title: Caged xanthones: Potent inhibitors of global predominant MRSA USA300.
abstract: Total of 22 caged xanthones were subjected to susceptibility testing of global epidemic MRSA USA300. Natural morellic acid showed the strongest potency (MIC of 12.5μM). However, its potent toxicity diminishes MRSA therapeutic potential. We synthetically modified natural morellic acid to yield 13 derivatives (3a-3m). Synthetically modified 3b retained strong potency in MRSA growth inhibition, yet the toxicity was 20-fold less than natural morellic acid, permitting the possibility of using caged xanthones for MRSA therapeutic.
authors.affiliation: Department of Chemistry and Center for Innovation in Chemistry (PERCH-CIC), Faculty of Science, Mahidol University, Rama VI Road, Bangkok 10400, Thailand.
authors.forename: Pongkorn
authors.initials: P
authors.lastname: Chaiyakunvat
authors.affiliation: Department of Pharmacognosy and Center for Innovation in Chemistry (PERCH-CIC), Faculty of Pharmacy, Mahidol University, Sri-Ayudhaya Road, Bangkok 10400, Thailand.
authors.forename: Natthinee
authors.initials: N
authors.lastname: Anantachoke
authors.affiliation: Department of Chemistry and Center for Innovation in Chemistry (PERCH-CIC), Faculty of Science, Mahidol University, Rama VI Road, Bangkok 10400, Thailand.
authors.forename: Vichai
authors.initials: V
authors.lastname: Reutrakul
authors.affiliation: Department of Chemistry and Center for Innovation in Chemistry (PERCH-CIC), Faculty of Science, Mahidol University, Rama VI Road, Bangkok 10400, Thailand.
authors.forename: Chutima
authors.initials: C
authors.lastname: Jiarpinitnun
mesh_terms: D000072283:A549 Cells; D000596:Amino Acids / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D000667:Ampicillin / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D001422:Bacterial Adhesion / Q000187:drug effects; D029760:Garcinia; D057809:HEK293 Cells; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000302:isolation & purification / Q000494:pharmacology / Q000633:toxicity; D006572:Heterocyclic Compounds, Bridged-Ring / Q000138:chemical synthesis / Q000302:isolation & purification / Q000494:pharmacology* / Q000633:toxicity; D006801:Humans; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects* / Q000502:physiology; D008826:Microbial Sensitivity Tests; D010068:Oxacillin / Q000494:pharmacology; D044004:Xanthones / Q000138:chemical synthesis / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D000596:Amino Acids; D000900:Anti-Bacterial Agents; D006571:Heterocyclic Compounds; D006572:Heterocyclic Compounds, Bridged-Ring; D044004:Xanthones; C482271:forbesione; C558352:morellic acid; D000667:Ampicillin; C052659:gambogic acid; D010068:Oxacillin
keywords: Bacterial invasion; Caged xanthones; Methicillin resistant Staphylococcus aureus; USA300