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Modulation of rabbit muscle sarcoplasmic reticulum Ca(2+)-ATPase activity by novel quercetin derivatives.

Blaškovič D, Zižková P, Držík F, Viskupičová J, Veverka M, Horáková L - Interdiscip Toxicol (2013)

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: Institute of Experimental Pharmacology and Toxicology, Slovak Academy of Sciences, Dúbravská cesta 9, 841 01 Bratislava, Slovak Republic.

ABSTRACT
Sarcoplasmic reticulum Ca(2+)-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.

No MeSH data available.


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Effect of quercetin or its derivatives on SERCA activity. Values are mean ± SEM and represent three independent experiments with at least three parallels. The statistical analysis of the data was performed using un-paired ANOVA test with Turkey comparison. ***p<0.001, control versus treated SERCA
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Figure 0001: Effect of quercetin or its derivatives on SERCA activity. Values are mean ± SEM and represent three independent experiments with at least three parallels. The statistical analysis of the data was performed using un-paired ANOVA test with Turkey comparison. ***p<0.001, control versus treated SERCA

Mentions: Quercetin had little effect on SERCA activity up to 100 µM. We observed slight inhibition of SERCA by quercetin at 150 µM (Figure 1B). Figure 1A shows that 5-morpholinohydroxypropoxyQ, di(prenylferuloyl)Q, di(diacetylcaffeoyl)-mono-(monoacetylcaffeoyl)Q and monoacetylferuloylQ stimulated SERCA activity. MonochloropivaloylQ, tri(chloropivaloyl)Q and diquercetin remarkably inhibited SERCA activity (Figure 1B). Tri(trimethylgalloyl)Q and pentaacetylQ inhibited the pump slightly.


Modulation of rabbit muscle sarcoplasmic reticulum Ca(2+)-ATPase activity by novel quercetin derivatives.

Blaškovič D, Zižková P, Držík F, Viskupičová J, Veverka M, Horáková L - Interdiscip Toxicol (2013)

Effect of quercetin or its derivatives on SERCA activity. Values are mean ± SEM and represent three independent experiments with at least three parallels. The statistical analysis of the data was performed using un-paired ANOVA test with Turkey comparison. ***p<0.001, control versus treated SERCA
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3795314&req=5

Figure 0001: Effect of quercetin or its derivatives on SERCA activity. Values are mean ± SEM and represent three independent experiments with at least three parallels. The statistical analysis of the data was performed using un-paired ANOVA test with Turkey comparison. ***p<0.001, control versus treated SERCA
Mentions: Quercetin had little effect on SERCA activity up to 100 µM. We observed slight inhibition of SERCA by quercetin at 150 µM (Figure 1B). Figure 1A shows that 5-morpholinohydroxypropoxyQ, di(prenylferuloyl)Q, di(diacetylcaffeoyl)-mono-(monoacetylcaffeoyl)Q and monoacetylferuloylQ stimulated SERCA activity. MonochloropivaloylQ, tri(chloropivaloyl)Q and diquercetin remarkably inhibited SERCA activity (Figure 1B). Tri(trimethylgalloyl)Q and pentaacetylQ inhibited the pump slightly.

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: Institute of Experimental Pharmacology and Toxicology, Slovak Academy of Sciences, Dúbravská cesta 9, 841 01 Bratislava, Slovak Republic.

ABSTRACT
Sarcoplasmic reticulum Ca(2+)-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.

No MeSH data available.


Related in: MedlinePlus