Compounds from Polyphaga plancyi and their inhibitory activities against JAK3 and DDR1 kinases

Fitoterapia. 2016 Oct:114:163-167. doi: 10.1016/j.fitote.2016.09.005. Epub 2016 Sep 15.

Abstract

Plancyamides A (1) and B (3), plancypyrazine A (2), and plancyols A (4) and B (5), five new compounds (1-5), and three known ones (6-8), were isolated from the whole bodies of Polyphaga plancyi Bolivar. Their structures were elucidated by a combination of spectroscopic analyses including 1D and 2D NMR, and HRESIMS. Among them, compound 3 is racemic, chiral HPLC separation afforded its respective enantiomers. The absolute configuration of 1 was assigned by computational methods. Biological evaluation of all the compounds with exception of 7 and 8 discloses that compounds 2 and 4 could inhibit JAK3 kinase with IC50 values of 12.6 and 5.0μM, respectively. In addition, compound 4 exhibit inhibitory activity towards DDR1 kinase with IC50 value of 4.87μM.

Keywords: Computational methods; DDR1; Insect; JAK3; Polyphaga plancyi Bolivar.

MeSH terms

  • Animals
  • Biological Products / chemistry*
  • Biological Products / isolation & purification
  • Coleoptera / chemistry*
  • Discoidin Domain Receptor 1 / antagonists & inhibitors*
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / isolation & purification
  • Janus Kinase 3 / antagonists & inhibitors*
  • Molecular Structure
  • Stereoisomerism

Substances

  • Biological Products
  • Enzyme Inhibitors
  • Discoidin Domain Receptor 1
  • Janus Kinase 3