Nocerini M R, Carlson J R, Yost G S
Xenobiotica. 1984 Jul;14(7):561-4. doi: 10.3109/00498258409151448.
[methyl-14C]-3-Methylindole (3MI) was incubated with goat-lung microsomes, an NADPH-generating system and glutathione. An adduct between an oxidative metabolite of 3MI and glutathione was formed only when the complete system was employed. The adduct, which was detected by u.v. absorbance and scintillation counting of h.p.l.c. fractions, was purified to homogeneity by reverse-phase h.p.l.c. The ability of 3MI to bind to microsomal protein was reduced to 52% and 46% of controls when 2 mM and 4 mM glutathione, respectively, were included in the incubations. These results suggest the involvement of an electrophilic metabolite as the toxic intermediate in 3MI-mediated pulmonary oedema.
将[甲基 - 14C] - 3 - 甲基吲哚(3MI)与山羊肺微粒体、一个产生NADPH的系统以及谷胱甘肽一起温育。只有当使用完整系统时,才会形成3MI的氧化代谢物与谷胱甘肽之间的加合物。通过高效液相色谱(h.p.l.c.)馏分的紫外吸光度和闪烁计数检测到该加合物,并通过反相高效液相色谱将其纯化至同质。当在温育中分别加入2 mM和4 mM谷胱甘肽时,3MI与微粒体蛋白结合的能力分别降至对照的52%和46%。这些结果表明亲电代谢物作为3MI介导的肺水肿中的毒性中间体参与其中。