Baker M A, Tappel A L
Biochem Pharmacol. 1986 Jul 15;35(14):2417-22. doi: 10.1016/0006-2952(86)90470-3.
Gold inhibits selenium-dependent glutathione peroxidase (GSH Px) in vitro. Chrysotherapy has been used for over five decades without complete understanding of its pharmacodynamics. This study shows that gold is potentially an inhibitor of GSH Px in vivo. Reported are conditions for assay of GSH-Px activity showing that the inhibition by gold species can be reversed. The study demonstrates the high affinity of gold for the selenohydryl-active site of GSH Px relative to the affinities of other physiological ligands; GSH Px was inhibited to a greater extent by a small molecular-weight fraction isolated from kidneys of gold-treated rats than by the fraction isolated from kidneys of rats not treated with gold. The data provide a new perspective on the action of gold-containing drugs in vivo.
金在体外可抑制硒依赖性谷胱甘肽过氧化物酶（GSH Px）。金疗法已应用了五十多年，但对其药效学尚未完全了解。本研究表明，金在体内可能是GSH Px的抑制剂。报道了GSH - Px活性测定的条件，表明金物种的抑制作用可被逆转。该研究证明，相对于其他生理配体的亲和力，金对GSH Px的硒氢活性位点具有高亲和力；与从未用金处理的大鼠肾脏中分离出的组分相比，从用金处理的大鼠肾脏中分离出的小分子量组分对GSH Px的抑制作用更大。这些数据为含金黄体内作用提供了新的视角。
