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Revista Cubana de Farmacia

versión impresa ISSN 0034-7515


PEREZ GUERRA, Yohani et al. Effect of D-002 on 5-lipooxygenase (5-LOX) enzyme activity in vitro. Rev Cubana Farm [online]. 2012, vol.46, n.2, pp.259-266. ISSN 0034-7515.

Introduction: D-002, a mixture of six high molecular weight primary aliphatic alcohols purified from beeswax, has been shown to produce anti-inflammatory effects with no secondary gastrotoxicity in experimental models. Oral treatment with D-002 was effective for lowering the concentrations of B4 leukotriene (LTB4) in pleural exudates of rats with carragenin-induced pleurisy, suggesting that it could inhibit 5-lipooxigenase (5-LOX) enzyme activity. The mechanisms of the anti-inflammatory action of D-002, however, had not been explored yet. Objective: to evaluate the effects of D-002 on 5-LOX enzyme activity in vitro by using the cytosolic preparations from rat liver homogenates. Methods: testing conditions were as follows: cytosolic fraction (50 µg of protein) dissolved in 0.2 mol/L borate buffer solution (pH 9) and linoleic acid (7.8-250 mmol/L) as substrate. Parallel samples were incubated with Tween-20/H2O (2 %) only (vehicle, control samples), D-002 (0.9-1 000 µg/mL) or Lyprinol (500 µg/mL) (reference substance). The enzyme activity, evaluated through the formation of conjugated dienes, was assessed by the absorbance changes at 234 nm (5-lox) measured in a UV-visible spectrophotometer. Results: the in vitro addition of D-002 produced a significant, dose-dependent (r=0.980; p< 0.001) (IC50= 95.34 µg/mL) and uncompetitive inhibition of 5-LOX activity, whose maximal inhibition (70 %) was achieved with 500 µg/mL). Conclusions: this study demonstrates that D-002 effectively inhibits 5-LOX enzymatic activity, an effect that may partially explain the anti-inflammatory effects of D-002 in experimental models in vivo.

Palabras clave : D-002; anti-inflammatory; 5-LOX inhibition; LTB4; Lyprinol.

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