ArticleBritish journal of pharmacology2011
The flavonoid scaffold as a template for the design of modulators of the vascular Ca(v) 1.2 channels.
Article in British journal of pharmacology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 55 citations in OpenAlex.
- EGCG and Taxifolin Modulate Secretory Activity and Expression of Dentinogenesis Markers in Odontoblast-Like Cells.Scientifica · 2025Article
- Bioguided Identification of Polymethoxyflavones as Novel Vascular CaMolecules (Basel, Switzerland) · 2024Article
- Natural L-type calcium channels antagonists from Chinese medicine.Chinese medicine · 2024Article
- VietnameseMolecules (Basel, Switzerland) · 2022Article
- Extra Virgin Olive Oil Extracts of Indigenous Southern Tuscany Cultivar Act as Anti-Inflammatory and Vasorelaxant Nutraceuticals.Antioxidants (Basel, Switzerland) · 2022Article
- VariousTurkish journal of pharmaceutical sciences · 2020Article
- Predictive QSAR model confirms flavonoids in Chinese medicine can activate voltage-gated calcium (CaV) channel in osteogenesis.Chinese medicine · 2020Article
- The ellagitannin metabolite urolithin C is a glucose-dependent regulator of insulin secretion through activation of L-type calcium channels.British journal of pharmacology · 2019Article
- The Selective Rat Toxicant Norbormide Blocks KFrontiers in pharmacology · 2019Article
- Article
- Geraniol as a novel antivirulence agent against bacillary dysentery-causing Shigella sonnei.Virulence · 2018Article
- Inhibition of transmembrane member 16A calcium-activated chloride channels by natural flavonoids contributes to flavonoid anticancer effects.British journal of pharmacology · 2017Article
- Fisetin Imparts Neuroprotection in Experimental Diabetic Neuropathy by Modulating Nrf2 and NF-κB Pathways.Cellular and molecular neurobiology · 2016Article
- Natural and synthetic flavonoid modulation of TRPC5 channels.British journal of pharmacology · 2016Article
- Wnt/β-catenin coupled with HIF-1α/VEGF signaling pathways involved in galangin neurovascular unit protection from focal cerebral ischemia.Scientific reports · 2015Article
- Pharmacological potential of Populus nigra extract as antioxidant, anti-inflammatory, cardiovascular and hepatoprotective agent.Asian Pacific journal of tropical biomedicine · 2013Article
- Quercetin induces insulin secretion by direct activation of L-type calcium channels in pancreatic beta cells.British journal of pharmacology · 2013Article
- Mouse sperm membrane potential hyperpolarization is necessary and sufficient to prepare sperm for the acrosome reaction.The Journal of biological chemistry · 2012Article
- By improving regional cortical blood flow, attenuating mitochondrial dysfunction and sequential apoptosis galangin acts as a potential neuroprotective agent after acute ischemic stroke.Molecules (Basel, Switzerland) · 2012Article
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5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposePrevious studies have pointed to the plant flavonoids myricetin and quercetin as two structurally related stimulators of vascular Ca(v) 1.2 channel current (I(Ca1.2) ). Here we have tested the proposition that the flavonoid structure confers the ability to modulate Ca(v) 1.2 channels. EXPERIMENTAL APPROACH: Twenty-four flavonoids were analysed for their effects on I(Ca1.2) in rat tail artery myocytes, using the whole-cell patch-clamp method. KEY
resultsMost of the flavonoids stimulated or inhibited I(Ca1.2) in a concentration- and voltage-dependent manner with EC(50) values ranging between 4.4 µM (kaempferol) and 16.0 µM (myricetin) for the stimulators and IC(50) values between 13.4 µM (galangin) and 100 µM [(±)-naringenin] for the inhibitors. Key structural requirements for I(Ca1.2) stimulatory activity were the double bond between C2 and C3 and the hydroxylation pattern on the flavonoid scaffold, the latter also determining the molecular charge, as shown by molecular modelling techniques. Absence of OH groups in the B ring was key in I(Ca1.2) inhibition. The functional interaction between quercetin and either the stimulator myricetin or the antagonists resokaempferol, crysin, genistein, and 5,7,2'-trihydroxyflavone revealed that quercetin expressed the highest apparent affinity, in the low µM range, for Ca(v) 1.2 channels. Neither protein tyrosine kinase nor protein kinase Cα were involved in quercetin-induced stimulation of I(Ca1.2). CONCLUSIONS AND IMPLICATIONS: Quercetin-like plant flavonoids were active on vascular Ca(v)1.2 channels. Thus, the flavonoid scaffold may be a template for the design of novel modulators of vascular smooth muscle Ca(v)1.2 channels, valuable for the treatment of hypertension and stroke.
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