Publication: Derivados de quinazolina para el tratamiento del asma
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2016-02
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Abstract
El asma es una enfermedad inflamatoria crónica respiratoria que afecta a alrededor 300 millones de personas en el mundo con un esperado aumento en los próximos años. A pesar de los avances en diagnosis y tratamientos, actualmente sigue constituyendo un problema público serio, particularmente debido a las dianas y efectos secundarios de los fármacos antiasmáticos disponibles. La vasicina y vasicinona obtenida de las hojas de Adhatoda vasica, se relaciona con una actividad broncodilatadora de grado moderado. En base a observaciones de distintos estudios y al objetivo de encontrar posibles nuevos potenciales antiasmáticos, como moléculas con potente actividad broncodilatadora y antialérgica, llegamos a la búsqueda de análogos de quinazolina para el tratamiento del asma. En la revisión de los estudios experimentales realizados sobre derivados de quinazolina y las actividades con las que se describen, se exponen algunas de éstas moléculas como posibles futuros antiasmáticos: 95.4 mostró una marcada actividad broncodilatadora; RLX inhibía la degranulación de mastocitos inducida por antígenos y liberaba histamina de los tejidos diana, se la describe como broncodilatadora, antiinflamatoria, antiartrítica e involucrada en la mediación celular y componentes humorales del sistema inmune; KP-496 mostró ser un antagonista dual potente y selectivo para los receptores de LTD4 y TXA2; y por último, R8 mostró reducir las características del asma ya que suprime significantemente la producción de citoquinas TH2 y la reclusión de eosinófilos a las vías respiratorias.
Asthma is a chronic inflammatory airway disease affecting over 300 million people worldwide with a expected increase in next years. Despite remarkable advances in diagnosis and treatment, asthma is still a serious public health problema, particularly due to off targets and side efects of commonly available anti-asthma drugs. Vasicine and vasicinone obtained from leaves of Adhatoda vasica, have been reported for moderate degree of bronchodilator activity. Based on observations of different studies, and in order to find a possible new anti-asthmatic potential, like molecules with strong bronchodilating and antiallergic activity leads to search quinazoline analogs for asthma treatment. In a review of experimental studies about quinazoline derivatives and their decribed activities, certain molecules whose activities are related as possible future anti-asthmatic, are reported: 95.4 showed a marked bronchodilator activity; RLX inhibited antigen-induced mast cell degranulation and released of histamine from target tissues; it is described as a bronchodilator, antiinflammatory, antiarthritic and involved in cellular and humoral components of the immune system mediated. KP-496 showed to be a potent and selective dual receptor antagonist for LTD4 and TX2 receptors. Finally, R8 reduced the features of asthma because of supression of TH2 cytokines production, confinement of eosinophils to airways.
Asthma is a chronic inflammatory airway disease affecting over 300 million people worldwide with a expected increase in next years. Despite remarkable advances in diagnosis and treatment, asthma is still a serious public health problema, particularly due to off targets and side efects of commonly available anti-asthma drugs. Vasicine and vasicinone obtained from leaves of Adhatoda vasica, have been reported for moderate degree of bronchodilator activity. Based on observations of different studies, and in order to find a possible new anti-asthmatic potential, like molecules with strong bronchodilating and antiallergic activity leads to search quinazoline analogs for asthma treatment. In a review of experimental studies about quinazoline derivatives and their decribed activities, certain molecules whose activities are related as possible future anti-asthmatic, are reported: 95.4 showed a marked bronchodilator activity; RLX inhibited antigen-induced mast cell degranulation and released of histamine from target tissues; it is described as a bronchodilator, antiinflammatory, antiarthritic and involved in cellular and humoral components of the immune system mediated. KP-496 showed to be a potent and selective dual receptor antagonist for LTD4 and TX2 receptors. Finally, R8 reduced the features of asthma because of supression of TH2 cytokines production, confinement of eosinophils to airways.