放射性榄香烯三羰基铼配合物在荷小细胞肺癌裸鼠体内的分布及其对肿瘤的生长抑制作用

目的 观察放射性榄香烯三羰基铼(ETRC)对荷小细胞肺癌裸鼠模型的肿瘤生长抑制作用,并分析其在裸鼠体内的分布、靶向性。方法 以中草药有效成分β-榄香烯为起始原料,人工合成ETRC;制备荷H128小细胞肺癌BALB/c裸鼠模型,12只荷瘤裸鼠尾静脉注射ETRC,分别在不同时间测量肿瘤组织及各器官的放射性,计算每克组织百分注射剂量率(%ID/g)。将20只荷瘤裸鼠随机分为4组:①对照组;②榄香烯治疗组;③188Re治疗组;④ETRC治疗组。尾静脉注射相应试剂后24d比较肿瘤的体积和质量。结果 给药后6h肿瘤组织的放射性最强,为(6.35±0.33)%ID/g,此时肿瘤/血液放射性比值为2.59,肿瘤/肝放射性比值为4.07,肿瘤/脾放射性比值为3.87.给药后24d,肿瘤体积和质量分别为①组:(2.945±0.567)cm3,(5.438±1.232)g;②组:(1.860±0.263)cm3,(4.876±0.621)g;③组:(1.861±0.896)cm3,(4.691±1.595)g;④组:(0.601±0.152)cm3,(1.602±0.194)g。ETRC治疗组显着好于其他各组。结论 ETRC能有效抑制裸鼠小细胞肺癌的生长,对小细胞肺癌治疗有潜在的应用前景。

Anti-tumor effect of elemene tricarbonyl rhenium-188 complex to small cell lung cancer and its biodistribution in nude mice

Objective To observe the anti-tumor effect of elemene tricarbonyl rhenium-188 complex(ETRC)on small cell lung cancer(SCLC)bearing nude mice model,and also its biodistribution,tumor targeting features.Methods ETRC was synthesized from β-elemene,which is a active ingredient in Chinese herbal medicine.Twelve SCLC bearing nude mice were infused ETRC through tail vein.The radioactivity of tumor and diferent organs were measured in various time phase.And ％ID/g was calculated.All 20 mice models were divided into four groups randomly,concluding①Physiological saline infusion group;②Elemene infusiongroup;③~(188)Re infusion group;④ETRC infusion group.Twenty four days after infusion,the volume and weight of tumors were measured and analyzed.Results Six hours after infusion of ETRC,the highest radioactive upmke[(6.35±0.33)％ID/g]was found in tumor mass.Ratio of tumor/blood was 2.59,ratio of tumor/liver was 4.07 and ratio of tumor/spleen was 3.87.The volume and weight of tumor in four groups were:groups①:(2.945±0.567)cm~3,(5.438±1.232)g;groups②:(1.860±0.263)cm~3,(4.876±0.621)g;groups③:(1.861±0.896)cm~3,(4.691±1.595)g;groups④:(0.601±0.152)cm~3,(1.602±0.194)grespectively.There was significant difference between ETRC infusion group and each of other groups.Conclusion ETRC can effectively depress the growth of tumor and it is a promising agent for the treatment of SCLC.