NDLI: Inhibition of Cruzain by Ocotea Leaf Essential Oils from Monteverde, Costa Rica

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Inhibition of Cruzain by Ocotea Leaf Essential Oils from Monteverde, Costa Rica

Content Provider	Semantic Scholar
Author	Setzer, William N. Takaku, Sayaka Stokes, Sean L. Penton, Ashley F.
Copyright Year	2006
Abstract	Summary Introduction: Over 18 million people in tropical and subtropical America are afflicted by American trypanosomiasis or Chagas disease. Symptoms of the disease include fever, swelling, and heart and brain damage, usually leading to death. There is currently no effective treatment for this disease. Cruzain is a cysteine protease from Trypanosoma cruzi that is key to replication and differentiation of the parasite and has been identified as an important biochemical target for treatment of this parasitic infection. Materials and Methods: The leaf essential oils of ten species of Ocotea from Monteverde, Costa Rica, were obtained by hydrodistillation and analyzed by GC-MS. The enzyme inhibitory activities of the essential oils against cruzain have been examined using a fluorometric assay. Results: O. meziana leaf oil was the most active (IC50 = 14.9 µg/mL) followed by O. whitei (15.8 µg/mL), Ocotea sp. nov. "los llanos" (17.1 µg/mL), Ocotea sp. nov. "small leaf" (19.2 µg/mL) and O. holdridgeana (76.9 µg/mL). The leaf oils of O. floribunda, O. tonduzii, and O. valeriana were somewhat active (IC50 100-200 µg/mL), but O. sinuata and O. veraguensis essential oils were inactive (IC50 > 500 µg/mL). The Ocotea leaf essential oils are generally dominated by the monoterpenes α- and β-pinene and the sesquiterpenes β-caryophyllene and germacrene D. α-Pinene and β- pinene show slight cruzain inhibitory activity (IC50 = 160 and 155 µg/mL, respectively), but neither β-caryophyllene nor germacrene D are active (IC50 > 500 µg/mL). Conclusions: The cruzain inhibitory activity of Ocotea leaf essential oils cannot be explained by the activities of the major components alone. There may be synergistic effects of the components or the activities may be due to minor components.
File Format	PDF HTM / HTML
Alternate Webpage(s)	http://pharmacologyonline.silae.it/files/archives/2006/vol3/092.Setzer2.pdf
Language	English
Access Restriction	Open
Content Type	Text
Resource Type	Article

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