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ONO-5046 is a potent inhibitor of neutrophil elastase in human pleural effusion after lobectomy

1998; Elsevier BV; Volume: 353; Issue: 2-3 Linguagem: Inglês

10.1016/s0014-2999(98)00412-9

1879-0712

Tsutomu Sakuma, Keiji Takahashi, Nobuo Ohya, Katsuo Usuda, Masashi Handa, Tatsuya Abé,

Chronic Obstructive Pulmonary Disease (COPD) Research

The imbalance of neutrophil elastase and α1-antitrypsin in pleural effusion after lobectomy and the effects of the neutrophil elastase inhibitors, sodium N-[2-[4-(2,2-Dimethylpropionyloxy)phenyl-sulfonylamino]benzoyl]aminoacetic acid (ONO-5046) and purified α1-antitrypsin, on neutrophil elastase activity were determined. The amount of neutrophil elastase complexed to α1-antitrypsin, measured by an enzyme-linked immunosorbent assay, was 170 times higher in pleural effusion than in blood 3 h after lobectomy. The α1-antitrypsin levels measured by laser nephelometry did not increase in either blood or pleural effusion. Although neutrophil elastase activity, measured by the hydrolysis of succinyl-(Ala)3-p-nitroanilide, was not detected in blood, it was increased in pleural effusion 3 h and 24 h after lobectomy. ONO-5046, but not α1-antitrypsin, reduced the neutrophil elastase activity in pleural effusion. There is an imbalance of neutrophil elastase and α1-antitrypsin in pleural effusion after lobectomy. ONO-5046 is a potent inhibitor of neutrophil elastase activity in human pleural effusion.