Effect of azelastine on sulphur dioxide induced impairment of ciliary motility in airway epithelium.
OBJECTIVE
The effect of azelastine on airway mucociliary transport function was studied by measuring ciliary motility of human bronchial epithelium in vitro with a photoelectric method.


METHODS
Bronchial epithelial cells were obtained by fibreoptic bronchoscopy, mounted in a Rose chamber, and perfused with Krebs-Henseleit solution. The preparations were placed on a microscope stage equipped with an illuminator, and the variations of light intensity caused by ciliary beating were detected by a photometer.


RESULTS
The addition of azelastine to the perfusate increased ciliary beat frequency (CBF) in a dose dependent manner without ciliary discoordination. The mean (SE) maximal increase from the baseline value and the concentration required to produce a half maximal effect were 27.0 (4.2)% and 9.2 x 10(-6) mol/l, respectively. Exposure of the cells to the perfusate containing 3 ppm sulphur dioxide rapidly decreased CBF by 59.2 (5.0)%, and was accompanied by a reduction in intracellular cyclic AMP levels from 38.1 (4.3) to 10.1 (2.4) pmol/mg protein. This effect was prevented by pretreatment of cells with azelastine in a dose dependent manner.


CONCLUSIONS
Azelastine not only stimulates ciliary motility of airway epithelium and hence mucociliary transport function, but may also protect against sulphur dioxide induced ciliary dysfunction, probably by inhibiting intracellular cyclic AMP loss.
Tamaoki
J
J
First Department of Medicine, Tokyo Women's Medical College, Japan.
Chiyotani
A
A
Sakai
N
N
Takeyama
K
K
Konno
K
K
D001980:Bronchi / Q000187:drug effects*; D001993:Bronchodilator Agents / Q000494:pharmacology*; D002478:Cells, Cultured; D002923:Cilia / Q000187:drug effects*; D004847:Epithelial Cells; D004848:Epithelium / Q000187:drug effects; D006801:Humans; D009079:Mucociliary Clearance / Q000187:drug effects; D010783:Photometry; D010793:Phthalazines / Q000494:pharmacology*; D013268:Stimulation, Chemical; D013458:Sulfur Dioxide / Q000494:pharmacology
D001993:Bronchodilator Agents; D010793:Phthalazines; D013458:Sulfur Dioxide; C020976:azelastine