Effect of myricetin and other flavonoids on the liver plasma membrane Ca2+ pump kinetics and structure-function relationships

Thiyagarajah, Pangajavalli; Kuttan, S.C.; Lim, Soh Chan; Teo, Tian Seng; Das, N.P.

doi:10.1016/0006-2952(91)90065-d

Cited by 37 publications

(29 citation statements)

References 19 publications

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“…The increase on the maximum contractile response was more evident when PMA was used to induce the contractions. This observation suggests that potentiation induced by myricetin may be related to the activation of protein kinase C. However, myricetin inhibits the ATP-dependent Ca 2+ transport system of rat liver plasma membrane (Thiyagarajah et al, 1991). This inhibition is thought to serve as a mechanism for augmenting or sustaining the elevation of intracellular Ca 2+ that occurs following the release of Ca 2+ from an intracellular store (Pumey, 1990;Chen and Van Breemen, 1993).…”

Section: Discussionmentioning

confidence: 96%

Effects of flavonoids on rat aortic smooth muscle contractility: Structure-activity relationships

Herrera

Zarzuelo

Jiménez

et al. 1996

General Pharmacology: The Vascular System

107

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ABSTRACT. 1. Flavonoidsproducedaconcentration.dependentrelaxationofthecontractileresponses induced by noradrenaline, KCI, or phorbo112-myristate-13-acetate in rat aortic rings. Only the flavonoid with three contiguous hydroxyls in B rings (myricetin), at low concentrations, potentiates the contractions evoked by these agonists.2. The relaxant effects of flavanone on the noradrenaline-induced contractions were potentiated by isoprenaline and those of morin, chrysin, flavanone, and naringenin by sodium nitroprusside.3. Several mechanisms are implicated in the vasodilatory effects of flavonoids: inhibition of protein kinase C; inhibition of cyclic nucleotide phosphodiesterases; and/or decreased Ca z + uptake. OEN PHAP.MAC 27;2:273-277, 1996.

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Section: Discussionmentioning

confidence: 96%

Effects of flavonoids on rat aortic smooth muscle contractility: Structure-activity relationships

Herrera

Zarzuelo

Jiménez

et al. 1996

General Pharmacology: The Vascular System

107

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“…In the past decade, some flavonoids have been implicated in the modulation of P-gp-type MDR in cancers and shown to inhibit a variety of ATP-binding proteins such as plasma membrane ATPase (24,44), cyclic AMP-dependent protein kinase (25), and protein kinase C (17). It is thought that the modulating activity of the flavonoids arises from competitive binding to the NBDs of P-gp through their ability to mimic the adenine moiety of ATP.…”

mentioning

confidence: 99%

Flavonoid Dimers as Bivalent Modulators for Pentamidine and Sodium StiboglucanateResistance in Leishmania

Wong

Chan

Burkett

et al. 2007

Antimicrob Agents Chemother

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Drug resistance by overexpression of ATP-binding cassette (ABC) transporters is an impediment in the treatment of leishmaniasis. Flavonoids are known to reverse multidrug resistance (MDR) in Leishmania and mammalian cancers by inhibiting ABC transporters. Here, we found that synthetic flavonoid dimers with three (compound 9c) or four (compound 9d) ethylene glycol units exhibited a significantly higher reversing activity than other shorter or longer ethylene glycol-ligated dimers, with ϳ3-fold sensitization of pentamidine and sodium stibogluconate (SSG) resistance in Leishmania, respectively. This modulatory effect was dosage dependent and not observed in apigenin monomers with the linker, suggesting that the modulatory effect is due to its bivalent nature. The mechanism of reversal activity was due to increased intracellular accumulation of pentamidine and total antimony in Leishmania. Compared to other MDR modulators such as verapamil, reserpine, quinine, quinacrine, and quinidine, compounds 9c and 9d were the only agents that can reverse SSG resistance. In terms of reversing pentamidine resistance, 9c and 9d have activities comparable to those of reserpine and quinacrine. Modulators 9c and 9d exhibited reversal activity on pentamidine resistance among LeMDR1 ؊/؊ , LeMDR1 ؉/؉ , and LeMDR1-overexpressed mutants, suggesting that these modulators are specific to a non-LeMDR1 pentamidine transporter. The LeMDR1 copy number is inversely related to pentamidine resistance, suggesting that it might be involved in importing pentamidine into the mitochondria. In summary, bivalency could be a useful strategy for the development of more potent ABC transporter modulators and flavonoid dimers represent a promising reversal agent for overcoming pentamidine and SSG resistance in parasite Leishmania.

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“…This agent was recently reported to reduce the cellular content of superoxide anion in both resting and Ca2+-loaded brain neurons [15]. Thiyagarajah et al, [21] reported that the ATPdependent Ca2+ transport system located on the liver plasma membrane and endoplasmic reticulum was inhibited by myricetin. The inhibition induced by this agent could be caused by its interference with the binding of Ca2+ to the Ca2+-binding site, although whether it interferes with the ATP-binding site is not clear.…”

Section: Discussionmentioning

confidence: 99%

Cytochemical Localization of Ca2+-, Mg2+-ATPase on the Limiting Membrane of Peroxisomes Isolated from Renal Tubules of Rats.

Wresdiyati

Makita

1998

Acta Histochem. Cytochem

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Effect of myricetin and other flavonoids on the liver plasma membrane Ca2+ pump kinetics and structure-function relationships

Cited by 37 publications

References 19 publications

Effects of flavonoids on rat aortic smooth muscle contractility: Structure-activity relationships

Effects of flavonoids on rat aortic smooth muscle contractility: Structure-activity relationships

Flavonoid Dimers as Bivalent Modulators for Pentamidine and Sodium StiboglucanateResistance in Leishmania

Cytochemical Localization of Ca2+-, Mg2+-ATPase on the Limiting Membrane of Peroxisomes Isolated from Renal Tubules of Rats.

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