Xanthone Information

Xanthone Research

Antifungal activity of xanthones: evaluation of their effect on ergosterol biosynthesis by high-performance liquid chromatography.

Chem Biol Drug Des. 2011 Mar;77(3):212-22. doi: 10.1111/j.1747-0285.2010.01072.x. Epub 2011 Jan 19.
Pinto E, Afonso C, Duarte S, Vale-Silva L, Costa E, Sousa E, Pinto M.

Research Center of Medicinal Chemistry - University of Porto (CEQUIMED-UP), R. Aníbal Cunha, 164, 4050-047, Porto, Portugal. epinto@ff.up.pt

Abstract

The increasing resistance of pathogenic fungi to antifungal compounds and the reduced number of available drugs led to the search for therapeutic alternatives among natural products, including xanthones. The antifungal activity of 27 simple oxygenated xanthones was evaluated by determination of their minimal inhibitory concentration on clinical and type strains of Candida, Cryptococcus, Aspergillus and dermatophytes, and their preponderance on the dermatophytic filamentous fungi was observed. Furthermore, a simple and efficient HPLC method with UV detection to study the effect of the active xanthones on the biosynthesis of ergosterol was developed and validated. Using this methodology, the identification and quantification of fungal sterols in whole cells of Candida albicans, Cryptococcus neoformans, Aspergillus fumigatus, and Trichophyton mentagrophytes were accomplished. In summary, 1,2-dihydroxyxanthone was found to be the most active compound against all strains tested, showing its effect on sterol biosynthesis by reducing the amount of ergosterol detected.

PMID: 21244637 [PubMed - in process]

Therapeutic activity of two xanthones in a xenograft murine model of human chronic lymphocytic leukemia.

J Hematol Oncol. 2010 Dec 7;3:49.
Loisel S, Le Ster K, Meyer M, Berthou C, Youinou P, Kolb JP, Billard C.

EA 2216, Université de Bretagne, Brest, France.

Abstract

BACKGROUND: We previously reported that allanxanthone C and macluraxanthone, two xanthones purified from Guttiferae trees, display in vitro antiproliferative and proapoptotic activities in leukemic cells from chronic lymphocytic leukemia (CLL) and leukemia B cell lines.

RESULTS: Here, we investigated the in vivo therapeutic effects of the two xanthones in a xenograft murine model of human CLL, developed by engrafting CD5-transfected chronic leukemia B cells into SCID mice. Treatment of the animals with five daily injections of either allanxanthone C or macluraxanthone resulted in a significant prolongation of their survival as compared to control animals injected with the solvent alone (p = 0.0006 and p = 0.0141, respectively). The same treatment of mice which were not xenografted induced no mortality.

CONCLUSION: These data show for the first time the in vivo antileukemic activities of two plant-derived xanthones, and confirm their potential interest for CLL therapy.

PMID: 21138552 [PubMed - in process]PMCID: PMC3016254

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