Abstract
BackgroundLichens produce a huge diversity of bioactive compounds with several biological effects. Gyrophoric acid (GA) is found in high concentrations in the common lichen Umbilicaria hirsuta, however evidence for biological activity was limited to anti-proliferative activity described on several cancer cell lines.MethodsWe developed and validated a new protocol for GA isolation, resulting in a high yield of highly pure GA (validated by HPLC and NMR) in an easy and time saving manner. Anti-proliferative and pro-apoptotic activity, oxygen radicals formation and stress/survival proteins activity changes was study by flow cytometry.ResultsThe highly purified GA showed anti-proliferative activity against HeLa (human cervix carcinoma) and other tumor cells. Moreover, GA threated cells showed a significant increase in caspase-3 activation followed by PARP cleavage, PS externalization and cell cycle changes mediated by oxidative stress. Production of oxygen radicals led to DNA damage and changes in stress/survival pathways activation.ConclusionsGA treatment on HeLa cells clearly indicates ROS production and apoptosis as form of occurred cell death. Moreover, DNA damage and changing activity of stress/survival proteins as p38MAPK, Erk1/2 and Akt mediated by GA treatment confirm pro-apoptotic potential. The pharmacological potential of U. hirsuta derived GA is discussed.
Highlights
Lichens produce a huge diversity of bioactive compounds with several biological effects
In our experiments we focused on influence of Gyrophoric acid (GA) treatment on modulation stress/survival pathways p38 MAPK, Erk1/2, Akt and possible pro-oxidant and genotoxic activity
Identification of lichen secondary metabolites by High-performance liquid chromatography (HPLC) and Nuclear magnetic resonance (NMR) The HPLC chromatogram of the acetone extract of U. hirsuta is shown in Additional file 1 (A, B)
Summary
Lichens produce a huge diversity of bioactive compounds with several biological effects. Gyrophoric acid (GA) is found in high concentrations in the common lichen Umbilicaria hirsuta, evidence for biological activity was limited to anti-proliferative activity described on several cancer cell lines. Lichens represent chemically important symbiotic organisms of fungi (mycobiont) and algae/ cyanobacteria (photobiont) which produce a various secondary metabolites. A wide spectrum of biological activity of secondary metabolites is known so far. One of the most studied lichen polyphenolic compounds with high biological activity, including antiproliferative effect, are depsides and depsidones [7,8,9]. Bačkorová et al [4] showed antiproliferative activity and induction of apoptosis mediated by well-known depside atranorin in wide spectrum of cancer cell lines. Promising results showed treatments with another depside as lobaric acid
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