dc.contributor.author | Vrabec, Rudolf | |
dc.contributor.author | Maříková, Jana | |
dc.contributor.author | Ločárek, Miroslav | |
dc.contributor.author | Korábečný, Jan | |
dc.contributor.author | Hulcová, Daniela | |
dc.contributor.author | Hošťálková, Anna | |
dc.contributor.author | Kuneš, Jiří | |
dc.contributor.author | Chlebek, Jakub | |
dc.contributor.author | Kučera, Tomáš | |
dc.contributor.author | Hrabinová, Martina | |
dc.contributor.author | Jun, Daniel | |
dc.contributor.author | Soukup, Ondřej | |
dc.contributor.author | Andrisano, Vincenza | |
dc.contributor.author | Jenčo, Jaroslav | |
dc.contributor.author | Šafratová, Marcela | |
dc.contributor.author | Nováková, Lucie | |
dc.contributor.author | Opletal, Lubomír | |
dc.contributor.author | Cahlíková, Lucie | |
dc.date.issued | 2022 | |
dc.identifier.uri | https://hdl.handle.net/20.500.14178/1705 | |
dc.description.abstract | One undescribed indole alkaloid together with twenty-two known compounds have been isolated from aerial parts of Vinca minor L. (Apocynaceae). The chemical structures of the isolated alkaloids were determined by a combination of MS, HRMS, 1D, and 2D NMR techniques, and by comparison with literature data. The NMR data of several alkaloids have been revised, corrected, and missing data have been supplemented. Alkaloids isolated in sufficient quantity were screened for their in vitro acetylcholinesterase (AChE; E.C. 3.1.1.7) and butyrylcholinesterase (BuChE; E.C. 3.1.1.8) inhibitory activity. Selected compounds were also evaluated for prolyl oligopeptidase (POP; E.C. 3.4.21.26), and glycogen synthase 3 beta-kinase (GSK-3 beta; E.C. 2.7.11.26) inhibition potential. Significant hBuChE inhibition activity has been shown by (-)-2-ethyl-3[2-(3-ethylpiperidinyl)-ethyl]-1H-indole with an IC50 value of 0.65 +/- 0.16 mu M. This compound was further studied by enzyme kinetics, along with in silico techniques, to reveal the mode of inhibition. This compound is also predicted to cross the blood-brain barrier (BBB) through passive diffusion. | en |
dc.language.iso | en | |
dc.relation.url | http://www.sciencedirect.com/science/article/pii/S0031942221003666 | |
dc.rights | Creative Commons Uveďte původ-Neužívejte dílo komerčně-Nezpracovávejte 4.0 International | cs |
dc.rights | Creative Commons Attribution-NonCommercial-NoDerivativeWorks 4.0 International | en |
dc.title | Monoterpene indole alkaloids from Vinca minor L. (Apocynaceae): Identification of new structural scaffold for treatment of Alzheimer's disease | en |
dcterms.accessRights | openAccess | |
dcterms.license | https://creativecommons.org/licenses/by-nc-nd/4.0/legalcode | |
dc.date.updated | 2023-10-02T06:14:38Z | |
dc.subject.keyword | Vinca minor | en |
dc.subject.keyword | Apocynaceae | en |
dc.subject.keyword | Alzheimer's disease | en |
dc.subject.keyword | Docking studies | en |
dc.subject.keyword | Alkaloids | en |
dc.subject.keyword | Butyrylcholinesterase | en |
dc.subject.keyword | Vincaminorudeine | en |
dc.subject.keyword | (-)-2-ethyl-3[2-(3-ethylpiperidinyl)-ethyl]-1H-indole | en |
dc.relation.fundingReference | info:eu-repo/grantAgreement/MSM/EF/EF16_018/0002736 | |
dc.relation.fundingReference | info:eu-repo/grantAgreement/GA0/GC/GC20-29633J | |
dc.relation.fundingReference | info:eu-repo/grantAgreement/UK/COOP/COOP | |
dc.relation.fundingReference | info:eu-repo/grantAgreement/UK/SVV/SVV260550 | |
dc.date.embargoStartDate | 2023-10-02 | |
dc.type.obd | 73 | |
dc.type.version | info:eu-repo/semantics/publishedVersion | |
dc.identifier.doi | 10.1016/j.phytochem.2021.113017 | |
dc.identifier.utWos | 000723419500004 | |
dc.identifier.eidScopus | 2-s2.0-85119275604 | |
dc.identifier.obd | 611439 | |
dc.identifier.riv | RIV/00216208:11160/22:10443781 | |
dc.identifier.riv | RIV/00179906:_____/22:10443781 | |
dc.identifier.pubmed | 34798410 | |
dc.subject.rivPrimary | 30000::30100::30104 | |
dcterms.isPartOf.name | Phytochemistry | |
dcterms.isPartOf.issn | 0031-9422 | |
dcterms.isPartOf.journalYear | 2022 | |
dcterms.isPartOf.journalVolume | 194 | |
dcterms.isPartOf.journalIssue | February | |
uk.faculty.primaryId | 113 | |
uk.faculty.primaryName | Farmaceutická fakulta v Hradci Králové | cs |
uk.faculty.primaryName | Faculty of Pharmacy in Hradec Kralove | en |
uk.faculty.secondaryId | 51 | |
uk.faculty.secondaryName | Fakultní nemocnice Hradec Králové | cs |
uk.faculty.secondaryName | University Hospital Hradec Králové | en |
uk.department.primaryId | 113 | |
uk.department.primaryName | Farmaceutická fakulta v Hradci Králové | cs |
uk.department.primaryName | Faculty of Pharmacy in Hradec Kralove | en |
uk.department.secondaryId | 368 | |
uk.department.secondaryId | 5000002805 | |
uk.department.secondaryId | 366 | |
uk.department.secondaryId | 100036469221 | |
uk.department.secondaryId | 367 | |
uk.department.secondaryName | Katedra analytické chemie | cs |
uk.department.secondaryName | Department of Analytical Chemistry | en |
uk.department.secondaryName | Centrum biomedicínského výzkumu | cs |
uk.department.secondaryName | Biomedical Research Center | en |
uk.department.secondaryName | Katedra organické a bioorganické chemie | cs |
uk.department.secondaryName | Department of Organic and Bioorganic Chemistry | en |
uk.department.secondaryName | Katedra farmakognozie a farmaceutické botaniky | cs |
uk.department.secondaryName | Department of Pharmacognosy and Pharmaceutical Botany | en |
uk.department.secondaryName | Katedra farmaceutické botaniky | cs |
uk.department.secondaryName | Department of Pharmaceutical Botany | en |
dc.description.pageRange | nestránkováno | |
dc.type.obdHierarchyCs | ČLÁNEK V ČASOPISU::článek v časopisu::původní článek | cs |
dc.type.obdHierarchyEn | JOURNAL ARTICLE::journal article::original article | en |
dc.type.obdHierarchyCode | 73::152::206 | en |
uk.displayTitle | Monoterpene indole alkaloids from Vinca minor L. (Apocynaceae): Identification of new structural scaffold for treatment of Alzheimer's disease | en |