Screening of plant extracts in search of new agents to treat cancer resulted in the discovery of Englerin A. A natural product, isolated from Phyllanthus engleri, shows potent selective cytotoxicity against renal cancer cells. But very little was known about its mechanism of action.
Recently it was recovered that sesquiterpene (-)-englerin A was selectively killing renal cancer cells through activation of calcium-permeable nonselective transient receptor potential canonical (TRPC) calcium channels. TRPC4/5 activation raises the calcium concentration in the renal cancer cells which leads to cell death.
Again a natural compound is showing novel opportunities for drug discovery. Please check out our website. Cfm Oskar Tropitzsch GmbH offers a broad range of phytochemicals for your research projects.
- (-)-Englerin A is a potent and selective activator of TRPC4 and TRPC5 calcium channels. Akbulut Y, Gaunt HJ, Muraki K, Ludlow MJ, Amer MS, Bruns A, Vasudev NS, Radtke L, Willot M, Hahn S, Seitz T, Ziegler S, Christmann M, Beech DJ, Waldmann H. Angew Chem Int Ed Engl. 2015 Mar 16;54(12):3787-91. doi: 10.1002/anie.201411511. Epub 2015 Feb 23.
- Renal cancer-selective Englerin A induces multiple mechanisms of cell death and autophagy. Williams RT, Yu AL, Diccianni MB, Theodorakis EA, Batova A. J Exp Clin Cancer Res. 2013 Aug 20;32:57. doi: 10.1186/1756-9966-32-57.