MICROCHEMICAL JOURNAL
·
2023
·
IF 4.8
Jianfang Jiang,Kuaqian Deng,Fanglin Dao,Panyang Li,Jiali Huang
Trichlorfon (TCF) is an important chemical for pest and parasite control, but it poses risks to public and environmental health. Thus, the detection of TCF is of great value. In this study, we report a strategy to prepare an AChE-nanoprobe for detecting TCF. Benefiting from the unique and excellent structure of CHO-β-CD, this AChE-nanoprobe can wrap nano-Fe 3 O 4 and covalently bind AChE. As a proof of concept, we prepared an AChE-nanoprobe with a hydrated particle size of 717 nm and a saturation magnetic strength of 64.11 emu/g Fe. The properties were studied in detail. Its catalytic activity was 90 % of that of free AChE, and it had broadened pH, thermal, organic solvents and storage in addition to good reusability, with a residual catalytic activity of 42 % after the 10th cycle and a cumulative catalytic activity 6.9 times higher than that of the free enzyme. The AChE-nanoprobe exhibited good performance in TCF detection; the linear range of TCF was 40–4000 ng/L, and the limit of detection for TCF was 2.8 ng/L. Furthermore, our results suggest that the AChE-nanoprobe has several attractive features, such as easy preparation, outstanding stability and reusability, providing a novel and promising tool for the analysis of TCF.
研究领域:
环境科学
·
分析化学
·
纳米技术
✓ 已验证
产品关联
DOI
高影响因子
Nanoscale
·
2020
·Vol. 13
·期 2
·1283-1290
·
IF 6.895
Chang Liu,Yuxin Luo,Huijie Wen,Yanxia Qi,Guoyue Shi,Jingjing Deng,Tianshu Zhou
Herein, combined with a pervasive smartphone installed with a color recognition app, dual-responsive CDs@Eu/GMP ICPs were designed as a red-to-blue paper-based colorimetric sensor for the point-of-use analysis of cerebral acetylcholinesterase (AChE) upon Cd2+ exposure. Blue-emitting CDs with multi-functional groups as guests were encapsulated into the network of Eu/GMP ICPs to obtain CDs@Eu/GMP ICPs with the sensitized red fluorescence of Eu3+. With the presence of thiocholine (TCh), derived from acetylthiocholine (ATCh) hydrolyzed by AChE, the coordination environment of the CDs@Eu/GMP ICPs was interrupted, leading to the collapse of the CDs@Eu/GMP ICP network and the corresponding release of guest CDs into the surrounding environment. Consequently, the sensitized red fluorescence of Eu3+ decreased and the blue fluorescence of the CDs increased. This obvious red-to-blue fluorescent color changes of CDs@Eu/GMP ICPs on test paper could then be integrated with the smartphone for point-of-use analysis of cerebral AChE upon Cd2+ exposure, which not only offers a new analytical platform for a better understanding of the environmental risk of Alzheimer's Dementia (AD), but also holds great potential in the early diagnosis of AD even at the asymptomatic stage with the decrease in CSF AChE as an early biomarker.
