Abstract
Based on the prodrug principle, aspirin eugenol ester (AEE) was synthesized, which can reduce the side effects of aspirin and eugenol. As a good candidate for new antithrombotic and anti-inflammatory medicine, it is essential to evaluate its preventive effect on thrombosis. Preventive effect of AEE was investigated in κ-carrageenan-induced rat tail thrombosis model. AEE suspension liquids were prepared in 0.5% sodium carboxymethyl cellulose (CMC-Na). AEE was administrated at the dosage of 18, 36 and 72 mg/kg. Aspirin (20 mg/kg), eugenol (18 mg/kg) and 0.5% CMC-Na (30 mg/kg) were used as control drug. In order to compare the effects between AEE and its precursor, integration of aspirin and eugenol group (molar ratio 1:1) was also designed in the experiment. After drugs were administrated intragastrically for seven days, each rat was injected intraperitoneally with 20 mg/kg BW κ-carrageen dissolved in physiological saline to induce thrombosis. The length of tail-thrombosis was measured at 24 and 48 hours. The blank group just was given physiological saline for seven days without κ-carrageenan administrated. The results indicated that AEE significantly not only reduced the average length of thrombus, PT values and FIB concentration, but also reduced the red blood cell (RBC), hemoglobin (HGB), hematocrit (HCT) and platelet (PLT). The effects of AEE on platelet aggregation and anticoagulant in vitro showed that AEE could inhibit adenosine diphosphate (ADP)-induced platelet aggregation as dose-dependence but no notable effect on blood clotting. From these results, it was concluded that AEE possessed positive effect on thrombosis prevention in vivo through the reduction of FIB, PLT, inhibition of platelet aggregation and the change of TT and PT values.
Highlights
Since aspirin was invented, its use has become wide spread in the prevention and treatment of inflammation, headache, fever and cardiovascular disease [1,2,3,4,5,6]
After 4 hours of κ-carrageenan treatment, swelling and redness were observed in model group, while swelling and redness did not occur in the group which was given aspirin eugenol ester (AEE) at the dosage of 72 mg/ kg
There was no difference between model group and CMC-Na group in thrombosis length at 48 hours, which indicated that CMC-Na had no influence on thrombosis formation at 48 hours
Summary
Its use has become wide spread in the prevention and treatment of inflammation, headache, fever and cardiovascular disease [1,2,3,4,5,6]. Preventive Effect of Aspirin Eugenol Ester on Thrombosis has been recognized as safe essential oil by Food and Chemical Administration. Eugenol has been known for its various therapeutic effects, including anticoagulation, antivirus, analgesia, antipyretic, anti-inflammation, antibacterial, anti-platelet aggregation, antioxidation, anti-diarrhea, anti-hypoxia, antiulcer, and inhibition of intestinal movement and arachidonic acid metabolism [7,8,9,10,11]. In order to reduce their side effect and improve therapeutic effect and stabilization, aspirin eugenol ester (AEE) was synthesized [13]. The acute toxicity, teratogenicity, metabolism, pharmacodynamics, stability and mutagenicity of AEE have been investigated. A 15-day oral dose toxicity study showed that no-observed-adverse-effect level (NOAEL) value of AEE was considered to be 50 mg/kg/day under the study conditions [14]. The evaluation for its anti-inflammatory, analgesic and antipyretic effects through animal model showed that AEE possessed similarity effects with aspirin, but lasted for a longer time [17,18]
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