Objectives This work aimed to evaluate the antifungal and cytotoxic activity of the EtOH extract and fractions of Banisteriopsis argyrophylla leaves, and to perform the identification of these bioactive metabolites. Methods The EtOAc fraction (EAF) obtained from the ethanolic extract of B. argyrophylla leaves showed better antifungal potential against Candida spp. In this fraction, ten flavonoids have been identified by UHPLC‐ESI‐MSn. Then, EAF was submitted to column chromatography to give four new fractions (A1–A4). The cytotoxicity was determined against Vero cells. Key findings The EAF showed better antifungal potential against Candida spp. with minimum inhibitory concentrations (MICs) between 31.25 and 93.75 μg/ml. The (–)‐catechin (fraction A1) showed a MIC of 2.83 μg/ml against Candida glabrata. Fractions A2, A3 and A4 were rich in quercetins and kaempferols and showed good inhibitory concentrations (5.86–46.87 μg/ml) against C. albicans, C. glabrata and C. tropicalis. Conclusions The EtOH extract, fractions and the isolated (–)‐catechin showed lower toxicity to Vero cells than cisplatin, used as a positive control. Thus, the leaves of B. argyrophylla are a promising source of antifungal agents.
Scheelea phalerata Mart. ex Spreng (Arecaceae) is a palm tree found in the Brazilian cerrado. There are no topics related to volatile oils from S. phalerata leaves in the literature. This work determines its chemical composition and evaluates the biological activity under two different seasonal conditions (dry and rainy seasons). The dry essential oil yield was 0.034 ± 0.001% and the rainy essential oil yield was 0.011 ± 0.003%. Both essential oils presented different qualitative and quantitative compositions (99.4 and 98.5%). The main constituents of the dry essential oil were phytol (36.7%), nonadecane (9.7%), linolenic acid (9.1%), (Z)-hex-3-en-1-ol (4.2%), and squalene (4.0%). The main constituents of the rainy essential oil were phytol (26.1%), palmitic acid (18.7%), hexan-1-ol (15.6%), (Z)-hex-3-en-1-ol (9.7%), and oleic acid (4.0%). The antileishmanial activity against promastigotes of Leishmania amazonensis was observed only for the rainy season essential oil (IC 50 value of 165.05 ± 33.26 μg mL −1 ). A molecular docking study showed that alcohols exert a paramount efficacy and that the action of some essential oil compounds may be similar to that of amphotericin B. Still, only the essential oil from the dry season showed moderate antibacterial activity against S. sanguinis (MICs 200−400 μg mL −1 ). The cytotoxicity against Vero cells was identical (>512) for both essential oils. The novel data here for both chemical characterization and biological activity, in particular, evidence that the action of these compounds is similar to that of amphotericin B, provide valuable information to the drug-discovery field.
Hemopressin is a nonapeptide derived from the α-1 chain of mammalian hemoglobin known for its hypotensive, analgesic and appetite suppressive effects. This peptide acts as a CB1 cannabinoid receptor inverse agonist or antagonist. Dysfunctions in the endocannabinoid system are associated with some pathologies and morbidity, such as obesity, neuropathic pain, depression, inflammation, Alzheimer and Parkinson diseases.This study was focused on the production and purification of synthetic and recombinant hemopressin, aiming future evaluation of their biological properties. To obtain the recombinant peptide, the nucleotide sequence encoding hemopressin was inserted into the expression vector pGEX-4T-1 (GE Healthcare) fused to the tag-GST and expressed in Escherichia coli BL21-CodonPlus. Several expression conditions were tested to determine the best expression parameters. Solid-phase synthesis of human and murine hemopressin was performed using the Fmoc/t-butyl strategy. The amino acid sequences of both forms of hemopressin was confirmed by MALDI mass spectrometry in the LIFT TM mode at an Autoflex speed equipment (BrukerDaltonics, Bilerica, USA).Purification of the synthetic peptide was performed by reversed-phase chromatography (Shimadzu LC-20AT) on a C18 semi-preparative column (Jupiter 5 µm 300 Å). Mass spectrometric analysis of human and murine hemopressins showed synthetic peptides with a molecular mass of 1,053.6 Da and 1,087.6 Da, respectively. The molecular mass of murine recombinant hemopressin fused to GST was approximately 31 kDa, a value that was obtained by SDS-PAGE analysis and confirmed by Western Blotting. The expression yield was evaluated by densitometry, which showed an equivalent expression yield of 147,8 mg/L of the recombinant protein.
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