Flavones from Struthiola argentea with anthelmintic activity in vitro

被引：44

作者：

Ayers, Sloan ^{[1
]}

Zink, Deborah L. ^{[1
]}

Mohn, Kenneth ^{[2
]}

Powell, Joanne S. ^{[2
]}

Brown, Christine M. ^{[2
]}

Murphy, Terry ^{[2
]}

Brand, Robert ^{[3
]}

Pretorius, Seef ^{[4
]}

Stevenson, Dennis ^{[3
]}

Thompson, Donald ^{[2
]}

Singh, Sheo B. ^{[1
]}

机构：

[1] Merck Res Labs, Rahway, NJ 07065 USA

[2] Merck & Co Inc, Branchburg Farm, Somerville, NJ 08876 USA

[3] New York Bot Garden, Bronx, NY 10458 USA

[4] Univ Orange Free State, Dept Soil Crop & Climate Sci, ZA-9300 Bloemfontein, South Africa

来源：

PHYTOCHEMISTRY | 2008年 / 69卷 / 02期

关键词：

flavones; Struthiola argentea; anthelmintics; Haemonchus contortus; Heligmosomoides polygyrus; Thymelaeaceae;

D O I：

10.1016/j.phytochem.2007.08.003

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：

Parasitic diseases caused by helminthes lead to significant health hazards to animals resulting in enormous economic impact. While a number of anthelmintics are currently available, all are encountering resistance and ones with a mode of action are needed. We report herein bioassay-guided isolation of three anthelmintic flavones 1-3, including the flavone, 5,6,2',5',6'-pentamethoxy-3',4'-methylenedioxyflavone (3) from the methanol extract of Struthiola argentea (Thymelaeaceae). The structure of 3 was elucidated by analysis of its ID and 2D NMR and MS data. The two major flavones produced by this plant were also isolated and identified as yuankanin (4) and amentoflavone (5). A number of flavones related to the compounds isolated from S. argentea were acquired and tested to ascertain structure activity relationships. The isolation, structure, anthelmintic activity and structure activity relationships of the flavones are described. Compound 3 exhibited the most potent in vitro activity with 90% inhibition of larval motility at 3.1 mu g/mL and compound 15 showed modest in vivo activity. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：541 / 545

页数：5

共 10 条

[1] Lipophilic flavones of Primula veris L. from field cultivation and in vitro cultures [J].