Faculty of Pharmacy, Keio University, 1-5-30 Shibakoen, Minato-ku, Tokyo, 105-8512, Japan.
J Nat Med. 2014 Jan;68(1):125-31. doi: 10.1007/s11418-013-0781-0. Epub 2013 Jun 5.
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 μM, which is comparable to the activity of the positive control, meclofenamic acid (IC50 5.4 μM).
从益母草（Leonurus sibiricus L. 的地上部分）的丙酮提取物中分离得到了四个新的二萜类化合物（1-4）和八个已知的二萜类化合物（5-12）。通过光谱方法确定了化合物的结构。在所分离的化合物中，化合物 2、3、8、9 和 10 对人肝胞质雌激素硫酸转移酶（E-ST）表现出抑制活性，E-ST 在维持细胞内雌激素水平方面起着关键作用。化合物 2 表现出最强的活性，IC50 值为 7.9 μM，与阳性对照药物甲氯芬酸（IC50 5.4 μM）的活性相当。
