title: In vitro and in vivo antimalarial activity of essential oils and chemical components from three medicinal plants found in northeastern Brazil.
abstract: The prophylactic and therapeutic arsenal against malaria is quite restricted and all the antimalarials currently in use have limitations. Thus, there is a need to investigate medicinal plants in the search for phytochemicals which can be developed into drugs. In our investigation, essential oils (EOs) were obtained from Vanillosmopsis arborea (Gardner) Baker, Lippia sidoides Cham. and Croton zehntneri Pax & K. Hoffm., aromatic plants abundant in northeastern Brazil, which are found in the caatinga region and are used in traditional medicine. The chemical composition of these EOs was characterized by GC-MS, and monoterpenes and sesquiterpenes were well represented. We assessed the in vitro activity of these EOs and also individual EO chemical components against the human malaria parasite Plasmodium falciparum (K1 strain) and the in vivo activity of EOs in mice infected with Plasmodium berghei. The acute toxicity of these oils was assessed in healthy mice and in vitro cytotoxicity was determined at different concentrations against HeLa cells and mice macrophages. The EO of V. Arborea was partially active only when using the subcutaneous route (inhibited from 33 up to 47 %). In relation to the EOs, L. sidoides and C. zehntneri were active only by the oral route (per gavage) and partially inhibited the growth of P. berghei from 43 up to 55 % and showed good activity against P. falciparum in vitro (IC (50) = 7.00, 10.50, and 15.20 µg/mL, respectively). Individual EO constituents α-bisabolol, estragole, and thymol also exhibited good activity against P. falciparum (IC (50) = 5.00, 30.70, and 4.50 µg/mL, respectively). This is the first study showing evidence for the antimalarial activity of these species from northeastern Brazil and the low toxicity of their EOs.
authors.affiliation: Laboratório de Biologia da Malária e Toxoplasmose, Departamento de Microbiologia e Parasitologia, Universidade Federal do Rio Grande do Norte, Natal, Brazil.
authors.forename: Magaly L
authors.initials: ML
authors.lastname: Mota
authors.forename: Lis Tavares Coelho
authors.initials: LT
authors.lastname: Lobo
authors.forename: José M Galberto da
authors.initials: JM
authors.lastname: Costa
authors.forename: Leandro S
authors.initials: LS
authors.lastname: Costa
authors.forename: Hugo A O
authors.initials: HA
authors.lastname: Rocha
authors.forename: Luiz F
authors.initials: LF
authors.lastname: Rocha e Silva
authors.forename: Adrian M
authors.initials: AM
authors.lastname: Pohlit
authors.forename: Valter F de Andrade
authors.initials: VF
authors.lastname: Neto
mesh_terms: D000284:Administration, Oral; D000081248:Allylbenzene Derivatives; D000818:Animals; D000840:Anisoles / Q000008:administration & dosage; D000962:Antimalarials / Q000008:administration & dosage*; D019659:Asteraceae / Q000737:chemistry*; D001938:Brazil; D029802:Croton / Q000737:chemistry*; D006367:HeLa Cells / Q000187:drug effects; D006801:Humans; D055104:Infusions, Subcutaneous; D032411:Lippia / Q000737:chemistry*; D016778:Malaria, Falciparum / Q000188:drug therapy*; D051379:Mice; D000081222:Monocyclic Sesquiterpenes; D009822:Oils, Volatile / Q000008:administration & dosage*; D008517:Phytotherapy; D018515:Plant Leaves / Q000737:chemistry; D028321:Plant Preparations / Q000008:administration & dosage; D018547:Plant Stems / Q000737:chemistry; D010946:Plants, Medicinal / Q000737:chemistry; D010962:Plasmodium berghei / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects; D012717:Sesquiterpenes / Q000008:administration & dosage; D013943:Thymol / Q000008:administration & dosage
chemical_list: D000081248:Allylbenzene Derivatives; D000840:Anisoles; D000962:Antimalarials; D000081222:Monocyclic Sesquiterpenes; D009822:Oils, Volatile; D028321:Plant Preparations; D012717:Sesquiterpenes; C004497:bisabolol; D013943:Thymol; C007633:estragole