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Chinese Journal of Chemistry 2013年第9期31卷 1228-1233页

作者： Guofei Jin Zhongduo Yang Weiwei Xue Jie Sheng Yin Shi Xiaojun Yao School of Life Science and Engineering Lanzhou University of Technology Lanzhou Gansu 730050 China Department of Chemistry Lanzhou University Lanzhou Gansu 730000 China Key Lab of New Animal Drug Project Gansu Province Key Lab of Veterinary Pharmaceutical Development Ministry of Agriculture Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS Lanzhou Gansu 730050 China

New isoconessimine derivatives were synthesized from conessine （1） and evaluated as acetylcholinesterase （ACHE） inhibitors. The derivatives were prepared via two reaction steps, N-demethylation and nuc]eophilic substi- tution. All of the synthesized derivatives exhibited more potential anti-acetylcholinesterase activities than conessine （1）（IC50=16μmol·L^-1） and isoconessimine （2）（IC50〉300 μmol·L ^-1）. Compound 7b （3fl-[methyl-[2-（4-nitro- phenoxy）ethyl]amino]con-5-enine） showed the most potent inhibitory activity with an IC50 of 110 μmol/L which is close to that of reference compound huperzine A （IC50= 70 μmol/L）. The mode of AChE inhibition by 7h was re- versible and non-competitive. In addition, molecular modeling was performed to explore the binding mode of in- hibitor 7b at the active site of AChE and the results showed that 7b could be docked into the acetylcholinesterase active site and compound 7h had hydrophobic interactions with Trp279 and Leu282.

关键词： isoconessimine derivatives acetylcholinesterase inhibitors molecular docking

Synthesis and Biological Evaluation of 3,6-Diaryl-7H-thiazolo[3,2-b][1,2,4]triazin-7-one Derivatives as acetylcholinesterase inhibitors

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Synthesis and Biological Evaluation of 3,6-Diaryl-7H-thiazol...

QSAR study of berberine derivatives as acetylcholinesterase inhibitors

有机合成创新—产业化的新动力——中国化学会全国第三届有...

作者： Zhe,Jin~a Liu,Yang~a Liu,Sijie~a Wang,Jian~a Li,Shuo~b Lin,Huangquan~b Wan,David Chi Cheong~b Hu,Chun~(*,a) (a Key Laboratory of Structure-Based Drug Design & Discovery,Ministry of Education School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016) (b Department of Biochemistry,The Chinese University of Hong Kong,Hong Kong SAR,China)

＜正＞To date,acetylcholinesterase（ACHE） inhibitors are the main type of drugs used to treat *** medications that have received FDA approval for the treatment of AD include ACHE inhibitors,such as tacrine,donepezil, rivastigmine,galanthamine,and an NMDA receptor antagonist,memantine. Our previous work has shown 5H-thiazolo[3,2-a]pyrimidine derivatives exhibited ACHE inhibitory activity, and the molecular docking exhibited the compounds interacted with the PAS of ACHE.

关键词： acetylcholinesterase inhibitors synthesis triazin

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QSAR study of berberine derivatives as acetylcholinesterase ...

Aptamer-induced in-situ growth of acetylcholinesterase-Cu_(3)(PO_(4))_(2)hybrid nanoflowers for electrochemical detection of organophosphorus inhibitors

第十一届全国计算（机）化学学术会议

作者：夏冬辉任旭东李华 Institute of Analytical Science School of Chemistry and Material SciencesNorthwest UniversityXi’an 710069

acetylcholinesterase inhibitors(AChEIs) are currently considered as potential drugs for treating Alzheimer *** this work,quantitative structure-activity relationship(QSAR) analyses have been carried out for 56 kinds of berberine derivatives as *** groups of 3D descriptors which were obtained from E-DRAGON:geometrical,3D molecule representation of structures based on electron diffraction(3D-MoRSE);Randic molecular profiles;geometry, topology and atom weights assembly(GETAWAY);radial distribution function(RDF);and weigthed covariance matrices(WHIM) descriptors have been used to generate QSAR *** whole data set was grouped into two subsets based on the k-means clustering *** Carlo variable selection(MCVS) method was adopted to choose *** descriptors involving geometrical,RDF and Randic molecular profiles descriptors were selected and used to build QSAR model with multi-linear regression(MLR) and artificial neural network(ANN) modeling *** with MLR model,ANN model shows better predictive ability with the determination coefficient R of 0.869,0.843 and 0.855 for training,validation and test set, *** results of 100 times’ leave-half-out cross validation showed the robustness of this *** obtained models suggest that inhibitory activity of berberine derivates is related to the shape of the molecule and the three-dimensional distribution of atomic mass in the *** studies can offer some useful references for developing AChE inhibitors of natural product berberine as a lead molecule.

