云南霉素-RGD二甲酯偶联物的合成及其抗肿瘤细胞侵袭活性  

Synthesis of yunnanmycin-RGD(OCH_3)_2 conjugate compound and its anti-invasive activity against cancer cells

作　　者：郑艳波[1] 许先栋[1] 黄云虹[1] 甄永苏[1] 

机构地区：[1]中国医学科学院北京协和医学院医药生物技术研究所,北京100050

出　　处：《中国抗生素杂志》2009年第2期83-86,共4页Chinese Journal of Antibiotics

基　　金：国家自然科学基金项目(30400597)

摘　　要：目的制备云南霉素(yunnanmycin,YNM)与抗黏附肽RGD(Arg-Gly-Asp)的偶联物,增强RGD肽的细胞毒作用。方法化学方法合成云南霉素与RGD肽的偶联物,MTT法检测偶联物的细胞毒作用,Boyden chamber法分析偶联物的抗肿瘤细胞侵袭活性。结果合成了云南霉素与RGD肽的偶联物,其主要成份为云南霉素-RGD二甲酯。偶联物的细胞毒作用较RGD肽强,但与云南霉素相比有所下降;偶联物具有抗肿瘤细胞侵袭的能力,抗侵袭的能力与RGD肽相当。结论偶联物具有抗肿瘤细胞侵袭的活性,且细胞毒作用较RGD肽强。Objective To prepare the conjugate of yunnanmycin （YNM） and RGD （Arg-Gly-Asp） peptide for enhancing the cytotoxicity of RGD peptide. Methods YNM and RGD peptide were coupled by chemical conjugation. The cytotoxicity of the conjugate compound was tested by MTF assay. Boyden chamber assay was employed to investigate the anti-invasive activity of the conjugate compound against cancer cells. Results The major constituent of the compound was YNM-RGD（OCH3）2, and had stronger cytotoxicity than that of RGD but weaker than that of YNM. The inhibition of the invasion of cancer cells, and the anti-invasive activity was nearly the same as RGD peptide. Conclusions The conjugate compound has the anti-invasive activity against cancer cells, and its cytotoxicity is stronger than that of RGD peptide.

关 键 词：云南霉素-RGD二甲酯 RGD肽 云南霉素 抗侵袭活性 

分 类 号：R978.19[医药卫生—药品]