Isolation, Chemical Modification, and Anticancer Activity of Major Metabolites of the Lichen Parmotrema mesotropum

摘要

Extensive chromatographic purification of the chloroform-methanol (1:1) extract of the lichen Parmotrema mesotropum led to the isolation of methyl hematommate (1), methyl-2,4-dihydroxy-3,6-dimethylbenzoate (2), orcinol (3), and atranorin (4). The two major metabolites (1 and 2) were subjected to chemical modification and a total of 15 analogues were synthesized. The synthesized analogues and their parent compounds were evaluated for their anticancer potential against a panel of five human cancer cell lines. Among the tested samples, compound 1g showed potent activity against three cancer cell lines, namely DU145 (IC50 20.07 mu M), MCF-7 (IC50 20.94 mu M), and U87MG (IC50 25.32 mu M). This compound can be considered as lead a molecule for further development.