Molina-Molina M, Serrano-Mollar A, Bulbena O, Fernandez-Zabalegui L, Closa D, Marin-Arguedas A, Torrego A, Mullol J, Picado C, Xaubet A
Servei de Pneumologia, Institut Clínic del Tórax, Hospital Clínic, c/Villarroel 170, Barcelona 08036, Spain.
Thorax. 2006 Jul;61(7):604-10. doi: 10.1136/thx.2005.051946. Epub 2006 Apr 6.
The angiotensin system has a role in the pathogenesis of pulmonary fibrosis. This study examines the antifibrotic effect of losartan, an angiotensin II type 1 receptor antagonist, in bleomycin induced lung fibrosis and its possible implication in the regulation of prostaglandin E(2) (PGE(2)) synthesis and cyclooxygenase-2 (COX-2) expression.
Rats were given a single intratracheal instillation of bleomycin (2.5 U/kg). Losartan (50 mg/kg/day) was administrated orally starting one day before induction of lung fibrosis and continuing to the conclusion of each experiment.
Losartan reduced the inflammation induced by bleomycin, as indicated by lower myeloperoxidase activity and protein content in the bronchoalveolar lavage fluid. Collagen deposition induced by bleomycin was inhibited by losartan, as shown by a reduction in the hydroxyproline content and the amelioration of morphological changes. PGE(2) levels were lower in fibrotic lungs than in normal lungs. Losartan significantly increased PGE(2) levels at both 3 and 15 days. A reduction in COX-2 expression by bleomycin was seen at 3 days which was relieved by losartan.
The antifibrotic effect of losartan appears to be mediated by its ability to stimulate the production of PGE(2). Losartan, which is already widely used clinically, could be assessed as a new treatment in lung fibrosis.
血管紧张素系统在肺纤维化发病机制中起作用。本研究探讨血管紧张素II 1型受体拮抗剂氯沙坦对博来霉素诱导的肺纤维化的抗纤维化作用及其对前列腺素E2(PGE2)合成和环氧合酶-2(COX-2)表达调节的可能影响。
给大鼠气管内单次注入博来霉素(2.5 U/kg)。从诱导肺纤维化前一天开始口服氯沙坦(50 mg/kg/天),持续至每个实验结束。
氯沙坦减轻了博来霉素诱导的炎症,支气管肺泡灌洗液中髓过氧化物酶活性和蛋白质含量降低表明了这一点。氯沙坦抑制了博来霉素诱导的胶原沉积,羟脯氨酸含量降低和形态学改变改善表明了这一点。纤维化肺中的PGE2水平低于正常肺。氯沙坦在第3天和第15天均显著提高了PGE2水平。博来霉素在第3天使COX-2表达降低,而氯沙坦可缓解这一现象。
氯沙坦的抗纤维化作用似乎是通过其刺激PGE2产生的能力介导的。已在临床上广泛使用的氯沙坦可作为肺纤维化的一种新治疗方法进行评估。