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替莫唑胺衍生物治疗人脑胶质瘤的实验研究 被引量:4

Experimental study on temozolomide derivatives for the treatment of human gliomas
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摘要 目的观察替莫唑胺(TMZ)类水溶性衍生物2T-P400、2T-P600对人脑胶质瘤的抑制效应。方法体外抑瘤实验:以MTT法测定2T-P400、2T-P600、PEG400、PEG600、TMZ相对于空白对照组对胶质瘤细胞SHG-44的抑制率。体内抑瘤实验:制备荷SHG44人脑胶质瘤裸小鼠模型,将荷瘤鼠随机分为TMZ组、2T-P400组、2T-P600组、聚乙二醇(PEG)组及生理盐水组,TMZ口服给药,其他药物均为鼠尾静脉注射给药,每4天测量肿瘤体积。结果体外抑瘤效应:2T-P400和2T-P600对SHG44细胞的杀伤效果与TMZ相近,均明显优于PEG400和PEG600(P<0.01)。体内抑瘤效应:TMZ组、2T-P400组和2T-P600组抑瘤率亦明显高于PEG组及生理盐水组(P<0.05),未见明显药物不良反应。结论 2T-P400、2T-P600保留TMZ的抑瘤活性,为胶质瘤病人在术后TMZ类药物化疗提供新的药物及用药途径选择。 Objective To observe the tumor suppression effect of temozolomide(TMZ) water-soluble derivatives(2T-P400,2T-P600) against human gliomas.Methods Anti-tumor test in vitro: The tumor control rate of 2T-P400,2T-P600,PEG400,PEG600 and TMZ were assayed by MTT method in the blank control group.Anti-tumor test in vivo: SHG44 glioma-bearing nude mice models were prepared,and divided randomly into TMZ group,2T-P400 group,2T-P600 group,PEG group and normal saline(NS) group.TMZ was administered orally,and the other drugs were administered via tail vein injection.Tumor volumes of the mice were measured once every four days.Results Anti-tumor effect in vitro: The anti-glioma effects of 2T-P400 and 2T-P600 were almost the same level with that of TMZ against SHG44 cells,and the effects were much better than those in PEG group and NS group(P 0.01).Anti-tumor test in vivo: Tumor inhibition ratios in TMZ,2T-P400 and 2T-P600 groups were higher than those in PEG and NS groups(P 0.05).No obvious adverse drug reactions occurred.Conclusions 2T-P400 and 2T-P600 retain anti-tumor activity of TMZ,and will provide new drugs and treatment option for chemotherapy with TMZs in post-operative glioma patients.
出处 《中国微侵袭神经外科杂志》 CAS 2012年第3期124-126,共3页 Chinese Journal of Minimally Invasive Neurosurgery
基金 国家自然科学基金(编号:81071766) 江苏省自然科学基金(编号:BK2010227)
关键词 神经胶质瘤 替莫唑胺 替莫唑胺衍生物 动物 实验 小鼠 glioma temozolomide temozolomide derivatives animals laboratory mice nude
作者简介 通讯作者:董军,Email:djdongjun@163.com
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  • 1http://www.accessdata.fda.gov/scripts/cder/onctools/summary.cfm?ID=192;http://www.accessdata.fda.gov/drugsatfda_ docs/label/2006/021029s0121bl.pdf.
  • 2Wesolowski J R,Rajdev P,Mukheiji S K.Temaozolomide(Temadar)[J].Am J Neuroradiol,2010,31(8):1383-1384.
  • 3http://www.nottingham.ac.uk/pharmacy/people/malcolm.stevens.
  • 4Ege Q Gilbert K.[7+2]-and [1 l+2]-cycloadditionreactions of diazo-azoles with isocyanates to azolo[5,l-d][1,2,3,5] tetrazine-4-ones [J].Tetrahedron Lett,1979,20(44):4253-4256.
  • 5Stevens M F,Hickman J A,Stone R,et al.Antitumorimidazotetrazines.1.Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3H)-one,a novel broad-spectrum anti tumor agent [J].J MedChem,1984,27(2):196-201.
  • 6http://info.cancerresearchuk.org/cancerandresearch/progress/cancer.drags/drug_discovery/temozolomide/.
  • 7Hickman J A,Stevens M F,Gibson N W,et al.Experimentalantitumor activity against murine tumor model systems of8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-l,2,3?5-tetrazin-4(3H)-one(mitozolomide),a novel broad-spectrum agent[J].Cancer Res,1985,45(7):3008-3013.
  • 8Stevens M F,Hickman J A,Langdon S P,et al.Antitumoractivity and pharmacokinetics in mice of 8-carbamoyl-3-methyl-imidazo[5,l-d]-l,2,3,5-tetrazin-4(3H)-one(CCRG81045; M & B 39831),a novel drug with potential as analternative to dacarbazine [J].Cancer Res,1987,47(22):5846-5852.
  • 9Wang Y F,Stevens M F Q al.Alternative syntheses tothe antitumour drug temozolomide avoiding the use ofmethyl isocyanate [J].J Chem Soc Chem Commun,1994,1687-1689.
  • 10Wang Y F,Stevens M F Q e/ al.Antitumourimidazotetrazines.Part 34.new syntheses of the antitumourdrug temozolomide using "Masked" methyl isocyanates [J].JChem Soc Perkin Trans,1995,2783-2787.

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