Synthesis of two 7,8-dioxabicyclo[4.1.1]octan-3-yl)-steroid derivatives and evaluation of their inotropic activity in an animal model

Autor:	Diaz Cedillo Francisco, Borges Yaritza, Rosas Marcela, Mateu Armand Virginia, Figueroa Lauro, Lopez Maria, Garcimarrero Alejandra
Rok vydání:	2020
Předmět:	Inotrope biology Chemistry Chemical structure medicine.medical_treatment Calcium channel Mühendislik Pharmacology In vitro Steroid Nitric oxide synthase Engineering Nifedipine medicine biology.protein Ventricular pressure Steroid dioxabicyclo inotropic medicine.drug
Zdroj:	Volume: 48, Issue: 1 1-12 Hacettepe Journal of Biology and Chemistry
ISSN:	2687-475X
DOI:	10.15671/hjbc.602029
Popis:	The aim of this study was synthesizing two 7,8-dioxabicyclo[4.1.1]octan-3-yl)-steroid derivatives (compounds 3 or 4) to evaluate their inotropic activity in vitro. The first stage was achieved by the preparation of two 7,8-dioxabicyclo[4.1.1]octan-3-yl)-steroid derivatives using some chemical strategies. Then, the inotropic activity of both steroid derivatives against left ventricular pressure (LVP) was evaluated in an isolated rat heart model using Bay-k-8644, nifedipine, aucubin, and L-NAME as controls. The results showed that compound 3 increased LVP in a dose-dependent manner and this effect was inhibited by nifedipine. Other results showed that compound 4 decreased LVP in a dose-dependent manner and this effect was blocked in the presence of L-NAME. All these data indicate that 1) the positive inotropic activity exerted by compound 3 was through type L calcium channel activation; 2) the negative inotropic effect of 4 was via nitric oxide synthase activation. These phenomena could be due to the different functional groups involved in the chemical structure of compounds 3 and 4.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3afec37346b9615a1f7134b7ff8c74eb https://doi.org/10.15671/hjbc.602029 Zobrazit plný text záznamu