title: Marchantin A, a macrocyclic bisbibenzyl ether, isolated from the liverwort Marchantia polymorpha, inhibits protozoal growth in vitro.
abstract: In vitro anti-plasmodial activity-guided fractionation of a diethyl ether extract of the liverwort species Marchantia polymorpha, collected in Iceland, led to isolation of the bisbibenzyl ether, marchantin A. The structure of marchantin A (1) was confirmed by NMR and HREIMS. Marchantin A inhibited proliferation of the Plasmodium falciparum strains, NF54 (IC(50)=3.41μM) and K1 (IC(50)=2.02μM) and showed activity against other protozoan species Trypanosoma brucei rhodesiense, T. cruzi and Leishmania donovani with IC(50) values 2.09, 14.90 and 1.59μM, respectively. Marchantin A was tested against three recombinant enzymes (PfFabI, PfFabG and PfFabZ) of the PfFAS-II pathway of P. falciparum for malaria prophylactic potential and showed moderate inhibitory activity against PfFabZ (IC(50)=18.18μM). In addition the cytotoxic effect of marchantin A was evaluated. This is the first report describing the inhibitory effects of the liverwort metabolite marchantin A against these parasites in vitro.
authors.affiliation: School of Health Sciences, University of Iceland, Reykjavik, Iceland.
authors.forename: Sophie
authors.initials: S
authors.lastname: Jensen
authors.forename: Sesselja
authors.initials: S
authors.lastname: Omarsdottir
authors.forename: Angela Gono
authors.initials: AG
authors.lastname: Bwalya
authors.forename: Morten Agertoug
authors.initials: MA
authors.lastname: Nielsen
authors.forename: Deniz
authors.initials: D
authors.lastname: Tasdemir
authors.forename: Elin Soffia
authors.initials: ES
authors.lastname: Olafsdottir
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000302:isolation & purification*; D001632:Bibenzyls / Q000302:isolation & purification* / Q000494:pharmacology; D002460:Cell Line; D004791:Enzyme Inhibitors / Q000302:isolation & purification*; D004988:Ethers, Cyclic / Q000302:isolation & purification* / Q000494:pharmacology; D047008:Marchantia / Q000737:chemistry*; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000201:enzymology; D051381:Rats; D018675:Toxicity Tests
chemical_list: D000981:Antiprotozoal Agents; D001632:Bibenzyls; D004791:Enzyme Inhibitors; D004988:Ethers, Cyclic; C096123:marchantin A