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2015, Number 1

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Rev Cubana Farm 2015; 49 (1)

Effects of octacosanol and triacontanol alcohols on ciclooxygenase and 5-lipoxygenase enzyme activities in vitro

Pérez GY, Mas FR, Oyarzábal YÁ, Jiménez DS, Molina CV

Language: English
References: 39
Page: 117-131
PDF size: 201.07 Kb.


ABSTRACT

Introduction: policosanol, a mixture of eight primary aliphatic alcohols purified from sugar cane wax, contains octacosanol as major component. D-002, a mixture of six primary aliphatic alcohols purified from beeswax, presents triacontanol as the main component. Although both substances are high molecular weight alcohol mixtures, they have different compositions and pharmacological effects such as their distinct effects on arachidonic acid metabolism enzymes; whereas policosanol inhibits cyclooxygenase (COX)-1, D-002 inhibits COX and 5-lipoxygenase (5-LOX) activities.
Objective: to study the effects of octacosanol and triacontanol, which are main components of policosanol and D-002, respectively on the COX and the 5-LOX enzyme in vitro activities.
Methods: triacontanol and octacosanol were suspended in a Tween-20/H2O (2%) (0.6-5000g/mL) vehicle. The effects of adding these alcohols on COX-1, COX-2 and 5-LOX enzymes activities were assessed in rat platelet microsomes, rat seminal vesicle microsomes and rat polymorphonuclear (PMN) preparations, respectively. Indomethacin (0.4µg/mL) was used as reference inhibitor of COX-1 and COX-2, and Lyprinol as 5-LOX inhibitor.
Results: octacosanol showed significant, marked (70% with highest concentration) (IC50=143.54 g/mL) and dose-dependent (r=0.991, p ‹ 0.001) inhibitory action on COX-1 activity. However, Triacontanol did not affect COX-1, but inhibited significantly, depending on dose (r=0.985, p ‹ 0.001) the COX-2 activity to 50% with 1250g/mL. In contrast, octacosanol did not change COX-2 activity. Indomethacin inhibited both COX-1 and COX-2 by 83%. Octacosanol addition was ineffective whereas triacontanol had significant, dose-dependent (r=0.978, p ‹ 0.001) and marked effect (79%) on the 5-LOX activity (IC50=58.74g/mL). Lyprinol inhibited 5-LOX by 89%. The inhibitions induced by octacosanol and triacontanol were competitive.
Conclusions: in vitro addition of octacosanol and triacontanol caused differential effects on COX-1, COX-2 and 5-LOX enzyme activities. Whereas octacosanol markedly inhibited COX-1 activity and did not change those of COX-2 and 5-LO, triacontanol markedly inhibited 5-LOX activity, but had moderate effect on COX-2 and did not change COX-1 activity.


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