摘要
目的研究天然活性化合物奥科呋喃[C18H17NO6,6-乙酰基-2-(1-氨基-亚乙基)-7,9-二羟基-8,9b-二甲基-9b H-二苯呋喃-1,3-二酮]纳米脂质体的体外和体内抗肿瘤作用。方法采用薄膜分散-超声法制备纳米脂质体,采用HPLC法测定纳米脂质体载药量。体外培养人肝癌Hep G2细胞、人结肠癌HCT-116细胞、云南宣威肺癌XWLC-05细胞,采用MTT法评价纳米脂质体体外抗癌作用。制备HCT-116裸鼠移植瘤模型,观察载药纳米脂质体体内对裸鼠移植肿瘤的生长抑制作用。结果载药纳米脂质体的载药量为1.26 mg/m L。载药纳米脂质体对XWLC-05、HCT-116、Hep G2细胞的半数抑制浓度(IC50)分别为2.48、0.86、1.86μg/m L,且在4μg/m L时对XWLC-05、HCT-116、Hep G2细胞的增殖抑制率分别为85.59%、99.95%、96.91%(P<0.01)。裸鼠肿瘤相对增殖率最小为50.98%,具有体内抗肿瘤作用。结论天然活性化合物奥科呋喃可制备为纳米脂质体;体外细胞实验表明,奥科呋喃纳米脂质体对癌细胞作用呈明显的剂量-效应关系;裸鼠体内实验发现,载药纳米脂质体对裸鼠移植瘤的生长有抑制作用。
Objective To study the antitumor effect of natural active compound usenamine(C18 H17 NO6, 6-acety1-2-(1-amino-ethylidene)-7,9-dihydroxy-8,9 b-dimethy1-9 b H-dibenzofuran-1,3-dione) nano-liposomes in vitro and in vivo. MethodsNano-liposomes were prepared by thin film dispersion-ultrasonic method. The drug loading of nano-liposomes was determined by HPLC. The cancer cells were cultured in vitro, and the absorbance values were measured by MTT method to evaluate the anticancer effect in vitro. A nude mouse xenograft model was established to observe the growth inhibitory effect of drug-loaded nano-liposomes on tumor growth in nude mice. Results The drug loading of drug-loaded nano-liposomes was 1.26 mg/m L. The IC50 of the drug-loaded nano-liposomes in the XWLC-05, HCT-116, and Hep G2 cells were 2.48 μg/m L, 0.86 μg/m L, and 1.86 μg/m L, respectively, and the inhibition rates of XWLC-05, HCT-116, and Hep G2 cells administered at a dose of 4 μg/m L were 85.59%, 99.95%, and 96.91%, respectively(P < 0.01). The minimum relative tumor proliferation rate of nude mice was 50.98%, and usenamine nano-liposomes had antitumor effect in vivo. Conclusion The natural active compound usenamine can be prepared as a nano-liposome. In vitro cell experiments showed that usenamine nano-liposomes had a dose-effect relationship with cancer cells. In vivo experiments in nude mice found that drug-loaded nano-liposomes had inhibitory effect on tumors.
引文
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