Discovery of mitochondria-targeting berberine derivatives as the inhibitors of proliferation, invasion and migration against rat C6 and human U87 glioma cells

Shengnan Fu, Yanqi Xie, Jue Tuo, Yalong Wang, Wenbo Zhu, Sihan Wu, Guangmei Yan, Haiyan Hu

Research output: Contribution to journalArticlepeer-review

19 Scopus citations

Abstract

This research aims to synthesize lipophilic berberine derivatives and evaluate their antiglioma effects on C6 and U87 cells. The introduction of substituents with various carbon chain lengths on C-13- or C-9-O-position of the berberine scaffold led to the discovery of several potent inhibitors against glioblastoma cells. Derivatives substituted with the carbon chains of moderate length (twelve carbons) displayed improved lipophilicity and the strongest inhibitory effects. Several compounds presented dose-dependent repression against proliferation (IC50, 1.12-6.12 μM) and blocked migration and invasion by over 60% at lower dose levels. Furthermore, preliminary research about the underlying mechanism for the enhanced antiglioma ability indicated that these analogues preferentially localized into mitochondria, inducing the up-regulation of ROS production. Overall, these compounds represent promising candidates to combat glioblastoma and highlight new insight into the antiglioma therapy through interaction with mitochondria. This journal is

Original languageEnglish (US)
Pages (from-to)164-173
Number of pages10
JournalMedChemComm
Volume6
Issue number1
DOIs
StatePublished - Jan 1 2015
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

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