A direct assay of butyrylcholinesterase activity using a fluorescent substrate

2016 ◽  
Vol 14 (37) ◽  
pp. 8815-8820 ◽  
Author(s):  
Seungyoon Kang ◽  
Suji Lee ◽  
Woojin Yang ◽  
Jiwon Seo ◽  
Min Su Han
Keyword(s):  
Fluorescent Substrate ◽  
Bche Activity ◽  
Direct Assay ◽  
Butyrylcholinesterase Activity ◽  
Potential Inhibitors ◽  
Continuous Assay

We report a fluorescent substrate for a direct and continuous assay of BChE activity and screening of its potential inhibitors.

scholarly journals Serum Butyrylcholinesterase Activity: A Biomarker for Parkinson’s Disease and Related Dementia

2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
Mei-Xue Dong ◽  
Xiao-Min Xu ◽  
Ling Hu ◽  
Yang Liu ◽  
Yuan-Jun Huang ◽  
...  
Keyword(s):  
Parkinson’S Disease ◽  
Parkinson's Disease ◽  
Sensitivity And Specificity ◽  
Rating Scale ◽  
Roc Curves ◽  
Healthy Controls ◽  
Bche Activity ◽  
Disease Rating ◽  
Independent Risk Factors ◽  
Butyrylcholinesterase Activity

Objective. This study aim to determine changes of serum butyrylcholinesterase (BChE) activity in PD patients and related dementia. Patients and Methods. Consecutive PD patients and healthy controls were included and clinical data were collected. Fast serum BChE activity was determined and compared between healthy controls and PD patients. Independent risk factors were performed for BChE activity, PD, and related dementia. The relationship between BChE activity and disease severity was also evaluated. Receiver operating characteristic (ROC) curves were obtained to explore serum BChE activity in distinguishing PD patients and related dementia. Results. Serum BChE activity mainly independently correlated with gender, albumin, triglyceride, body mass index, and PD. Serum BChE activity decreased in PD patients compared with healthy controls. Based on the ROC curve, the optimal cut-off point was 6864.08 IU/L for distinguishing PD patients, and the sensitivity and specificity values were 61.8% and 72.1%. It inversely correlated with Unified Parkinson’s Disease Rating Scale score. BChE activity decreased in PD-related dementia compared with those without dementia. The sensitivity and specificity values were 70.6% and 76.3%, respectively, with an optimal cut-off point of 6550.00 IU/L. Conclusions. Serum BChE activity can be regarded as a biomarker for PD and related dementia.

scholarly journals Reduced Serum Butyrylcholinesterase Activity Indicates Severe Systemic Inflammation in Critically Ill Patients

2015 ◽  
Vol 2015 ◽  
pp. 1-11 ◽  
Author(s):  
Aleksandar R. Zivkovic ◽  
Karsten Schmidt ◽  
Annette Sigl ◽  
Sebastian O. Decker ◽  
Thorsten Brenner ◽  
...  
Keyword(s):  
Immune Response ◽  
Critically Ill ◽  
Systemic Inflammation ◽  
Critically Ill Patients ◽  
Point Of Care ◽  
Inverse Correlation ◽  
Hepatic Function ◽  
Bche Activity ◽  
Assessment And Treatment ◽  
Butyrylcholinesterase Activity

Systemic inflammation is an immune response to a nonspecific insult of either infectious or noninfectious origin and remains a challenge in the intensive care units with high mortality rate. Cholinergic neurotransmission plays an important role in the regulation of the immune response during inflammation. We hypothesized that the activity of butyrylcholinesterase (BChE) might serve as a marker to identify and prognose systemic inflammation. By using a point-of-care-testing (POCT) approach we measured BChE activity in patients with severe systemic inflammation and healthy volunteers. We observed a decreased BChE activity in patients with systemic inflammation, as compared to that of healthy individuals. Furthermore, BChE activity showed an inverse correlation with the severity of the disease. Although hepatic function has previously been found essential for BChE production, we show here that the reduced BChE activity associated with systemic inflammation occurs independently of and is thus not caused by any deficit in liver function in these patients. A POCT approach, used to assess butyrylcholinesterase activity, might further improve the therapy of the critically ill patients by minimizing time delays between the clinical assessment and treatment of the inflammatory process. Hence, assessing butyrylcholinesterase activity might help in early detection of inflammation.

