Autor: |
da Silva IP; Department of Botany and Ecology, Institute of Biosciences, Federal University of Mato Grosso, Cuiabá, MT, Brazil., Brissow E; Department of Botany and Ecology, Institute of Biosciences, Federal University of Mato Grosso, Cuiabá, MT, Brazil., Kellner Filho LC; Natural Products Research Group, Center for Research in Mathematical Sciences and Technology, University of Franca, Franca, SP, Brazil., Senabio J; Department of Biological Sciences, University of Santa Cruz, Ilheus, BA, Brazil., de Siqueira KA; Department of Biological Sciences, University of Santa Cruz, Ilheus, BA, Brazil., Vandresen Filho S; Department of Basic Sciences in Health, School of Medicine, Federal University of Mato Grosso, Cuiabá, MT, Brazil., Damasceno JL; Natural Products Research Group, Center for Research in Mathematical Sciences and Technology, University of Franca, Franca, SP, Brazil., Mendes SA; Natural Products Research Group, Center for Research in Mathematical Sciences and Technology, University of Franca, Franca, SP, Brazil., Tavares DC; Natural Products Research Group, Center for Research in Mathematical Sciences and Technology, University of Franca, Franca, SP, Brazil., Magalhães LG; Natural Products Research Group, Center for Research in Mathematical Sciences and Technology, University of Franca, Franca, SP, Brazil., Junior PA; Research Center René Rachou, Oswaldo Cruz Foundation, Belo Horizonte, MG, Brazil., Januário AH; Natural Products Research Group, Center for Research in Mathematical Sciences and Technology, University of Franca, Franca, SP, Brazil., Soares MA; Department of Botany and Ecology, Institute of Biosciences, Federal University of Mato Grosso, Cuiabá, MT, Brazil. drmasoares@gmail.com. |
Abstrakt: |
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 (IC 50 ranged 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 IC 50 of 34.4 and 17.4 µM, respectively, while compound 3 afforded IC 50 of 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 IC 50 of 15.3 × 10 3 , 3.4 × 10 3 , and 5.8 × 10 3 µM, 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. |