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-9bH-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HepG2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/mL。载药纳米脂质体对XWLC-05、HCT-116、HepG2细胞的半数抑制浓度（IC₅₀）分别为2.48、0.86、1.86 μg/mL，且在4 μg/mL时对XWLC-05、HCT-116、HepG2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 (C₁₈H₁₇NO₆, 6-acety1-2-(1-amino-ethylidene)-7,9-dihydroxy-8,9b-dimethy1-9bH-dibenzofuran-1,3-dione) nano-liposomes in vitro and in vivo. Methods Nano-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/mL. The IC₅₀ of the drug-loaded nano-liposomes in the XWLC-05, HCT-116, and HepG2 cells were 2.48 μg/mL, 0.86 μg/mL, and 1.86 μg/mL, respectively, and the inhibition rates of XWLC-05, HCT-116, and HepG2 cells administered at a dose of 4 μg/mL 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.

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国家自然科学基金资助项目（81760538）；云南省科技厅科技计划项目（2018FE001）；昆明医科大学重大成果培育项目（CGPY201603）