ANTIPROLIFERATIVE ACTIVITY OF NOVEL ACETYLENIC DERIVATIVES OF BETULIN AGAINST G-361 HUMAN MELANOMA CELLS.

Abstract

Acetylenic derivatives of betulin were tested in vitro for their antiproliferative activity against G-361 human melanoma cells. Two types of betulin derivatives were studied: monoesters, obtained by modification of the hydroxyl group at C-28 position, and diesters modified at both C-28 and C-3 positions. To assess cell proliferation, a colorimetric sulforhodamine B based method was used. All the tested monoesters inhibited cellular growth and 28-O-propynoylbetulin showed the strongest cytotoxic effect. Esterification of the C-3 hydroxyl group of the molecule abolished its growth inhibitory activity.

• Authors: Ewa Bębenek, Ewa Chodurek, Arkadiusz Orchel, Zofia Dzierżewicz, Stanisław Boryczka
• Journal: Acta poloniae pharmaceutica (Acta Pol Pharm) 2015 Jul-Aug Vol. 72 Issue 4 Pg. 699-703 ISSN: 0001-6837 [Print] Poland
• PMID: 26647626 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• 28-O-propynoylbetulin
• Antineoplastic Agents
• Triterpenes
• betulin

Topics

• Antineoplastic Agents (pharmacology)
• Cell Proliferation (drug effects)
• Humans
• Melanoma (drug therapy, pathology)
• Structure-Activity Relationship
• Triterpenes (pharmacology)
• Tumor Cells, Cultured