Potential antimalarial lead structures from fungi of marine origin.
Antiplasmodial and cytotoxicity testing of five highly oxygenated natural products (6R,12R,14R-colletoketol, 6R,11R,12R,14R-colletoketodiol, dihydrobotrydial, pycnidione, and 3R,4S-hydroxymellein), all derived from fungi of marine origin, showed one of them, pycnidione, to have activities against three different strains of Plasmodium falciparum in the sub-micromolar (microM) range. Although the mean selectivity index of 1 for the observed antiplasmodial activity of 4 is low, pycnidione's usefulness as a potential lead structure should not be ignored.
Wright
Anthony D
AD
Australian Institute of Marine Science, Townsville MC, Queensland 4810, Australia. a.wright@aims.gov.au
Lang-Unnasch
Naomi
N
D000818:Animals; D000962:Antimalarials / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D005658:Fungi; D006576:Heterocyclic Compounds, 4 or More Rings / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D007624:KB Cells / Q000187:drug effects; D016778:Malaria, Falciparum / Q000188:drug therapy; D021261:Parasitic Sensitivity Tests; D008517:Phytotherapy; D010963:Plasmodium falciparum / Q000187:drug effects*; D012623:Seawater; D013329:Structure-Activity Relationship; D014334:Tropolone / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use
D000962:Antimalarials; D000972:Antineoplastic Agents, Phytogenic; D006576:Heterocyclic Compounds, 4 or More Rings; C572726:pycnidione; D014334:Tropolone