Modulation of rabbit muscle sarcoplasmic reticulum Ca2+-ATPase activity by novel quercetin derivatives

Sarcoplasmic reticulum Ca2+-ATPase (SERCA) is the pump crucial for calcium homeostasis and its impairment results in pathologies such as myopathy, heart failure or diabetes. Modulation of SERCA activity may represent an approach to the therapy of diseases with SERCA impairment involvment. Quercetin...

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Main Authors:	Blaškovič, Dušan, Žižková, Petronela, Držík, Filip, Viskupičová, Jana, Veverka, Miroslav, Horáková, Ľubica
Format:	Online
Language:	English
Published:	Slovak Toxicology Society SETOX 2013
Online Access:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3795314/

id	pubmed-3795314
recordtype	oai_dc
spelling	pubmed-37953142013-10-29 Modulation of rabbit muscle sarcoplasmic reticulum Ca2+-ATPase activity by novel quercetin derivatives Blaškovič, Dušan Žižková, Petronela Držík, Filip Viskupičová, Jana Veverka, Miroslav Horáková, Ľubica Original Article Sarcoplasmic reticulum Ca2+-ATPase (SERCA) is the pump crucial for calcium homeostasis and its impairment results in pathologies such as myopathy, heart failure or diabetes. Modulation of SERCA activity may represent an approach to the therapy of diseases with SERCA impairment involvment. Quercetin is flavonoid known to modulate SERCA activity. We examined the effect of nine novel quercetin derivatives on the activity of the pump. We found that 5-morpholinohydroxypoxyquercetin, di(prenylferuoyl)quercetin, di(diacetylcaffeoyl)-mono-(monoacetylcaffeoyl)quercetin and monoacetylferuloylquercetin stimulated the activity of SERCA. On the contrary, monochloropivaloylquercetin, tri(chloropivaloyl)quercetin, pentaacetylquercetin, tri(trimethylgalloyl)quercetin and diquercetin inhibited the activity of the pump. To identify compounds with a potential to protect SERCA against free radicals, we assessed the free radical scavenging activity of quercetin derivatives. We also related lipophilicity, an index of the ability to incorporate into the membrane of sarcoplasmic reticulum, to the modulatury effect of quercetin derivatives on SERCA activity. In addition to its ability to stimulate SERCA, di(prenylferuloyl)quercetin showed excellent radical scavenging activity. Slovak Toxicology Society SETOX 2013-03 2013-03 /pmc/articles/PMC3795314/ /pubmed/24170972 http://dx.doi.org/10.2478/intox-2013-0001 Text en Copyright © 2013 Slovak Toxicology Society SETOX http://creativecommons.org/licenses/by/2.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
repository_type	Open Access Journal
institution_category	Foreign Institution
institution	US National Center for Biotechnology Information
building	NCBI PubMed
collection	Online Access
language	English
format	Online
author	Blaškovič, Dušan Žižková, Petronela Držík, Filip Viskupičová, Jana Veverka, Miroslav Horáková, Ľubica
spellingShingle	Blaškovič, Dušan Žižková, Petronela Držík, Filip Viskupičová, Jana Veverka, Miroslav Horáková, Ľubica Modulation of rabbit muscle sarcoplasmic reticulum Ca2+-ATPase activity by novel quercetin derivatives
author_facet	Blaškovič, Dušan Žižková, Petronela Držík, Filip Viskupičová, Jana Veverka, Miroslav Horáková, Ľubica
author_sort	Blaškovič, Dušan
title	Modulation of rabbit muscle sarcoplasmic reticulum Ca2+-ATPase activity by novel quercetin derivatives
title_short	Modulation of rabbit muscle sarcoplasmic reticulum Ca2+-ATPase activity by novel quercetin derivatives
title_full	Modulation of rabbit muscle sarcoplasmic reticulum Ca2+-ATPase activity by novel quercetin derivatives
title_fullStr	Modulation of rabbit muscle sarcoplasmic reticulum Ca2+-ATPase activity by novel quercetin derivatives
title_full_unstemmed	Modulation of rabbit muscle sarcoplasmic reticulum Ca2+-ATPase activity by novel quercetin derivatives
title_sort	modulation of rabbit muscle sarcoplasmic reticulum ca2+-atpase activity by novel quercetin derivatives
description	Sarcoplasmic reticulum Ca2+-ATPase (SERCA) is the pump crucial for calcium homeostasis and its impairment results in pathologies such as myopathy, heart failure or diabetes. Modulation of SERCA activity may represent an approach to the therapy of diseases with SERCA impairment involvment. Quercetin is flavonoid known to modulate SERCA activity. We examined the effect of nine novel quercetin derivatives on the activity of the pump. We found that 5-morpholinohydroxypoxyquercetin, di(prenylferuoyl)quercetin, di(diacetylcaffeoyl)-mono-(monoacetylcaffeoyl)quercetin and monoacetylferuloylquercetin stimulated the activity of SERCA. On the contrary, monochloropivaloylquercetin, tri(chloropivaloyl)quercetin, pentaacetylquercetin, tri(trimethylgalloyl)quercetin and diquercetin inhibited the activity of the pump. To identify compounds with a potential to protect SERCA against free radicals, we assessed the free radical scavenging activity of quercetin derivatives. We also related lipophilicity, an index of the ability to incorporate into the membrane of sarcoplasmic reticulum, to the modulatury effect of quercetin derivatives on SERCA activity. In addition to its ability to stimulate SERCA, di(prenylferuloyl)quercetin showed excellent radical scavenging activity.
publisher	Slovak Toxicology Society SETOX
publishDate	2013
url	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3795314/
_version_	1612017894545162240

Modulation of rabbit muscle sarcoplasmic reticulum Ca2+-ATPase activity by novel quercetin derivatives

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