Solid-phase synthesis of melittin of anti-tumor peptide
-
摘要: 目的 合成具有抗肿瘤活性的二十六肽蜂毒素。 方法 采用Fmoc固相逐步化学合成,确立了以Wang树脂为固相载体,HOBt/DCC为缩合剂的合成工艺。 结果 通过本法能够顺利合成得到二十六肽蜂毒素,收率达32%。 结论 该合成方法具有可行性强、操作简便、总收率高等特点,适用于长链多肽的合成。Abstract: Objective To synthesize the antitumor activity of twenty-six peptide melittin. Methods The melittin was synthesized by stepwise solid-phase peptide synthesis (SPPS). During the synthesis of melittin, wang-resin was chosen as solid supporter and HOBt/DCC were used as the coupling reagent. Results The melittin was synthesized with yield of 32%. Conclusion The synthetic method was feasible, simple and with high yield for long chain polypeptide synthesis.
-
Key words:
- melittin /
- solid-phase peptide synthesis /
- stepwise synthesis
-
[1] Huh JE, Kang JW, Nam D, et al. Melittin suppresses VEGF-A-induced tumor growth by blocking VEGFR-2 and the COX-2-mediated MAPK signaling pathway[J]. J Nat Prod,2012, 75(11), 1922-1929. [2] 高启龙, 李寒冰, 姚亚民, 等. 蜂毒素(Mel)对裸鼠骨肉瘤的抑制作用与影响肿瘤血管生成、细胞增殖和凋亡的关系[J]. 复旦学报:医学版, 2012, 39 (03):283-288. [3] Jo M, Park MH, Kollipara PS, et al. Anti-cancer effect of bee venom toxin and melittin in ovarian cancer cells through induction of death receptors and inhibition of JAK2/STAT3 pathway[J].Toxicol Appl Pharmacol,2012, 258(1), 72-81. [4] Liu S, Yu M, He Y, et al. Melittin prevents liver cancer cell metastasis through inhibition of the Rac1-dependent pathway[J]. Hepatology, 2008, 47(6), 1964-1973. -
点击查看大图
计量
- 文章访问数: 4278
- HTML全文浏览量: 507
- PDF下载量: 306
- 被引次数: 0
下载:
