Two new diterpenoids from the stems of Rhododendron dauricum as GABAA receptor agonists

Guo-Sheng Liu; Zhao-Xin Zhang; Guo-Zhu Su; Shang-Yi Wang; Cheng-Shuo Yang; Hai-Bo Yu; Ya-Nan Wang; Yong Li

doi:10.1080/10286020.2021.2007089

Two new diterpenoids from the stems of Rhododendron dauricum as GABA_A receptor agonists

J Asian Nat Prod Res. 2022 Jun;24(6):542-549. doi: 10.1080/10286020.2021.2007089. Epub 2021 Dec 2.

Authors

Guo-Sheng Liu¹, Zhao-Xin Zhang¹, Guo-Zhu Su¹, Shang-Yi Wang¹, Cheng-Shuo Yang¹, Hai-Bo Yu¹, Ya-Nan Wang¹, Yong Li¹

Affiliation

¹ State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.

PMID: 34854776
DOI: 10.1080/10286020.2021.2007089

Abstract

Two new diterpenoids, dauricumins A (1) and B (2), together with two known aromatic meroterpenoids (3 and 4), were isolated from the petroleum ether soluble fraction of the stems from Rhododendron dauricum through an HPLC-MS-SPE-NMR combination strategy. The absolute configurations of 1 and 2 were elucidated by ECD calculations and [Rh₂ (OCOCF₃)₄]-induced CD spectrum analysis. In a membrane potential FLIPR assay, confluentin (4) showed an agonistic effect on GABA_A receptor (EC₅₀ = 20 µM).

Keywords: Ericaceae; HPLC-MS-SPE-NMR; Rhododendron dauricum; agonist of GABAA receptors; diterpenoids.

MeSH terms

Diterpenes* / chemistry
Diterpenes* / pharmacology
GABA-A Receptor Agonists
Molecular Structure
Receptors, GABA-A
Rhododendron* / chemistry

Substances

Diterpenes
GABA-A Receptor Agonists
Receptors, GABA-A