研究领域:
分析化学
·
环境科学
·
神经科学
·
材料科学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
·
2025
·
IF 4
Yuhan Zhao,Xiaojie Zhou,Mei Li,Xinghui Qiu
The Asian tiger mosquito Aedes albopictus transmits several arboviruses, including chikungunya, Zika, and dengue, posing serious public health threats. The excessive use of insecticides has led to increasing resistance to commonly applied insecticides in this species. We previously observed that enhanced expression of a CYP6Z8 homolog (AalbCYP6Z8) was associated with insecticide resistance in two field populations of Ae. albopictus ; however, its capacity in insecticide metabolism had not been biochemically characterized. In this study, to explore the potential role of AalbCYP6Z8 in insecticide metabolism, a fully functional enzyme system was reconstituted in vitro by using Escherichia coli –produced recombinant AalbCYP6Z8 and NADPH-dependent cytochrome P450 reductase along with cytochrome b 5. Our metabolism assays showed that CYP6Z8 was capable of metabolizing organophosphates (temephos and malathion) and carbamates (propoxur and bendiocarb), but not pyrethroids (deltamethrin and permethrin). Mass spectrometry analyses tentatively identified the structures of specific metabolites, revealing that AalbCYP6Z8 transforms organophosphates through oxidative desulfurization and carbamates through dealkylation and hydroxylation. This work demonstrates that AalbCYP6Z8 is a versatile metabolizer of acetylcholinesterase-inhibiting insecticides.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
·
2026
·
IF 6.7
Li Dong,Jing Yang,Yunniao Meng,Sisi Yang,Changluan Pan,Fangxing Luo,Haiyan Long,Shaofang Lv,Yaozhen Gong,Juan Xu,Ying Xiong,Yongxi Dong
The optimal compound AJ-4 showed potent GSK-3β inhibitor activity with an IC 50 value of 4.7 nM. • AJ-4 exerted superior AChE inhibitor with an IC 50 value of 2.97 μM. • AJ-4 exhibited favorable selectivity against selected serine/threonine and tyrosine kinases. • AJ-4 presented favorable pharmacokinetic characteristics and tissue distribution. • AJ-4 obviously ameliorated scopolamine-induced learning and memory impairments in AD mice. The pathogenesis of Alzheimer's disease (AD) is closely related with glycogen synthase kinase 3β (GSK-3β) and acetylcholinesterase (AChE). Our previous work verified that GL10a displayed superior GSK-3β inhibitory and neuroprotective activities relative to Tideglusib. Accordingly, a molecular hybridization strategy was applied to design and synthesize a series of dual target inhibitors against GSK-3β and AChE by conjugating GL10a and carbamate fragment of Rivastigmine's pharmacophore. After in vitro evaluations, the compound AJ-4 was screened as the most remarkable compound with potent inhibitory activities against GSK-3β (IC 50 : 4.7 nM) and AChE (IC 50 : 2.97 μM). Meanwhile, in vitro and in vivo data revealed that the optimal compound AJ-4 with excellent enzyme selectivity could decrease amyloid precursor protein (APP) and phosphorylated Tau expressions and increase phosphorylated GSK-3β levels. With favorable pharmacokinetic characteristics and tissue distribution, AJ-4 obviously ameliorated scopolamine-induced learning and memory impairments and alleviated hippocampal neuronal injury in AD mice. In conclusion, GSK-3β/AChE dual inhibitors represent a promising strategy for developing multi-target anti-AD drugs. Download: Download high-res image (495KB) Download: Download full-size image
✓ 已验证
DOI
PubMed
高影响因子
International Journal of Electrochemical Science
·
2023
·
IF 1.5
Kai Zhang,Liangzi Wang,Jingitao liu,Shiyu Zhao,Longfei Ding,Binhua Zhou,Bo Zhao
Despite the harmful effects of organophosphorus pesticides (OPPs), few rapid detection methods of OPPs multi-residue have been practically applied; thus, it is important to improve existing methods and develop rapid detection methods and techniques. Reduced graphene oxide-chitosan (RGO-CHI)/methamidophos electrochemical biosensor was developed to detect multiple OPPs based on the principle of acetylcholinesterase (AChE) activity inhibition in the presence of OPPs. One OPP (methamidophos) that can combine with AChE in the incubation solution was immobilized on the electrode. The proposed method shows good linear relationships of nine OPPs and methomyl, a carbamate pesticide, with limits of detection between 0.05 and 0.52 ppb, indicating high accuracy for the application in real sample detection.
