血卟啉-铂（II）共轭物对人膀胱细胞的联合化疗和光动力治疗

Combined chemotherapeutic and photodynamic treatment on human bladder cells by hematoporphyrin-platinum(II) conjugates.

作者信息

Lottner Christian, Knuechel Ruth, Bernhardt Guenther, Brunner Henri

机构信息

Institute of Inorganic Chemistry, University of Regensburg, Regensburg 93040, Germany.

出版信息

Cancer Lett. 2004 Jan 20;203(2):171-80. doi: 10.1016/j.canlet.2003.09.001.

DOI:10.1016/j.canlet.2003.09.001

PMID:14732225

Abstract

Four porphyrin-platinum complexes, conceived as a new approach in cancer therapy by combining the cytostatic activity of cisplatin or oxaliplatin and the photodynamic effect of hematoporphyrin in the same molecule, were studied in detail with respect to solubility and stability in cell culture medium as well as in terms of cytotoxicity and phototoxicity against J82 bladder cancer cells and UROtsa, normal urothelial cells. This study demonstrated that the most active and promising compound among the porphyrin-platinum conjugates investigated was the water-soluble porphyrin-platinum complex 4 (diammine[7,12-bis[1-(polyethyleneglycol-750-monomethylether-1-yl)ethyl]-3,8,13,17-tetramethylporphyrin-2,18-dipropionato]platinum(II)) which exhibited a synergistic antiproliferative effect compared to cisplatin and hematoporphyrin alone or a combination of the drugs.

摘要

四种卟啉 - 铂配合物被详细研究，它们通过在同一分子中结合顺铂或奥沙利铂的细胞生长抑制活性与血卟啉的光动力效应，被视为癌症治疗的一种新方法。研究内容涉及它们在细胞培养基中的溶解度和稳定性，以及对J82膀胱癌细胞和正常尿路上皮细胞UROtsa的细胞毒性和光毒性。这项研究表明，在所研究的卟啉 - 铂共轭物中，最具活性和前景的化合物是水溶性卟啉 - 铂配合物4（二胺[7,12 - 双[1 - （聚乙二醇 - 750 - 单甲醚 - 1 - 基）乙基] - 3,8,13,17 - 四甲基卟啉 - 2,18 - 二丙酸酯]铂（II）），与单独的顺铂和血卟啉或药物组合相比，它表现出协同的抗增殖作用。