目的 制備槲皮素聚氰基丙烯酸正丁酯納米粒子（QT-PBCA）并考察其理化性質(zhì)、體外抗人子宮內(nèi)膜癌作用。方法 采用陰離子乳液聚合法制備QT-PBCA納米粒子。透射電鏡觀察納米粒子的形態(tài)，Zeta電位儀檢測(cè)粒徑和Zeta電位，紅外光譜儀檢測(cè)QT-PBCA納米粒子、BCA單體、QT、空載體PBCA納米粒子的紅外吸收光譜，MTT法檢測(cè)細(xì)胞存活率。結(jié)果 QT-PBCA納米粒子呈球形或橢圓形，表面光滑，在透射電鏡下因PBCA固有的黏合特性而處于略微聚集的狀態(tài)，其平均粒徑為（161.1±0.44）nm，Zeta電位為（-7.28±0.60）mV，平均包封率為（79.86±0.45）%。在納米粒子的封裝以及制備的過(guò)程中槲皮素與聚合物之間可能發(fā)生的反應(yīng)。槲皮素封存到PBCA納米粒子中是靠分子間作用力（如氫鍵）完成的。隨著順鉑、納米粒子濃度的增加，JEC、LO2細(xì)胞的存活率降低，且順鉑組相比于納米粒子組的存活率要更低（P<0.05）。納米粒子在6.67 mg/L對(duì)LO2細(xì)胞有一定的毒性，但隨著濃度增高，反而會(huì)產(chǎn)生促進(jìn)細(xì)胞增殖的作用。結(jié)論 QT-PBCA納米粒子具有良好的理化性質(zhì)和抗腫瘤作用且對(duì)正常細(xì)胞無(wú)害，有潛力成為新型抗癌藥物。

Objective To prepare Quercetin Polybutylcyanoacrylate (QT-PBCA) Nanoparticles and study its physicochemical properties and anti-human endometrial cancer effect in vitro. Methods QT-PBCA nanoparticles were prepared by anionic emulsion polymerization method. Morphology of the nanoparticles was observed with transmission electron microscopy. Particle size and Zeta potential were detected with Zeta potentiometer. IR of QT-PBCA nanoparticles, BCA monomers, QT, and empty carrier PBCA nanoparticles were measured with infrared spectrometer. Cell proliferation rate was measured by MTT method. Results The prepared QT-PBCA nanoparticles were spherical or elliptical, indicating that they were smooth. They were slightly aggregated under the transmission electron microscope due to the inherent adhesion characteristics of PBCA. The average particle diameter was (161.1 ±0.44) nm, and the Zeta potential was (−7.28 ±0.60) mV, and the average encapsulation rate was (79.86 ±0.45)%. The possible reaction between quercetin and polymer happened during the encapsulation and preparation of nanoparticles. Quercetin was encapsulated into PBCA nanoparticles by intermolecular forces, such as hydrogen bonds. After the treatment of JEC and LO2 cells with different concentrations of cisplatin and QT-PBCA nanoparticles, the survival rate of JEC and LO2 cells decreased with the increase of cisplatin concentration, and the survival rate was lower than that of the treatment group (P<0.05). QT-PBCA nanoparticles had certain toxicity to LO2 cells at a concentration of 6.67 mg/L, but as the concentration increased, they could instead promote cell proliferation. Conclusion QT-PBCA nanoparticles have good physical and chemical properties, anti-tumor effects, and are not harmful to normal cells. They have the potential to become new anticancer drugs.

R944

河南省科技發(fā)展計(jì)劃項(xiàng)目（182102310184、182102311190）