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Eugenol a valuable compound for in vitro experimental research and worthwhile for further in vivo investigation

1990; Wiley; Volume: 4; Issue: 3 Linguagem: Inglês

10.1002/ptr.2650040304

1099-1573

Gert Laekeman, L. Van Hoof, Achiel Haemers, D. A. Vanden Berghe, A. G. Herman, A. J. Vlietinck,

Traditional and Medicinal Uses of Annonaceae

Abstract Eugenol and isoeugenol are responsible for several pharmacological activities exhibited by nutmeg preparations. We studied their antimicrobial and antiaggregation activity in vitro and their influence on platelet function ex vivo . At the same time biogenetically or metabolically related derivatives were tested. Eugenol and isoeugenol (1 mg/mL) showed pronounced antibacterial properties: growth inhibition of 6 out of 10 Gram + and Gram – microorganisms was comparable with neomycin (500 μg/mL). Growth inhibition was even more pronounced for Candida species in comparison with nystatin (5000 U/mL). Eugenol and some of its analogues inhibited growth of Aspergillus and Trichophyton species at concentrations of 100 μg/mL. However, cytotoxicity of the compounds will limit their systemical use. The IC 50 , of eugenol (3.0 × 10 −7 M ) and isoeugenol (7.2 × 10 −7 M ), were comparable with indomethacin (2.2 × 10 −7 M ) on platelet aggregation. Their free hydroxy group was necessary for pharmacological activity. Ex vivo results revealed a dose‐dependent blocking effect on the thromboxane biosynthesis by rat blood platelets: 66% inhibition by 50 mg/kg to 96% inhibition by 400 mg/kg. Eugenol and acetyleugenol given orally to rabbits had mean biological half‐lives of 95 and 60 min respectively. Eugenol might be an interesting basic structure for drug design.