GLUTATHIONE S-SULFONATE, A SULFUR-DIOXIDE METABOLITE, AS A COMPETITIVE INHIBITOR OF GLUTATHIONE S-TRANSFERASE, AND ITS REDUCTION BY GLUTATHIONE-REDUCTASE
GLUTATHIONE S-SULFONATE, A SULFUR-DIOXIDE METABOLITE, AS A COMPETITIVE INHIBITOR OF GLUTATHIONE S-TRANSFERASE, AND ITS REDUCTION BY GLUTATHIONE-REDUCTASE
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DOI：
10.1016/0041-008x(85)90178-4
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发表时间：
1985-01-01
影响因子：
3.8
通讯作者：
MENZEL, DB
中科院分区：
文献类型：
--
作者：
LEUNG, KH;POST, GB;MENZEL, DB
谷胱甘肽S-磺酸盐（GSSO 3 H）是谷胱甘肽二硫化物（GSSG）和亚硫酸盐（SO2的水合形式）的反应产物。GSSO 3 H是大鼠肝（Ki = 14 μ M）和肺（Ki = 9 μ M）以及人肺肿瘤衍生的A549细胞（Ki = 4 μ M）中谷胱甘肽S-转移酶（GST）的有效竞争性抑制剂。在大鼠肝（Km = 313 μ M）和肺（Km = 200 mM）以及人肺A549细胞（Km = 400 μ m）中，GSSO 3 H也被胞质酶还原。SO2可能通过抑制谷胱甘肽（GSH）和反应性亲电体的酶结合，通过形成GSSO 3 H，影响异生化合物的解毒作用。虽然GSSO 3 H可以被酶降解，但高底物Km值表明该化合物在低浓度下可能不容易被还原。
Glutathione S-sulfonate (GSSO3H) is a reaction product of glutathione disulfide (GSSG) and sulfite, the hydrated form of SO2. GSSO3H was a potent competitive inhibitor of glutathione S-transferases (GST) in the rat liver (Ki = 14 .mu.M) and lung (Ki = 9 .mu.M), and in human lung tumor-derived A549 cells (Ki = 4 .mu.M). GSSO3H was also reduced by a cytosolic enzyme in the rat liver (Km = 313 .mu.M) and lung (Km = 200 mM), and human lung A549 cells (Km = 400 .mu.m). SO2 may have affected the detoxification of xenobiotic compounds by inhibiting, via formation of GSSO3H, the enzymatic conjugation of glutathione (GSH) and reactive electrophiles. Although GSSO3H can be enzymatically degraded, the high substrate Km value suggested that this compound may not have been readily reduced at low concentrations.