苯并卟啉衍生物对小鼠肉瘤180的光动力疗效  

Efficacies of Benzoporphyrin Derivatives in Photodynamic Therapyfor Sarcoma 180 in Mice

作　　者：余建鑫[1] 许德余[1] 陈文晖[1] 张蕾[1] 

机构地区：[1]第二军医大学

出　　处：《中国激光医学杂志》1999年第2期85-87,共3页Chinese Journal of Laser Medicine & Surgery

摘　　要：目的探讨包括苯并卟啉衍生物单酸环Ａ（ＢｐＤＭＡ）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ＢｐＤＭＡ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（３７５％）。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４５７％。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 study the efficacy of benzoporphyrin derivative monoacid ring A (BpDMA), a new drug used for tumorphotodynamic therapy in phase II clinical trial abroad, and 7 other new benzoporphyrin derivatives (BpDs) synthesized by authors in photodynamic therapy for transplanted sarcoma 180 in mice. Methods After received intravenous injection of 6 g/g or 2 g/g of BpDs, respectively, for 1.5 h, tested mice were irradiated by dye laser at 630 nm, its output was set at 180 mW/cm2, irradiating for 20 min and the incident light dose of 150 J/cm2 was applied.HXResults It was shown that in 5 of the 8 tested BpDs, the cure rates of sarcoma 180 in the 6 g/g group were over 40% and significantly higher than 10% of HpD. BpDMA was shown to be the best and its cure rate was as high as 80%. In the 2 g/g group, the inhibitory rates of these 5 BpDs were 77.5% for BpDMA, 70.8% for 8methoxyethylBpD, 68.2% for 3methoxyethylBpD, 50.9% for 8hydroxyethylBpD and 45.7% for BpD monoacid ring B. Compared with the control group, the paired ttest of mean tumor weight indicated a significant difference ( P <0.01). Conclusions BpD is currently one of the promising candidates of new drugs for tumorphotochemotherapy, yet more work is necessary to study these compounds and their biological activities.

关 键 词：光动力疗法 肉瘤180 苯并卟啉衍生物 

分 类 号：R730.57[医药卫生—肿瘤]