摘要
目的:设计并合成具有抗肿瘤侵袭活性的含Arg-Gly-Asp(RGD)和Tyr-Ile-Gly-Ser-Arg(YIGSR)新型肽类化合物。方法:RGD和YIGSR均有抗肿瘤侵袭活性,在此基础上设计了α-精甘天冬氨酰-ε-酪异亮甘丝精氨酰赖氨酸甲酯,并采用固相法合成。观察其对小鼠肺腺癌细胞自发肺转移模型抗肿瘤转移的影响。结果:目标化合物总收率56%,结构经质谱鉴定。静脉给药每只100μg,5次可显著抑制移植LA795细胞肺转移小鼠的肺脏重量和肺转移结节数。结论:目标化合物具有较强的抗肿瘤侵袭活性。
Objective: To synthesize a peptide with Arg-Gly-Asp (RGD) and Tyr-Ile-Gly-Ser-Arg(YIGSR) fragments with the anti-tumor activity. Methods: The peptide, α-arginylglycylaspartyl-ε-tyrosyliesoleucylglycyl-serylarginylysine methyl ester, was synthesized. The biological activity of the peptide against metastatic lung cancer was evaluated in mouse adenocarcinoms LA795 cell model. Results: The peptide yielded by 56%. The peptide structure was verified by the mass spectrum. The mice with metastatic LA795 lung cancer intravenously receiving 1 000μg/mouse of the peptide solution for five injections had significant reductions of the number of metastatic LA795 lung nodule and the weight of lung tissues. Conclusion: The synthetic peptide shows powerful activities against invasive tumors.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2005年第6期729-731,共3页
Chinese Journal of New Drugs
