The present study evaluated the anti-inflammatory activity of
amburoside A (a
phenol glucoside) and
isokaempferide (a
flavonol) isolated from the trunk bark of Amburana cearensis, a medicinal plant used in northeast Brazil for the treatment of
asthma. Animals (male Wistar rats or Swiss mice) pre-treated with
amburoside A (25 and 50 mg/kg) or
isokaempferide (12.5, 25 and 50 mg/kg), orally or intraperitoneally, showed a significant inhibition of the paw oedema induced by
carrageenan (1%),
prostaglandin E(2) (30 nmol/paw),
histamine (200 microg/paw) or
serotonin (200 microg/paw). Histological and morphometric evaluations of the rat paw oedema induced by
carrageenan showed that
amburoside A and
isokaempferide also inhibited the accumulation of inflammatory cells.
Amburoside A reduced significantly the paw oedema and the increase in vascular permeability induced by
dextran, as related to the control group. Similar results were observed with the
isokaempferide pre-treatment. Furthermore,
amburoside A or
isokaempferide inhibited both leucocyte and neutrophil migrations, in mouse peritoneal cavity, after the
carrageenan injection. The
polyphenols were not cytotoxic and blocked N-formyl-methyl-
leucyl-phenylalanine-induced
myeloperoxidase release and activity in human neutrophils. In addition,
amburoside A and
isokaempferide at 50 and 100 microg/ml concentrations reduced significantly the
lipopolysaccharide-mediated increase in tumour
necrosis factor-alpha (
TNF-alpha) levels. These results provide, for the first time, evidence to support the anti-inflammatory activity of
amburoside A and
isokaempferide that seems to be related to an inhibition of inflammatory mediators, such as
TNF-alpha, as well as
histamine,
serotonin and
prostaglandin E(2), besides leucocyte infiltration in a dose- or concentration-dependent manner. These anti-inflammatory effects can be explained, at least in part, by the ability of these compounds to reduce neutrophil degranulation,
myeloperoxidase activity, mediators as well as
TNF-alpha secretion.