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In recent years, natural products with biological activities have been increasingly researched. The elucidation of phytoconstituents is necessary for the development of drugs as a natural alternative for the treatment of various diseases. The work aimed to evaluate in vitro and in silico bioactivities of hexane (CCHE) and methanol (CCME) fractions of ethanolic extract from Centrosema coriaceum Benth (Fabaceae) leaves and elucidate their phytoconstituents. CCHE and CCME showed antifungal activity for Candida glabrata (MIC of 1000 μg/mL) with fungistatic effect and action in cell envelope by sorbitol and ergosterol assays. CCHE and CCME presented promising antioxidant activity against the DPPH radical with IC 50 of 13.61 � 0.50 and 6.31 � 0.40 μg/mL, respectively, and relative antioxidant activity (RAA%) of 45.77 � 3.61/ 28.53 � 2.25 % for CCHE and 82.18 � 2.25/ 51.99 � 3.23 % for CCME when compared to rutin and quercetin, respectively. Moreover, these fractions demonstrated promising results for the inhibition of lipid peroxidation by β-carotene/linoleic acid assay. For antiinflammatory and cytotoxicity activities, CCHE and CCME significantly inhibited the production of nitric oxide and TNF-α, without toxicity on murine intraperitoneal macrophages, respectively. Esters, alkanes, steroids, tocopherols, and terpenes were identified in CCHE by GC/MS. Flavonoids, phenolic acids, and disaccharides were detected in CCME by UFLC-QTOF-MS and FACE. Furthermore, rutin was purified from CCME. In silico predictions evidenced that compounds present in both fractions have high affinity to the fungal membrane besides antioxidant and anti-inflammatory activities. Based on these observations, CCHE and CCME have a noteworthy potential for the design of novel antifungal and anti-inflammatory agents that should be explored in future studies.

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O presente estudo teve como objetivo extrair e avaliar o potencial antimicrobiano e citotóxico de frações ricas em alcaloides obtidas a partir das partes aéreas de Mitracarpus frigidus. O isolamento de alcaloides foi realizado por meio de extração ácido-base e cromatografia em coluna com Sephadex LH-20 como fase estacionária. A atividade antimicrobiana foi avaliada pelo método de microdiluição em caldo para determinação da concentração inibitório mínima (CIM) e também por parâmetros quantitativos antimicrobianos (atividade total, percentual de atividade e índice de susceptibilidade microbiano) contra nove linhagens de microrganismos: Staphylococcus aureus, Pseudomonas aeruginosa, Salmonella typhimurium, Shigella sonnei, Klebsiella pneumoniae, Escherichia coli, Bacillus cereus, Candida albicans e Cryptococcus neoformans. A citotoxicidade foi testada frente a Artemia salina e duas linhagens de células leucêmicas, HL60 e Jurkart. A fração mais rica em alcaloides apresentou atividade expressiva para S. aureus, S. typhimurium, B. cereus, P. aeruginosa, S. sonnei e C. neoforman com CIM abaixo de 0,100 mg/mL. As amostras não apresentaram efeito citotóxico frente a A. salina e em relação as linhagens de células tumorais, somente as frações mais ricas em alcaloides apresentaram uma moderada atividade com cerca 50 e 35% de diminuição da viabilidade celular para HL60 e Jurkart, respectivamente. Os resultados apresentados abrem perspectivas para o futuro isolamento, purificação e identificação de substâncias bioativas de M. frigidus que possam ser utilizadas, principalmente no tratamento de infecções microbianas.

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Objectives This study aimed to evaluate the potential of aqueous extract from Mitracarpus frigidus aerial parts (MFAq) in the treatment of inflammation and oxidative stress, as well as to characterize its chemical constituents. Methods Total phenolic and flavonoid contents were determined, and phytoconstituents were detected by ultra-fast liquid chromatography/quadrupole-time-of-flight tandem mass spectrometry (UFLC-QTOF-MS). The antioxidant activity was evaluated by DPPH, TAC and β-carotene/linoleic acid assays. In-vitro anti-inflammatory activity, cell viability and cell cycle were performed in J774A.1 cell line. In-vivo anti-inflammatory activity was investigated by two ear oedema assays (croton oil and phenol). Key findings Chlorogenic acid, clarinoside, quercetin-hexosylpentoside, rutin, kaempferol-3-O-rutinoside, kaempferol-rhamnosylhexoside, quercetin-pentosylrhamnosylhexoside, harounoside, 2-azaanthraquinone and sucrose were identified by UFLC-QTOF-MS. MFAq showed antioxidant activity, which was positively correlated to the content of phenolic compounds. MFAq significantly inhibited the production of nitric oxide, did not decrease viability in MTT assay (all concentrations) and showed no changes in membrane permeability and cell cycle of J774A.1 cell line. Furthermore, MFAq showed a reduction in ear oedema in all tested doses. Conclusion MFAq was effective in some antioxidant and inflammatory parameters, in the experimental conditions that were used in the study. This is the first report of chemical composition and bioactivities from this extract.