title: Antiprotozoal, antimycobacterial, and anti-inflammatory evaluation of Cnidoscolus chayamansa (Mc Vaugh) extract and the isolated compounds.
abstract: Cnidoscolus chayamansa is a medicinal and edible plant known as Chaya, is commonly used as an anti-inflammatory, antiprotozoal, antibacterial agent and as a remedy for respiratory illness, gastrointestinal disorders, and vaginal infections related with the inflammation process. In this paper, we describe the plant's phytochemical analysis and biological activities (antimycobacterial, antibacterial, antiprotozoal, and anti-inflammatory properties) of the CHCl3:MeOH (1:1) leaves extract and isolated compounds, as well as the acute and sub-acute toxic effects. Chemical identification of isolated compounds was performed by1H- and13C NMR spectra data. In vitro antibacterial and antimycobacterial activities were determined by disc diffusion and MABA assays, respectively; antiprotozoal test by means of the sub-culture test. Topical and systemic anti-inflammatory effects were tested by TPA and carrageenan assay on BALB/c mice. Moretenol, moretenyl acetate, kaempferol-3,7-dimethyl ether, and 5-hydroxy-7-3',4'-trimethoxyflavanone were the main compounds isolated. The CHCl3:MeOH extract showed antiprotozoal (IC50≤65.29μg/mL), antimycobacterial (MIC≤50μg/mL), and anti-inflammatory activities (ED50=1.66mg/ear and 467.73mg/kg), but was inactive against the bacterial strains tested. The LD50for extract was >2g/kg. In the sub-acute toxicity test, the extract was administered at 1g/kg for 28days and did not cause lethality or any alteration in hematological and biochemical parameters; in addition, liver, kidney, and spleen histological analysis exhibited no structural changes. Moretenol and moretenyl acetate showed MIC=25μg/mL against Mycobacterium tuberculosis H37Rv and against four monoresistant strains of M. tuberculosis H37Rv. Both compounds exhibited moderate activity against Entamoeba histolytica and Giardia lamblia (IC50≤71.70μg/mL). Kaempferol-3,7-dimethyl ether and 5-hydroxy-7-3',4'-trimethoxy-flavanone were more active than the extract against E. histolytica and G. lamblia, showing IC50≤27.43μg/mL. As topical anti-inflammatory agents, moretenol and kaempferol-3,7-dimethyl ether were the most active compounds inhibiting the edema in 30.52 and 26.67%, respectively. Moretenol and moretenyl acetate showed significant antimycobacterial and antiprotozoal activities; in addition, important antiprotozoal effect was detected with kaempferol-3,7-dimethyl ether and 5-hydroxy-7-3',4'-trimethoxyflavanone. The extract and the terpenoids possess good anti-inflammatory activity. The extract did not produce lethality or adverse effects in acute and sub-acute tests.
authors.affiliation: Unidad de Investigación Médica en Farmacología, Hospital de Especialidades, CMNS XXI, IMSS, Av. Cuauhtémoc 330, Col. Doctores, Delg, Cuauhtémoc 06720, CDMX, Mexico.
authors.forename: Mariana Z
authors.initials: MZ
authors.lastname: Pérez-González
authors.affiliation: Unidad de Investigación Médica en Farmacología, Hospital de Especialidades, CMNS XXI, IMSS, Av. Cuauhtémoc 330, Col. Doctores, Delg, Cuauhtémoc 06720, CDMX, Mexico.
authors.forename: Gabriel A
authors.initials: GA
authors.lastname: Gutiérrez-Rebolledo
authors.affiliation: Unidad de Investigación Médica en Enfermedades Infecciosas y Parasitarias, Hospital de Pediatría, CMN-SXXI, IMSS, Av. Cuauhtémoc 330, Col. Doctores, Delg, Cuauhtémoc 06720, CDMX, Mexico.
authors.forename: Lilián
authors.initials: L
authors.lastname: Yépez-Mulia
authors.affiliation: Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía, Av. Insurgentes Sur 3877, Col. La Fama, Delg, Tlalpan 14269, CDMX, Mexico.
authors.forename: Irma S
authors.initials: IS
authors.lastname: Rojas-Tomé
authors.affiliation: Departamento de Inmunología, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Plan de Ayala s/n, Col. Casco de Santo Tomás, Delg, Miguel Hidalgo 11340, CDMX Mexico.
authors.forename: Julieta
authors.initials: J
authors.lastname: Luna-Herrera
authors.affiliation: Unidad de Investigación Médica en Farmacología, Hospital de Especialidades, CMNS XXI, IMSS, Av. Cuauhtémoc 330, Col. Doctores, Delg, Cuauhtémoc 06720, CDMX, Mexico. Electronic address: adelinajim08@prodigy.net.mx.
authors.forename: María A
authors.initials: MA
authors.lastname: Jiménez-Arellanes
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000494:pharmacology*; D024881:Drug Resistance, Bacterial / Q000187:drug effects; D004748:Entamoeba histolytica / Q000187:drug effects; D019665:Euphorbiaceae / Q000737:chemistry* / Q000633:toxicity; D016829:Giardia lamblia / Q000187:drug effects; D007249:Inflammation / Q000139:chemically induced / Q000517:prevention & control; D007928:Lethal Dose 50; D008297:Male; D008800:Mexico; D008807:Mice, Inbred BALB C; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D000900:Anti-Bacterial Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000981:Antiprotozoal Agents; D000995:Antitubercular Agents; D010936:Plant Extracts
keywords: 5-hydroxy-7-3′,4′-trimethoxyflavanone; Cnidoscolus chayamansa; Flavonoids; Kaempferol-3,7-dimethyl ether; Moretenol; Moretenyl acetate; Terpenoids