Lung cancer and matrix metalloproteinases inhibitors of polyphenols from Selaginella tamariscina with suppression activity of migration

Bioorg Med Chem Lett. 2018 Aug 1;28(14):2413-2417. doi: 10.1016/j.bmcl.2018.06.024. Epub 2018 Jun 18.


Cancer metastasis has been a major impediment to effective cancer treatment and is the major cause of cancer-related death. Polyphenols compounds have been reported to possess anti-metastasis activity through their inhibitory activity of matrix metalloproteinases (MMPs). In this paper, twelve polyphenols compounds, including three novel phenols, named selaphenins A-C (1-3), two known selaginellin derivatives (4 and 5), together with seven known biflavonoids (6-12) were isolated from the plant of Selaginella tamariscina. Their structures were elucidated by extensive spectroscopic analyses. Notably, polyphenols compound 10 suppressed the migration of A549 cells by primary targeting MMP-9. The antitumor activity of compound 10 was possibly due to the induction of cell apoptosis through intrinsic apoptosis pathways, accompanied by increasing the expression of Bax and caspase-3 in a dose-dependent manner. This study provides evidence that polyphenols analogues from S. tamariscina as inhibitors of MMP-9 exhibited potential migration inhibition activities.

Keywords: Anticancer activity; Matrix metalloproteinases; Migration; Polyphenols; Selaginella tamariscina.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • A549 Cells
  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / isolation & purification
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Cell Line, Tumor
  • Cell Movement / drug effects
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Humans
  • Matrix Metalloproteinase 9 / metabolism*
  • Matrix Metalloproteinase Inhibitors / chemistry
  • Matrix Metalloproteinase Inhibitors / isolation & purification
  • Matrix Metalloproteinase Inhibitors / pharmacology*
  • Molecular Structure
  • Polyphenols / chemistry
  • Polyphenols / isolation & purification
  • Polyphenols / pharmacology*
  • Selaginellaceae / chemistry*
  • Structure-Activity Relationship


  • Antineoplastic Agents, Phytogenic
  • Matrix Metalloproteinase Inhibitors
  • Polyphenols
  • Matrix Metalloproteinase 9