Cruzain Inhibitory Activity of Leaf Essential Oils of Neotropical Lauraceae and Essential Oil Components

Author:

Setzer William N.1,Stokes Sean L.1,Penton Ashley F.1,Takaku Sayaka1,Haber William A.2,Hansell Elizabeth3,Caffrey Conor R.3,McKerrow James H.3

Affiliation:

1. Department of Chemistry, University of Alabama in Huntsville, Huntsville, Alabama 35899, USA

2. Missouri Botanical Garden, St. Louis, Missouri 63166, USA Apdo. 50-5655, Monteverde, Puntarenas, Costa Rica, Central America

3. Department of Pathology, University of California, San Francisco, California 94143, USA

Abstract

The leaf essential oils of twenty-three species of Lauraceae from Monteverde, Costa Rica, have been screened for inhibition of the cysteine protease cruzain. Of these, nine showed promising cruzain inhibitory activity (IC50 < 100 μg/mL), six showed marginal activity (IC50, 100–500 μg/mL), and eight were inactive (IC50 > 500 μg/mL). The cruzain inhibitory activities of the essential oils can be attributed to active sesquiterpenoid components as well as synergistic effects between two or more components. The sesquiterpenes α-copaene, β-caryophyllene, α-humulene, and germacrene D are active (IC50 ~5–30 μg/mL) alone, but also show increased activity in combination with other essential oil components.

Publisher

SAGE Publications

Subject

Complementary and alternative medicine,Plant Science,Drug Discovery,Pharmacology,General Medicine

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