Anticancer activity studies of cubebin isolated from Piper cubeba and its synthetic derivatives

Bioorg Med Chem Lett. 2016 Apr 1;26(7):1767-71. doi: 10.1016/j.bmcl.2016.02.041. Epub 2016 Feb 16.

Abstract

(-)-Cubebin, isolated from the seeds of Piper cubeba, and its five different types of derivatives (a total of 17), with varying functionalities, were tested for their in vitro anticancer activity against six human cancer cell lines (A549, K562, SiHa, KB, HCT116 and HT29) using MTT assay. Cubebin as well as its derivatives containing lactone and amide groups showed significant anticancer activity. In some of the tested cell lines, the amide derivatives showed higher activity. Morphological analysis indicated that these compounds act through apoptosis mediated pathway of cell death and we expect that these results will pave new paths in the development of novel anticancer agents by the derivatization of (-)-cubebin.

Keywords: Amide derivatives; Anticancer activity; Apoptosis; Cubebin; Hinokinin; Morphological analysis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents, Phytogenic / chemistry*
  • Antineoplastic Agents, Phytogenic / isolation & purification
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Apoptosis / drug effects*
  • Cell Line, Tumor
  • Humans
  • Lignans / chemistry*
  • Lignans / isolation & purification
  • Lignans / pharmacology*
  • Models, Molecular
  • Neoplasms / drug therapy
  • Neoplasms / pathology
  • Piper / chemistry*
  • Seeds / chemistry

Substances

  • Antineoplastic Agents, Phytogenic
  • Lignans
  • cubebin