Background and Aims: Rupatadine is an N-alkyl pyridine derivative with anti-inflammatory properties through the inhibition of a range of mediators involved in the early-to late-phase inflammatory response. Rupatadine mainly acts through the histamine H1 receptor, exerting potent anti-inflammatory effects at concentrations in the nanomolar range. In addition, this anti-inflammatory activity is strengthened by its antagonist activity towards PAF. For its strong anti-inflammatory properties, rupatadine may display a positive effect against atherosclerosis development. Methods: Thirty apoE-KO mice were randomized into two experimental groups, so that the initial weight distribution was not different (21.2 ± 1.3 g in Control vs 21.2 ± 1.2 g in Rupatadine). Mice were fed for 12 weeks either Western-type diet or Western-type diet containing 0.17 g/kg rupatadine. Results: During the study, no differences were detected in the weight gain between the two groups. Likewise, no differences in both food and water consumption were recorded. Atherosclerosis was evaluated at the whole aorta and at the aortic sinus. No differences were detected between the two groups for the percentage of atherosclerotic lesions covering the aortic surface (aortic arch: 32.8±6.2% vs 36.6±7.1%, thoracic aorta 5.6±3.6% vs 5.2±2.6%, abdominal aorta 3.7±2.4% vs 4.9±3.9% in Control vs Rupatadine mice, respectively, p>0.05). Similarly, the two groups developed comparable atherosclerotic lesions at the aortic sinus (614,014±91,193 mm2 vs 686,421±110,826 mm2 in Control vs Rupatadine, p>0.05). Conclusions: Rupatadine treatment in apoE-KO mice fed Western diet unexpectedly did not affect atherosclerosis development both at the whole aorta and at the aortic sinus.

Rupatadine Does Not Affect Atherosclerosis Development In ApoE-KO Mice / G. Chiesa, M. Busnelli, L. Capparini, S. Manzini. - In: ATHEROSCLEROSIS. - ISSN 0021-9150. - 287(2019 Aug). (Intervento presentato al 87. convegno European Atherosclerosis Society Congress 2019 tenutosi a Maastricht nel 2019) [10.1016/j.atherosclerosis.2019.06.771].

Rupatadine Does Not Affect Atherosclerosis Development In ApoE-KO Mice

G. Chiesa
;
M. Busnelli;S. Manzini
2019

Abstract

Background and Aims: Rupatadine is an N-alkyl pyridine derivative with anti-inflammatory properties through the inhibition of a range of mediators involved in the early-to late-phase inflammatory response. Rupatadine mainly acts through the histamine H1 receptor, exerting potent anti-inflammatory effects at concentrations in the nanomolar range. In addition, this anti-inflammatory activity is strengthened by its antagonist activity towards PAF. For its strong anti-inflammatory properties, rupatadine may display a positive effect against atherosclerosis development. Methods: Thirty apoE-KO mice were randomized into two experimental groups, so that the initial weight distribution was not different (21.2 ± 1.3 g in Control vs 21.2 ± 1.2 g in Rupatadine). Mice were fed for 12 weeks either Western-type diet or Western-type diet containing 0.17 g/kg rupatadine. Results: During the study, no differences were detected in the weight gain between the two groups. Likewise, no differences in both food and water consumption were recorded. Atherosclerosis was evaluated at the whole aorta and at the aortic sinus. No differences were detected between the two groups for the percentage of atherosclerotic lesions covering the aortic surface (aortic arch: 32.8±6.2% vs 36.6±7.1%, thoracic aorta 5.6±3.6% vs 5.2±2.6%, abdominal aorta 3.7±2.4% vs 4.9±3.9% in Control vs Rupatadine mice, respectively, p>0.05). Similarly, the two groups developed comparable atherosclerotic lesions at the aortic sinus (614,014±91,193 mm2 vs 686,421±110,826 mm2 in Control vs Rupatadine, p>0.05). Conclusions: Rupatadine treatment in apoE-KO mice fed Western diet unexpectedly did not affect atherosclerosis development both at the whole aorta and at the aortic sinus.
rupatadine; atherosclerosis; lipid metabolism; drug repositioning; drug repurposing
Settore BIO/14 - Farmacologia
Settore BIO/16 - Anatomia Umana
Settore BIO/17 - Istologia
ago-2019
European Atherosclerosis Society
https://www.atherosclerosis-journal.com/article/S0021-9150(19)31228-6/pdf
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/675545
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