Synthesis and synergetic anti-tumor activity evaluation of dihydroartemisinin-organogermanium(IV) compound

Bioorg Med Chem Lett. 2014 Nov 15;24(22):5294-7. doi: 10.1016/j.bmcl.2014.09.048. Epub 2014 Sep 28.

Abstract

Dihydroartemisinin (DHA), a semi-synthetic derivative of the herb artemisinin, has shown commendable bioactivity. In this paper, a novel dihydroartemisinin-organogermanium (DHA-Ge) compound was synthesized, characterized and its potential anti-tumor activity was evaluated by various methods. MTT results demonstrated that DHA-Ge could effectively inhibit the proliferation of HepG2 cells and showed their dose-dependent properties. The IC50 value of inhibition effect on HepG2 cells of DHA-Ge was 10.23 μg/ml which was lower than 39.44 μg/ml of DHA. Flow cytometric results suggested that DHA-Ge could induce apoptosis of HepG2 cells and the apoptosis rate was 20.26% after 24h treatment with 56.8 μg/ml DHA-Ge concentration. Atomic force microscopy images showed that HepG2 cells were collapsed and the cell nucleus were fragmented after 24h treatment. All these results together showed that the DHA-Ge possessed desirable synergetic enhanced anti-tumor effects and could be developed as a suitable tumor therapeutic agent.

Keywords: Dihydroartemisinin; Ge-132; Organogermanium; Synergetic anti-tumor activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Apoptosis / drug effects
  • Artemisinins / chemistry*
  • DNA Fragmentation / drug effects
  • Germanium / chemistry
  • Hep G2 Cells
  • Humans
  • Microscopy, Atomic Force
  • Organometallic Compounds / chemistry*

Substances

  • Antineoplastic Agents
  • Artemisinins
  • Organometallic Compounds
  • Germanium
  • artenimol