趋化肽fMLP与博安霉素偶联物制备及其体内抗肿瘤活性的初步评价  

Preparation of Conjugate of Chemotactic Peptide fMLP-Boanmycin and Initial Evaluation of its Antitumor Activity in Vivo

作　　者：李忠东[1] 

机构地区：[1]空军总医院药学部药理室,北京100036

出　　处：《中国药师》2010年第1期20-22,共3页China Pharmacist

摘　　要：目的:建立fMLP与博安霉素(BAM)的偶联物制备方法,初步评价其抗肿瘤活性。方法:以偶联剂EDC和NHS-SO_3将fMLP与BAM进行偶联,以MALDI-TOF质谱检测其偶联效果,以Sephadex G_(15)分离纯化偶联物;以TTC法观察偶联物的抗菌作用,采用小鼠肝癌H22移植瘤模型来观察其抗肿瘤作用。结果:通过Sephadex G_(15)分离纯化,收集第1峰前半部分获得了较纯的偶联物;偶联物fMLP-BAM的抗菌活性是BAM的17.0%,偶联物BAM-fMLP 5 mg·kg^(-1)组抑瘤率为52.3%,BAM 5 mg·kg^(-1)组抑瘤率为67.6%(P>0.05)。结论:根据本文提供的方法可以制备fMLP与BAM的偶联物,但该偶联物体内抗肿瘤活性与博安霉素相比略有下降。Objective： To set up a method for linking Chemotaetic peptide fMLP with boanmycin （BAM） and initially evaluate its antitumor activity. Method： BAM and fMLP were conjugated with EDC and NHS-SO3. The conjugates were identified by MALDI-TOF. Sephadex G15 was used to purified conjugate. Antibacterial activity was determined by TTC assay. The model of subcutaneously transplanted hepatoma 22 in mice was used to evaluate antitumor activity. Result： Pure conjugate may be obtained by Sephadex G15. Antibacterial activity of the BAM-fMLP conjugate was 17% of BAM＇ s. The conjugate or BAM inhibited the growth of tumor by 52.3% or 67.6%. Conclusion ： According to the method presented by this paper,fMLP-BAM conjugates may be prepared. But its antitumor activity is slightly lower than that of BAM＇ s.

关 键 词：趋化肽 FMLP 博安霉素 偶联物 

分 类 号：R965.1[医药卫生—药理学]