Vasorelaxant activity of some structurally related triterpenic acids from Phoradendron reichenbachianum (Viscaceae) mainly by NO production: Ex vivo and in silico studies

Rios, Marı́a Yolanda; López-Martínez, Sugey; López‐Vallejo, Fabian; Medina-Franco, José L.; Villalobos‐Molina, Rafael; Ibarra-Barajas, Maximiliano; Navarrete‐Vázquez, Gabriel; Hidalgo-Figueroa, Sergio; Hernández-Abreu, Oswaldo; Estrada‐Soto, Samuel

doi:10.1016/j.fitote.2012.05.014

Cited by 42 publications

(30 citation statements)

References 20 publications

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“…Taken together, these findings suggest that malbrancheamides could bind at C1 and C2 pockets of e NOS in an allosteric fashion promoting its activation. Similar results were previously found for dihydrospinochalcone‐A and some triterpenes; however, the flavonoid bound only to C1 [25,26]…”

Section: Discussionsupporting

confidence: 88%

“…Similar results were previously found for dihydrospinochalcone-A and some triterpenes; however, the flavonoid bound only to C1. [25,26] The conformational changes caused by Ca 2+ -CaMbinding to eNOS (a short flexible alpha-helix amphiphilic peptide of 15-20 amino acids) are important in stimulating efficient electron transfer within the NOS enzymes. To explore whether malbrancheamides would preferably bind to Ca 2+ -CaM or to eNOS, a docking study using the co-crystallized structure of Ca 2+ -CaM bound to the Ca 2+ -CaM-binding peptide of eNOS (PDB 1NIW) was performed.…”

Section: Molecular Dockingmentioning

confidence: 99%

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Insights on the vasorelaxant mode of action of malbrancheamide

Madariaga-Mazón

Hernández-Abreu

Estrada-Soto

et al. 2015

Journal of Pharmacy and Pharmacology

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Experimental evidence revealed that malbrancheamides induced both endothelium-independent and endothelium-dependent relaxant effects. According to theoretical studies, it is feasible that the endothelium-independent relaxation exerted by malbrancheamide could be mediated by its calmodulin inhibitory properties throughout an interference with myosin light chain phosphorylation and a positive modulation of eNOS.

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Section: Discussionsupporting

confidence: 88%

Section: Molecular Dockingmentioning

confidence: 99%

Insights on the vasorelaxant mode of action of malbrancheamide

Madariaga-Mazón

Hernández-Abreu

Estrada-Soto

et al. 2015

Journal of Pharmacy and Pharmacology

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“…The vasorelaxant effects of UOAs, which from Phoradendron reichenbachianum Oliv. (Viscaceae) were mainly by NO production (Rios et al 2012). UA, with the highest content in UOAs and EFE (Table 1, Figure 1), was reported to inhibit ovalbumininduced airway inflammation (Kim et al 2013) and exert relaxant effects in rat aortic rings via NO release (Aguirre-Crespo et al 2006).…”

Section: Discussionmentioning

confidence: 98%

Study on the mechanisms of the bronchodilator effects ofFolium Eriobotryaeand the selected active ingredient on isolated guinea pig tracheal strips

Gao

Zhang

et al. 2016

Pharmaceutical Biology

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“…Docking experiments were directed to the known binding site of each target. The NOS grid‐box center was located at (24.16, 12.55, 30.29) with a size of 14 × 14 × 24 Å 3 ; this box was sufficient to cover S, M, C2, and C1 sites, as reported by Ríos et al (). The L‐type calcium channel grid center was at (0, 0, 0) with a size of 22.50 × 22.50 × 22.50 Å 3 .…”

Section: Methodsmentioning

confidence: 99%

Functional mechanism of tracheal relaxation, antiasthmatic, and toxicological studies of 6‐hydroxyflavone

Flores‐Flores

Estrada‐Soto

Millán‐Pacheco

et al. 2018

Drug Development Research

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Previously, we described tracheal rat rings relaxation by several flavonoids, being 6‐hydroxyflavone (6‐HOF) the most active derivative of the series. Thus, its mechanism of action was determined in an ex vivo tracheal rat ring bioassay. The anti‐asthmatic effect was assayed in in vivo OVAlbumin (OVA)‐sensitized guinea pigs. Finally, the toxicological profile of 6‐HOF was studied based on Organization of Economic Cooperation and Development guidelines with modifications. 6‐HOF–induced relaxation appears to be related with receptor‐operated calcium channel and voltage‐operated calcium channel blockade as the main mechanism of action, and also through the production of relaxant second messengers NO and cGMP. Molecular docking supports that 6‐HOF acts as calcium channel blocker and by activation of nitric oxide synthase. In addition, the in vivo anti‐asthmatic experiments demonstrate the dose‐dependent significant anti‐allergic effect of 6‐HOF induced by OVA, with best activity at 50 /kg. Finally, toxicological studies determined a LD50 > 2,000 mg/kg and, after 28 day of treatment with 6‐HOF (50 mg/kg) by intragastric route, mice did not exhibit evidence of any significant toxicity. In conclusion, experiments showed that 6‐HOF exerts significant relaxant activity through calcium channel blockade, and possibly, by NO/cGMP‐system stimulation on rat trachea, which interferes with the contraction mechanism of smooth muscle cells in the airways. In addition, the flavonoid shows potential anti‐asthmatic properties in an anti‐allergic pathway. Furthermore, because the pharmacological and safety evidence, we propose this flavonoid as lead for the development of a novel therapeutic agent for the treatment of asthma and related respiratory diseases.

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Vasorelaxant activity of some structurally related triterpenic acids from Phoradendron reichenbachianum (Viscaceae) mainly by NO production: Ex vivo and in silico studies

Cited by 42 publications

References 20 publications

Insights on the vasorelaxant mode of action of malbrancheamide

Insights on the vasorelaxant mode of action of malbrancheamide

Study on the mechanisms of the bronchodilator effects ofFolium Eriobotryaeand the selected active ingredient on isolated guinea pig tracheal strips

Functional mechanism of tracheal relaxation, antiasthmatic, and toxicological studies of 6‐hydroxyflavone

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