1,8-Cineole induces relaxation in rat and guinea-pig airway smooth muscle

Nascimento, Nilberto Robson Falcão do; Refosco, Rafael Mohana De Carvalho; Vasconcelos, Elainne Cristine Félix; Kerntopf, Marta Regina; Santos, Cláudia Ferreira; Batista, Francisco José Arnaud; Sousa, Clauber Mota De; Fonteles, M. C.

doi:10.1211/jpp.61.03.0011

Cited by 39 publications

(22 citation statements)

References 17 publications

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“…Contractions of tracheal smooth muscles by K + were also inhibited by 1,8-cineole [ 42 ] . These fi ndings were confi rmed on non-sensitized or ovalbumin-sensitized airway smooth muscle cells [ 43 ] .…”

Section: In Vitro Studiesmentioning

confidence: 67%

Anti-inflammatory Properties of the Monoterpene 1.8-cineole: Current Evidence for Co-medication in Inflammatory Airway Diseases

2014

Drug Res (Stuttg)

211

128

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1,8-cineole is a natural monoterpene, also known as eucalyptol. It is a major compound of many plant essential oils, mainly extracted from Eucalyptus globulus oil. As an isolated compound, 1,8-cineole is known for its mucolytic and spasmolytic action on the respiratory tract, with proven clinical efficacy. 1,8-cineole has also shown therapeutic benefits in inflammatory airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD). This clinical evidence refers to its anti-inflammatory and anti-oxidant mode of action, which has been proven in numerous pre-clinical studies. In vitro studies found strong evidence that 1,8-cineole controls inflammatory processes and mediator production of infection- or inflammation-induced mucus hypersecretion by its action as anti-inflammatory modifier rather than a simple mucolytic agent. The aim of this review is to present these preclinical studies performed with the pure monoterpene, and to summarize the current knowledge on the mode of action of 1,8-cineole. The actual understanding of the pure 1,8-cineole compared to mixtures of natural volatile oils containing 1,8-cineole as a major compound and to mixtures of natural terpenes, known as essential oils, will be discussed. Based on the anti-oxidative and anti-inflammatory properties, recent clinical trials with 1,8-cineole have shown first evidence for the beneficial use of 1,8-cineole as long-term therapy in the prevention of COPD-exacerbations and to improve asthma control.

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Section: In Vitro Studiesmentioning

confidence: 67%

Anti-inflammatory Properties of the Monoterpene 1.8-cineole: Current Evidence for Co-medication in Inflammatory Airway Diseases

2014

Drug Res (Stuttg)

211

128

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“…Eucalyptol‐containing products are widely used as a remedy for symptoms of the common cold and other respiratory infections and for alleviating pain (Juergens, ). In animal studies, eucalyptol was shown to counteract carrageenan‐induced oedema formation, acid‐, formalin‐ and heat‐evoked pain behaviour, gastric injury, colitis, allergen‐induced bronchoconstriction and inflammation, respiratory irritation due to inhalation of smoke irritants and endotoxin‐induced pulmonary inflammation and liver failure (Santos and Rao, , ; Santos et al, , ; Liapi et al, ; Bastos et al, ; Nascimento et al, ; Willis et al, ; Liu et al, ; Zhao et al, ; Ha et al, ; Rocha Caldas et al, ). Clinical studies administering eucalyptol observed anti‐inflammatory effects in asthmatics, alleviation of symptoms of rhino‐sinusitis and reduced chronic obstructive pulmonary disease (COPD) exacerbations (Juergens et al, ; Kehrl et al, ; Worth et al, ; Juergens, ).…”

Section: Introductionmentioning

confidence: 99%

Transient Receptor Potential Cation Channel Subfamily M Member 8 channels mediate the anti‐inflammatory effects of eucalyptol

Caceres

Liu

Jabba

et al. 2017

British J Pharmacology

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Among the pharmacological targets of eucalyptol, TRPM8 channels were essential for its anti-inflammatory effects in mice. Human TRPM8 channels are more sensitive to eucalyptol than rodent TRPM8 channels explaining the higher potency of eucalyptol in humans. Metabolites of eucalyptol could contribute to its anti-inflammatory effects. The development of more potent and selective TRPM8 agonists may yield novel anti-inflammatory agents.

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“…The broadest field of application for 1,8-cineole is in the therapy of severe pulmonary diseases such as asthma, where the compound exhibits mucolytic, bronchodilating, and anti-inflammatory properties [6,7,8,9]. Similar effects play a role in the treatment of acute sinusitis, where 1,8-cineole is the pharmacologically active agent in some non-prescription pharmaceuticals [10,11].…”

Section: Introductionmentioning

confidence: 99%

Characterisation of the Metabolites of 1,8-Cineole Transferred into Human Milk: Concentrations and Ratio of Enantiomers

Kirsch

Buettner

2013

Metabolites

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1,8-Cineole is a widely distributed odorant that also shows physiological effects, but whose human metabolism has hitherto not been extensively investigated. The aim of the present study was, thus, to characterise the metabolites of 1,8-cineole, identified previously in human milk, after the oral intake of 100 mg of this substance. Special emphasis was placed on the enantiomeric composition of the metabolites since these data may provide important insights into potential biotransformation pathways, as well as potential biological activities of these substances, for example on the breastfed child. The volatile fraction of the human milk samples was therefore isolated via Solvent Assisted Flavour Evaporation (SAFE) and subjected to gas chromatography-mass spectrometry (GC-MS). The absolute concentrations of each metabolite were determined by matrix calibration with an internal standard, and the ratios of enantiomers were analysed on chiral capillaries. The concentrations varied over a broad range, from traces in the upper ng/kg region up to 40 µg/kg milk, with the exception of the main metabolite α2-hydroxy-1,8-cineole that showed concentrations of 100–250 µg/kg. Also, large inter- and intra-individual variations were recorded for the enantiomers, with nearly enantiomerically pure α2-hydroxy- and 3-oxo-1,8-cineole, while all other metabolites showed ratios of ~30:70 to 80:20.

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1,8-Cineole induces relaxation in rat and guinea-pig airway smooth muscle

Abstract: 1,8-Cineole relaxed rat and guinea-pig (nonsensitized and ovalbumin-sensitized) airway smooth muscle by a nonspecific mechanism.

Cited by 39 publications

References 17 publications

Anti-inflammatory Properties of the Monoterpene 1.8-cineole: Current Evidence for Co-medication in Inflammatory Airway Diseases

Anti-inflammatory Properties of the Monoterpene 1.8-cineole: Current Evidence for Co-medication in Inflammatory Airway Diseases

Transient Receptor Potential Cation Channel Subfamily M Member 8 channels mediate the anti‐inflammatory effects of eucalyptol

Characterisation of the Metabolites of 1,8-Cineole Transferred into Human Milk: Concentrations and Ratio of Enantiomers

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