Jatrophane diterpenes from Euphorbia guyoniana are new potent inhibitors of atrial GIRK channels

Norbert Kúsz, Péter Orvos, Attila Csorba, László Tálosi, Mohammad Chaieb, Judit Hohmann, Dóra Rédei

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

Two new jatrophane diterpenes, guyonianin G (1) and H (2), were isolated from the methanol extract of Euphorbia guyoniana Boiss. & Reut. The structures were established by means of a combined spectroscopic data analysis, including HRESIMS, and 1D- and 2D-NMR techniques. The isolated compounds were not identical with the previously reported compounds of E. guyoniana, indicating the high chemical diversity of this species. Electrophysiological effects of guyonianin G (1) and H (2), together with four jatrophane diterpenes previously isolated from Euphorbia mongolica, Euphorbia serrulata and Euphorbia salicifolia were investigated on stable transfected HEK–GIRK1/4 (Kir3.4) cell lines using automated patch clamp equipment. Significant blocking activity on GIRK channel was exerted by diterpenes 1–5, but no blocking activity of 6 was detected. The common jatropha-6(17),11E-diene, guyonianin G (1) with three large ester groups (one benzoyl and two isobutanoyl groups) was the most active (70% at 10 μM) GIRK channel inhibitory compound.

Original languageEnglish
Pages (from-to)5724-5728
Number of pages5
JournalTetrahedron
Volume72
Issue number37
DOIs
Publication statusPublished - Jan 1 2016

Keywords

  • Euphorbia guyoniana
  • GIRK channel inhibitory activity
  • Guyonianin G and H
  • Jatrophane diterpenes

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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