title: Bioactive compounds of Aspergillus terreus-F7, an endophytic fungus from Hyptis suaveolens (L.) Poit.
abstract: The compounds terrein (1), butyrolactone I (2), and butyrolactone V (3) were isolated from the ethyl acetate extract (EtOAc) of the endophytic fungus Aspergillus terreus-F7 obtained from Hyptis suaveolens (L.) Poit. The extract and the compounds presented schistosomicidal activity against Schistosoma mansoni; at 100 µg/mL for EtOAc extract, 1297.3 µM for compound 1, 235.6 µM for compound 2, and 454.1 µM for compound 3, they killed 100% of the parasites after 72 h of treatment. Compounds 1, 2, and 3 exerted moderate leishmanicidal activity against Leishmania amazonensis (IC50ranged from 23.7 to 78.6 µM). At 235.6 and 227.0 µM, compounds 2 and 3, respectively, scavenged 95.92 and 95.12% of the DPPH radical (2,2-diphenyl-1-picryl-hydrazyl), respectively. Regarding the cytotoxicity against the breast tumor cell lines MDA-MB-231 and MCF-7, compound 2 gave IC50of 34.4 and 17.4 µM, respectively, while compound 3 afforded IC50of 22.2 and 31.9 µM, respectively. At 117.6 µM, compound 2 inhibited the growth of and killed the pathogen Escherichia coli (ATCC 25922). Compounds 1, 2, and 3 displayed low toxicity against the normal line of human lung fibroblasts (GM07492A cells), with IC50of 15.3 × 103, 3.4 × 103, and 5.8 × 103µM, respectively. This is the first report on (i) the in vitro schistosomicidal and leishmanicidal activities of the EtOAc extract of A. terreus-F7 and compounds 1, 2, and 3; and (ii) the antitumor activity of compounds 2 and 3 against MDA-MB-231 and MCF-7 cells.
authors.affiliation: Department of Botany and Ecology, Institute of Biosciences, Federal University of Mato Grosso, Cuiabá, MT, Brazil.
authors.forename: Igor Pereira
authors.initials: IP
authors.lastname: da Silva
authors.affiliation: Department of Botany and Ecology, Institute of Biosciences, Federal University of Mato Grosso, Cuiabá, MT, Brazil.
authors.forename: Elson
authors.initials: E
authors.lastname: Brissow
authors.affiliation: Natural Products Research Group, Center for Research in Mathematical Sciences and Technology, University of Franca, Franca, SP, Brazil.
authors.forename: Luis Claudio
authors.initials: LC
authors.lastname: Kellner Filho
authors.affiliation: Department of Biological Sciences, University of Santa Cruz, Ilheus, BA, Brazil.
authors.forename: Jaqueline
authors.initials: J
authors.lastname: Senabio
authors.affiliation: Department of Biological Sciences, University of Santa Cruz, Ilheus, BA, Brazil.
authors.forename: Kátia Aparecida
authors.initials: KA
authors.lastname: de Siqueira
authors.affiliation: Department of Basic Sciences in Health, School of Medicine, Federal University of Mato Grosso, Cuiabá, MT, Brazil.
authors.forename: Samuel
authors.initials: S
authors.lastname: Vandresen Filho
authors.affiliation: Natural Products Research Group, Center for Research in Mathematical Sciences and Technology, University of Franca, Franca, SP, Brazil.
authors.forename: Jaqueline Lopes
authors.initials: JL
authors.lastname: Damasceno
authors.affiliation: Natural Products Research Group, Center for Research in Mathematical Sciences and Technology, University of Franca, Franca, SP, Brazil.
authors.forename: Suzana Amorim
authors.initials: SA
authors.lastname: Mendes
authors.affiliation: Natural Products Research Group, Center for Research in Mathematical Sciences and Technology, University of Franca, Franca, SP, Brazil.
authors.forename: Denise Crispim
authors.initials: DC
authors.lastname: Tavares
authors.affiliation: Natural Products Research Group, Center for Research in Mathematical Sciences and Technology, University of Franca, Franca, SP, Brazil.
authors.forename: Lizandra Guidi
authors.initials: LG
authors.lastname: Magalhães
authors.affiliation: Research Center René Rachou, Oswaldo Cruz Foundation, Belo Horizonte, MG, Brazil.
authors.forename: Policarpo Ademar Sales
authors.initials: PA
authors.lastname: Junior
authors.affiliation: Natural Products Research Group, Center for Research in Mathematical Sciences and Technology, University of Franca, Franca, SP, Brazil.
authors.forename: Ana Helena
authors.initials: AH
authors.lastname: Januário
authors.affiliation: Department of Botany and Ecology, Institute of Biosciences, Federal University of Mato Grosso, Cuiabá, MT, Brazil. drmasoares@gmail.com.
authors.forename: Marcos Antônio
authors.initials: MA
authors.lastname: Soares
mesh_terms: D015107:4-Butyrolactone / Q000031:analogs & derivatives / Q000302:isolation & purification; D000818:Animals; D000871:Anthelmintics / Q000302:isolation & purification / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000302:isolation & purification / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000302:isolation & purification / Q000494:pharmacology; D001230:Aspergillus / Q000737:chemistry*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D003517:Cyclopentanes / Q000302:isolation & purification / Q000494:pharmacology*; D060026:Endophytes / Q000378:metabolism; D005663:Furans / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D031331:Hyptis / Q000382:microbiology*; D007783:Lactones / Q000302:isolation & purification / Q000494:pharmacology*; D007891:Leishmania / Q000187:drug effects; D061986:MCF-7 Cells; D012547:Schistosoma / Q000187:drug effects
chemical_list: D000871:Anthelmintics; D000970:Antineoplastic Agents; D000981:Antiprotozoal Agents; D003517:Cyclopentanes; D005663:Furans; D007783:Lactones; C439087:terrein; C082868:butyrolactone I; D015107:4-Butyrolactone
keywords: Antioxidant; Antitumor; Butyrolactones; Leishmanicidal; Schistosomicidal; Terrein