16-妊娠双烯醇酮脂质体的体内外抗肿瘤作用研究  

Antitumor Effect of 16-Dehydropregnenolone Liposomes

作　　者：秦峥[1,2] 邓振雪[1] 刘希[1] 解雨婷 崔钰琪 徐翠玲[1] 郑尚季 孙立新[1] 

机构地区：[1]沈阳药科大学药学院,沈阳110016 [2]大连市药品检验所,辽宁大连116021

出　　处：《中国药学杂志》2015年第14期1202-1207,共6页Chinese Pharmaceutical Journal

基　　金：辽宁省教育厅创新团队资助项目(LT2012018);沈阳市科技局资助项目(F11-148-9-00);辽宁特聘教授资助课题(辽教发[2014]187)

摘　　要：目的研究16-妊娠双烯醇酮脂质体的体内外抗肿瘤作用。方法采用噻唑蓝比色法测定16-妊娠双烯醇酮脂质体对多种人肿瘤细胞的生长抑制作用;建立人宫颈癌(He La)裸鼠移植模型,以空白脂质体为阴性对照组,顺铂为阳性对照组,16-妊娠双烯醇酮脂质体为实验组,经尾静脉注射给药,观察16-妊娠双烯醇酮脂质体的体内抗肿瘤作用。结果 16-妊娠双烯醇酮脂质体对人肝癌HepG2细胞,人口腔癌KB细胞,人乳腺癌T47D细胞,人胃癌SGC7901细胞,人成纤维肉瘤HT1080细胞,人卵巢癌SKOV3细胞,人前列腺癌PC3细胞,人前列腺癌DU145细胞,人肺癌A549细胞,人横纹肌肉瘤A204细胞和人宫颈癌HeLa细胞的IC50值分别为44.69,9.17,26.22,19.58,28.01,37.18,24.58,21.38,54.69,4.18和8.96μg·m L-1。尾静脉注射16-妊娠双烯醇酮脂质体7.5、15和30 mg·kg-1·d-1,28 d对人宫颈癌裸鼠移植瘤的相对肿瘤增殖率分别为93.7%、60.52%和37.84%,瘤重抑制率分别为23.05%、48.84%和69.70%。结论 16-妊娠双烯醇酮脂质体具有体内外抗肿瘤作用。OBJECTIVE To investigate the antitumor effect of 16-dehydropregnenolone （16-DHP） liposomes. METHODS Twelve kinds of tumor cells were used to determine the cytotoxic effect of 16-DHP liposome by MTT assay. The established tumor xenograft in nude mouse model was used to evaluate anti-tumor effect of 16-DHP liposomes after tail vein injection. RESULTS IC50 value of 16-DHP liposomes to the human hepatoma cell HepG2, human oral carcinoma KB cell, human breast cancer T47D, human gastric cancer cell SGC7901, human fibrosarcoma cell HT1080, human ovarian cancer cell SKOV3 ,human prostate cancer cell PC3, human prostrate cancer cell DU145, human lung cancer cell A549, human rhabdomyosarcoma A204 cell and human cervical carcinoma cell HeLa were 44. 69, 9. 17,26. 22, 19. 58, 28.01,37.18, 24. 58, 21.38, 54. 69,4.18 and 8. 96 μg·mL^-1, respectively. The relative tumor increment rate and inhibition rates of tumor weight were 93.7% , 60. 52%, 37.84% and 23.05% ,48.84% ,69. 70% respectively after treated with 16-DHP liposomes （7. 5, 15 and 30 mg·kg^-1·d^-1）. CONCLUSION 16-DHP liposomes possess in vitro and in vivo anti-tumor activities.

关 键 词：16-妊娠双烯醇酮 脂质体 抗肿瘤作用 人宫颈癌 

分 类 号：R965[医药卫生—药理学]