Vasodilation and Blood Pressure-Lowering Effect of 3-Demethyl-2-Geranyl-4-Prenylbellidifoline, a Xanthone Obtained from <i>Garcinia achachairu</i>, in Hypertensive Rats
3-demethyl-2-geranyl-4-prenylbellidifoline (DGP), a natural xanthone isolated from <i>Garcinia achachairu</i>, has previously demonstrated remarkable diuretic and renal protective actions. The present study expands its actions on the cardiovascular system by evaluating its vasorelaxant a...
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MDPI AG
2024-02-01
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| Series: | Plants |
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| author | Luísa Nathália Bolda Mariano Rita de Cássia Vilhena da Silva Rivaldo Niero Valdir Cechinel Filho José Eduardo da Silva-Santos Priscila de Souza |
| author_facet | Luísa Nathália Bolda Mariano Rita de Cássia Vilhena da Silva Rivaldo Niero Valdir Cechinel Filho José Eduardo da Silva-Santos Priscila de Souza |
| author_sort | Luísa Nathália Bolda Mariano |
| collection | DOAJ |
| description | 3-demethyl-2-geranyl-4-prenylbellidifoline (DGP), a natural xanthone isolated from <i>Garcinia achachairu</i>, has previously demonstrated remarkable diuretic and renal protective actions. The present study expands its actions on the cardiovascular system by evaluating its vasorelaxant and blood pressure-lowering effects in spontaneously hypertensive rats (SHRs). Aortic endothelium-intact (E+) preparations of SHRs pre-contracted by phenylephrine and exposed to cumulative concentrations of <i>G. achachairu</i> extract, fractions, and DGP exhibited a significant relaxation compared to vehicle-only exposed rings. The non-selective muscarinic receptor antagonist (atropine), the non-selective inhibitor of nitric oxide synthase (L-NAME), as well as the inhibitor of soluble guanylate cyclase (ODQ) altogether avoided DGP-induced relaxation. Tetraethylammonium (small conductance Ca<sup>2+</sup>-activated K<sup>+</sup> channel blocker), 4-aminopyridine (a voltage-dependent K<sup>+</sup> channel blocker), and barium chloride (an influx-rectifying K<sup>+</sup> channel blocker) significantly reduced DGP capacity to induce relaxation without the interference of glibenclamide (an ATP-sensitive inward rectifier 6.1 and 6.2 K<sup>+</sup> channel blocker). Additionally, administration of DGP, 1 mg/kg i.v., decreased the mean, systolic, and diastolic arterial pressures, and the heart rate of SHRs. The natural xanthone DGP showed promising potential as an endothelium-dependent vasorelaxant, operating through the nitric oxide pathway and potassium channels, ultimately significantly reducing blood pressure in hypertensive rats. |
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| language | English |
| last_indexed | 2024-03-07T22:17:30Z |
| publishDate | 2024-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Plants |
| spelling | doaj.art-fce8a903dac044e6b344129fd084499c2024-02-23T15:31:59ZengMDPI AGPlants2223-77472024-02-0113452810.3390/plants13040528Vasodilation and Blood Pressure-Lowering Effect of 3-Demethyl-2-Geranyl-4-Prenylbellidifoline, a Xanthone Obtained from <i>Garcinia achachairu</i>, in Hypertensive RatsLuísa Nathália Bolda Mariano0Rita de Cássia Vilhena da Silva1Rivaldo Niero2Valdir Cechinel Filho3José Eduardo da Silva-Santos4Priscila de Souza5Laboratory of Cardiovascular Biology, Department of Pharmacology, Universidade Federal de Santa Catarina (UFSC), Florianópolis 88040-900, SC, BrazilPostgraduate Program in Pharmaceutical Sciences, Núcleo de Investigações Químico-Farmacêuticas (NIQFAR), Universidade do Vale do Itajaí (UNIVALI), Rua Uruguai, 458, Centro, Itajaí 88302-901, SC, BrazilPostgraduate Program in Pharmaceutical Sciences, Núcleo de Investigações Químico-Farmacêuticas (NIQFAR), Universidade do Vale do Itajaí (UNIVALI), Rua Uruguai, 458, Centro, Itajaí 88302-901, SC, BrazilPostgraduate Program in Pharmaceutical Sciences, Núcleo de