Ungeremine effectively targets mammalian as well as bacterial type I and type II topoisomerases

被引：50

作者：

Casu, Laura ^{[2
]}

Cottiglia, Filippo ^{[2
]}

Leonti, Marco ^{[2
]}

De Logu, Alessandro ^{[3
]}

Agus, Emanuela ^{[3
]}

Tse-Dinh, Yuk-Ching ^{[4
]}

Lombardo, Valentina ^{[1
]}

Sissi, Claudia ^{[1
]}

机构：

[1] Univ Padua, Dept Pharmaceut Sci, Padua, Italy

[2] Univ Cagliari, Dipartimento Farmaco Chim Tecnol, I-09124 Cagliari, Italy

[3] Univ Cagliari, Dipartimento Sci & Tecnol Biomed, Sez Microbiol Med, I-09124 Cagliari, Italy

[4] New York Med Coll, Dept Biochem & Mol Biol, Valhalla, NY 10595 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 23期

关键词：

Topoisomerase; Alkaloid; Anticancer; Antibacterial; Pancratium illyricum L; ANTICANCER DRUG DESIGN; AMARYLLIDACEAE ALKALOIDS; DNA TOPOISOMERASES; NATURAL-PRODUCTS; LYCORINE; CELLS; LYCOBETAINE; DERIVATIVES; BLOOD;

D O I：

10.1016/j.bmcl.2011.09.097

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

From the methanol extract of the bulbs of Pancratium illyricum L., three phenanthridine type alkaloids, ungeremine (1), (-)-lycorine (2) and (+)-vittatine (3) were isolated. For the evaluation of their anticancer and antibacterial potential, compounds 1-3 were tested against human (I, II alpha) and bacterial (IA, IV) topoisomerases. Our data demonstrated that ungeremine impairs the activity of both, human and bacterial topoisomerases. Remarkably, ungeremine was found to largely increments the DNA cleavage promoted by bacterial topoisomerase IA, a new target in antimicrobial chemotherapy. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：7041 / 7044

页数：4

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