(±)-Ganoapplanin, a Pair of Polycyclic Meroterpenoid Enantiomers from Ganoderma applanatum

Org Lett. 2016 Dec 2;18(23):6078-6081. doi: 10.1021/acs.orglett.6b03064. Epub 2016 Nov 18.

Abstract

(±)-Ganoapplanin (1), a pair of novel meroterpenoid enantiomers featuring an unprecedented dioxaspirocyclic skeleton constructed from a 6/6/6/6 tetracyclic system and an unusual tricyclo[4.3.3.03',7']dodecane motif, were isolated from Ganoderma applanatum. Its structure and absolute configurations were determined by spectroscopic analyses, X-ray crystallography, and ECD (electronic circular dichroism calculations). A plausible biogenetic pathway, involving a key Gomberg-Bachmann reaction, was also proposed for (±)-1. Biological studies showed that (±)-1 and its enantiomers exhibited different inhibitory activities on T-type voltage-gated calcium channels.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Calcium Channel Blockers / chemistry
  • Calcium Channel Blockers / isolation & purification
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels, T-Type / metabolism*
  • Crystallography, X-Ray
  • Ganoderma / chemistry*
  • HEK293 Cells
  • Humans
  • Models, Molecular
  • Molecular Structure
  • Stereoisomerism
  • Terpenes / chemistry
  • Terpenes / isolation & purification
  • Terpenes / pharmacokinetics*

Substances

  • Calcium Channel Blockers
  • Calcium Channels, T-Type
  • Terpenes
  • ganoapplanin