Garattini E, Broggini M, Coccia P, Colombo T, Rossi C, D'Incalci M
Biochem Pharmacol. 1984 Sep 1;33(17):2715-22. doi: 10.1016/0006-2952(84)90686-5.
The metabolism of 14C-PMM and its irreversible interaction with DNA and proteins were studied in M5076/73A reticular cell sarcoma, a murine solid tumor previously shown to be sensitive to the drug. Metabolism and irreversible binding were determined 0.25, 1, 8 and 104 hours after a single i.p. injection of radiolabelled PMM, tumor and liver macromolecular binding were compared with two differently 14C-labelled PMM, i.e. ring- and methyl-PMM. Ring-PMM derived macromolecular binding appeared to have more relevance in vivo and had a similar time profile in both liver and tumor. Ring-PMM derived DNA binding was then related to metabolic steps between PMM and 2,2,4,6 TMM and 2,2,4,6 TMM itself and 2,4,6 TriMM.
在M5076/73A网状细胞肉瘤（一种先前已证明对该药物敏感的小鼠实体瘤）中研究了14C-PMM的代谢及其与DNA和蛋白质的不可逆相互作用。在单次腹腔注射放射性标记的PMM后0.25、1、8和104小时测定代谢和不可逆结合，将肿瘤和肝脏大分子结合与两种不同的14C标记的PMM（即环-PMM和甲基-PMM）进行比较。环-PMM衍生的大分子结合在体内似乎更具相关性，并且在肝脏和肿瘤中具有相似的时间分布。然后将环-PMM衍生的DNA结合与PMM和2,2,4,6-TMM以及2,2,4,6-TMM本身和2,4,6-三甲基甲硅烷基甲基（TriMM）之间的代谢步骤相关联。
