1.4 - dihidropiridīnu efekti uz kalcija kanāliem šūnās
Date
2013
Authors
Otersbergs, Matīss
Journal Title
Journal ISSN
Volume Title
Publisher
Latvijas Universitāte
Abstract
Kalcija antagonisti jeb kalcija kanālu blokatori klīniskajā medicīnā tika ieviesti jau 20 gs. 60os gados. Šodien tās ir vienas no biežāk izrakstītajām zālēm kardiovaskulāro slimību ārstēšanā. 1.4-dihidropiridīns ir visefektīvākais dihidropiridīnu klases kalcija kanālu blokators, kam ir atklātas ne vien asinsspiedienu pazeminošas īpašības, bet arī pretvēža, antioksidanta un antimikrobiālo aģenta īpašības. Darba mērķis bija noteikt jauna 1,4-dihidropiridīna atvasinājuma A3-13 antioksidanta spēju in vitro testā un kalcija kanālu blokatora efektu SH-5YSH šūnu līnijā, kas ekspresē L- un N-tipa kalcija kanālus. Rezultāti rāda, ka A3-13 piemīt neliela (par 6-8%) brīvā radikāļa DPPH līmeņa samazināšanas spēja, kas raksturo tā antioksidanta potenciālu. A3-13 nepiemīt kalcija kanālu agonista īpašības, bet ar IC50 koncentrācijā 9 ± 3 μM šis savienojums uzrāda kalcija kanālu antagonista īpašības.
Calcium antagonists or calcium channel blockers in clinical medicine were introduced in the late 20th century. Today they are among the most frequently prescribed drugs for the treatment of cardiovascular diseases. 1.4-Dihydropyridine is the most effective member of the dihydropyridine class calcium channel blockers, which is prescribed not only for the blood pressure lowering, but also as anti-tumor, anti-oxidant and anti-microbial agent. The aim of the study was to investigate antioxidant capacity of a new 1,4-dihydropyridine derivative A3-13 in vitro DPPH assay and calcium channel blocking effect in SH-5YSH cell line, expressing L-and N-type calcium channels. The results show that the A3-13 has a low (about 6-8%) free radical DPPH scavenging effect that is characterized as its antioxidant potential. A3-13 does not possess calcium channel agonist properties, but with IC50 concentration of 9 ± 3 μM this compound shows calcium channel antagonist properties.
Calcium antagonists or calcium channel blockers in clinical medicine were introduced in the late 20th century. Today they are among the most frequently prescribed drugs for the treatment of cardiovascular diseases. 1.4-Dihydropyridine is the most effective member of the dihydropyridine class calcium channel blockers, which is prescribed not only for the blood pressure lowering, but also as anti-tumor, anti-oxidant and anti-microbial agent. The aim of the study was to investigate antioxidant capacity of a new 1,4-dihydropyridine derivative A3-13 in vitro DPPH assay and calcium channel blocking effect in SH-5YSH cell line, expressing L-and N-type calcium channels. The results show that the A3-13 has a low (about 6-8%) free radical DPPH scavenging effect that is characterized as its antioxidant potential. A3-13 does not possess calcium channel agonist properties, but with IC50 concentration of 9 ± 3 μM this compound shows calcium channel antagonist properties.
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Keywords
Farmācija