Abstract
Vasorelaxant and antioxidant activities are important in the therapy for cardiovascular
diseases. We aimed at investigating the vasorelaxant and antioxidant activities of
six xanthones isolated from Brazilian medicinal plants. Xanthone (1), 1-hydroxyxanthone (2), 4-hydroxyxanthone (3), 1-hydroxy-8-methoxyxanthone (4), 1,3-dihydroxy-7-methoxyxanthone (5) and 2,6,8-trihydroxy-1-methoxyxanthone (6) induced concentration-dependent vasorelaxant effects in endothelium-intact mice
aortic rings. The presence of a hydroxy group in position 1 seemed to decrease the
vasodilator effect while a hydroxy in position 4 and an increased number of hydroxy
groups improved the vasorelaxatory potential of xanthones. All xanthones showed antioxidant
activity but their potencies did not correlate with the vasodilator effect. Our results
suggest that the tested xanthones are potentially vasorelaxant and antioxidant compounds
but the two activities are not interrelated.
Key words
xanthones - vasorelaxation - antioxidant effect - aorta
References
- 1
Saraiva L, Fresco P, Pinto E, Sousa E, Pinto M, Goncalves J.
Inhibition of protein kinase C by synthetic xanthone derivatives.
Bioorg Med Chem.
2003;
11
1215-25
- 2
Saraiva L, Fresco P, Pinto E, Kijjoa A, Gonzalez M J, Goncalves J.
Differential activation of protein kinase C isoforms by euxanthone, revealed by an
in vivo yeast phenotypic assay.
Planta Med.
2002;
68
1039-41
- 3
Saraiva L, Fresco P, Pinto E, Sousa E, Pinto M, Goncalves J.
Synthesis and in vivo modulatory activity of protein kinase C of xanthone derivatives.
Bioorg Med Chem.
2002;
10
3219-27
- 4
Cheng Y W, Kang J J.
Mechanism of vasorelaxation of thoracic aorta caused by xanthone.
Eur J Pharmacol.
1997;
336
23-8
- 5
Wang L W, Kang J J, Chen I J, Teng C M, Lin C N.
Antihypertensive and vasorelaxing activities of synthetic xanthone derivatives.
Bioorg Med Chem.
2002;
10
567-72
- 6
Jiang D J, Jiang J L, Tan G S, Du Y H, Xu K P, Li Y J.
Protective effects of daviditin A against endothelial damage induced by lysophosphatidylcholine.
Naunyn Schmiedebergs Arch Pharmacol.
2003;
367
600-6
- 7
Paravicini T M, Touyz R M.
NADPH oxidases, reactive oxygen species, and hypertension: clinical implications and
therapeutic possibilities.
Diabet Care.
2008;
31
S170-80
- 8
Grossman E.
Does increased oxidative stress cause hypertension?.
Diabet Care.
2008;
31
S185-9
- 9
Hiraku Y, Ito K, Hirakawa K, Kawanishi S.
Photosensitized DNA damage and its protection via a novel mechanism.
Photochem Photobiol.
2007;
83
205-12
- 10
Rabelo L A, Cortes S F, Alvarez-Leite J I, Lemos V S.
Endothelium dysfunction in LDL receptor knockout mice: a role for H2O2.
Br J Pharmacol.
2003;
138
1215-20
- 11
Georgetti S R, Casagrande R, Di Mambro V M, Azzolini A E, Fonseca M J.
Evaluation of the antioxidant activity of different flavonoids by the chemiluminescence
method.
AAPS Pharm Sci.
2003;
5
E20-5
- 12
Carvalho M J, Carvalho L M, Ferreira A M, Silva A M.
A new xanthone from Hedychium gardnerianum.
.
Nat Prod Res.
2003;
17
445-9
- 13 Finnegan R A, Patel J K. Constituents of Mammea americana X. Isolation of mono- and dihydroxyxanthones. Synthesis of 1,5-, 3,5-, 1,6-, and
1,7-dihydroxyxanthone. J Chem Soc 1972: 1896-901
- 14 Silveira J C. Alguns constituintes de Haploclathra paniculata [dissertation]. Belo Horizonote: Federal University of Minas Gerais 1984
Steyner F. Cortes
Department of Pharmacology
Instituto de Ciências Biológicas
Universidade Federal de Minas Gerais
31270–901 Belo Horizonte MG
Brazil
Phone: +55-31-3409-2726
Fax: +55-31-3409-2695
Email: sfcortes@icb.ufmg.br