Dissociation of Phospholamban Regulation of Cardiac Sarcoplasmic Reticulum Ca2+ATPase by Quercetin

McKenna, Edward J.; Smith, Jeffrey S.; Coll, Kathleen E.; Mazack, E K; Mayer, Ernest; Antanavage, Joanne; Wiedmann, Richard T.; Johnson, Robert G.

doi:10.1074/jbc.271.40.24517

Cited by 40 publications

(29 citation statements)

References 38 publications

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“…Several¯avones have been shown to interact with other ATPases, such as Ca 2+ -ATPase (McKenna et al, 1996) and Na + /K + -ATPase (Hirano et al, 1989), in addition to their eects on F0F1-ATPase (Lang & Racker, 1974;Di Pietro et al, 1975). However, resveratrol and genistein had little eect on Na + /K + -ATPase, as shown in Figure 5.…”

Section: Discussionmentioning

confidence: 92%

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Inhibition of mitochondrial proton F0F1‐ATPase/ATP synthase by polyphenolic phytochemicals

Zheng¹,

Ramírez²

2000

British J Pharmacology

401

291

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1 Mitochondrial proton F0F1-ATPase/ATP synthase synthesizes ATP during oxidative phosphorylation. In this study, we examined the eects of several groups of polyphenolic phytochemicals on the activity of the enzyme. 2 Resveratrol, a stilbene phytoalexin that is present in grapes and red wine, concentrationdependently inhibited the enzymatic activity of both rat brain and liver F0F1-ATPase/ATP synthase (IC 50 of 12 ± 28 mM). 3 Screening of other polyphenolic phytochemicals using rat brain F0F1-ATPase activity resulted in the following ranking potency (IC 50 in parenthesis): piceatannol (8 mM)4resveratrol (19 mM)= (7)epigallocatechin gallate (17 mM)4(7)epicatechin gallate, curcumin (45 mM)4genistein=biocha-nin A=quercetin=kaempferol=morin (55 ± 65 mM)4phloretin=apigenin=daidzein (approx. 100 mM). Genistin, quercitrin, phloridzin, (+)catechin, (+)epicatechin, (7)epicatechin and (7)epigallocatechin had little eect at similar concentrations. Tannic acid, thea¯avins (tea extract) and grape seed proanthocyanidin extract (GSPE) had IC 50 values of 5, 20 and 30 mg ml 71 , respectively. Several monophenolic antioxidants and non-phenolic compounds were ineective at concentrations of 210 mM or higher. 4 The inhibition of F0F1-ATPase by resveratrol and genistein was non-competitive in nature. 5 The eects of polyphenolic phytochemicals were additive. 6 Both resveratrol and genistein had little eect on the Na + /K + -ATPase activity of porcine cerebral cortex, whereas quercetin had similar inhibitory potency as for F0F1-ATPase. 7 In conclusion, the ATP synthase is a target for dietary phytochemicals. This pharmacological property of these phytochemicals should be included in the examination of their health bene®ts as well as potential cytotoxicity.

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Section: Discussionmentioning

confidence: 92%

“…-ATPase and more than a dozen other enzymes (Fewtrell & Gomperts, 1977;Ferrell et al, 1979;Hirano et al, 1989;McKenna et al, 1996).…”

Section: Introductionmentioning

confidence: 99%

Inhibition of mitochondrial proton F0F1‐ATPase/ATP synthase by polyphenolic phytochemicals

Zheng¹,

Ramírez²

2000

British J Pharmacology

401

291

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“…Many reports show that the effect of polyphenols on the endothelium is mainly due to NO production (Andriambeloson et al, 1997;Duarte et al, 2004;Zenebe et al, 2003), increase in intracellular concentration of Ca 2+ ([Ca 2+ ]i), activation of K + channels in the endothelium, inhibition of Ca 2+ -ATPases of the endoplasmic reticulum in endothelial cells (Li et al, 2000;McKenna et al, 1996), or modulation of NO levels by the action on the phosphodiesterases (PDE) PDE-2 and PDE-4 in endothelial cells (Beretz et al, 1986a;Beretz et al, 1986b;Lugnier & Schini, 1990).…”

Section: Discussionmentioning

confidence: 99%

Effects of extract, fractions and 2,3-dihydromyricetin-3-O-α-L-rhamnoside from Pradosia huberi (Ducke) Ducke on rat isolated mesenteric arteries

Medeiros

Queiroz³

et al. 2010

Rev. bras. farmacogn.

