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目的探讨包括苯并卟啉衍生物单酸环A(BpDMA)在内的8种苯并卟啉衍生物对小鼠肉瘤180的光动力治疗效果。方法荷肉瘤180小鼠分别按6μg/g和2μg/g的剂量静脉注射BpD,1.5h后用波长630nm的铜蒸气染料激光照射,激光功率密度为180mW/cm2,照射时间20min,每次光剂量150J/cm2。同时设相同剂量血卟啉衍生物(HpD)对照组和空白对照组。结果6μg/g剂量时,8种BpD中有5种对小鼠肉瘤180的治愈率接近或超过40%,明显高于HpD的10%。其中BpDMA的疗效最好,治愈率高达80%,以下依次为8甲氧乙基BpD(60%)、3甲氧乙基BpD(50%)、8羟乙基BpD(40%)和BpD单酸环B(375%)。2μg/g剂量时,这5种BpD对肉瘤180的抑制率分别为77.5%、70.8%、68.2%、50.9%和457%。与HpD对照组比较,治疗后平均瘤重的差异均有非常显著意义(P<0.01)。结论BpD是一类疗效较好的光化学治疗药物,为研究开发光敏剂新药提供了思路。
Objective To investigate the photodynamic therapy effects of eight benzoporphyrin derivatives including benzoporphyrin derivative mono-acid ring A (BpD-MA) on mouse sarcoma 180. Methods The sarcoma 180 mice were injected with BpD intravenously at a dose of 6 μg/g and 2 μg/g respectively. After 1.5 hours, they were irradiated with a copper vapor dye laser with a wavelength of 630 nm. The laser power density was 180 mW/cm2, and the irradiation time was 20 min. Dosage 150J/cm2. At the same time, the same dose of hematoporphyrin derivative (HpD) control group and blank control group were set. Results At a dose of 6 μg/g, 5 out of 8 BpDs had a cure rate of approximately 40% or higher for mouse sarcoma 180, which was significantly higher than that of HpD by 10%. Among them, BpD-MA had the best curative effect, with a cure rate of 80%, followed by 8-methoxyethyl BpD (60%), 3-methoxyethyl BpD (50%), and 8-hydroxyethyl BpD (40 %) and BpD monoacid ring B (37.5%). At a dose of 2 μg/g, the inhibitory rates of these five BpDs on sarcoma 180 were 77.5%, 70.8%, 68.2%, 50.9% and 45.7%, respectively. Compared with the HpD control group, the difference in average tumor weight after treatment was significant (P<0.01). Conclusion BpD is a kind of photochemotherapeutic drug with good curative effect, which provides the idea for the research and development of new drugs for photosensitizers.