抗肿瘤前列腺素对拓扑异构酶的抑制特性。
Inhibitory properties of antitumor prostaglandins against topoisomerases.
作者信息
Suzuki Keitarou, Uyeda Masaru
机构信息
Laboratory of Pharmaceutical Microbiology, Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
出版信息
Biosci Biotechnol Biochem. 2002 Aug;66(8):1706-12. doi: 10.1271/bbb.66.1706.
Prostaglandins (PGs) having antitumor activity such as delta12,14-PGJ2, delta12-PGJ2, PGA2 and PGA1 strongly inhibited topoisomerase II (topo II) from human placenta, the potential order of inhibitory activity of the PGs resembling that of the antitumor activity. PGs having no antitumor activity did not inhibit topo II. Delta12,14-PGJ2 to be a potent inhibitor showed inhibitions to some extent against topo I from wheat germ, NIH3T3 and calf thymus gland, and showed no inhibition against the enzymes from Vero, A549, HeLa and COLO 201 cells. Delta12,14-PGJ2 differentially inhibited topo I from different sources. Delta12,14-PGJ2 was a topo inhibitor of the cleavable complex-nonforming type without DNA intercalation.
具有抗肿瘤活性的前列腺素（PGs），如δ12,14 - PGJ2、δ12 - PGJ2、PGA2和PGA1，强烈抑制人胎盘的拓扑异构酶II（topo II），这些PGs的抑制活性潜在顺序与抗肿瘤活性相似。没有抗肿瘤活性的PGs不抑制topo II。作为一种有效抑制剂的δ12,14 - PGJ2对来自小麦胚芽、NIH3T3和小牛胸腺的拓扑异构酶I有一定程度的抑制作用，而对来自非洲绿猴肾细胞（Vero）、人肺癌细胞（A549）、人宫颈癌细胞（HeLa）和人结肠癌细胞（COLO 201）的酶没有抑制作用。δ12,14 - PGJ2对不同来源的拓扑异构酶I有不同程度的抑制作用。δ12,14 - PGJ2是一种不形成可裂解复合物且无DNA嵌入的拓扑异构酶抑制剂。
Zotero 插件