Young S W, Qing F, Harriman A, Sessler J L, Dow W C, Mody T D, Hemmi G W, Hao Y, Miller R A
Pharmacyclics, Inc., Sunnyvale, CA 94086, USA.
Proc Natl Acad Sci U S A. 1996 Jun 25;93(13):6610-5. doi: 10.1073/pnas.93.13.6610.
Gadolinium(III) texaphyrin (Gd-tex2+) is representative of a new class of radiation sensitizers detectable by magnetic resonance imaging (MRI). This porphyrin-like complex has a high electron affinity [E1/2 (red.) approximately = -0.08 V versus normal hydrogen electrode] and forms a long-lived pi-radical cation upon exposure to hydrated electrons, reducing ketyl radicals, or superoxide ions. Consistent with these chemical findings, Gd-tex2+ was found to be an efficient radiation sensitizer in studies carried out with HT29 cells in in vitro as well as in in vivo single and multifraction irradiation studies with a murine mammary carcinoma model. Selective localization of Gd-tex2+ in tumors was confirmed by MRI scanning.
钆(III) texaphyrin(Gd-tex2+)是一类可通过磁共振成像(MRI)检测到的新型辐射敏化剂的代表。这种类卟啉配合物具有高电子亲和力[相对于标准氢电极,E1/2(还原)约为-0.08 V],并且在暴露于水合电子、还原酮基自由基或超氧离子时形成长寿命的π-自由基阳离子。与这些化学发现一致,在体外对HT29细胞进行的研究以及在小鼠乳腺癌模型的体内单次和多次分割照射研究中,发现Gd-tex2+是一种有效的辐射敏化剂。通过MRI扫描证实了Gd-tex2+在肿瘤中的选择性定位。