Nitric oxide-donating derivatives of hederacolchiside A1: Synthesis and biological evaluation in vitro and in vivo as potential anticancer agents

Bioorg Med Chem Lett. 2017 Jan 1;27(1):98-101. doi: 10.1016/j.bmcl.2016.11.021. Epub 2016 Nov 10.

Abstract

A series of nitric oxide (NO) donating derivatives of hederacolchiside A1 bearing triterpenoid saponin motif were designed, synthesized and evaluated for their anticancer activity. All of the tested furoxan-based NO releasing compounds showed significant proliferation inhibitory activities. Especially compound 6a exhibited strong cytotoxicity (IC50=1.6-6.5μM) against four human tumor cell lines (SMMC-7721, NCI-H460, U251, HCT-116) in vitro and the highest level of NO releasing. Furthermore, compound 6a was revealed low acute toxicity to mice and weak haemolytic activity with potent tumor growth inhibition against mice H22 hepatocellular cells in vivo (51.5%).

Keywords: Anticancer activity; Furoxan; Hederacolchiside A(1); Nitric oxide; Triterpenoid saponin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Humans
  • Mice
  • Molecular Structure
  • Neoplasms, Experimental / drug therapy
  • Neoplasms, Experimental / pathology
  • Nitric Oxide / chemistry
  • Nitric Oxide / pharmacology*
  • Saponins / chemical synthesis
  • Saponins / chemistry
  • Saponins / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Saponins
  • hederacolchisid A1
  • Nitric Oxide