目的:比较齐墩果酸(OA)/乳酸羟基乙酸共聚物纳米粒(OPN)、OA/乳酸羟基乙酸共聚物-水溶性维生素E纳米粒(OPTN)和OA/聚己内酯-聚乳酸-水溶性维生素E纳米粒(OPPTN)对小鼠腹水型肝癌高淋巴道转移细胞(HCa-F)的体外抑制作用.方法:采用水溶性四氮唑(WST-1)法比较低、中、高浓度(2.5、10、20μg·mL-1)的OPN、OPTN、OPPTN、OA溶液剂(OS)组和阳性对照(氟尿嘧啶注射液)组对HCa-F细胞培养24、48、72h后的细胞生长抑制率(IR)和3种纳米粒的半数抑制浓度(IC50),另设立空白纳米粒(NPs)组、空白组(不加任何物质)、阴性对照组(加入培养液).结果:浓度分别为2.5、10、20 μg·mL-1的OPN组在72h时的IR分别为(42.9±0.9)％、(63.6±1.1)％、(75.4±1.3)％,OPTN组分别为(54.3±1.2)％、(79.2±1.4)％、(92.6±1.5)％,OPPTN组分别为(50.8±0.8)％、(71.7±1.3)％、(83.9±1.2)％,阳性对照组分别为(31.5±0.9)％、(50.3±0.8)％、(60.6±0.9)％.与阳性对照组相同浓度比较,72 h时OPN、OPTN、OPPTN组的中、高浓度的IR均明显升高(P均＜0.01).3种纳米粒对HCa-F细胞的IC50均随时间延长逐渐减小,其中OPTN组(8.64、1.39、0.38 μg·mL-1)明显小于OPPTN组(11.86、5.52、3.46 μg·mL-1)和OPN组(30.27、8.21、5.00 μg· mL-1)(P＜0.05或P＜0.01).结论:OPTN对HCa-F细胞的IR最高,表明OPTN体外具有良好的细胞相容性和显著的抗肿瘤活性.%OBJECTIVE: To compare inhibition effects of Oleanolic acid-loaded polylactic-co-glycolic acid nanoparticles (OPN) , Oleanolic acid-loaded polylactic-co-glycolic acid D-a-tocopherol polyethylene glycol 1 000 succinate nanoparticles (OPTN), Oleanolic acid-loaded poly(e-caprolactone)-polylactic acid D-a-tocopherol polyethylene glycol 1 000 succinate nanoparticles (OPP-TN) against high lymphatic metastasis cell (Hca-F) in ascetic hepatocarcinoma mice in vitro. METHODS: The inhibition ratio for OPN, OPTN, OPPTN (2.5,10,20 μg·mL-1), Oleanolic acid solutions (OS) group at various drug concentrations on Hca-F cultivated in vitro were assessed by WST-1 assay method after 24,48,72 hours of incubation, compared with Fluorouracil injection as positive control group. IC50 of 3 kinds of nanoparticles were determined, and blank nanoparticles (NPs) group, blank group (without any drug) and negative control group (culture medium added) were set up. RESULTS: IR of OPN group at the drug concentrations of 2.5,10,20 μg·mL-1 against Hca-F after 72 hours of incubation were (42.9 ±0.9)%, (63.6 ±1.1)%, (75.4 ±1.3)%; those of OPTN group were (54.3±1.2)%, (79.2 ±1.4)%, (92.6 ±1.5)%; those of OPPTN group were (50.8±0.8)%, (71.7±1.3)%, (83.9 ± 1.2)% ; but those of positive control group were (31.5 ± 0.9)% , (50.3±0.8)%, (60.6±0.9)%, respectively at the same time. The medium and high concentrations of IR in OPN group, OPTN group and OPPTN group were increased significantly after 72 hours, compared with corresponding concentration of positive control group (all P<0.01). IC50 of 3 kinds of nanoparticles against Hca-F were decreased as time going on, and that of OPTN group (8.64,1.39,0.38 μg·mL-1) was significantly lower than that of OPPTN group (11.86,5.52,3.46 μg-mL-1) and OPN group (30.27,8.21,5.00 ug-mL"') (P<0.05 or P<0.01), respectively. CONCLUSION: The IR of OPTN against Hca-F is the highest, which indicates that OPTN is characterized with considered biorncompatibity and significant anticancer activity in vitro.
展开▼
