Propargilgrupu saturošo 1,4 - dihidropiridīnu atvasinājumu neiroprotektīvās darbības pētījumi primārajās smadzeņu garozas nervu šūnās
Loading...
Date
Authors
Advisor
Journal Title
Journal ISSN
Volume Title
Publisher
Latvijas Universitāte
Language
N/A
Abstract
Svarīga ir tādu neiroprotektīvu vielu izpēte, kuru darbība būtu vērsta uz mitohondriju
aizsardzību. Darba mērķis bija izpētīt jaunu propargilaizvietotu 1,4-dihidropiridīna atvasinājumu
iespējamo neiroprotektīvo aktivitāti mitohondriju toksicitātes modelī primārajās nervu šūnu
kultūrās.
Iegūtie dati parādīja, ka propargilaizvietotais atvasinājums ESF-M10 un tā struktūras
analogs – ESF-M2, savienojums bez propargilgrupas, neietekmēja 1-metil-4-fenilpiridīna
(MPP+) izraisīto toksicitāti. Propargilaizvietotais atvasinājums D3-72-2 un savienojums bez
propargilgrupas - ESF-M1 izraisīja 100% šūnu nāvi 100 μM koncentrācijā, pievienoti per se un
10 un 100 μM koncentrācijās pievienoti preinkubācijai un kopā ar toksīnu MPP+. Dati parāda, ka
pētīto savienojumu aktivitātēs izmantotajā MPP+ toksicitātes modelī propargilgrupa nespēlē
būtisku lomu.
Atslēgvārdi: propargilgrupa, 1,4-dihidropirīdini, 1-metil-4-fenilpiridīns, neiroprotekcija,
mitohondriju disfunkcija.
Studies of the neuroprotective agents have been targeted on the mitochondrial protection. The aim of our study was to investigate the new propargyl group-containing 1,4-dihydropyridine (DHP) derivatives in mitochondrial toxicity model in primary cortical neurons. Obtained results demonstrated that propargyl group-containing compound ESF-M10 and its structural analog – ESF-M2 (compound without propargyl group) did not effect 1-metil-4- phenylpyridine (MPP+)-induced toxicity. Propargyl group-containing ESF-M10 and its structural analog – ESF-M2 (without propargyl group) induced complete cell death (100%) added (100 μM) per se, as well as added for preincubation and together with MPP+. Data show, that the propargyl group attached to the 1,4-DHP structures did not play the essential role in activities of studied compounds in MPP+ model. Keywords: propargyl group, 1,4-dihydropyridine, 1-methyl-4-phenylpyridinium, neuroprotection, mitochondrial dysfunction.
Studies of the neuroprotective agents have been targeted on the mitochondrial protection. The aim of our study was to investigate the new propargyl group-containing 1,4-dihydropyridine (DHP) derivatives in mitochondrial toxicity model in primary cortical neurons. Obtained results demonstrated that propargyl group-containing compound ESF-M10 and its structural analog – ESF-M2 (compound without propargyl group) did not effect 1-metil-4- phenylpyridine (MPP+)-induced toxicity. Propargyl group-containing ESF-M10 and its structural analog – ESF-M2 (without propargyl group) induced complete cell death (100%) added (100 μM) per se, as well as added for preincubation and together with MPP+. Data show, that the propargyl group attached to the 1,4-DHP structures did not play the essential role in activities of studied compounds in MPP+ model. Keywords: propargyl group, 1,4-dihydropyridine, 1-methyl-4-phenylpyridinium, neuroprotection, mitochondrial dysfunction.