论文部分内容阅读
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 establish a method for the preparation of conjugates of fMLP with bamycin (BAM) and to evaluate its anti-tumor activity. METHODS: FMLP and BAM were coupled by coupling reagents EDC and NHS-SO_3. The coupling effect was detected by MALDI-TOF mass spectrometry. The conjugates were separated and purified by Sephadex G_ (15) Antibacterial effect, the use of mouse hepatoma H22 xenograft model to observe its anti-tumor effect. Results: The pure conjugate was obtained by Sephadex G_ (15) purification and the first half of peak 1 was collected. The antibacterial activity of conjugate fMLP-BAM was 17.0% of BAM and conjugate BAM-fMLP 5 mg · The tumor inhibition rate was 52.3% in the group of kg -1 (-1) and 67.6% in the group of 5 mg · kg -1 of BAM (P> 0.05). Conclusions: Conjugates of fMLP with BAM can be prepared according to the methods provided herein, but the in vivo antitumor activity of the conjugate slightly decreases compared to that of boeamycin.