来自波氏锡叶藤的DNA聚合酶β抑制剂。

DNA polymerase beta inhibitors from Tetracera boiviniana.

作者信息

Ma J, Starck S R, Hecht S M

机构信息

Department of Chemistry, University of Virginia, Charlottesville 22901, USA.

出版信息

J Nat Prod. 1999 Dec;62(12):1660-3. doi: 10.1021/np990326p.

DOI:10.1021/np990326p

PMID:10654414

Abstract

Bioassay-guided fractionation of an active methyl ethyl ketone extract of Tetracera boiviniana, using a sensitive assay to monitor DNA polymerase beta inhibition, resulted in the isolation of three known triterpenoids, betulinic acid (1), 3-cis-p-coumaroyl maslinic acid (2), and 3-trans-p-coumaroyl maslinic acid (3). Compounds 1-3 inhibited DNA polymerase beta with IC50 values of 14, 15, and 4.2 microM in the presence of bovine serum albumin (BSA) and 6.5, 7.5, and 2.0 microM in the absence of BSA, respectively. Further, compounds 1-3 potentiated the effects of bleomycin in cultured P-388D1 cells.

摘要

使用灵敏的测定法监测DNA聚合酶β抑制作用，对波氏刺蒴麻的活性甲乙酮提取物进行生物测定引导的分级分离，结果分离出三种已知的三萜类化合物，桦木酸（1）、3-顺式对香豆酰山楂酸（2）和3-反式对香豆酰山楂酸（3）。在存在牛血清白蛋白（BSA）的情况下，化合物1-3抑制DNA聚合酶β的IC50值分别为14、15和4.2微摩尔，在不存在BSA的情况下分别为6.5、7.5和2.0微摩尔。此外，化合物1-3增强了博来霉素在培养的P-388D1细胞中的作用。