Morgan A R, Garbo G M, Keck R W, Selman S H
Department of Chemistry, University of Toledo, Ohio 43606.
Cancer Res. 1988 Jan 1;48(1):194-8.
A series of metallopurpurins was tested for their photodynamic activity against transplantable N-[4-(5-nitro-2-furyl)-2-thiazoyl]formamide-induced urothelial tumors growing in male Fischer CDF (F344/CrlBR) rats. Histological examination of tumors in animals treated with the metallopurpurins and red light (greater than 590 nm, 360 J/cm2) revealed tumor necrosis 24 h after completion of therapy. Control tumors showed no histological change. In 30-day tumor regrowth studies, 70% of animals treated with the metallopurpurin derivative SnET2 were free of tumors while 50% of the animals treated with the free-base purpurin ET2 were free of tumor. Metallopurpurins have intense absorptions in the red region of the visible spectrum, a region with good tissue penetration. The metallopurpurins are easily prepared from the corresponding purpurins with a high degree of purity. This study demonstrates the potential of these photosensitizers for photodynamic cancer therapy.
对一系列金属紫质进行了测试，考察其对移植于雄性Fischer CDF（F344/CrlBR）大鼠体内、由N-[4-(5-硝基-2-呋喃基)-2-噻唑基]甲酰胺诱导产生的尿路上皮肿瘤的光动力活性。在用金属紫质和红光（波长大于590 nm，360 J/cm²）处理的动物中，对肿瘤进行组织学检查发现，治疗结束24小时后肿瘤出现坏死。对照肿瘤未显示组织学变化。在为期30天的肿瘤再生研究中，用金属紫质衍生物SnET2治疗的动物中有70%无肿瘤，而用游离碱紫质ET2治疗的动物中有50%无肿瘤。金属紫质在可见光谱的红色区域有强烈吸收，该区域具有良好的组织穿透性。金属紫质很容易由相应的紫质以高纯度制备得到。本研究证明了这些光敏剂在光动力癌症治疗中的潜力。