研究领域:
分析化学
·
环境科学
·
生物技术
✓ 已验证
产品关联
DOI
高影响因子
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
·
2026
·
IF 4.8
Yu Wang,Conghui Wang,Chuhua Zeng,Wensheng Wang,Yu Liu
CoFe NPs was synthesized for catalytic oxidation of TH. • Cysteine inhibits oxidation of TH oxidation catalyzed by CoFe NPs. • A catalytic cascade combining ACTh hydrolysis and CoFe NPs catalysis. • The system rapidly and specifically senses OPs with an ultralow LOD (0.5 ng/mL). Traditional methods for pesticide residue detection often rely on expensive instruments, are time-consuming, and lack cost efficiency. This investigation developed a fluorescence-based assay that utilizes cascade amplification through cholinesterase hydrolysis and thiamine (TH) oxidation for the detection of organophosphorus pesticides (OPs). A Prussian blue analog (CoFe NPs) with high catalytic activity for TH oxidation was synthesized. Cholinesterase hydrolyzes acetylthiocholine to produce thiocholine, which subsequently inhibits the CoFe NPs-catalyzed oxidation of TH. In the presence of paraoxon, acetylcholinesterase activity is inhibited, leading to restored TH oxidation and generating a strong fluorescence signal. The increase in fluorescence intensity is proportional to paraoxon concentration. This novel assay demonstrates a linear detection range of 0–10 ng/mL, achieving a limit of detection (LOD) of 0.5 ng/mL, indicating sensitivity superior to that reported in previous studies. This work presents a sensitive and innovative strategy for OPs detection. Download: Download high-res image (144KB) Download: Download full-size image
✓ 已验证
DOI
高影响因子
Food & Function
·
2018
·Vol. 9
·期 2
·1173-1178
·
IF 3.289
Zhipeng Yu,Sijia Wu,Wenzhu Zhao,Long Ding,Yue Fan,David Shiuan,Jingbo Liu,Feng Chen
Alzheimer's disease (AD) is a global health issue affecting millions of elderly people worldwide. The aim of the present study was to identify novel anti-AD peptides isolated from albumin. Anti-AD activities of the peptides were evaluated via inhibitory activities on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Furthermore, the potential molecular mechanisms of the KLPGF/AChE were investigated by CDOCKER of Discovery studio 2017. The results revealed that peptide KLPGF could effectively inhibit AChE with an inhibition rate of 61.23% at a concentration of 50 μg mL−1. In addition, the peptide KLPGF came in contact with acylation sites and peripheral anion sites of AChE. The present study demonstrates that the peptide KLPGF could become a potential functional food intervention in AD.
研究领域:
神经生物学
·
药理学
·
分子生物学
·
老年医学
·
药物开发
✓ 已验证
DOI
高影响因子
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
·
2023
·
IF 6.7
Ziwen Zhang,Shi-Long Zhang,Chengyao Wu,Huan-Huan Li,Liang Zha,Jingbo Shi,Xinhua Liu,Hua-Li Qin,Wenjian Tang
SuFEx click chemistry has been a method for the rapid synthesis of functional molecules with desirable properties. Here, we demonstrated a workflow that allows for in situ synthesis of sulfonamide inhibitors based on SuFEx reaction for high-throughput testing of their cholinesterase activity. According to fragment-based drug discovery (FBDD), sulfonyl fluorides [R–SO 2 F] with moderate activity were identified as fragment hits, rapidly diversified into 102 analogs in SuFEx reactions, and the sulfonamides were directly screened to yield drug-like inhibitors with 70-fold higher potency (IC 50 = 94 nM). Moreover, the improved molecule J8-A34 can ameliorate cognitive function in A β 1−42 -induced mouse model. Since this SuFEx linkage reaction succeeds on picomole scale for direct screening, this methodology can accelerate the development of robust biological probes and drug candidates.
研究领域:
化学
·
药物发现
·
神经科学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
·
2021
·
IF 3.196
Xiaodi Kou,Juanjuan Liu,Yuhong Chen,Aihong Yang,Rui Shen
Four new emodin derivatives which inhibit Alzheimer's disease were designed and the related activities such as cholinesterase inhibitor, anti-oxidant and metal chelator were evaluated. Among them, compounds a and b had comparable inhibitory activities of acetylcholinesterase to control drug tacrine. In particular, compound a had the strongest inhibitory effect on acetylcholinesterase with IC 50 value of 0.067 μM. Kinetic analysis of a and b indicated the mixed-type inhibition. Molecular simulation studies showed that they could bind both the catalytically active site and the peripheral anion site of acetylcholinesterase. The antioxidant activities were determined using the superoxide radical ( . O 2 – ) and hydroxyl radical ( . OH) assays. All derivatives showed high anti-oxidative activities. The mechanisms of electrochemical oxidation of emodin and its derivations were studied by cyclic voltammetry. In addition, compounds a-d exhibited obvious chelating abilities with Cu 2+ , Fe 3+ , Zn 2+ and Al 3+ ions. Interestingly, complexes chelated with Cu 2+ and Zn 2+ showed better acetylcholinesterase inhibitory activities and antioxidative activities. Taken together, emodin derivatives have multi-factor anti-Alzheimer's disease activities, and they are worthy of further study as potential candidate drugs for Alzheimer's disease.
