δ-ALA-D is a metalloenzyme that has 3 vicinal thiol/thiolate groups that coordinate with Zn(II). The proximity between the sulfhydryl groups renders δ-ALA-D extremely sensitive to oxidation by soft electrophiles, such as Pb(II), Hg(II), As(III) and organoseleno and organotellurium compounds. In fact, blood δ-ALA-D is a classical biomarker of lead exposure in humans. The inhibition of δ-ALA-D can increase the concentration of 5-aminolevulinate (δ-ALA), which is a pro-oxidant compound. δ-ALA can generate oxidative stress that can further increase δ-ALA-D inhibition. Recently, data have been obtained indicating that the δ-ALA-D could be a marker of oxidative stress in human pathologies. In summary, considering its high sensitivity to pro-oxidant situations, δ-ALA-D can be considered a universal marker of oxidative stress.

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The oil obtained from the Caryocar coriaceum Wittm. ( pequi) fruit pulp (C. coriaceum fixed oil -CCFO), rich in fatty acids, has been secularly employed by traditional medicine in the treatment of respiratory affections, skin inflammation, and wounds. These observations encouraged us to investigate the antimicrobial activity of CCFO and to investigate its effect in combination with aminoglycosides. The minimum inhibitory concentration (MIC) of CCFO alone and associated with aminoglycosides against Escherichia coli and Staphylococcus aureus strains were determined using microdilution assay. CCFO alone had a MIC of 512 mg/mL against E. coli and S. aureus resistant strains. Combining the CCFO with aminoglycosides reduced the MIC of aminoglycosides against the resistant strains of E. coli and S. aureus. The results obtained indicate that CCFO displays a significant synergistic antibiotic effect when combined with aminoglycosides, demonstrating that the oil constituents (fatty acids) may act as potentiators of the antibiotic activity of aminoglycosides. These properties make CCFO oil an interesting alternative as a remedy or nutraceutical against multiresistant bacteria, preventing the development of resistance by these microorganisms.Practical applications: This article demonstrates the capacity of the C. coriaceum oil to enhance the antibiotic activity of aminoglycosides. This activity could represent a new way to combat the growing bacterial resistance to antibiotics, an important problem of public health.

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Knowledge of medicinal plants is often the only therapeutic resource of many communities and ethnic groups. “Erva-baleeira”, Cordia verbenacea DC., is one of the species of plants currently exploited for the purpose of producing a phytotherapeutic product extracted from its leaves. In Brazil, its major distribution is in the region of the Atlantic Forest and similar vegetation. The crude extract is utilized in popular cultures in the form of hydroalcoholic, decoctions and infusions, mainly as antimicrobial, anti-inflammatory and analgesic agents. The aim of the present study was to establish a chemical and comparative profile of the experimental antibacterial activity and resistance modifying activity with ethnopharmacological reports. Phytochemical prospecting and HPLC analysis of the extract and fractions were in agreement with the literature with regard to the presence of secondary metabolites (tannins and flavonoids). The extract and fraction tested did not show clinically relevant antibacterial activity, but a synergistic effect was observed when combined with antibiotic, potentiating the antibacterial effect of aminoglycosides. We conclude that tests of antibacterial activity and modulating the resistance presented in this work results confirm the ethnobotanical and ethnopharmacological information, serving as a parameter in the search for new alternatives for the treatment of diseases.

Alzheimer's disease (AD) is a progressive and neurodegenerative pathology that can affect people over 65 years of age. It causes several complications, such as behavioral changes, language deficits, depression, and memory impairments. One of the methods used to treat AD is the increase of acetylcholine (ACh) in the brain by using acetylcholinesterase inhibitors (AChEIs). In this study, we used the ZINC databank and the Lipinski's rule of five to perform a virtual screening and a molecular docking (using Auto Dock Vina 1.1.1) aiming to select possible compounds that have quaternary ammonium atom able to inhibit acetylcholinesterase (AChE) activity. The molecules were obtained by screening and further in vitro assays were performed to analyze the most potent inhibitors through the IC50 value and also to describe the interaction models between inhibitors and enzyme by molecular docking. The results showed that compound D inhibited AChE activity from different vertebrate sources and butyrylcholinesterase (BChE) from Equus ferus (EfBChE), with IC50 ranging from 1.69 ± 0.46 to 5.64 ± 2.47 µM. Compound D interacted with the peripheral anionic subsite in both enzymes, blocking substrate entrance to the active site. In contrast, compound C had higher specificity as inhibitor of EfBChE. In conclusion, the screening was effective in finding inhibitors of AChE and BuChE from different organisms.

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