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RGD和YIGSR衍生物的抗肿瘤侵袭、转移活性

ACTIVITIES OF RGD AND YIGSR DERIVATIVE ON ANTI TUMOR INVASION AND METASTASIS

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【作者】 赵铁华; 杨鹤松; 高巍; 邓淑华; 石艳华; 施波;

【Author】 ZHAO Tie hua, YANG He song, GAO Wei,et al. Chengde Medical College,Chengde 067000,China

【机构】 承德医学院!承德067000; 中国医学科学院药物研究所!北京100050;

【摘要】 目的 研究抗肿瘤转移肽Arg Gly Asp(RGD)和Tyr Ile Gly Srg Arg(YIGSR)的均叉、杂叉聚合肽的抗肿瘤侵袭、转移作用。方法 MTT法测定药物对PG和LA795细胞粘附Matrigel能力的影响 ;Transwell细胞培养小室测定药物对PG细胞侵袭重组基底膜能力的影响 ;观察药物对LA795小鼠肺腺癌细胞自发肺转移模型抗肿瘤转移的影响。结果 在 5 0~ 10 0 μg/ml浓度范围 ,RGD和YIGSR的杂叉肽WF12和YIGSR的均叉肽WF2 7的抗粘附作用强于RGD和YIGSR肽 ;以上二肽在 10 0 μg/ml浓度的抗肿瘤侵袭作用优于RGD和YIGSR肽 ;以上二肽 10 0 μg/只 ,静脉给药仅 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 RGD与YIGSR的杂叉肽WF12和YIGSR的均叉肽WE2 7具有较强的抗肿瘤侵袭、转移活性。

【Abstract】 Objective Study of identical/un identical fork peptides Arg Gly Asp(RGD) and Tyr Ile Gly Ser Arg(YIGSR) on anti tumor invasion and metastasis was carried out. Methods MTT method was used to assay the effect of drug on PG cell and the LA795 cell adhesive capability on Matrigel. Transwell was used to assay the effect of drug on PG cell invasive capability on reformed basement membrane. The effect of anti metastatic drug was observed in mouse adenocarcinoma LA795 cell model that will automatically metastasize to lung. Results The un identical fork peptide WF12 of RGD and identical fork peptide of YIGSR WF27 had better anti adhesion effect than that of RGD and YIGSR at 50~100 μg/ml concentration. The former two peptides had better anti tumor invasion effect at dose of 100 μg/ml than the RGD and YIGSR. After five consecutive intravenous administrations of WF12 or WF27 at a dose of 100 μg/time/mouse, the LA795 lung metastatic nodule number and the weight of metastatic lung could be decreased significantly.Conclusion Un identical fork peptide WF12 of RGD and of YIGSR and identical fork poptide WF27 of YIGSR had much better anti tumor invasive and metastatic activities.$$$$

【基金】 河北省自然科学基金资助 (编号 3 962 70 )
  • 【分类号】R73-36
  • 【被引频次】7
  • 【下载频次】166
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