Investigações Químico-Farmacêuticas (NIQFAR), Universidade do Vale do Itajaí (UNIVALI), Rua Uruguai, 458, Centro, Itajaí 88302-901, SC, BrazilLaboratory of Cardiovascular Biology, Department of Pharmacology, Universidade Federal de Santa Catarina (UFSC), Florianópolis 88040-900, SC, BrazilPostgraduate Program in Pharmaceutical Sciences, Núcleo de Investigações Químico-Farmacêuticas (NIQFAR), Universidade do Vale do Itajaí (UNIVALI), Rua Uruguai, 458, Centro, Itajaí 88302-901, SC, Brazil3-demethyl-2-geranyl-4-prenylbellidifoline (DGP), a natural xanthone isolated from <i>Garcinia achachairu</i>, has previously demonstrated remarkable diuretic and renal protective actions. The present study expands its actions on the cardiovascular system by evaluating its vasorelaxant and blood pressure-lowering effects in spontaneously hypertensive rats (SHRs). Aortic endothelium-intact (E+) preparations of SHRs pre-contracted by phenylephrine and exposed to cumulative concentrations of <i>G. achachairu</i> extract, fractions, and DGP exhibited a significant relaxation compared to vehicle-only exposed rings. The non-selective muscarinic receptor antagonist (atropine), the non-selective inhibitor of nitric oxide synthase (L-NAME), as well as the inhibitor of soluble guanylate cyclase (ODQ) altogether avoided DGP-induced relaxation. Tetraethylammonium (small conductance Ca<sup>2+</sup>-activated K<sup>+</sup> channel blocker), 4-aminopyridine (a voltage-dependent K<sup>+</sup> channel blocker), and barium chloride (an influx-rectifying K<sup>+</sup> channel blocker) significantly reduced DGP capacity to induce relaxation without the interference of glibenclamide (an ATP-sensitive inward rectifier 6.1 and 6.2 K<sup>+</sup> channel blocker). Additionally, administration of DGP, 1 mg/kg i.v., decreased the mean, systolic, and diastolic arterial pressures, and the heart rate of SHRs. The natural xanthone DGP showed promising potential as an endothelium-dependent vasorelaxant, operating through the nitric oxide pathway and potassium channels, ultimately significantly reducing blood pressure in hypertensive rats.https://www.mdpi.com/2223-7747/13/4/528bioactivehypertensionspontaneously hypertensive ratsvasculaturexanthone |
| spellingShingle | Luísa Nathália Bolda Mariano Rita de Cássia Vilhena da Silva Rivaldo Niero Valdir Cechinel Filho José Eduardo da Silva-Santos Priscila de Souza Vasodilation and Blood Pressure-Lowering Effect of 3-Demethyl-2-Geranyl-4-Prenylbellidifoline, a Xanthone Obtained from <i>Garcinia achachairu</i>, in Hypertensive Rats Plants bioactive hypertension spontaneously hypertensive rats vasculature xanthone |
| title | Vasodilation and Blood Pressure-Lowering Effect of 3-Demethyl-2-Geranyl-4-Prenylbellidifoline, a Xanthone Obtained from <i>Garcinia achachairu</i>, in Hypertensive Rats |
| title_full | Vasodilation and Blood Pressure-Lowering Effect of 3-Demethyl-2-Geranyl-4-Prenylbellidifoline, a Xanthone Obtained from <i>Garcinia achachairu</i>, in Hypertensive Rats |
| title_fullStr | Vasodilation and Blood Pressure-Lowering Effect of 3-Demethyl-2-Geranyl-4-Prenylbellidifoline, a Xanthone Obtained from <i>Garcinia achachairu</i>, in Hypertensive Rats |
| title_full_unstemmed | Vasodilation and Blood Pressure-Lowering Effect of 3-Demethyl-2-Geranyl-4-Prenylbellidifoline, a Xanthone Obtained from <i>Garcinia achachairu</i>, in Hypertensive Rats |
| title_short | Vasodilation and Blood Pressure-Lowering Effect of 3-Demethyl-2-Geranyl-4-Prenylbellidifoline, a Xanthone Obtained from <i>Garcinia achachairu</i>, in Hypertensive Rats |
| title_sort | vasodilation and blood pressure lowering effect of 3 demethyl 2 geranyl 4 prenylbellidifoline a xanthone obtained from i garcinia achachairu i in hypertensive rats |
| topic | bioactive hypertension spontaneously hypertensive rats vasculature xanthone |
| url | https://www.mdpi.com/2223-7747/13/4/528 |
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