol and by 57.2%-63.9%by the cannabis resin/tramadol combined treatment;(iii)Cannabis resin at dose of 20 mg/kg increased serum PONl activity by 25.7%.In contrast,tramadol given at 5,10 and 20 mg/kg resulted in a dose-dependent decrease in serum PON1 activity by 19%,36.7%,and 46.1%,respectively.Meanwhile,treatment with cannabis resin plus tramadol resulted in 40.2%,35.8%,30.7%inhibition of PONl activity compared to the saline group.Conclusions:these data suggest that cannabis resin exerts different effects on AChE and BChE activities which could contribute to the memory problems and the decline in cognitive function in chronic users.
基金Supported by the National Natural Science Foundation of China(Nos.20333050 and 20673044), PCSIRT(No.IRT0625) Key Subject of Science and Technology by Jilin Province, China
文摘The density functional theory at the B3LYP/6-311G（d, p） level was applied to exploring the inhibition mechanism of cholinesterases by carbamate. The results indicate that the inhibition reactions with or without the catalytic effect of the catalytic triad in eholinesterases underwent a two-step addition-elimination mechanism, which is in good agreement with the proposed mechanism. The solvent has a strong effect on the inhibition reactions and the reaction with the catalytic triad in the solvent phase is close to the real reaction under biological condition.
基金the Scientific and Technological Research Council of Turkey(TUBITAK)for the scholarship provided her for Ph.D.program
文摘Objective:To explore cholinesterase inhibitory and antioxidant effect of six coniferous trees(Abies bornmulleriana,Picea pungens,Juniperus communis,Cedrus libani,Taxus baccata,and Cupressus sempervirens var.horizantalis).Methods:Acetone(Ace),ethyl acetate(EtOAc),and ethanol(EtOH)extracts prepared from the needles and shoots of the six coniferous trees were screened for their acetylcholinesterase(AChE)and butyrylcholinesterasc(BChE)inhibitory activity at 100μg/mL.Antioxidant activity of the extracts was tested using 2,2-diphenyl-1-picrylhydrazyl(DPPH)and N,N-dimethyl-p-phenylendiamine(DMPD)radical scavenging,nietal-chelation capacity,ferric-(FRAP)and phosphomolibdenum-reducing antioxidant power(PRAP)assays.All of the assays were performed in ELISA microplate reader.Total phenol and flavonoid amounts in the extracts were determined spectrophotometrically.Results:Among thirty-six extracts in total,the shoot-Ace extract of Cupressus sempervirens var.horizantalis exerted the highest inhibition against AChE[(54.84±2.51)%],while the needle-Ace extract of Cedrus libani was the most effective in inhibiting BChE[(67.54±0.30)%].The highest DPPH radical scavenging effect,FRAP and PRAP was observed in the shoot-Ace and EtOAc extracts from Taxus baccata.whereas all the extracts showed a variable degree of scavenging effect against DPMD radical.The shoot-EtOAc extract of Cedrus libani had the highest metalchelation capacity[(58.04±0.70)%].The shoot extracts of Taxus baccata were determined to have the richest total phenol content,which may contribute to its marked antioxidant activity.Conclusions:The conifer species screened in this study may contain cholinesterase-inhibiting and antioxidant properties,which might be useful against Alzheimer's disease.
文摘Acetylcholine is an essential neurotransmitter found throughout the nervous system. Its action on postsynaptic receptors is regulated through hydrolysis by various carboxylesterases, especially cholinesterases (ChEs). The acute toxicity of organophosphate (OP) compounds is directly linked to their action as inhibitors of ChE. One widely used assay for evaluating ChE activity is a spectrophotometric method developed by Ellman et al. When the enzyme source is from tissues or, in particular, blood, hemoglobin displays a spectrophotometric peak at the same wave-length used to analyze cholinergic activity. This creates a substantial background that interferes with the Ellman’s assay and must be overcome in order to accurately monitor cholinesterase activity. Herein, we directly compare blood processing methods: classical method (1.67 ± 0.30 U/mL) and HemogloBindTM treatment (1.51 ± 0.17 U/mL), and clearly demonstrate that pretreatment of blood samples with HemoglobindTM is both a sufficient and rapid sample preparation method for the assessment of ChE activity using the Ellman’s method.
