Therapeutic effects of JLX-001 on ischemic stroke by inducing autophagy via AMPK-ULK1 signaling pathway in rats

Brain Res Bull. 2019 Nov:153:162-170. doi: 10.1016/j.brainresbull.2019.08.017. Epub 2019 Aug 28.

Abstract

(3β,5α,16α,20S)-4,4,14-trimethyl-3,20-bis(methylamino)-9,19-cyclopregnan-16-ol-dihydrochloride (JLX-001), a structural analogue of cyclovirobuxine D (CVB-D), is a novel compound from synthesis. This study aims to confirm the therapeutic effects of JLX001 on ischemic stroke (IS) and research its induction of autophagy function via 5'-AMP-activated protein kinase (AMPK)-Human Serine/threonine-protein kinase (ULK1) signaling pathway activation. The therapeutic effects of JLX001 were evaluated by infarct sizes, brain edema, neurological scores and proportion of apoptotic neurons in Sprague-Dawley (SD) rats with middle cerebral artery occlusion/reperfusion (MCAO/R). The number of autophagosomes was obtained by transmission electron microscopy. The expression of LC3-II was measured by immunofluorescence. p-AMPK and activated ULK1 were detected by western blots. Results showed that JLX001 treatment markedly alleviated cerebral infarcts, edema, neurological scores and proportion of apoptotic neurons in MCAO/R rats. The number of autophagosomes was increased, accompanying with the increased expressions of LC3-II, p-AMPK and ULK1. In summary, JLX001 attenuates cerebral ischemia injury and the underlying mechanisms may relate to inducing autophagy via AMPK-ULK1 signaling pathway activation.

Keywords: AMPK; Autophagy; Ischemic stroke; JLX-001.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • AMP-Activated Protein Kinases / metabolism
  • Animals
  • Autophagy / drug effects*
  • Autophagy / physiology
  • Autophagy-Related Protein-1 Homolog / metabolism
  • Brain Edema
  • Brain Ischemia / drug therapy*
  • Infarction, Middle Cerebral Artery
  • Male
  • Rats
  • Rats, Sprague-Dawley
  • Signal Transduction / drug effects
  • Stroke / drug therapy
  • TOR Serine-Threonine Kinases / metabolism
  • Triterpenes / pharmacology*
  • Triterpenes / therapeutic use

Substances

  • JLX001
  • Triterpenes
  • Autophagy-Related Protein-1 Homolog
  • TOR Serine-Threonine Kinases
  • ULK1 protein, rat
  • AMP-Activated Protein Kinases