Antiangiogenic activity of 2-formyl-8-hydroxy-quinolinium chloride

Biomed Pharmacother. 2016 May:80:145-150. doi: 10.1016/j.biopha.2016.03.014. Epub 2016 Mar 26.

Abstract

Tumour growth is closely related to the development of new blood vessels to supply oxygen and nutrients to cancer cells. Without the neovascular formation, tumour volumes cannot increase and undergo metastasis. Antiangiogenesis is one of the most promising approaches for antitumour therapy. The exploration of new antiangiogenic agents would be helpful in antitumour therapy. Quinoline is an aromatic nitrogen compound characterized by a double-ring structure which exhibits a benzene ring fused to pyridine at two adjacent carbon atoms. The high stability of quinoline makes it preferable in a variety of therapeutic and pharmaceutical applications, including antitumour treatment. This work is to examine the potential antiangiogenic activity of the synthetic compound 2-Formyl-8-hydroxy-quinolinium chloride. We found that 2-Formyl-8-hydroxy-quinolinium chloride could inhibit the growth of human umbilical vein endothelial cells in vitro. Using the diethylnitrosamine-induced hepatocarcinogenesis model, 2-Formyl-8-hydroxy-quinolinium chloride showed strong antiangiogenic activity. Furthermore, 2-Formyl-8-hydroxy-quinolinium chloride could inhibit the growth of large Hep3B xenografted tumour from the nude mice. We assume that 2-Formyl-8-hydroxy-quinolinium chloride could be a potential antiangiogenic and antitumour agent and it is worthwhile to further study its underlying working mechanism.

Keywords: 2-Formyl-8-hydroxy-quinolinium chloride; Antiangiogenesis; Antitumour; Diethylnitrosamine-induced hepatocarcinogenesis; Hepatoma xenograft.

MeSH terms

  • Angiogenesis Inhibitors / chemistry
  • Angiogenesis Inhibitors / pharmacology*
  • Angiogenesis Inhibitors / therapeutic use
  • Animals
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Carcinogenesis / pathology
  • Carcinoma, Hepatocellular / blood supply
  • Carcinoma, Hepatocellular / drug therapy
  • Carcinoma, Hepatocellular / pathology
  • Cell Death / drug effects
  • Cell Proliferation / drug effects
  • Diethylnitrosamine
  • Human Umbilical Vein Endothelial Cells / drug effects
  • Humans
  • Hydroxyquinolines / chemistry
  • Hydroxyquinolines / pharmacology*
  • Hydroxyquinolines / therapeutic use
  • Liver Neoplasms / blood supply
  • Liver Neoplasms / drug therapy
  • Liver Neoplasms / pathology
  • Mice, Inbred C57BL
  • Mice, Nude
  • Quinolinium Compounds / chemistry
  • Quinolinium Compounds / pharmacology*
  • Quinolinium Compounds / therapeutic use
  • Tumor Burden / drug effects
  • Xenograft Model Antitumor Assays

Substances

  • 2-formyl-8-hydroxyquinolinium
  • Angiogenesis Inhibitors
  • Antineoplastic Agents
  • Hydroxyquinolines
  • Quinolinium Compounds
  • Diethylnitrosamine