Action of Dation 500 mg on the Principal Inflammatory Mediators

Abstract

Objective:

To review the in vivo and in vitro studies having elicited an action of Daflon 500 mg^*, a purified micronized flavonoid fraction, on inflammatory processes.

Design:

Antioedematous and antichemotactic effects were investigated in rats in three studies. Moreover, the effect of Daflon 500 mg on free radicals, lipoperoxide and arachidonic acid metabolites known as inflammatory mediators was studied mainly in vitro to help understand mechanisms responsible for the anti-inflammatory activity.

Results:

The in vivo studies demonstrated that at the single oral dose of 100 mg/kg, Daflon 500 mg inhibited oedema induced by carrageenan injection into the plantar tissue of a hind paw. On a more chronic inflammatory condition, administered at the same dose during the 15 days preceding subcutaneous implantation of sponges and continued until sacrifice, it reduced granuloma weights (reflecting plasma extravasation) and density of phagocytic cells, and at a dose of 300 mg/kg/day for 1 month it mitigated mononuclear infiltration in the pancreas of diabetic rats. On the other hand, Daflon 500 mg in vitro elicited antiradical activity by inhibition of chemiluminesence, inhibited lipid peroxidation induced after hypoxia/reoxygenation in bovine aorto-endothelial cells and after UVA exposure in human fibroblasts. Besides, Daflon 500 mg decreased leukotriene production in rat stimulated mast cells as well as prostaglandins (PGE₂, PGF_2α) and thromboxane (TxB₂) in a granuloma model.

Conclusion:

The effects of Daflon 500 mg on experimental oedema probably result from interference with inflammatory mediators as demonstrated using in vivo and in vitro models, and may serve as a rational basis to explain its efficacy in diseases such as chronic venous insufficiency and more specifically in haemorrhoidal attacks.