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RESUMO: "Efeito do extrato, frações e da 2,3-diidromiricetina-3-O-α-L-raminosídeo obtidos da Pradosia huberi (Ducke) Ducke em artéria mesentérica isolada de rato". Pradosia huberi (Ducke) Ducke (Sapotaceae), espécie Amazônica popularmente conhecida como "casca-doce" é utilizada na medicina tradicional no tratamento de gastrite. O extrato etanólico de suas cascas é rico em polifenóis que podem apresentar um grande número de atividades, incluindo efeito vasorelaxante e cardioprotetor. O objetivo deste estudo foi avaliar as propriedades farmacológicas do extrato etanólico (EPH), de frações e da 2,3-diidromiricetina-3-O-α-L-raminosídeo isolados de P. huberi, em artéria mesentérica isolada de rato. O EPH foi fracionado resultando nas seguintes frações: CHCl 3 , CHCl 3 :AcOEt (1:1), AcOEt, AcOEt:MeOH (1:1) e MeOH. Da fração MeOH foi isolada a 2,3-diidromiricetina-3-O-α-L-raminosídeo e identificada através de espectro de RMN de 1 H e 13 C, além de comparações com os dados de literatura. EPH (1-100 μg/mL) promoveu relaxamento dependente de concentração no tônus vascular induzido por 10 μM de fenilefrina (CE 50 =17,1±2,9 µg/ mL; E max =87,4±2,9 %, n=8). A fração MeOH também relaxou os anéis mesentéricos (CE 50 =31±2,0 µg/mL; E max =54±12,5%, n=6), porém com menor eficácia quando comparado ao efeito de EPH. Unitermos: Pradosia huberi, artéria mesentérica, vasodilatação, endotélio dependente, 2,3-diidromiricetina-3-O-α-L-raminosídeo, floresta amazônica.ABSTRACT: Pradosia huberi (Ducke) Ducke (Sapotaceae), an Amazonian species, is popularly known as "casca-doce" and used in the folk medicine for the treatment of gastritis. The ethanol extract of the bark contains mainly polyphenolic compounds, which are known to show a large number of activities, including cardioprotective and vasorelaxant effects. The aim of this study was to evaluate the pharmacological properties induced by P. huberi ethanol extract (PHEE) and fractions and 2-3-dihydromyricetin-3-O-α-L-rhamnoside derived from this extract, in isolated rat mesenteric arteries. PHEE was separated and the following fractions were obtained: CHCl 3 , CHCl 3 :AcOEt (1:1), AcOEt, AcOEt:MeOH (1:1) and MeOH. We isolated 2-3-dihydromyricetin-3-O-α-L-rhamnoside from the MeOH fraction, which was identified by 1 H and 13 C NMR spectra and compared with data in the literature. PHEE (1-100 μg/mL) induced concentration-dependent relaxations of 10 μM phenylephrine-induced tone (EC 50 =17,1±2,9 µg/mL; E max =87.4±2.9 %, n=8). The MeOH fraction also relaxed mesenteric rings (EC 50 =31±2.0 μg/mL; E max =54±12.5%, n=6) but less effectively when compared to PHEE. Both effects were completely abolished after removal of the vascular endothelium. The AcOEt:MeOH (1:1) fraction and the isolated flavonoid were ineffective in eliciting vasorelaxation. The study demonstrates that PHEE and MeOH fraction of Pradosia huberi possess a vasorelaxant effect, which may be completely dependent upon endothelium. The isolated flavonoid is not responsible for this vasorelaxant effect.

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“…Therefore the level of SERCA phosphoenzyme can be used to estimate the active SERCA pump level, which reflects the availability of SR Ca 2ϩ ATPase molecules to transport Ca 2ϩ (39,40). To our knowledge there are no reports on using cardiac tissue homogenates for the measurement of SERCA E-P level.…”

Section: The Formation Of Serca E-p Can Be Measured In Cardiac Homogementioning

confidence: 99%

Analysis of Sarcoplasmic Reticulum Ca2+Transport and Ca2+ATPase Enzymatic Properties Using Mouse Cardiac Tissue Homogenates

Loukianov

Periasamy

1999

Analytical Biochemistry

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Dissociation of Phospholamban Regulation of Cardiac Sarcoplasmic Reticulum Ca2+ATPase by Quercetin

Cited by 40 publications

References 38 publications

Inhibition of mitochondrial proton F0F1‐ATPase/ATP synthase by polyphenolic phytochemicals

Inhibition of mitochondrial proton F0F1‐ATPase/ATP synthase by polyphenolic phytochemicals

Effects of extract, fractions and 2,3-dihydromyricetin-3-O-α-L-rhamnoside from Pradosia huberi (Ducke) Ducke on rat isolated mesenteric arteries

Analysis of Sarcoplasmic Reticulum Ca2+Transport and Ca2+ATPase Enzymatic Properties Using Mouse Cardiac Tissue Homogenates

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