scholarly journals A randomized crossover trial assessing the effects of acute exercise on appetite, circulating ghrelin concentrations, and butyrylcholinesterase activity in normal-weight males with variants of the obesity-linked FTO rs9939609 polymorphism

2019 ◽  
Vol 110 (5) ◽  
pp. 1055-1066 ◽  
Author(s):  
James L Dorling ◽  
David J Clayton ◽  
Jenny Jones ◽  
Wayne G Carter ◽  
Alice E Thackray ◽  
...  
Keyword(s):  
Energy Intake ◽  
Acute Exercise ◽  
Peak Oxygen Uptake ◽  
Normal Weight ◽  
Obesity Risk ◽  
Bche Activity ◽  
Ad Libitum ◽  
Acyl Ghrelin ◽  
Butyrylcholinesterase Activity ◽  
Fto Rs9939609

ABSTRACT Background The fat mass and obesity-associated gene (FTO) rs9939609 A-allele is associated with higher acyl-ghrelin (AG) concentrations, higher energy intake, and obesity, although exercise may mitigate rs9939609 A-allele–linked obesity risk. Butyrylcholinesterase (BChE) hydrolyzes AG to des-acyl-ghrelin (DAG), potentially decreasing appetite. However, the effects of the FTO rs9939609 genotype and exercise on BChE activity, AG, DAG, and energy intake are unknown. Objective We hypothesized that individuals homozygous for the obesity-risk A-allele (AAs) would exhibit higher postprandial AG and energy intake than individuals homozygous for the low obesity-risk T-allele (TTs), but that exercise would increase BChE activity and diminish these differences. Methods Twelve AA and 12 TT normal-weight males completed a control (8 h rest) and an exercise (1 h of exercise at 70% peak oxygen uptake, 7 h rest) trial in a randomized crossover design. A fixed meal was consumed at 1.5 h and an ad libitum buffet meal at 6.5 h. Appetite, appetite-related hormones, BChE activity, and energy intake were assessed. Results AAs displayed lower baseline BChE activity, higher baseline AG:DAG ratio, attenuated AG suppression after a fixed meal, and higher ad libitum energy intake compared with TTs [effect sizes (ESs) ≥ 0.72, P ≤ 0.049]. Exercise increased Δ BChE activity in both genotypes (ESs = 0.37, P = 0.004); however, exercise lowered AG and the AG:DAG ratio to a greater extent in AAs (P ≤ 0.023), offsetting the higher AG profile observed in AAs during the control trial (ESs ≥ 1.25, P ≤ 0.048). Exercise did not elevate energy intake in either genotype (P = 0.282). Conclusions Exercise increases BChE activity, suppresses AG and the AG:DAG ratio, and corrects the higher AG profile observed in obesity-risk AA individuals. These findings suggest that exercise or other methods targeting BChE activity may offer a preventative and/or therapeutic strategy for AA individuals. This trial was registered at clinicaltrials.gov as NCT03025347.

scholarly journals Betaine Increases the Butyrylcholinesterase Activity in Rat Plasma

2016 ◽  
pp. 101-108 ◽  
Author(s):  
K. ŠIŠKOVÁ ◽  
M. DUBNIČKOVÁ ◽  
Ľ. PAŠKOVÁ ◽  
D. RAJDL ◽  
Z. ĎURAČKOVÁ ◽  
...  
Keyword(s):  
High Fat Diet ◽  
Physiological Function ◽  
Rat Plasma ◽  
Plasma Triglyceride ◽  
High Fat ◽  
Fat Utilization ◽  
Bche Activity ◽  
Butyrylcholinesterase Activity ◽  
Regular Intake

The physiological function of butyrylcholinesterase (EC 3.1.1.8, BChE) is not clearly understood, but a role was suggested in the fat utilization process, resulting in positive correlation between plasma triglyceride (TG) levels and BChE activity. Consequently we tested the hypothesis that regular intake of betaine, a natural compound intervening in the liver TG metabolism could influence the BChE activity. The BChE activity was estimated spectrophotometrically in plasma of rats fed with betaine enriched standard (B) or high-fat diet (HFB). The results confirmed decreased TG plasma levels after betaine treatment independently on the type of diet (0.15±0.03 (B) vs. 0.27±0.08 (control) mmol/l; p=0.003 and 0.13±0.03 (HFB) vs. 0.27±0.08 (control) mmol/l; p=0.005). The BChE activity increased significantly with betaine administration, however the change was more distinct in the HFB group (0.84±0.34 (HFB) vs. 0.22±0.04 (control) O.D./min/mg; p<0.001 and 0.41±0.11 (B) vs. 0.22±0.04 (control) O.D./min/mg; p=0.001). In conclusion, betaine intake led to elevated BChE activity in plasma and this effect was potentiated by the HF diet. Since betaine is in general used as a supplement in the treatment of liver diseases accompanied by TG overload, its impact on the BChE activity in the role of the liver function marker should be taken into account.

