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目的 为证实生物导向药物TGFα SAP对增殖平滑肌细胞特异性的细胞毒性作用。方法 我们用SPDP化学联结法合成了TGFα SAP ,并用3 H TdR参入法和3 H Leucine参入法探讨了TGFα SAP对平滑肌细胞及内皮细胞的DNA合成及蛋白质合成的影响。结果 联结后的TGFα SAP对增殖平滑肌细胞的3 H TdR参入量有明显抑制作用 ,与空白对照组比较3 H TdR参入量降低了 4 4 0 % ,同时TGFα SAP亦可明显抑制平滑肌细胞的蛋白质合成 ,而saporin本身显示出的细胞毒性作用则很弱。相反 ,TGFα SAP对增殖的内皮细胞的DNA和蛋白质合成却未显示出明显的抑制作用。结论 TGFα SAP具有较saporin明显增强的细胞毒性作用 ,而与内皮细胞相比 ,TGFα SAP对增殖平滑肌细胞表现出明显受体选择的特异性抑制作用
Aim To demonstrate the cytotoxicity of TGFα SAP, a biocontrol agent, on the proliferation of smooth muscle cells. Methods We synthesized TGFα SAP by SPDP chemical conjugation and investigated the effects of TGFα SAP on DNA synthesis and protein synthesis in VSMCs and endothelial cells by 3 H TdR incorporation and 3 H Leucine incorporation. Results TGFα SAP significantly inhibited the 3H-TdR incorporation in VSMCs. Compared with the blank control group, the incorporation of 3H-TdR decreased by 44.0%, and TGFα-SAP also significantly inhibited the protein synthesis of smooth muscle cells , While saporin itself shows a weak cytotoxic effect. In contrast, TGFα SAP did not show significant inhibition of DNA and protein synthesis in proliferating endothelial cells. Conclusion TGFα SAP has a significantly enhanced cytotoxic effect compared with saporin, whereas TGFα SAP shows specific inhibitory effect on the proliferation of smooth muscle cells compared with endothelial cells