title: Potential antimalarial derivatives from astraodorol.
abstract: Astraodorol, a major lanostane-type triterpene isolated from the edible mushroom Astraeus odoratus, was subjected to chemical modifications. Ten derivatives have been synthesized and their biological activities were evaluated. Compounds 5, 6, 7a, 7c, 7e, 7f, and 7 g exhibited strong antimalarial activity with IC50 values of 4.85, 4.48, 4.16, 4.46, 3.45, 3.23, and 3.41 µg/mL, respectively. Compounds 7a, 7c, and 7e showed moderate cytotoxicity against NCI-H187 with IC50 values of 23.36, 34.28, and 9.84 µg/mL. Compound 7e demonstrated moderate cytotoxicity against KB, MCF-7, and Vero cell lines with IC50 values of 16.94, 49.60, and 26.48 µg/mL, respectively.
authors.affiliation: Natural Products Research Unit, Centre of Excellence for Innovation in Chemistry, Department of Chemistry, Faculty of Science, Khon Kaen University, Khon Kaen, 40002, Thailand, nphita@kku.ac.th.
authors.forename: Pitak
authors.initials: P
authors.lastname: Nasomjai
authors.forename: Kittibhorn
authors.initials: K
authors.lastname: Arpha
authors.forename: Sirirath
authors.initials: S
authors.lastname: Sodngam
authors.forename: Simon D
authors.initials: SD
authors.lastname: Brandt
mesh_terms: D000363:Agaricales / Q000737:chemistry*; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D006801:Humans; D020128:Inhibitory Concentration 50; D007624:KB Cells; D061986:MCF-7 Cells; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D014709:Vero Cells
chemical_list: D000962:Antimalarials; D000970:Antineoplastic Agents; D014315:Triterpenes