关键词： acetylcholinesterase inhibitors berberine derivatives QSAR 3D descriptors Monte Carlo variable selection

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Nano Research 2023年第10期16卷 12134-12143页

作者： Limin Yang Linjiao Qu Xiaolong Zhang Mingming Li Zhen Liu State Key Laboratory of Heavy Oil Processing and Center for Bioengineering and Biotechnology China University of Petroleum(East China)Qingdao 266580China Institute of Biomedical Engineering Shenzhen Bay LaboratoryShenzhen 518055Chin

Enzyme-inorganic hybrid nanoflowers(HNFs)have shown excellent sensing capabilities due to their large specific surface area as well as the simplicity and mildness of the preparation ***,coupling HNFs to electrodes to fabricate a uniform and controllable enzymatic electrochemical sensing interface remains a ***,we proposed an aptamer-induced insitu fabrication strategy for preparing an HNF-based electrochemical sensor with ideal *** to this strategy is the introduction of acetylcholinesterase(AChE)-specific binding aptamer(Apt),which induces the in-situ growth of AChE-copper phosphate(Cu_(3)(PO_(4))_(2))HNFs on the surface of carbon paper(CP).In addition,a dense gold nanoparticle(AuNP)layer was electrodeposited on the CP for anchoring Apt and further extending the electroactive surface *** prepared AChECu_(3)(PO_(4))_(2)HNF/Apt/AuNP/CP biosensor exhibited a wide detection range from 1 to 107 pM for the four organophosphorus inhibitors,including isocarbophos,dichlorvos,methamidophos,and parathion,with detection limits down to 0.016,0.028,0.071,and 0.113 pM,*** the reactivation of pralidoxime chloride,the electrode can still recover 98.1%of the response after five times of repeated *** real sample detection,the biosensor achieved high recoveries from 96.45%to 100.13%.The detection target may be extendable to other AChE inhibitors(e.g.,drugs for Alzheimer’s disease).This study demonstrates for the first time the feasibility of using aptamers as an inducer to fabricate an electrochemical enzyme sensing interface *** strategy can be used to fabricate other enzyme-based biosensors and therefore has broader applications.

关键词： in-situ fabrication aptamer enzyme-inorganic hybrid nanoflowers electrochemical biosensor acetylcholinesterase inhibitors

Highly Sensitive Fluorometric Assay Method for Acetylcholine- sterase Inhibitor Based on Nile Red-Adsorbed Gold Nanoparticles

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Chinese Journal of Chemistry 2013年第8期31卷 1072-1078页

作者： Wenting Han Shuzhen Liao Chonghua Zhang Huazhi Ding Zhaoyang Wu[*] Guoli Shen Ruqin Yu State Key Laboratory of Chemo/Biosensing and Chemometrics College of Chemistry and Chemical Engineering Hunan University Changsha Hunan 410082 China Email: Zhaoyang Wu (zywu@***)[*]State Key Laboratory of Chemo/Biosensing and Chemometrics College of Chemistry and Chemical Engineering Hunan University Changsha Hunan 410082 China Tel. 0086-0731-88821989

A new sensitive fluorometric assay method for acetylcholinesterase （ACHE） and its inhibitor was developed us- ing a fluorescent dye, nile red （NR）. Due to the fluorescence resonance energy transfer between the NR and the gold nanoparticle （AuNPs）, the fluorescence was quenched. AChE can break down acetylthiocholine to produce a thiol-bearing compound, thiocholine. In the presence of thiocholine, the nile red is replaced from the AuNPs sur- faces and simultaneously transformed to a derivative of nile red. The fluorescence intensity of the derivative is much stronger than that of the native nile red with the same concentration and its maximum emission wavelength has a blue shift so that the sensor achieves a good signal-to-background ratio. In addition, when organophosphate pesticide （OPs） exists, the activity of AChE can be inhibited, the generation of thiocholine will be prevented and no fluorescence enhancement occurs. The results show that the method is sensitive to AChE and paraoxon with the de- tection limits of 0.2 mU/mL and 0.05 ng/mL, respectively.