文摘Cholinergic dysfunction is common to Alzheimer’s dementia and Schizophrenia. The objective of this study is to undertake a systematic review and meta-analysis of the literature on the cognitive and clinical effects of cholinesterase inhibitors administered to patients with schizophrenia and co-morbid Alzheimer’s disease dementia. A literature search of the MEDLINE, CINAHL, PubMed, PsycINFO, EMBASE, AMED, BNI, HMIC and Health Business Elite databases has been performed (up to January 2013) to investigate the use of cholinesterase inhibitors in patients with schizophrenia and dementia. The terms “schizophrenia”, “dementia”, “rivastigmine”, “donepezil”, “galantamine” and “cognitive deficit” have been searched, with a restriction for English language. Five published studies including 1 RCT have been included for the qualitative review. Treatments include Donepezil 5 mg and 10 mg as well as Rivastigmine 9 mg. The numbers of participants vary from 2 incase report to20 inthe RCT. Only 1 study qualifies for meta-analysis. There is a very limited evidence on the efficacy and safety of using acetylcholinesterase inhibitors in the management of dementia co-morbid with schizophrenia. The only randomised controlled study shows lack of evidence in terms of efficacy in using cholinesterase inhibitors in the management of dementia with schizophrenia. Future research projects will have to look at an adequate sample size to explore treatment on various cognitive and noncognitive domains and the sample should be selected by using definitive and internationally acceptable diagnostic criteria.
文摘Introduction: Dementia is frequently associated with Parkinson’s disease, especially in later stages. Efficacy of cholinesterase inhibitors (ChI) in Alzheimer’s dementia is well established. However, treatment with ChI in Parkinson’s disease dementia (PDD) remains controversial. The objective of this systematic review and meta-analysis was to assess the effects of ChI in PDD. Methods: A comprehensive literature search was performed in MEDLINE, EMBASE and Cochrane library up to March 2014 using the descriptors “Parkinson’s disease”, “dementia in Parkinson’s disease”, “cognition”, “acetylcholinesterase inhibitors”, “cholinesterase inhibitors”, “anticholinesterase agents”, “rivastigmine”, “donepezil” and “galantamine” (Pubmed search strategy). All randomized, doubleblinded, placebo-controlled trials that met the eligibility criteria and assessed the effects of ChI in PDD were considered for analysis. There were no restrictions regarding paper language. Summary effect-sizes were presented as standardized mean differences (SMD) and the pooled analysis was performed with a fixed-effects model. Outcomes considered for analysis were the Mini Mental Status Exam (MMSE) score and the cognition scale for evaluation of dementia ADAS-Cog. The degree of heterogeneity between included studies was assessed through the I2 test. Results: After a comprehensive search, 175 references were retrieved. From these, five randomized trials involving 946PDD subjects were included in the review. Four studies used donepezil and only one study used rivastigmine. The pooled analysis of five studies that assessed the effects of ChI in MMSE total score showed a SMD of 0.24 (CI 95% 0.11 - 0.38). Three studies considered the effects of ChI on Adas-Cog and the pooled results showed a SMD of 0.21 (CI 95% 0.07 - 0.35). There was no significant heterogeneity between the studies. Conclusions: The results of this systematic review and meta- analysis suggest that ChI improves cognitive impairment in PDD subjects. Despite statistically significant, the translation of these results into relevant clinical improvement should be taken with caution, as the studies did not address what would be considered a clinically significant result.
文摘Two novel naphthol derivatives（1 and 2） were synthesized and characterized via IR,~1H NMR,and HRMS.The structure of compound 2 was verified by single-crystal X-ray crystallography.It crystallizes in monoclinic,space group C2/c with a = 21.6725（9）,b = 6.0127（3）,c = 25.5405（14） A,β = 94.716（5）o,V = 3316.9（3） A^3,Z = 8,F（000） = 1384,D_c = 1.511 Mg/m^3,M_r = 377.22 and μ = 2.487 mm^-1.In addition,their cholinesterase inhibitory activities in vitro toward Electrophorus electricus acetylcholinesterase（eel ACh E） and horse serum butyrylcholinesterase（eq BCh E） were further determined.The results showed that compound 1 as a new acetylcholinesterase（ACh E） inhibitor displayed higher ACh E inhibitory activity（IC_（50） = 1.4 μM）,which could be considered for Alzheimer＇s disease therapeutics.
