Huang L R, Straubinger R M, Kahl S B, Koo M S, Alletto J J, Mazurchuk R, Chau R I, Thamer S L, Fiel R J
Department of Biophysics, Roswell Park Cancer Institute, Buffalo, NY 14263.
J Magn Reson Imaging. 1993 Mar-Apr;3(2):351-6. doi: 10.1002/jmri.1880030210.
Porphyrins are a unique class of metal chelating agents that have shown specific affinity for neoplasms. The water-soluble free-base derivative, tetrakiscarborane carboxylate ester of 2,4-(alpha,beta-dihydroxyethyl) deuteroporphyrin IX (BOPP), an agent designed for neutron capture therapy, has previously demonstrated selective localization and retention in a C6 murine glioma. In the present work, the authors demonstrate that the manganese chelate of BOPP also selectively localizes in a rat 9L gliosarcoma and preferentially enhances the tumor-normal brain contrast of T1-weighted images for at least 92 hours. The data indicate a maximal enhancement of contrast between tumor and normal brain at 24 hours after injection, compared with 5 minutes for manganese (III) tetraphenylporphine sulfonate (TPPS4). The results also indicate that Mn-BOPP may have a slower uptake in the 9L glioma than Mn-TPPS4 but a longer retention in the tumor. Mn-BOPP is unique in that it represents, to the authors' knowledge, the first example of a single agent that can enhance contrast between tumor and normal tissue and be potentially effective as an agent for boron neutron capture therapy.
卟啉是一类独特的金属螯合剂，已显示出对肿瘤具有特异性亲和力。水溶性游离碱衍生物，即2,4-（α，β-二羟乙基）原卟啉IX的四碳硼烷羧酸酯（BOPP），一种专为中子俘获疗法设计的药物，此前已证明其在C6小鼠胶质瘤中具有选择性定位和滞留。在本研究中，作者证明BOPP的锰螯合物也选择性地定位于大鼠9L胶质肉瘤中，并在至少92小时内优先增强T1加权图像的肿瘤-正常脑对比度。数据表明，注射后24小时肿瘤与正常脑之间的对比度最大增强，而磺酸锰（III）四苯基卟啉（TPPS4）为5分钟。结果还表明，Mn-BOPP在9L胶质瘤中的摄取可能比Mn-TPPS4慢，但在肿瘤中的滞留时间更长。据作者所知，Mn-BOPP的独特之处在于它是第一种能够增强肿瘤与正常组织之间对比度并有可能作为硼中子俘获疗法药物有效的单一药物实例。