研究领域:
药理学
·
神经科学
✓ 已验证
产品关联
DOI
高影响因子
Journal of Applied Spectroscopy
·
2018
·Vol. 85
·期 3
·437-444
·
IF 0.611
Zhao Lingzhi,Zhao Liu,Zhang Chenxiao,Li Yanqi
We demonstrate the utility of 4-chloro-7-nitrobenzofurazan (NBD-Cl), a simple, low-cost probe, for colorimetrically and fluorescently detecting and differentiating similar thiol species, including cysteine, homocysteine, and glutathione, as well as for assaying acetylcholinesterase (AChE) activity. This assay is a potential tool for investigating thiol functions in disease and diagnosis, and for screening AChE inhibitors. We envision that this versatile probe, which is commercially available and inexpensive, will be useful for further elucidating the roles of thiols in biology and also shows applicability for analysis of AChE inhibitors in physiological samples.
研究领域:
分析化学
·
生物化学
·
分子生物学
·
诊断学
✓ 已验证
产品关联
DOI
高影响因子
METABOLIC BRAIN DISEASE
·
2018
·Vol. 34
·期 1
·173-181
·
IF 2.441
Sun Kaiyue,Bai Yuting,Zhao Rong,Guo Zijiao,Su Xiang,Li Peiqi,Yang Pengyu
The present study was designed to evaluate the effects of matrine (MAT) on scopolamine (SCOP)-induced learning and memory impairment. After successive oral administration of MAT to mice for three days at doses of 0.4, 2, and 10 mg/kg, we assessed improvements in learning and memory and investigated the mechanism of action of SCOP-induced amnesia. Donepezil at a dose of 3 mg/kg was used as a standard memory enhancer. MAT significantly improved SCOP-induced learning and memory impairment in novel object recognition and Y-maze tests at doses of 0.4, 2, and 10 mg/kg. Furthermore, MAT inhibited acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities and decreased oxidative stress in the brain, as evidenced by increased total antioxidant capacity, total superoxide dismutase levels, and catalase activities as well as decreased malondialdehyde levels. Additionally, there was a significant negative correlation between the percentage of spontaneous alternation in the Y maze and AChE activity in the cortex and hippocampus. MAT ameliorated SCOP-induced amnesia by the inhibition of both AChE/BuChE activities and oxidative stress. This study provides further evidence to encourage the development of MAT as a drug for the prevention or treatment of Alzheimer’s disease.
研究领域:
神经科学
·
药理学
·
阿尔茨海默病研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MICROCHEMICAL JOURNAL
·
2026
·
IF 5.2
Guozheng Zhao,Jianfeng Jia
Organophosphorus pesticides (OPs) pose significant risks to food safety and environmental health, making the development of sensitive and reliable detection methods highly desirable. In this work, a highly sensitive electrochemical biosensor based on a MXene/gold nanoparticles (AuNPs)/acetylcholinesterase (AChE) composite was constructed for the detection of OPs. Owing to the large specific surface area and excellent conductivity of MXene, together with the stable immobilization of AChE via Au S bonds, the proposed biosensor exhibits enhanced electron transfer efficiency and enzymatic activity retention. Under optimized conditions, the biosensor shows a wide linear response toward OPs, with a low detection limit of 0.008 ng·mL −1 , calculated based on the 3 σ / k criterion. The sensor also demonstrates good selectivity against common interfering species, satisfactory reproducibility, and excellent batch-to-batch repeatability. Furthermore, the applicability of the biosensor was validated by the determination of OP residues in various real samples, including apples, and cabbages, with recoveries ranging from 96.36% to 103.31% and relative standard deviations below 3.0%. Owing to its simple fabrication procedure and compatibility with portable electrochemical devices, the proposed sensing platform shows great potential for on-site and rapid monitoring of OPs in food and agricultural products.
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）