Kappas A, Drummond G S, Sardana M K
J Clin Invest. 1985 Jan;75(1):302-5. doi: 10.1172/JCI111689.
Sn-protoporphyrin is a potent competitive inhibitor of heme oxygenase, the rate-limiting enzyme in heme degradation to bile pigment, and has been successfully utilized to suppress hyperbilirubinemia in a variety of experimental and naturally occurring forms of jaundice in animals and man. The compound is presumed to act in vivo primarily by inhibiting heme oxidation; thus it would be reasonable to expect that preservation of some functional moiety of cellular heme from degradation by heme oxygenase would occur after Sn-protoporphyrin administration. We have examined this question in liver by studying the heme saturation of tryptophan pyrrolase, the heme-dependent enzyme which controls the first and rate-limiting step in the catabolism of L-tryptophan. Sn-protoporphyrin, in doses (10 mumol/kg body wt) which entirely suppress neonatal hyperbilirubinemia in the experimental animal, leads to a very rapid (approximately 30-60 min) increase in the heme saturation of tryptophan pyrrolase from normal levels of approximately 50-60% to nearly 100%. The effect peaks at 1-2 h and lasts for at least 12 h. Sn-protoporphyrin is also able to block the rapid and marked decline in heme saturation of tryptophan pyrrolase elicited by inorganic cobalt, a potent inducer of heme oxygenase in liver. These findings establish clearly that after the administration of Sn-protoporphyrin in the whole animal, a functionally active heme pool, the one related to tryptophan pyrrolase, is rapidly increased in liver, confirming that the metalloporphyrin inhibits the degradation of endogenous heme by heme oxygenase.
锡原卟啉是血红素加氧酶的一种强效竞争性抑制剂,血红素加氧酶是血红素降解为胆色素过程中的限速酶,并且已成功用于抑制动物和人类多种实验性及自然发生的黄疸中的高胆红素血症。据推测,该化合物在体内主要通过抑制血红素氧化起作用;因此,可以合理预期,在给予锡原卟啉后,细胞血红素的某些功能部分将得以保留而不被血红素加氧酶降解。我们通过研究色氨酸吡咯酶的血红素饱和度来探讨这个问题,色氨酸吡咯酶是一种血红素依赖性酶,它控制L-色氨酸分解代谢的第一步和限速步骤。给予实验动物能完全抑制新生儿高胆红素血症的剂量(10 μmol/kg体重)的锡原卟啉后,色氨酸吡咯酶的血红素饱和度会从正常水平约50%-60%非常迅速地(约30-60分钟)增加到近100%。该效应在1-2小时达到峰值,并持续至少12小时。锡原卟啉还能够阻断由无机钴引起的色氨酸吡咯酶血红素饱和度的快速且显著下降,无机钴是肝脏中血红素加氧酶的一种强效诱导剂。这些发现清楚地表明,在对整个动物给予锡原卟啉后,肝脏中与色氨酸吡咯酶相关的一个功能活跃的血红素池会迅速增加,证实金属卟啉抑制了血红素加氧酶对内源性血红素的降解。