Englerin A

Last updated on: 18.12.2020

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Definition
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Englerin A is a highly toxic natural product that owes its name to the botanist Heinrich Gustav Adolf Engler ( March 25, 1844 in Sagan, Lower Silesia; † October 10, 1930 in Berlin) .

General information
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Englerin A is a guaiane sesquiterpenoid and is isolated from the bark of Phyllanthus engleri, a plant native to Tanzania and Zimbabwe. Chemically, it is a cinnamate ester (glycolate ester). Englerin A is able to selectively inhibit the growth of renal cell carcinoma cell lines, with the cation channel TRPC4 being the efficacy target for englerin A, which is increasingly expressed by englerin A. Genetic experiments show that TRPC4 expression is a prerequisite for Englerin A-induced tumor cell line growth inhibition. Thus, these experiments confirm that activation of TRPC4/C5 channels inhibits proliferation of tumor cell lines.

However, the toxicity of the compound suggests that englerin A itself is probably unsuitable for further drug development. However, it could be a useful starting point for further research in this area.

Literature
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  1. Carson C et al. (2015) Englerin A Agonizes the TRPC4/C5 Cation Channels to Inhibit Tumor Cell Line Proliferation. PLoS ONE 10(: e0127498.

Last updated on: 18.12.2020