el-Far M, Abd el-Hamid N, Ghoneim M
Faculty of Science, Chemistry Department, Mansoura University, Egypt.
Biochimie. 1988 Oct;70(10):1379-84. doi: 10.1016/0300-9084(88)90010-7.
We were the first to report that uroporphyrin isomer I is a superior tumor localizer when compared with hematoporphyrin derivative. In the present study, we have examined the tumor localization of heptacarboxylic porphyrin isomer I (hepta-P) using a bladder tumor model. We have also compared it to that found with uroporphyrin isomer I (Uro-P). We now show, for the first time, that (hepta-P) isomer I can be selectively retained in bladder malignant cells, a novel observation which has not yet been described by other investigators. Furthermore, we have provided a novel technique to modulate and manipulate blood protein binding to porphyrin in a controlled manner, such that the tumor localization properties can be effectively utilized without prolonged retention in the skin and to produce high uptake in the tumor, i.e., a higher therapeutic ratio. The biodistribution of hepta-P in different organs is presented.
我们是首个报道与血卟啉衍生物相比,尿卟啉异构体I是一种更优的肿瘤定位剂的研究团队。在本研究中,我们使用膀胱肿瘤模型研究了七羧基卟啉异构体I(七羧基-P)的肿瘤定位情况。我们还将其与尿卟啉异构体I(尿卟啉-P)的定位情况进行了比较。我们首次表明,(七羧基-P)异构体I可选择性地保留在膀胱恶性细胞中,这是一项其他研究者尚未描述过的新发现。此外,我们提供了一种新技术,可对血蛋白与卟啉的结合进行可控的调节和操纵,从而在不使卟啉长时间滞留于皮肤的情况下有效利用其肿瘤定位特性,并使其在肿瘤中实现高摄取,即获得更高的治疗比。文中呈现了七羧基-P在不同器官中的生物分布情况。