title: Antibacterial and EGFR-tyrosine kinase inhibitory activities of polyhydroxylated xanthones from Garcinia succifolia.
abstract: Chemical investigation of the methanol extract of the wood of Garcinia succifolia Kurz (Clusiaceae) led to the isolation of 1,5-dihydroxyxanthone (1), 1,7-dihydroxyxanthone (2), 1,3,7-trihydroxyxanthone (3), 1,5,6-trihydroxyxanthone (4), 1,6,7-trihydroxyxanthone (5), and 1,3,6,7-tetrahydroxyxanthone (6). All of the isolated xanthones were evaluated for their antibacterial activity against bacterial reference strains, two Gram-positive (Staphylococcus aureus ATTC 25923, Bacillus subtillis ATCC 6633) and two Gram-negative (Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853), and environmental drug-resistant isolates (S. aureus B1, Enteroccoccus faecalis W1, and E. coli G1), as well as for their epidermal growth factor receptor (EGFR) of tyrosine kinase inhibitory activity. Only 1,5,6-trihydroxy-(4), 1,6,7-trihydroxy-(5), and 1,3,6,7-tetrahydroxyxanthones (6) exhibited antibacterial activity against Gram-positive bacteria, however none was active against vancomycin-resistant E. faecalis. Additionally, 1,7-dihydroxyxanthone (2) showed synergism with oxacillin, but not with ampicillin. On the other hand, only 1,5-dihydroxyxanthone (1) and 1,7-dihydroxyxanthone (2) were found to exhibit the EGFR-tyrosine kinase inhibitory activity, with IC50 values of 90.34 and 223 nM, respectively.
authors.affiliation: ICBAS-Instituto de Ciências Biomédicas Abel Salazar-Universidade do Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal. fscissw@ku.ac.th.
authors.forename: Susawat
authors.initials: S
authors.lastname: Duangsrisai
authors.affiliation: Department of Biochemistry, Faculty of Science, Kasetsart University, Paholyothin Road, Chatuchuck, Bangkok 10900, Thailand. kiattawee@hotmail.com.
authors.forename: Kiattawee
authors.initials: K
authors.lastname: Choowongkomon
authors.affiliation: ICBAS-Instituto de Ciências Biomédicas Abel Salazar-Universidade do Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal. lbessa@ciimar.up.pt.
authors.forename: Lucinda J
authors.initials: LJ
authors.lastname: Bessa
authors.affiliation: ICBAS-Instituto de Ciências Biomédicas Abel Salazar-Universidade do Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal. pmcosta@icbas.up.pt.
authors.forename: Paulo M
authors.initials: PM
authors.lastname: Costa
authors.affiliation: Traditional Uighur Medicine Department, Xinjiang Medical University, 393 Medical University Road, Urumqi 830011, Xinjiang, China. nur818@hotmail.com.
authors.forename: Nurmuhammat
authors.initials: N
authors.lastname: Amat
authors.affiliation: ICBAS-Instituto de Ciências Biomédicas Abel Salazar-Universidade do Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal. ankijjoa@icbas.up.pt.
authors.forename: Anake
authors.initials: A
authors.lastname: Kijjoa
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D004357:Drug Synergism; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000378:metabolism; D005658:Fungi / Q000187:drug effects; D029760:Garcinia / Q000737:chemistry*; D006900:Hydroxylation; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D044004:Xanthones / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D047428:Protein Kinase Inhibitors; D044004:Xanthones; D066246:ErbB Receptors