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目的:考察槲皮素(quercetin,QT)/香豆素-6(coumarin-6,C6)乙交酯丙交酯共聚物-维生素E聚乙二醇1000琥珀酸酯(polylactide-co-glycolide-D-α-tocopheryl polyethylene glycol 1000 succinate,PLGA-TPGS)纳米粒(QT/C6-loaded PLGATPGS nanoparticles,QCPTN)体外分别被人肝癌细胞株HepG2和小鼠腹水型高淋巴道转移肝癌细胞HCa-F的摄取情况,以及研究槲皮素PLGA-TPGS纳米粒(QT-loaded PLGA-TPGS nanoparticles,QPTN)体外对HepG2细胞的生长抑制率。方法:用激光共聚焦显微镜考察2种肝癌细胞HepG2和HCa-F对QCPTN的体外细胞摄取情况。采用WST-1法体外研究QPTN和槲皮素PLGA纳米粒(QT-loaded PLGA nanoparticles,QPN)对HepG2细胞生长的抑制性。试验分为6组,分别为阴性对照组、空白纳米粒(empty PLGA-TPGS nanoparticles,EPTN)组、氟尿嘧啶溶液(fluorouracil solutions,FS)组、槲皮素溶液(quercetin solutions,QTS)组、QPN组、QPTN组,分别在培育24、48、72 h加入WST-1后在酶标仪上450 nm下测定吸光度值,计算对HepG2细胞的生长抑制率。结果:在2种不同类型肝癌细胞摄取试验中,激光共聚焦显微镜镜下均可见显绿色荧光的QCPTN分布在2种肝癌细胞的细胞核周围,表明QCPTN可被HepG2和HCa-F细胞分别摄取进入细胞内。体外肝癌细胞生长抑制率试验结果表明,自制材料PLGA-TPGS对HepG2细胞生长无明显的抑制性;QPN和QPTN的体外对HepG2细胞生长抑制率有浓度依赖性和时间依赖性;QPTN对HepG2细胞的抑制率大于QPN、QTS和FS。结论:QCPTN通过细胞摄取作用可将模型药物QT和荧光标记物C6同时带入HepG2和HCa-F细胞内,QPTN体外显示对HepG2细胞生长具有较强的抑制性,与QPN、QTS和FS相比,具有较好的抑制肝癌细胞生长的作用。
Objective: To investigate the effects of quercetin (QT) / coumarin-6 (C6) glycolide-lactide copolymer-polylactide-co-glycolide- D-α-tocopheryl polyethylene glycol 1000 succinate (PLGA-TPGS) nanoparticles were respectively transfected into human hepatocellular carcinoma cell line HepG2 and mouse ascites hyperparathyroidism hepatocarcinoma HCa-F And the growth inhibition rate of HepG2 cells in vitro by QT-loaded PLGA-TPGS nanoparticles (QPTN). Methods: Laser confocal microscopy was used to investigate the uptake of QCPTN by HepG2 and HCa-F in two hepatocellular carcinoma cells in vitro. Inhibition of HepG2 cell growth by QPTN and QT-loaded PLGA nanoparticles (QPN) was investigated by WST-1 method in vitro. The experiment was divided into 6 groups: negative control group, empty PLGA-TPGS nanoparticles (EPTN) group, fluorouracil solution group (FS), quercetin solutions (QTS) group, QPN group , QPTN group, the absorbance values were measured at 450 nm on a microplate reader after adding WST-1 for 24, 48 and 72 h respectively, and the growth inhibition rate of HepG2 cells was calculated. Results: In the two different types of liver cancer cell uptake test, QCPTNs showing green fluorescence were observed around the nucleus of the two kinds of hepatocellular carcinoma cells under confocal laser scanning microscope, indicating that QCPTN can be ingested into the cells by HepG2 and HCa-F cells respectively Inside. The growth inhibition rate of HepG2 cells in vitro showed that PLGA-TPGS had no significant inhibitory effect on the growth of HepG2 cells in vitro. QPN and QPTN inhibited the growth of HepG2 cells in a concentration-dependent and time- The inhibition rate is greater than QPN, QTS and FS. CONCLUSION: QCPTN can induce both model drug QT and fluorescent marker C6 into HepG2 and HCa-F cells through cell uptake. QPTN shows strong inhibitory effect on HepG2 cells in vitro. Compared with QPN, QTS and FS , With better inhibition of the growth of liver cancer cells.