DNA拓扑异构酶I抑制剂羟基喜树碱对小鼠腹水肝癌细胞组蛋.PDF

BIBLID -ISSN 0253—9756 中国琦理学报 AetaP^㈣ ∞钟I曲 smc 1993NovF it(6)|546—550 Inhibition ofphosphorylation ofhistoneH Iand H sinducedby ’ 10-hydroxycamptothecin ·DNA topoisomeraseIinhibitor， in m urine asciteshepatom a cells LING Yi-He ，XU Bin (Depaltment Pharmacolo## ，ShauqhaiIust~tuteof M ateriaMediea，ChineseAcademyoySconces，Shanghal200031，China) ABSrRACT Hydroxycamptothecin (HCPT)·~olated topoisomerase II) inhibitor， etoposide and from Campl0^eca 口c mt≈口l口，is a powerfulantitumor DNA untwisting proteins (DNA topoiso- alketloid． PCe~ousstudiesindicated thatthemoleeuiat meraseI)inhibitor，camptothecni suppressed targetofthisasentwasDN A topoisomerase I· The histone H land H sphosphorylati0n， and led presentresults demonstrated that vigro treatmentof intocellsarrested atG 2inBHK cells∞ ． murnieasctteshepatomacellswith HCPT resultedjna 10-Hydroxycamptothecin ( HCPT ) marked reduction in DNA synthesisand the inhibition ofphosphorylation in histone wasina time-dependent showed a m orepotentaCt ivity againstseveral manner． Gele1eclroOhores扭 f0und thatHCPT hada kinds ofturn or cell lines vitro and in vivo， selectively inhibitory effectoo the phosphorylation of and Iess sideeffect ni the elinic tr幢．Is as corn - histoneH land H ，，butlesseffecton theotherkindsof paredto camptothecin[”． HCPT induced topo hj搴tones． ，#vivo-HCPT also exhibited a suppressive I-associated DNA singtestrandbreaks and in— effecton histone H】and H ，phosphorylation· These hibited the synthesisofchrom atinprotein[。’ ． d8ta sugges