New diterpenoids with estrogen sulfotransferase inhibitory activity from Leonurus sibiricus L

Yuuji Narukawa, Akiko Niimura, Hitomi Noguchi, Hiroomi Tamura, Fumiyuki Kiuchi

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18 Citations (Scopus)


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 IC 50 value of 7.9 μM, which is comparable to the activity of the positive control, meclofenamic acid (IC50 5.4 μM).

Original languageEnglish
Pages (from-to)125-131
Number of pages7
JournalJournal of Natural Medicines
Issue number1
Publication statusPublished - 2014 Jan



  • Estrogen sulfotransferase
  • Inhibitor
  • Labdane type diterpenoids
  • Leonurus sibiricus

ASJC Scopus subject areas

  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science
  • Complementary and alternative medicine
  • Medicine(all)

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