文摘<strong>Objective:</strong> To evaluate early prediction value of IPS<span> </span><span><span style="font-family:Verdana;">combined with SchE and D-dimer detection for infection and survival in critically ill patients. </span><b><span style="font-family:Verdana;">Methods:</span></b></span><b><span> </span></b><span style="font-family:Verdana;">199 critically ill patients admitted to the emergency intensive care unit (EICU) of our hospital from December 2018 to December 2019 were retrospectively analyzed, including 110 infection patients (infection group) and 89 non-infection</span><span> </span><span style="font-family:Verdana;">patients (non-infection group).</span><span> </span><span><span style="font-family:Verdana;">According to the survival, the infection group was divided into death group (68 cases) and survival group (42 cases). The IPS, APACHE II, SOFA and SchE, D-dimer expression levels were detected and compared;Univariate and logistic regression analysis were used to evaluate the independent prognostic factors. </span><b><span style="font-family:Verdana;">Results: </span></b><span style="font-family:Verdana;">The IPS and APACHE II of patients in the infected group were higher than those in the non-infected group, the level of SchE was lower than that in the non-infected group, and the level of D-dimer was higher than that in the non-infected group (</span><i><span style="font-family:Verdana;">P</span></i></span><i><span> </span></i><span style="font-family:Verdana;"><</span><span> </span><span style="font-family:Verdana;">0.001). IPS, SOFA, APACHE</span><span style="font-family:Verdana;"> II</span><span style="font-family:Verdana;">, SchE, D-dimer, invasive mechanical ventilation, septic shock, and ICU length</span><span style="font-family:Verdana;"> of stay had significant influence on the prognosis of critically ill patients</span><span> </span><span><span style="font-family:Verdana;">(</span><i><span style="font-family:Verdana;">P</span></i></span><i><span> </span></i><span style="font-family:Verdana;"><</span><span> </span><span><span style="font-family:Verdana;">0.001). Logistic regression analysis showed that IPS (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 2.821, </span><span><span style="font-family:Verdana;">95%</span><i><span style="font-family:Verdana;"> CI</span></i></span><span style="font-family:Verdana;"> 1.501</span></span><span style="font-family:Verdana;"> - </span><span><span style="font-family:Verdana;">5.227), SOFA (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 5.078, </span><span><span style="font-family:Verdana;">95% </span><i><span style="font-family:Verdana;">CI</span></i></span><span style="font-family:Verdana;"> 3.327 </span></span><span style="font-family:Verdana;">-</span><span><span style="font-family:Verdana;"> 7.690), APACHE II (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 14.308, </span><span><span style="font-family:Verdana;">95% </span><i><span style="font-family:Verdana;">CI</span></i></span><span style="font-family:Verdana;"> 8.901 </span></span><span style="font-family:Verdana;">-</span><span><span style="font-family:Verdana;"> 21.893), SchE (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 0.223, </span><span><span style="font-family:Verdana;">95%</span><i><span style="font-family:Verdana;"> CI</span></i></span><span style="font-family:Verdana;"> 0.165 </span></span><span style="font-family:Verdana;">-</span><span style="font-family:Verdana;"> 0.291), D-dimer</span><span style="font-family:Verdana;"> (</span><i><span style="font-family:Verdana;">OR</span></i><i><span> </span></i><span style="font-family:Verdana;">=</span><span> </span><span style="font-family:Verdana;">2.10</span><span style="font-family:Verdana;">, </span><span style="font-family:Verdana;">95%</span><i><span> </span></i><i><span style="font-family:Verdana;">CI</span></i><i><span> </span></i><span style="font-family:Verdana;">1.55</span><span style="font-family:Verdana;"> - </span><span style="font-family:Verdana;">2.85</span><span style="font-family:Verdana;">)</span><span><span style="font-family:Verdana;">, septic shock (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 9.948,</span></span><span> </span><span style="font-family:Verdana;">95%</span><span> </span><i><span style="font-family:Verdana;">CI</span></i><span style="font-family:Verdana;"> 7.012</span><span style="font-family:Verdana;"> - </span><span style="font-family:Verdana;">17.012)</span><span> </span><span style="font-family:Verdana;">were independent factors affecting the prognosis of critically ill patients with infection</span><span style="font-family:Verdana;"> (</span><i><span style="font-family:Verdana;">P</span></i><span> </span><span style="font-family:Verdana;"><</span><span> </span><span style="font-family:Verdana;">0.001</span><span style="font-family:Verdana;">)</span><span style="font-family:Verdana;">.</span><span> </span><b><span style="font-family:Verdana;">Conclusion:</span></b><b><span> </span></b><span style="font-family:Verdana;">IPS and D-dimer expression level in infected patients were increased and SchE decreased significantly compared with those in non-infected patients, and they significantly correlated with</span><span> </span><span style="font-family:Verdana;">disease severity of infected</span><span> </span><span style="font-family:Verdana;">patients</span><span> </span><span style="font-family:Verdana;">and could be early prediction</span><span> </span><span style="font-family:Verdana;">for prognosis.</span>
