In vitro inhibitory effect of rupatadine on histamine and TNF-α release from dispersed canine skin mast cells and the human mast cell line HMC-1

Queralt, Mireia; Brazı́s, Pilar; Merlos, Manuel; Mora, Fernando

doi:10.1007/pl00000216

Cited by 53 publications

(43 citation statements)

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“…Rupatadine inhibited mast cell degranulation induced by nonimmunological stimuli (compound 48/80 and calcium ionophore A23187) in rat peritoneal mast cells and also immunological stimuli (Ascaris) in isolated skinmast cells from sensitised dogs [34]. Rupatadine not only inhibited the release of preformed mediators, such as histamine, but also reduced tumour necrosis factor-a release from canine skin mast cells and in the human mast cell line HMC-1 [27,35]. Eosinophils and lymphocytes are key effector cells in the late-phase response of allergy.…”

Section: Platelet-activating Factor Antagonist Activity Other Anti-inmentioning

confidence: 94%

“…This activity was demonstrated in studies performed in vitro and in vivo in several animal species, including mice, rats, guinea pigs, rabbits and dogs. In addition, rupatadine has a profile as an anti-allergic drug with potentially beneficial effects, such as the inhibition of mast cell degranulation, inhibition of neutrophil and eosinophil migration and inhibition of cytokine release [27]. The human pharmacodynamic effects of rupatadine, both antihistamine and PAF-antagonist activities, were investigated in terms of its ability to inhibit the flares and wheals produced by intradermal injection of histamine [28,29] and PAF in comparison with placebo and other reference compounds.…”

Section: Pharmacodynamic Propertiesmentioning

confidence: 99%

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Rupatadine: pharmacological profile and its use in the treatment of allergic rhinitis

Rao¹,

Reddy

Murthy³

2009

Indian J Otolaryngol Head Neck Surg

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Keywords:Rupatadine is a once-daily, non-sedating, selective and long-acting new drug with a strong antagonist activity towards both histamine H1 receptors and plateletactivating factor receptors. The use of rupatadine is indicated in adult and adolescent patients (> 12 years of age) suffering from intermittent and persistent allergic rhinitis. In the treatment of these conditions, rupatadine is at least as effective as ebastine, cetirizine, loratadine and desloratadine. Avery good safety profile of rupatadine has been evidenced in various studies, including a long-term (1-year) safety study. Rupatadine does not present drug-drug interactions with azithromycin, fluoxetine and lorazepam, but should not be administered concomitantly with known CYP3A4 inhibitors.antihistamine, platelet-activating factor, rhinitis, rupatadine.

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Section: Platelet-activating Factor Antagonist Activity Other Anti-inmentioning

confidence: 94%

Section: Pharmacodynamic Propertiesmentioning

confidence: 99%

Rupatadine: pharmacological profile and its use in the treatment of allergic rhinitis

Rao¹,

Reddy

Murthy³

2009

Indian J Otolaryngol Head Neck Surg

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“…Apparent FcRI-mediated degranulation from the cells suggested that the cells could be used for functional assays of mast cells. Previous studies on canine cultured mast cells by de Mora et al [8,11,33] reported the efficacy of anti-allergic drugs on chemically induced or IgE-dependent histamine release from mast cells included in the dispersed cells obtained from enzymatically digested canine skin tissues. In their reports, they described that mast cells constituted only 1-2% of the skin-derived dispersed cells.…”

Section: Discussionmentioning

confidence: 99%

Cultivation and Characterization of Canine Skin-Derived Mast Cells

Kawarai

Masuda

Ohmori

et al. 2010

The Journal of Veterinary Medical Science

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ABSTRACT. It is essential to develop a technique to culture purified skin-derived mast cells (SMCs) to facilitate immunological research on allergic diseases in dogs. This study was performed to develop an efficient culture system for canine SMCs and to characterize the cells in comparison to canine bone marrow-derived mast cells (BMMCs). Enzymatically digested skin biopsy samples were cultivated in serum-free AIM-V medium supplemented with recombinant canine stem cell factor. Three to five weeks after the initiation of culture, mast cells were collected by a magnetic activated cell separation system using anti-c-Kit antibody. The collected cells were composed of a uniform population showing morphological characteristics of mast cells with a round or oval nucleus and abundant toluidine bluepositive metachromatic granules in the cytoplasm. The results of flow cytometric analysis for the presence of cell membrane c-Kit and Fc epsilon receptor I (FcRI) indicated that approximately 90% of the cells were mast cells. The cytoplasmic granules were positive for both tryptase and chymase. Apparent dose-dependent degranulation was induced by antibody-mediated cross-linking of immunoglobulin E (IgE) bound to the cells. These cytological and immunological characteristics observed in SMCs were mostly similar to those observed in BMMCs; however, IgE-mediated degranulation was significantly lower in SMCs than BMMCs. The culture system for canine SMCs developed in this study would be useful in understanding the pathophysiology and developing anti-allergic therapeutics in canine allergic dermatitis.KEY WORDS: bone marrow, canine, culture, mast cells, skin.J. Vet. Med. Sci. 72(2): 131-140, 2010 Allergic dermatitis in dogs is a complex of inflammatory skin diseases primarily mediated by type I hypersensitivity [8]. Cross-linking of the surface Fc epsilon receptor I (FcRI)-bound immunoglobulin E (IgE) with allergens results in the release of various mediators from mast cell granules, inducing type I hypersensitivity [5,6]. Studies using an experimental allergic model have revealed that cytokines and chemokines released from mast cells induce infiltration of leukocytes, leading to a late-phase reaction [42].In dogs, histopathological examination of the skin lesions of atopic dermatitis (AD) has revealed infiltration of mast cells, Langerhans cells, and lymphocytes in addition to a small number of eosinophils and neutrophils into the lesional skin [14]. The presence of allergen-specific IgEbearing mast cells in the dermis of allergic dogs has been shown [13], and both the number of mast cells and the histamine concentration in the dermis have been shown to correlate with clinical symptoms of AD [28]. As shown in the spontaneously developed AD in dogs, in a canine experimental model of AD, epicutaneous application of an allergen slurry has been shown to generate a penetration of allergen into the dermis, an elevated allergen-specific serum IgE, and localized pruritic dermatitis with typical histological changes by IgE-induced inf...