关键词： nile red gold nanoparticle fluorescence acetylcholinesterase inhibitors

The protective role of tacrine and donepezil in the retina of acetylcholinesterase knockout mice

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International Journal of Ophthalmology(English edition) 2015年第5期8卷 884-890页

作者： Yun-Min Yi Li Cai Yi Shao Man Xu Jing-Lin Yi Affiliated Eye Hospital of Nanchang University Jiangxi Research Institute of Ophthalmology and Visual Sciences Department of Ophthalmology the First Affiliated Hospital of Nanchang University

AIM: To determine the effect of different concentrations of the acetylcholinesterase (AChE) inhibitors tacrine and donepezil on retinal protection in AChE(+/-) mice (AChE knockout mice) of various ages. METHODS: Cultured ARPE -19 cells were treated with hydrogen peroxide (H2O2) at concentrations of 0, 250, 500, 1000 and 2000 mu mol/L and protein levels were measured using Western blot. Intraperitoneal injections of tacrine and donepezil (0.1 mg/mL, 0.2 mg/mL and 0.4 mg/mL) were respectively given to AChE4- mice aged 2mo and 4mo and wild-type S129 mice for 7d; phosphate buffered saline (PBS) was administered to the control group. The mice were sacrificed after 30d by cardiac perfusion and retinal samples were taken. AChE(+/-) deficient mice were identified by polymerase chain reaction (PCR) analysis using specific genotyping protocols obtained from the Jackson Laboratory website. H&E staining, immunofluorescence and Western blot were performed to observe AChE protein expression changes in the retinal pigment epithelial (RPE) cell layer. RESULTS: Different concentrations of H2O2 induced AChE expression during RPE cell apoptosis. AChE(+/-) mice retina were thinner than those in wild -type mice (P0.05). CONCLUSION: in viva, tacrine and donepezil can inhibit the expression of AChE; the decrease of AChE expression in the retina is beneficial for the development of the retina.

关键词： retinal pigment epithelium acetylcholinesterase apoptosis AChE(+/-) animal models acetylcholinesterase inhibitors

Third degree atrioventricular block associated with treatment with rivastigmine transdermal patch

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Journal of Geriatric Cardiology 2013年第1期10卷 113-115页

作者： Fredrikke C. Knudtzen Thomas B. Christophersen Department of Internal Medicine OUH Svendborg Hospital Valdemarsgade 53 5700 Svendborg Denmark

Rivastigmine transdermal patch is indicated for patientswithAlzheimer’s disease and dementia with Parkinson’s disease. Rivastigmine, an acetylcholinesterase inhibitor, has several common adverse effects, mainly involving the gastrointestinal tract, but few cardiovascular adverse effects have been reported. This report presents two cases of patients presenting with 3rd degree atrioventricular block. Both patients were treated with the acetylcholinesterase inhibitor, rivastigmine. In one case, the patient reverted to normal sinus rhythm following the discontinuation of rivastigmine, and the atrioventricular block reappeared after rivastigmine was reinstated. In the other case, the atrioventricular block did not revert and the patient required a permanent pacemaker. Both bradycardia and syncope have previously been reported as adverse events in patients treated with acetylcholinesterase inhibitors. However, the type of bradycardia and the etiology of the syncope are rarely specified. Rivastigmine, and other acetylcholinesterase inhibitors, are widely used in the pharmacological treatment of Alzheimer��s disease. We recommend that physicians are vigilant of possible warning signs, such as dizziness, syncope and bradycardia.

