氨基水杨酸药理作用研究进展

水杨酸偶氮磺胺吡啶（SASP）、5-氨基水杨酸（5-ASA）、对氨基水杨酸（4-ASA）是治疗溃疡性结肠炎卓有成效的药物。它们具有共同的氨基水杨酸结构,但三者作用机制不甚相同,确切作用机制不清。SASP、5-ASA抑制炎性介质,而4-ASA对PG、LT无影响。5-ASA清除反应性氧代谢产物作用明显,4-ASA作用较弱。氨基水杨酸影响多种细胞因子（如IL-1,IL-2,IL-6,INF-γ、TNF-α、GM-CSF等）的功能,可能是通过抑制细胞因子与受体结合,或减少一些细胞因子的合成与释放。SASP抑制中性粒细胞脱颗粒、释放溶酶体及一些酶,改变淋巴细胞活性。氨基水杨酸类药物对一氧化氮合成酶、粘附分子及肠道通透性等亦有影响。

Mechanisms of salicylates for ulcerative colitis

SASP, 5-ASA, 4ASA are effectivedrugs for ulcerative colitis. They contain the same structure, but their action modes are different. The precise mechanism of salicylates are unclear. SASP,5-ASA inhibit inflammatory mediators, but 4ASA has no effect on PG or LT. 5-ASA has a strong force to scavenge the reactive oxygen metabolites. 4-ASA is weak in this aspect. The salicylates influence the function of several cy-tokines at different degree, such as IL-1, IL-6, IL-2, INF-a, TNF-r, GM-CSF, etc, probably bypreventing the binding of cytokine and receptor, or decreasing some cytokine synthesis and liberation. SASP inhibits neutrophilial cell degrandulation, releases lysosome and other enzymes, and changes the activity of lymphacyte. The salicylates also effect nitric oxide synthesis,adhesion molecules and the intestine permeability.