Abstract
BackgroundEpanorin (EP) is a secondary metabolite of the Acarospora lichenic species. EP has been found in lichenic extracts with antimicrobial activity, and UV-absorption properties have been described for closely related molecules; however, its antiproliferative activity in cancer cells has not yet been explored. It has been hypothesized that EP inhibits cancer cell growth. MCF-7 breast cancer cells, normal fibroblasts, and the non-transformed HEK-293 cell line were exposed to increasing concentrations of EP, and proliferation was assessed by the sulforhodamine-B assay.ResultsMCF-7 cells exposed to EP were examined for cell cycle progression using flow cytometry, and DNA fragmentation was examined using the TUNEL assay. In addition, EP’s mutagenic activity was assessed using the Salmonella typhimurium reverse mutation assay. The data showed that EP inhibits proliferation of MCF-7 cells, and it induces cell cycle arrest in G0/G1 through a DNA fragmentation-independent mechanism. Furthermore, EP’s lack of overt cytotoxicity in the normal cell line HEK-293 and human fibroblasts in cell culture is supported by the absence of mutagenic activity of EP.ConclusionEP emerges as a suitable molecule for further studies as a potential antineoplastic agent.
Highlights
Epanorin (EP) is a secondary metabolite of the Acarospora lichenic species
Evidence is provided for the first time for EP inhibition of proliferation of cancer cells with special efficacy on the MCF-7 cancer cells, decreasing its viability by a DNA fragmentation-independent mechanism suggesting that EP does not induce apoptosis
reactive oxygen species (ROS) were not detected in EP treated MCF-7 cells, consistent with reports that showed that apoptosis is accompanied with oxidative stress [35]
Summary
Epanorin (EP) is a secondary metabolite of the Acarospora lichenic species. EP has been found in lichenic extracts with antimicrobial activity, and UV-absorption properties have been described for closely related molecules; its antiproliferative activity in cancer cells has not yet been explored. The contribution of natural origin products as anticancer and chemopreventive agents is widely recognized, as Lichens are symbiotic organisms consisting of a fungus and a photosynthetic partner. Their capacity to produce and accumulate secondary metabolites gives rise to their wide chemical diversity which includes over 1000 compounds. Palacios‐Moreno et al Biol Res (2019) 52:55 or UV radiation Some of these metabolites exhibit in vitro biological activities on prokaryotic and eukaryotic cell models, including antimicrobial, antioxidant and antiproliferative properties [5, 17, 24] which make them potential candidates as human therapeutic agents
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