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Open AccessArticle

Antibacterial and EGFR-Tyrosine Kinase Inhibitory Activities of Polyhydroxylated Xanthones from Garcinia succifolia

1
ICBAS—Instituto de Ciências Biomédicas Abel Salazar—Universidade do Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal
2
Department of Botany, Faculty of Science, Kasetsart University, Paholyothin Road, Chatuchuck, Bangkok 10900, Thailand
3
Department of Biochemistry, Faculty of Science, Kasetsart University, Paholyothin Road, Chatuchuck, Bangkok 10900, Thailand
4
Interdisciplinary Centre of Marine and Environmental Research (CIIMAR), Universidade do Porto, Rua dos Bragas 289, 4050-123 Porto, Portugal
5
Traditional Uighur Medicine Department, Xinjiang Medical University, 393 Medical University Road, Urumqi 830011, Xinjiang, China
*
Author to whom correspondence should be addressed.
Molecules 2014, 19(12), 19923-19934; https://doi.org/10.3390/molecules191219923
Received: 3 October 2014 / Revised: 13 November 2014 / Accepted: 24 November 2014 / Published: 28 November 2014
(This article belongs to the Collection Bioactive Compounds)
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. View Full-Text
Keywords: antibacterial activity; antibiotic synergism; EGFR-tyrosine kinase inhibitory activity; Garcinia succifolia; multidrug-resistant bacteria; polyhydroxylated xanthone antibacterial activity; antibiotic synergism; EGFR-tyrosine kinase inhibitory activity; Garcinia succifolia; multidrug-resistant bacteria; polyhydroxylated xanthone
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MDPI and ACS Style

Duangsrisai, S.; Choowongkomon, K.; Bessa, L.J.; Costa, P.M.; Amat, N.; Kijjoa, A. Antibacterial and EGFR-Tyrosine Kinase Inhibitory Activities of Polyhydroxylated Xanthones from Garcinia succifolia. Molecules 2014, 19, 19923-19934.

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