关键词： acetylcholinesterase inhibitors Alzheimer's disease Atrioventricular block Rivastigmine

Fungal symbionts of marine sponges from Rameswaram,southern India:species composition and bioactive metabolites

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Fungal Diversity 2012年第4期55卷 37-46页

作者： Nagamani Thirunavukkarasu Trichur S.Suryanarayanan Kozhikottu P.Girivasan Ambayeram Venkatachalam Venkatachalam Geetha Jagadesan P.Ravishankar Mukesh Doble Department of Plant Biology and Plant Biotechnology Ramakrishna Mission Vivekananda CollegeMylaporeChennai 600004India Vivekananda Institute of Tropical Mycology(VINSTROM) Ramakrishna Mission VidyapithMylaporeChennai 600004India Department of Plant Biology and Plant Biotechnology Government Arts College for Men(Autonomous)NandanamChennai 600035India Department of Biotechnology Indian Institute of Technology of MadrasChennai 600025India

Ten marine sponge species from Rameswaram,southern India were studied for their filamentous fungal *** results suggest that fungal symbionts of marine sponges are *** such as Acremonium,Alternaria,Aspergillus,Cladosporium,Fusarium and Penicillium were frequently isolated;no true marine fungal species were *** of Aspergillus were dominant and co-dominant in all the sponges *** fungal isolates produced antialgal,antifungal,antioxidant,antibiotic,antiinsect metabolites.A few fungi produced acetylcholinesterase inhibitors.

关键词： Marine sponge Sponge symbionts Fungal symbionts Bioactive compounds acetylcholinesterase inhibitors

Examination of Urinary Chlorpyrifos Biomarker Concentrations and Heart Rate in a Sample of US Children and Adolescents

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Occupational Diseases and Environmental Medicine 2020年第4期8卷 163-174页

作者： Alex LeBeau Desirae Sutherland Marie Bourgeois Jeffrey Driver Raymond Harbison Center for Environmental and Occupational Risk Analysis and Management College of Public Health University of South Florida Tampa Florida USA

Objective: The purpose of the investigation is to determine if a relationship exists between heart rate and urinary biomarkers of chronic, subacute chlorpyrifos pesticide exposure in youth. Methods: Using 2001-2002 NHANES data, a sample of 1233 children ages 6 - 18 was grouped based on detection status of 3,5,6-trichloropyridinol (TCPy) in urine. Radial pulse and brachial pulse were recorded as measures of heart rate by physicians. T-tests and linear regression analyses were performed to test for associations between TCPy concentrations and heart rate. Results: None of the associations between TCPy levels and heart rate outcomes were found to be significant. Nonsignificant effects in the TCPy-detected groups included a slightly reduced heart rate in girls, as well as a slightly elevated heart rate in boys when compared to the undetected controls. Neither was there any significant observable difference in heart rate due to detection status in the sample overall. Conclusions: At this time, an effect on heart rate attributable to chronic, low-level chlorpyrifos exposure in youth cannot be determined. Children and adolescents detected did not demonstrate a substantial change in pulse measures when compared to controls. It is recommended that subsequent studies examine chlorpyrifos biomarkers as they may relate to other indicators of cardiovascular health.

关键词： Chlorpyrifos Organophosphates Pesticides acetylcholinesterase inhibitors TCPy Heart Rate Pulse Cardiovascular Exposure Urinary Metabolites Children Youth Adolescents

Advances in the study of Alzheimer's disease

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Journal of Nanjing Medical University 2005年第6期19卷 279-283页

作者： Angue Nkoghe Francoise Department of Pharmacology China Pharmaceutical UniversityNanjing 210009 P.R.China.

Alzheimer＇ s disease （AD） is the most common cause of dementia, and the only treatment currently available for the disease is acetylcholinesterase inhibitors. Recent progress in understanding the molecular and cellular pathophysiology of Alzheimer＇s disease has suggested possible pharmacological interventions, including acetylcholineseterase inhibitors; secretase inhibitors; cholesterol lowering drugs; metal chelators and amyloid immunization. The objective of this paper is to review the main drugs possibly used for AD and their future therapeutic effects.

关键词： Alzheimer disease acetylcholinesterase inhibitors secretase inhibitors cholesterol lowering drugs metal chelators amyloid immunization