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;邓缅;孟延发;
Author：
收稿日期： 年卷（期）页码：2012,27(01):-1-4
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：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
Key words：
基金项目：国家自然科学基金资助项目(批准号:30770232)
中文摘要
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。
英文摘要
[1]张兴权,范江.艾滋病毒感染与艾滋病[M].北京:人民卫生出版社,1999:162-166.
[2]Ng TB,Liu WK,Sze SF,et al.Action of alpha-momorcharin,aribosome inactivating protein,on cultured tumor cell lines[J].Pharmacol,1994,25:75-77.
[3]Leung SO,Yeung HW,Leung KN.The immunosuppressive activi-ties of two abortifacient proteins isolated from the seeds of bittermelon(Momordica charantia)[J].Immunopharma,1987,13:159-171.
[4]Ng TB,Chan WY,Yeung HW.Proteins with abortifacient,ribo-some inactivating,immunomodulatory,antitumor and anti-AIDSactivities from Cucurbitaceae plants[J].General Pharmacology:Vascular Sys.1992,23:575-590.
[5]陈伊雯,刘敏,姚光川,等.α-苦瓜素和PEG-α-苦瓜素抑制绒癌JAR细胞迁移和侵袭的研究[J].华西药学杂志,2011,26(1):1-5.
[6]Bian XX,Shen FB,Chen YW,et al.PEGylation of alpha-mo-morcharin:synthesis and characterization of novel anti-tumorconjugates with therapeutic potential[J].Biotechnol Let,2010,32(7):883-900.
[7]伍黎黎,沈富兵,刘敏,等.聚乙二醇修饰对α-苦瓜素抗肿瘤活性的影响[J].华西药学杂志,2011,26(1):5-8.
[8]陈鸿珊,张兴全.抗病毒要去及其研究方法[M].北京:化学工业出版社,2006:148-149.
[9]Balzarini J,Degreve B,Andrei,et al.Superior cytostatic activityof the ganciclovir elaidic acid ester due to the prolonged intracel-lular retention of ganciclovir anabolites in herpes simplex virustype 1 thymidine kinase gene-transfected tumor cells[J].GeneTher,1998,5:419-426.
[10]Au TK,Collins RA,Lam TL,et al.The plant ribosome inactiva-ting proteins luffin and saporin are potent inhibitors of HIV-1integrase[J].FEBS Let,2000,471:169-172.
[11]Bourinbaiar AS,Lee Huang S.The activity of plant-derived an-tiretroviral proteins MAP3O and GAP31 against herpes simplexvirus infection in vitro[J].Biochem Biophys Res Comm,1996,219:923-929.
[12]Werlen M,Bernkop Schnurch A.Strategies to improve plasma halflife time of peptide and protein drugs[J].Amino Acids,2006,30:351-367.
【关闭】
