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<Emphasis Type="Italic">In vitro</Emphasis> leishmanicidal,antibacterial and antitumour potential of anhydrocochlioquinone A obtained from the fungus <Emphasis Type="Italic">Cochliobolus</Emphasis> sp.
Authors:Fernanda F Campos  Jonas P Ramos  Djalma M De Oliveira  Tânia M A Alves  Elaine M De Souza-Fagundes  Carlos L Zani  Fábio C Sampaio  Attilio Converti  Betania B Cota
Institution:1.Faculty of Medicine,Federal University of Vales do Jequitinhonha e Mucuri,Diamantina,Brazil;2.Laboratory of Chemistry of Bioactive Natural Products, Centro de Pesquisas René Rachou,Funda??o Oswaldo Cruz,Rio de Janeiro,Brazil;3.Department of Physiology and Biofisics,Federal University of Minas Gerais,Belo Horizonte,Brazil;4.Department of Chemistry,Southwest Bahia State University,Jequié,Brazil;5.Department of Pharmacy,Federal University of Vales do Jequitinhonha e Mucuri,Diamantina,Brazil;6.Department of Civil, Chemical and Environmental Engineering,University of Genova,Genova,Italy
Abstract:The bioassay-guided fractionation of the ethyl acetate extract of the fungus Cochliobolus sp. highlighted leishmanicidal activity and allowed for anhydrocochlioquinone A (ANDC-A) isolation. MS, 1D and 2D NMR spectra of this compound were in agreement with those published in the literature. ANDC-A exhibited leishmanicidal activity with EC50 value of 22.4 µg/mL (44 μM) and, when submitted to the microdilution assay against Gram-positive and Gram-negative bacteria, showed a minimal inhibitory concentration against Staphylococcus aureus ATCC 25295 of 128 μg/mL (248.7 μM). It was also active against five human cancer cell lines, showing IC50 values from 5.4 to 20.3 μM. ANDC-A demonstrated a differential selectivity for HL-60 (SI 5.5) and THP-1 (SI 4.3) cell lines in comparison with Vero cells and was more selective than cisplatin and doxorubicin against MCF-7 cell line in comparison with human peripheral blood mononuclear cells. ANDC-A was able to eradicate clonogenic tumour cells at concentrations of 20 and 50 μM and induced apoptosis in all tumour cell lines at 20 μM. These results suggest that ANDC-A might be used as a biochemical tool in the study of tumour cells biochemistry as well as an anticancer agent with durable effects on tumours.
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