A comparison of the mechanisms of action of VP-16-213 and podophyllotoxin.

Lloydia Pub Date : 1977-01-01
S B Horwitz, J D Loike
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Abstract

A comparison of the mechanism of action of VP 16-213 and podophyllotoxin has revealed that although both drugs inhibit nucleoside uptake in HeLa cells, they exhibit other biological properties which are quite distinct. Podophyllotoxin inhibits microtubule assembly in vitro while VP-16-213 has no effect in this system. VP-16-213 induces single-stranded breaks in DNA in HeLa cells, an effect which may explain the cytoxicity of VP-16-213. In contrast to VP-16-213-treated cells, cells treated with podophyllotoxin maintain DNA integrity and show no evidence of single-stranded breaks.

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VP-16-213与鬼臼毒素作用机制的比较。
通过对VP 16-213和鬼臼毒素作用机制的比较发现,虽然这两种药物都抑制HeLa细胞对核苷的摄取,但它们表现出截然不同的其他生物学特性。鬼臼毒素在体外抑制微管组装,而VP-16-213在体外无作用。VP-16-213诱导HeLa细胞DNA单链断裂,这一效应可能解释了VP-16-213的细胞毒性。与vp -16-213处理的细胞相比,用鬼臼毒素处理的细胞保持DNA完整性,没有单链断裂的迹象。
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