Synthesis of DTPA-c-myc Antisense Oligonucleotides and Labeling With ~(113)In~m
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摘要: 合成了DTPA-c-myc反义核酸,并对其进行了113Inm标记;考察了标记物113Inm-DTPA-c-myc反义核酸在生理盐水和牛血清中的稳定性和对平滑肌细胞增殖的影响。标记结果显示,在最佳标记条件下标记率为35%~40%,标记物纯化后放化纯度>90%1。13Inm-DTPA-c-myc反义核酸在生理盐水中48 h放化纯度>94.0%,在血清中48 h放化纯度仅为76.1%。细胞增殖结果显示:113Inm-DTPA-c-myc反义核酸浓度达到10μmol/L(92.5 GBq/L)时抑制率达到最大,113Inm-DTPA-c-myc反义核酸(放射性反义治疗组)和反义核酸(反义治疗组)1、13InmCl3溶液(放射性治疗组)、不加核酸或113InmCl3溶液(对照组)和c-myc正义核酸(正义治疗组)对平滑肌细胞增殖的抑制率分别为84.5%、69.3%、20.6%、15.2%、0,放射性反义治疗组与反义治疗组、放射性治疗组、对照组相比有显著性差异(P<0.05、P<0.01、P<0.01),反义治疗组和正义治疗组相比也有显著性差异(P<0.01)。这说明合成的113Inm-DTPA-c-myc反义核酸在体外可有效抑制猪血管平滑肌细胞增殖。
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关键词:
- DTPA-c-myc反义核酸 /
- 113Inm /
- 标记
Abstract: DTPA-c-myc antisense oligonucleotides is synthesized and labeled with ~(113)In~m.The stability of ~(113)In~m-DTPA-c-myc antisense oligonucleotides in saline and bovine serum and the inhibition of cell proliferation are studied.The labeling yield in the optimal conditions is 35%～40% and the radiochemical purity is more than 90% after purification.The radiochemical purity of ~(113)In~m-DTPA-c-myc is more than 94.0% for 48 h in saline,and(76.1%) for 48 h in serum.When the concentration of ~(113)In~m-DTPA-c-myc antisense oligonucleotides is 10 μmol/L(92.5 GBq/L),the inhibition rate reaches the highest.The inhibition rate of ~(113)In~m-DTPA-c-myc antisense oligonucleotides(radionuclide antisense-treated group),antisense oligonucleotides(antisense-treated group),~(113)In~mCl_3 solution(radionuclide-treated group),without oligonucleotides or ~(113)In~mCl_3 solution(control group) and c-myc sense oligonucleotides(sense-treated group)is 84.5%,69.3%,20.6%,15.2% and 0,respectively.The inhibition of radionuclide antisense-treated group is significantly higher than that of antisense-treated group(P<0.05),radionuclide-treated group(P<0.01) and control group(P<0.01),and the inhibition of antisense-treated group is significantly higher than that of sense-treated group(P<0.01). Which demonstrates that ~(113)In~m-DTPA-c-myc antisense oligonucleotides can inhibite the proliferation of porcine VSMCs in vitro.-
Keywords:
- DTPA-c-myc antisense oligonucleotides /
- ~(113)In~m /
- labeling
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