title: Antiamoebic and Antigiardial Activity of Clerodane Diterpenes from Mexican Salvia Species Used for the Treatment of Diarrhea.
abstract: Terpenoids from Salvia species have been identified to possess biological properties as antiprotozoal agents. Here, we evaluated the antiamoebic and antigiardial activities of 14 known clerodane and modified clerodane-type diterpenes isolated from five Mexican Salvia species against Entamoeba histolytica and Giardia lamblia, and analyzed the effects of the functionalities in decalin ring or in the whole clerodane framework to visualize the structural requirements necessary to produce an antiprotozoal activity. Among these, linearolactone was the most active clerodane diterpene against both protozoa with IC50 values of 22.9 μM for E. histolytica and of 28.2 μM in the case of G. lamblia. In this context it may be a lead compound for the development of novel therapeutic agent for the treatment of diarrhea and dysentery. The remaining diterpenes assayed showed moderate to weak activity against both protozoa. These findings give support to the use of Salvia species in the traditional medicine from México for the treatment of diarrhea.
authors.affiliation: Unidad de Investigación Médica en Farmacología, UMAE Hospital de Especialidades, 2° Piso CORCE, Centro Médico Nacional Siglo XXI, México D. F., México.
authors.forename: Fernando
authors.initials: F
authors.lastname: Calzada
authors.affiliation: Instituto de Química, Universidad Nacional Autónoma de México, Ciudad Universitaria, México D. F., México.
authors.forename: Elihú
authors.initials: E
authors.lastname: Bautista
authors.affiliation: Unidad de Investigación Médica en Enfermedades Infecciosas y Parasitarias, UMAE Hospital de Pediatría, 2° Piso, Centro Médico Nacional Siglo XXI, México City, México.
authors.forename: Lilian
authors.initials: L
authors.lastname: Yépez-Mulia
authors.affiliation: Unidad de Investigación Médica en Genética Humana, UMAE Hospital de Pediatría, Centro Médico Nacional Siglo XXI, IMSS, I, México City, México.
authors.forename: Normand
authors.initials: N
authors.lastname: García-Hernandez
authors.affiliation: Instituto de Química, Universidad Nacional Autónoma de México, Ciudad Universitaria, México D. F., México.
authors.forename: Alfredo
authors.initials: A
authors.lastname: Ortega
mesh_terms: D000981:Antiprotozoal Agents / Q000494:pharmacology; D003967:Diarrhea / Q000188:drug therapy*; D045785:Diterpenes, Clerodane / Q000494:pharmacology*; D004748:Entamoeba histolytica / Q000187:drug effects; D016829:Giardia lamblia / Q000187:drug effects; D008519:Medicine, Traditional; D008800:Mexico; D010936:Plant Extracts / Q000494:pharmacology*; D027544:Salvia / Q000737:chemistry
chemical_list: D000981:Antiprotozoal Agents; D045785:Diterpenes, Clerodane; D010936:Plant Extracts; C550304:linearolactone
keywords: Entamoeba histolytica; Giardia lamblia; Salvia species; antiprotozoal activity; clerodane diterpenes