The metabolite 5-methyl-1,3-benzenediol and its derivative methyl-2,4-dihydroxy-6-methylbenzoate from the lichen Parmotrema tinctorum with potent apoptotic and anti-angiogenesis effects.

Nature has been a rich resource of novel anticancer agents, one such source being lichens, which represent the symbiosis between algae and fungi with diverse range of secondary metabolites having therapeutic significance. With respect to this, the present study evaluates the in vitro apoptogenic profile of secondary metabolites from the lichen Parmotrema tinctorum towards cancer cell lines. Treatment with TLC-purified fraction 1 from P. tinctorum resulted in significant reduction in the cell viabilities of cancer cells with IC50 values ranging between 1.2 and 12.8 μg/ml. The potential anticancer effect of the bioactive fraction was further supported by Trypan blue cell viability, LDH and DNA fragmentation assays. At the cellular level, induction of apoptosis was confirmed through the activation of the caspase cascade and apoptotic cells accumulating in the Sub-G1 phase of cell cycle. Angiogenesis being one of the major characteristics needed for cancer growth, the ability of the lichen fraction to inhibit angiogenesis was checked through in ovo Yolk Sac Membrane (YSM) assay and was found to be significant. The study also verified the non-toxic nature of the bioactive fraction towards normal human peripheral lymphocytes. HPLC analysis and GC-MS characterisation of the bioactive fraction indicated the presence of 5-methyl-1,3-benzenediol and its derivative methyl-2,4-dihydroxy-6-methylbenzoate. © King Abdulaziz City for Science and Technology 2021.