MODE OF ACTION OF THE SCHISTOSOMICIDE HYCANTHONE - SITE OF DNA ALKYLATION

被引：21

作者：

ARCHER, S ^{[1
]}

ELHAMOULY, W ^{[1
]}

SEYEDMOZAFFARI, A ^{[1
]}

BUTLER, RH ^{[1
]}

PICAMATTOCCIA, L ^{[1
]}

CIOLI, D ^{[1
]}

机构：

[1] INST CELL BIOL,ROME,ITALY

来源：

MOLECULAR AND BIOCHEMICAL PARASITOLOGY | 1990年 / 43卷 / 01期

关键词：

Deoxyguanosine adduct; DNA alkylation; Drug action; Hycanthone; Schistosoma mansoni;

D O I：

10.1016/0166-6851(90)90133-7

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Condensation of hycanthone N-methylcarbamate (HNMC) with deoxyguanosine (dG) furnished a mixture of the N-1 and N2 adducts which were purified and characterized as their acetates. Condensation of HNMC with thymidine (T) gave the N-3 adduct in poor yield. Adenosine (A) and cytidine (C) did not react with HNMC. Incubation of schistosomes with either [3H]hycanthone (HC) or [3H]HNMC furnished DNA to which [3H]HC was covalently bound. The alkylated DNA was degraded enzymically and the radiolabeled nucleosides were separated using HPLC. Two major peaks were observed which coincided in retention time with the synthetic N-1 and N2 alkylated dG. Alkylated T was absent. Thus, the site of alkylation of DNA by either HC or HNMC is dG. © 1990.

引用

页码：89 / 96

页数：8

共 11 条

[1] PREPARATION AND ANTISCHISTOSOMAL AND ANTITUMOR-ACTIVITY OF HYCANTHONE AND SOME OF ITS CONGENERS - EVIDENCE FOR THE MODE OF ACTION OF HYCANTHONE [J].