title: New diterpenoids with estrogen sulfotransferase inhibitory activity from Leonurus sibiricus L.
abstract: 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).
authors.affiliation: Faculty of Pharmacy, Keio University, 1-5-30 Shibakoen, Minato-ku, Tokyo, 105-8512, Japan.
authors.forename: Yuji
authors.initials: Y
authors.lastname: Narukawa
authors.forename: Akiko
authors.initials: A
authors.lastname: Niimura
authors.forename: Hitomi
authors.initials: H
authors.lastname: Noguchi
authors.forename: Hiroomi
authors.initials: H
authors.lastname: Tamura
authors.forename: Fumiyuki
authors.initials: F
authors.lastname: Kiuchi
mesh_terms: D000096:Acetone; D000818:Animals; D004224:Diterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004958:Estradiol / Q000378:metabolism; D006801:Humans; D031332:Leonurus / Q000737:chemistry; D008099:Liver / Q000187:drug effects* / Q000201:enzymology; D008469:Meclofenamic Acid / Q000494:pharmacology; D015394:Molecular Structure; D008517:Phytotherapy; D035261:Plant Components, Aerial; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D010946:Plants, Medicinal; D012997:Solvents; D015238:Sulfotransferases / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D004224:Diterpenes; D004791:Enzyme Inhibitors; D010936:Plant Extracts; D012997:Solvents; D000096:Acetone; D008469:Meclofenamic Acid; D004958:Estradiol; D015238:Sulfotransferases; C020122:estrone sulfotransferase