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Molecules 2014, 19(12), 19923-19934; doi:10.3390/molecules191219923

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.
Received: 3 October 2014 / Revised: 13 November 2014 / Accepted: 24 November 2014 / Published: 28 November 2014
(This article belongs to the Collection Bioactive Compounds)
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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. 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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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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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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