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“…Histamine-1 receptor antagonist was shown to inhibit mast cell granule-stored mediators, as well as cytokine release from HMC-1 cells. 25,26) Quercetin has been reported to inhibit immunoglobulin (Ig)E-mediated release of histamine, tryptase and production of inflammatory cytokines, such as TNF-a, IL-6, and IL-8 in human cultured mast cells. 27,28) Epigallocatechin-3-gallate inhibited histamine and inflammatory cytokine release from RBL-2H3 cells mainly by inhibiting tyrosine phosphorylation, a critical event in the signal transduction leading to secretion.…”

Section: Discussionmentioning

confidence: 99%

Anti-inflammatory Effect of Columbianetin on Activated Human Mast Cells

Jeong

Kim

et al. 2009

Biological & Pharmaceutical Bulletin

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The inflammatory processes are orchestrated by inflammatory cells through a complex set of chemical signals and can arise in any tissue in response to traumatic, infectious, postischemic, toxic, allergic, or auto-immune injury. 1) In chronic inflammatory diseases, the injury persists and leads to tissue damage.1) During inflammation, the inflammatory region is infiltrated with mononuclear cells, producing a range of inflammatory mediators, including inflammatory cytokines. 2)Mast cells are widely distributed in the connective tissues of mammals and other vertebrates, where they are frequently located in close proximity to blood vessels.3) Mast cells are important effecter cells in allergic reactions as well as in inflammatory processes due to their ability to secrete numerous cytokines. 4,5) In view of such findings, the versatile role played by mast cells is now recognized, especially in allergic inflammation.6,7) Activated mast cells can produce histamine, as well as a wide variety of other inflammatory mediators such as eicosanoids, proteoglycans, proteases, and several proinflammatory and chemotactic cytokines such as tumor necrosis factor (TNF)-a, interleukin (IL)-1, IL-4, IL-6, IL-8, IL-13, and transforming growth factor (TGF)-b1. [8][9][10] Notably, modulation of the production of cytokines from mast cells can provide a useful therapeutic strategy for allergic inflammatory disease.In recent years, cyclooxygenase (COX)-2 plays important roles in various tumors and inflammatory diseases.11) COX-2, one of the major mediators of the inflammatory reactions, is also strongly induced in activated monocytes and macrophages. Several recent studies demonstrated that prostaglandin D2 (PGD2), the COX-2 metabolite released from activated mast cells, is also essential for the pathogenesis of eosinophilic airway inflammations.12) Previously, it has been reported that COX-2 inhibitors abolished the PGD2 synthesis and attenuated eosinophils accumulation in the airway's inflammations. 13)Corydalis heterocarpa has been used traditionally to treat the boil or dysentery as well as a poison in Korea. In this study, Columbianetin was isolated from Corydalis heterocarpa but its molecular mechanisms are not well understood. Ng et al., reported that Columbianetin inhibited lipid peroxidation in brain and kidney homogenates.14) It has been reported that one of the active compounds from roots of Angelica pubescens, Columbianetin acetate, significantly demonstrated anti-inflammatory and analgesic activities.15) Kang and Kim, reported that columbianetin-O-beta-D-glucopyranoside exhibited significant neuroprotective activities against glutamate-induced toxicity. 16)To investigate the effect of Columbianetin on phorbol 12-myristate 13-acetate (PMA) plus calcium ionophore-induced cytokine production in the present study, we analyzed the production of IL-1b, IL-6, IL-8, and TNF-a on the Columbianetin treated human mast cell line, HMC-1. We also investigated the COX-2 expression by Columbianetin.Our results revealed that Columbianetin, the...

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In vitro inhibitory effect of rupatadine on histamine and TNF-α release from dispersed canine skin mast cells and the human mast cell line HMC-1

Abstract: Rupatadine and loratadine showed similar inhibitory effect on histamine and TNF-alpha release, whereas SR-27417A only exhibited inhibitory effect against TNF-alpha.

Cited by 53 publications

References 21 publications

Rupatadine: pharmacological profile and its use in the treatment of allergic rhinitis

Rupatadine: pharmacological profile and its use in the treatment of allergic rhinitis

Cultivation and Characterization of Canine Skin-Derived Mast Cells

Anti-inflammatory Effect of Columbianetin on Activated Human Mast Cells

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