Tsuchida T, Zheng G, Pandey R K, Potter W R, Bellnier D A, Henderson B W, Kato H, Dougherty T J
Department of Radiation Biology, Roswell Park Cancer Institute, Buffalo, NY 14263-0001, USA.
Photochem Photobiol. 1997 Aug;66(2):224-8. doi: 10.1111/j.1751-1097.1997.tb08647.x.
Human serum albumin (HSA) is one of the key components in human blood that may influence drug distribution. As such, it is important to know the affinity of any drug for albumin. Previously, Photofrin, a mixture of monomeric, dimeric and oligomeric porphyrins, has been subjected to HSA binding studies. However, due to its complex nature, binding studies on Photofrin or other hematoporphyrin derivatives with HSA are inconclusive. In this report, the binding properties of some components (dimers and trimers) of Photofrin and the relationship between murine photosensitizing efficacy and those binding properties were investigated. The interaction of these porphyrins with HSA was investigated by direct ultrafiltration and fluorescent titration techniques with fluorescent probes such as dansyl-L-proline (DP), which is known to interact selectively with site II on HSA. Porphyrins also were tested for antitumor activity in a mouse model following intravenous administration and exposure to laser light. Together, the results suggest that the photosensitizers that were preferentially bound to site II of HSA were most effective at controlling murine tumor regrowth.
人血清白蛋白（HSA）是人体血液中可能影响药物分布的关键成分之一。因此，了解任何药物与白蛋白的亲和力很重要。此前，卟吩姆钠（一种单体、二聚体和寡聚体卟啉的混合物）已接受与人血清白蛋白结合的研究。然而，由于其性质复杂，关于卟吩姆钠或其他血卟啉衍生物与人血清白蛋白的结合研究尚无定论。在本报告中，研究了卟吩姆钠的一些成分（二聚体和三聚体）的结合特性以及小鼠光敏疗效与这些结合特性之间的关系。通过直接超滤和荧光滴定技术，使用诸如丹磺酰-L-脯氨酸（DP）等荧光探针研究了这些卟啉与人血清白蛋白的相互作用，已知DP可与人血清白蛋白上的位点II选择性相互作用。在静脉注射并暴露于激光后，还在小鼠模型中测试了卟啉的抗肿瘤活性。综合来看，结果表明优先与人血清白蛋白位点II结合的光敏剂在控制小鼠肿瘤再生长方面最有效。
