Enmein-type diterpenoid analogs from natural kaurene-type oridonin: Synthesis and their antitumor biological evaluation

Dahong Li, Shengtao Xu, Hao Cai, Lingling Pei, Hengyuan Zhang, Lei Wang, Hequan Yao, Xiaoming Wu, Jieyun Jiang, Yijun Sun, Jinyi Xu

Research output: Contribution to journalArticlepeer-review

34 Scopus citations

Abstract

A series of enmein-type diterpenoid analogs (11-20) derived from natural kaurene-type diterpenoid oridonin were synthesized and biologically evaluated. All target compounds showed improved anti-proliferative activities against four human cancer cell lines compared with natural oridonin and parent compound 10. Some compounds were more potent than positive control Taxol. Furthermore, mechanistic investigation showed that the representative compound 17 affected cell cycle and induced apoptosis at low micro-molar level in human hepatoma Bel-7402 cells, via an oxidative stress triggered mitochondria-related caspase-dependent pathway.

Original languageEnglish
Pages (from-to)215-221
Number of pages7
JournalEuropean Journal of Medicinal Chemistry
Volume64
DOIs
StatePublished - 2013

Bibliographical note

Funding Information:
This study was supported by a grant from the National Natural Science Foundation (No. 30973610 ), Specialized Research Fund for the Doctoral Program of Higher Education (No. 20100096110001 ), Project for Research and Innovation of Graduates in Universities of Jiangsu Province ( CXZZ11-0800 ), the Fundamental Research Funds for the Central Universities ( JKY2011030 ) and Key Fund of Ministry of Education of China (No. 108069 ) for financial assistance.

Keywords

  • Anti-proliferative activity
  • Apoptosis
  • Cell cycle analysis
  • Enmein-type diterpenoid
  • Oridonin

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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