α-苦瓜素及α-苦瓜素-PEG体外抗HSV-1的研究  

The anti-HSV-1 activity of α-momorcharin and its PEGylated conjugates in vitro

作　　者：黄文虎[1] 邓缅[1] 孟延发[1] 

机构地区：[1]四川大学生命科学学院生物资源与生态环境教育部重点实验室,四川成都610064

出　　处：《华西药学杂志》2012年第1期1-4,共4页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:30770232)

摘　　要：目的研究苦瓜籽核糖体失活蛋白α-苦瓜素(α-MMC)体外抗单纯疱疹病毒(HSV-1)的活性及其聚乙二醇修饰物(α-MMC-PEG)保留这一活性的程度。方法采用MTT法测定α-MMC和α-MMC-PEG对Vero细胞的体外毒性;通过对所培养的上清液中HSV-1囊膜糖蛋白抗原的测定、细胞和病毒的预处理试验,研究了α-MMC和α-MMC-PEG体外抗HSV-1的活性。结果α-MMC和α-MMC-PEG对HSV-1囊膜糖蛋白抗原分泌的抑制作用均呈剂量依赖性,IC50分别为0.67、2.94μmol.L-1;相同剂量下,α-MMC-PEG可保留60%天然α-MMC的抑制活性。3.3μmol.L-1的α-MMC和α-MMC-PEG直接作用病毒后使Vero细胞的存活率分别提高了22%、17%。结论α-MMC经PEG修饰后可保留较高的抗HSV-1活性,修饰前后都对HSV-1有一定的直接灭活作用。OBJECTIVE To study the anti-HSV-1 activity of alpha-momorcharin（α-MMC） and its PEGylated conjugates in vitro.METHODS MTT assay was used to investigate the toxicity of α-MMC and α-MMC-PEG conjugates in vero cells.Inhibition of proteins on HSV-1 antigen secretion,cell pretreatment and virus pretreatment assays were carried out to test the anti-HSV-1 activity of α-MMC and α-MMC-PEG conjugates.RESULTS α-MMC and α-MMC-PEG conjugates actively inhibited HSV-1 glycoprotein secretion in a dose-dependent manner with IC50 of 0.67 μmol·L-1 and 2.94 μmol·L-1,respectively.α-MMC-PEG preserved about 60% inhibiting activity of native.Compared with the positive control,the cell viability in virus pretreatment with 3.3 μmol·L-1α-MMC and α-MMC-PEG groups increased by 22% and 17%,respectively.CONCLUSION PEGylation of α-MMC preserved a high anti-HSV-1 activity of native,and both of them could inactivate HSV-1 directly in vitro.

关 键 词：α-苦瓜素 α-苦瓜素-PEG 聚乙二醇修饰 单纯疱疹病毒 抗病毒活性 

分 类 号：R96[医药卫生—药理学]