期刊论文详细信息
Molecules
Antibacterial and EGFR-Tyrosine Kinase Inhibitory Activities of Polyhydroxylated Xanthones from Garcinia succifolia
Susawat Duangsrisai2  Kiattawee Choowongkomon3  Lucinda J. Bessa2  Paulo M. Costa2  Nurmuhammat Amat1  Anake Kijjoa2 
[1] Traditional Uighur Medicine Department, Xinjiang Medical University, 393 Medical University Road, Urumqi 830011, Xinjiang, China; E-Mail:;ICBAS—Instituto de Ciências Biomédicas Abel Salazar—Universidade do Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal; E-Mails:;Department of Biochemistry, Faculty of Science, Kasetsart University, Paholyothin Road, Chatuchuck, Bangkok 10900, Thailand; E-Mail:
关键词: antibacterial activity;    antibiotic synergism;    EGFR-tyrosine kinase inhibitory activity;    Garcinia succifolia;    multidrug-resistant bacteria;    polyhydroxylated xanthone;   
DOI  :  10.3390/molecules191219923
来源: mdpi
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【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.

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