槲皮素固体脂质纳米粒对Aβ25-35损伤的PC12细胞雌激素样神经保护作用的研究  

Study on estrogen like neuroprotective effect of quercetin solid lipid nanoparticles on PC12 cells injured by Aβ25-35

作　　者：郭童林 甄艳杰 赵雨薇 沈丽霞 GUO Tong-lin;ZHEN Yan-jie;ZHAO Yu-wei;SHEN Li-xia(Dept of Pharmacy,Hebei North University, Hebei Key Lab of Neuropharmacology, Zhangjiakou Hebei 075000, China)

机构地区：[1]河北北方学院药学系,河北省神经药理学重点实验室,河北张家口075000

出　　处：《中国药理学通报》2020年第10期1409-1415,共7页Chinese Pharmacological Bulletin

基　　金：河北省自然科学基金资助项目(No H2019405057);河北省高等学校科学技术研究项目(No ZD2020136);河北省研究生创新项目(No CXZZSS2019147)。

摘　　要：目的考察槲皮素固体脂质纳米粒(quercetin solid lipid nanoparticles,Que-SLN)对Aβ25-35损伤的PC12细胞的雌激素样神经保护作用。方法通过熔融超声法制备Que-SLN并进行理化性质评价;Transwell小室考察Que-SLN体外血脑屏障通透性;MTT法测定不同处理组细胞活力、免疫荧光染色法和Western blot技术检测ERα和ERβ蛋白的表达。结果制备的Que-SLN包封率为(90.54±1.36)%,载药量(4.33±0.06)%,粒径(191.23±3.25)nm,电位(-24.40±1.24)mV,外观呈球形,形态较圆整,大小均一;与Que组相比,Que-SLN的血脑屏障通透性增加(P<0.01);Que-SLN(50、100、200μmol·L^-1)浓度组的细胞的存活率分别为(116.79±2.75)%(P<0.01),(119.46±1.89)%(P<0.01),(107.55±3.17)%(P<0.05),与Aβ25-35组相比,Que-SLN各浓度组均能增加细胞的存活率;免疫荧光染色和Western blot结果显示,与Aβ25-35组相比,Que-SLN能提高ERα蛋白表达量,对ERβ蛋白表达无影响。结论熔融超声法适用于Que-SLN的制备,制备成Que-SLN后增加了Que的血脑屏障通透性,Que-SLN对Aβ25-35诱导的PC12细胞的损伤具有雌激素样神经保护作用。Aim To study the estrogen like neuroprotective influence of quercetin solid lipid nanoparticles(Que-SLN)on PC12 cells injured by Aβ25-35.Methods Que-SLN was prepared by melt ultrasound andits physical and chemical properties were evaluated;Transwell chamber was used to investigate the permeability of blood-brain barrier of Que SLN in vitro;MTT assay was used to determine the activity of cells in different treatment groups,and immunofluorescence staining and Western blot were used to detect the expression of ERαand ERβ.Results The entrapment efficiency of Que-SLN was(90.54±1.36)%,drug loading was(4.33±0.06)%,particle size was(191.23±3.25)nm,potential was(-24.40±1.24)mV;the appearance was spherical,the shape was round,and thesize was uniform.Compared with Que,the permeability of BBB of Que-SLN increased(P<0.01).The survival rate of cells in Que-SLN(50,100,200μmol·L^-1)concentration group was(116.79±2.75)%(P<0.01),(119.46±1.89)%(P<0.01),(107.55±3.17)%(P<0.05),respectively.Compared with Aβ25-35 group,Que-SLN each concentration group could increase the survival rate of cells.The results of immunofluorescence staining and Western blot showed that Que-SLN significantly increased the expression of ERαprotein compared with the Aβ25-35 group,with no effect on the expression of ERβprotein.Conclusions Molten ultrasound is suitable for the preparation of Que-SLN.After the preparation of Que SLN,the permeability of blood-brain barrier of Que increases.Que-SLN has estrogen like neuroprotective effect on PC12 cell injury induced by Aβ25-35.

关 键 词：槲皮素 固体脂质纳米粒 血脑屏障 雌激素样作用 ERα ERΒ 

分 类 号：R285.5[医药卫生—中药学] R322.81[医药卫生—中医学]