Kolassa N, Becker R, Wiener H
Prostaglandins. 1985 Jan;29(1):133-42. doi: 10.1016/0090-6980(85)90158-3.
The effects of sulfasalazine (SASP) and its cleavage products 5-aminosalicylic acid (5-ASA) and sulfapyridine (SP) on prostanoid (PG) synthesis and degradation were determined in rabbit colonic mucosa fractions in vitro. When the microsomal fraction was incubated with (14C)arachidonic acid, 10(-3) M SASP and SP did not markedly change the formation of labeled PGE2, PGF2 alpha, TxB2 and 6-keto-PGF1 alpha X 10(-4) M 5-ASA increased synthesis about 2.7-fold; the pattern of PG identified was unaltered. In the presence of the 10-fold higher concentration of 5-ASA, PG synthesis remained elevated at a similar level. When the cytosolic fraction was incubated with (3H)PGE2, 10(-3) M 5-ASA was without influence and 10(-3) M SP decreased slightly PGE2 breakdown. However, SASP showed a pronounced inhibitory effect at 10(-5) M and inhibition of PGE2 degradation was complete at 10(-3) M SASP. The results are compatible with the assumption that stimulation of PG synthesis by 5-ASA is related to therapeutic benefit in the treatment of ulcerative colitis.
在体外对兔结肠黏膜组分测定柳氮磺胺吡啶(SASP)及其裂解产物5-氨基水杨酸(5-ASA)和磺胺吡啶(SP)对类前列腺素(PG)合成及降解的影响。当微粒体组分与(14C)花生四烯酸一起温育时,10^(-3)M的SASP和SP并未显著改变标记的PGE2、PGF2α、TxB2和6-酮-PGF1α的形成;10^(-4)M的5-ASA使合成增加约2.7倍;所鉴定的PG模式未改变。在5-ASA浓度高10倍的情况下,PG合成仍维持在相似的升高水平。当胞质溶胶组分与(3H)PGE2一起温育时,10^(-3)M的5-ASA无影响,10^(-3)M的SP使PGE2降解略有减少。然而,SASP在10^(-5)M时显示出明显的抑制作用,在10^(-3)M的SASP时PGE2降解被完全抑制。这些结果符合以下假设,即5-ASA对PG合成的刺激与溃疡性结肠炎治疗中的治疗益处相关。