scholarly journals A Bioorthogonally Synthesized and Disulfide-Containing Fluorescence Turn-On Chemical Probe for Measurements of Butyrylcholinesterase Activity and Inhibition in the Presence of Physiological Glutathione

Catalysts ◽  
2020 ◽  
Vol 10 (10) ◽  
pp. 1169
Author(s):  
Ming-Mao Gong ◽  
Chia-Yen Dai ◽  
Scott Severance ◽  
Chi-Ching Hwang ◽  
Bo-Kai Fang ◽  
...  
Keyword(s):  
Resonance Energy Transfer ◽  
Resonance Energy ◽  
Kinetic Studies ◽  
Chemical Probe ◽  
Turn On ◽  
Bche Activity ◽  
Substitution Mechanism ◽  
Butyrylcholinesterase Activity ◽  
Fluorescence Turn On ◽  
Derivatives Of

Butyrylcholinesterase (BChE) is a biomarker in human blood. Aberrant BChE activity has been associated with human diseases. Here we developed a fluorescence resonance energy transfer (FRET) chemical probe to specifically quantify BChE activity in serum, while simultaneously discriminating against glutathione (GSH). The FRET chemical probe 11 was synthesized from a key trifunctional bicyclononyne exo-6 and derivatives of 5-(2-aminoethylamino)-1-naphthalenesulfonic acid (EDANS) and 4-[4-(dimethylamino)phenylazo]benzoic acid (DABCYL). EDANS fluorescence visualization and kinetic analysis of 11 in the presence of diverse compounds confirmed the outstanding reactivity and specificity of 11 with thiols. The thiol-dependent fluorescence turn-on property of 11 was attributed to a general base-catalyzed SN2 nucleophilic substitution mechanism and independent of metal ions. Moreover, all thiols, except GSH, reacted swiftly with 11. Kinetic studies of 11 in the presence of covalently modified GSH derivatives corroborated that the steric hindrance of 11 imposing on GSH was the likely cause of the distinguished reactivity. Since GSH commonly interferes in assays measuring BChE activity in blood samples, the 11-based fluorescent assay was employed to directly quantify BChE activity without GSH interference, and delivered a linear range of 4.3–182.2 U L−1 for BChE activity with detection limit of 4.3 U L−1, and accurately quantified serum BChE activity in the presence of 10 μM GSH. Finally, the 11-based assay was exploited to determine Ki of 5 nM for tacrine inhibition on BChE catalysis. We are harnessing the modulated characteristics of 6 to synthesize advanced chemical probes able to more sensitively screen for BChE inhibitors and quantify BChE activity in serum.

Thiol–ene click reaction-induced fluorescence enhancement by altering the radiative rate for assaying butyrylcholinesterase activity

The Analyst ◽  
2019 ◽  
Vol 144 (2) ◽  
pp. 559-566 ◽  
Author(s):  
Guilin Chen ◽  
Hui Feng ◽  
Wenbin Xi ◽  
Jing Xu ◽  
Saifei Pan ◽  
...  
Keyword(s):  
Fluorescence Enhancement ◽  
Click Reaction ◽  
Molecular Probe ◽  
Bche Activity ◽  
Radiative Rate ◽  
Butyrylcholinesterase Activity

A fluorescent molecular probe for assaying BChE activity based on thiol-triggered fluorescence enhancement via a thiol–ene click reaction was developed.

A Novel Continuous Assay for the Mechanistic Characterization of Histone Deacetylases and Homologues Using a Small Molecule Fluorescent Substrate

2001 ◽  
pp. 541-542
Author(s):  
Jennifer L. Gronlund ◽  
Michael K. Yu ◽  
A. Melissa Concepcion ◽  
Shu He ◽  
Ravi Venkataramani ◽  
...  
Keyword(s):  
Small Molecule ◽  
Histone Deacetylases ◽  
Fluorescent Substrate ◽  
Continuous Assay
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