7-substituted coumarins inhibit proliferation and migration of laryngeal cancer cells in vitro.

Abstract

BACKGROUND:

Coumarins are a large group of naturally-occurring compounds with a wide range of biological properties, including anticancer activity. 7-Substituted coumarins (umbelliferone, scoparone, and herniarin) were analyzed for their potential anticancer activity against laryngeal cancer cells (LCC).

MATERIALS AND METHODS:

High-performance counter-current chromatography was applied for successful separation of umbelliferone from fruits of Heracleum leskowii. A two-phase solvent system composed of n-heptane-methanol-ethyl acetate-water (1:2:1:2, v/v/v) was successfully used. Cell proliferation was assessed after 48-72 h by means of MTT test, and tumor cell motility by a wound assay model. Measurement of cell death was estimated using enzyme-linked immunosorbent assay (ELISA), and cell-cycle analysis was performed by flow cytometry. Extracellular signal-regulated kinases-1/2 (ERK1/2) and AKT kinase activation status were analyzed by western blotting.

RESULTS:

Umbelliferone, scoparone, and, to a lesser extent, herniarin reduced viability and migration of RK33 LCC in a dose-dependent manner. Scoparone and herniarin were found to induce apoptosis of LCC. None of the tested compounds influenced the ERK1/2 and AKT kinase activity, nor significantly affected cell-cycle progression in the LCC line studied.

CONCLUSION:

Our findings suggest the therapeutic potential of 7-substituted coumarins in the treatment of laryngeal cancer.

• Authors: Michal Kielbus, Krystyna Skalicka-Wozniak, Aneta Grabarska, Witold Jeleniewicz, Magdalena Dmoszynska-Graniczka, Andrew Marston, Krzysztof Polberg, Piotr Gawda, Janusz Klatka, Andrzej Stepulak
• Journal: Anticancer research (Anticancer Res) Vol. 33 Issue 10 Pg. 4347-56 (Oct 2013) ISSN: 1791-7530 [Electronic] Greece
• PMID: 24123002 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Acetates
• Antineoplastic Agents, Phytogenic
• Coumarins
• Heptanes
• Plant Extracts
• Solvents
• Umbelliferones
• Water
• n-heptane
• herniarin
• 7-hydroxycoumarin
• ethyl acetate
• scoparone
• Methanol

Topics

• Acetates (chemistry)
• Antineoplastic Agents, Phytogenic (isolation & purification, pharmacology)
• Cell Cycle (drug effects)
• Cell Line, Tumor
• Cell Movement (drug effects)
• Cell Proliferation (drug effects)
• Chromatography, High Pressure Liquid
• Coumarins (isolation & purification, pharmacology)
• Fruit (chemistry)
• Heptanes (chemistry)
• Heracleum (chemistry)
• Humans
• Laryngeal Neoplasms
• Methanol (chemistry)
• Plant Extracts (isolation & purification, pharmacology)
• Solvents (chemistry)
• Umbelliferones (isolation & purification, pharmacology)
• Water (chemistry)