Kappas A, Drummond G S
Environ Health Perspect. 1984 Aug;57:301-6. doi: 10.1289/ehp.8457301.
The heme-cytochrome P-450 complexes represent sensitive metabolic systems for examining the biological impact of metals on important cellular functions. Many metals, both in the inorganic form and bound to organic moieties, potently induce heme oxygenase, the rate limiting enzyme of heme degradation. The resulting increase in the rate of heme breakdown is reflected in a marked depression of cellular cytochrome P-450 content and impairment of the oxidative metabolism of natural and foreign chemicals dependent on this hemeprotein. Organometal complexes do not mimic in all their aspects the actions of the inorganic elements which they contain. For example, organotins, in contrast to inorganic tin, produce a prolonged induction response of heme oxygenase in the liver but not in the kidney. Co-protoporphyrin is a much more potent inducer of heme oxygenase in liver than is inorganic cobalt; and Sn-protoporphyrin inhibits heme oxygenase activity nearly completely, whereas inorganic tin is a powerful inducer of the renal enzyme. Contrasting effects on heme metabolism exist as well within the metalloporphyrin species as demonstrated by the effects in vivo of Co-protoporphyrin and Sn-protoporphyrin on heme oxygenase activity; the former induces the enzyme whereas the latter potently inhibits it. In vitro, however, both compounds competitively inhibit heme oxidation activity. These differences, among others which characterize metal actions in vivo and in vitro attest to the importance of pharmacokinetic, adaptive and other host factors in defining the responses of the heme-cytochrome P-450 systems to the impact of metals in the whole animal.
血红素 - 细胞色素P - 450复合物代表了用于研究金属对重要细胞功能的生物学影响的敏感代谢系统。许多金属,无论是无机形式还是与有机部分结合,都能强烈诱导血红素加氧酶,即血红素降解的限速酶。血红素分解速率的增加反映在细胞色素P - 450含量的显著降低以及依赖于这种血红素蛋白的天然和外来化学物质氧化代谢的受损上。有机金属络合物在所有方面都不能模拟它们所含无机元素的作用。例如,与无机锡相比,有机锡在肝脏中产生血红素加氧酶的延长诱导反应,但在肾脏中则不然。与无机钴相比,原卟啉钴在肝脏中是血红素加氧酶的更强诱导剂;而锡原卟啉几乎完全抑制血红素加氧酶活性,而无机锡是肾脏中该酶的强诱导剂。正如原卟啉钴和锡原卟啉在体内对血红素加氧酶活性的影响所表明的那样,金属卟啉类物质对血红素代谢也存在相反的影响;前者诱导该酶,而后者则强烈抑制它。然而,在体外,这两种化合物都竞争性抑制血红素氧化活性。这些差异以及体内和体外金属作用的其他特征证明了药代动力学、适应性和其他宿主因素在确定血红素 - 细胞色素P - 450系统对全动物体内金属影响的反应中的重要性。