New diterpenoids with estrogen sulfotransferase inhibitory activity from Leonurus sibiricus L.

被引：31
|
作者：
Narukawa, Yuji [1 ]
Niimura, Akiko [1 ]
Noguchi, Hitomi [1 ]
Tamura, Hiroomi [1 ]
Kiuchi, Fumiyuki [1 ]
机构：
[1] Keio Univ, Fac Pharm, Minato Ku, Tokyo 1058512, Japan
来源：
JOURNAL OF NATURAL MEDICINES | 2014年 / 68卷 / 01期
关键词：
Leonurus sibiricus; Labdane type diterpenoids; Estrogen sulfotransferase; Inhibitor; LABDANE DITERPENES; BALLOTA-AUCHERI; HETEROPHYLLUS; LEOHETERIN;
D O I：
10.1007/s11418-013-0781-0
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Four new diterpenoids (1-4), along with eight known diterpenoids (5-12) were isolated from the acetone extract of Leonurus herb (aerial parts of Leonurus sibiricus L.). The structures of the compounds were determined by spectroscopic methods. Among the isolated compounds, compounds 2, 3, 8, 9 and 10 showed inhibitory activity against human liver cytosol estrogen sulfotransferase (E-ST), which plays a key role in the maintenance of cellular estrogen levels. Compound 2 showed the strongest activity with an IC50 value of 7.9 mu M, which is comparable to the activity of the positive control, meclofenamic acid (IC50 5.4 mu M).
引用
收藏
页码：125 / 131
页数：7
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