Anti-Trypanosoma cruzi Potential of Vestitol Isolated from Lyophilized Red Propolis.

Chagas disease (CD) is a worldwide public health problem, and the drugs available for its treatment have severe limitations. Red propolis is a natural extract known for its high content of phenolic compounds and for having activity against T. cruzi. The aim of this study was to investigate the trypanocidal potential of red propolis to isolate, identify, and indicate the mode of action of the bioactive compounds. The results revealed that the total phenolic content was 15.4 mg GAE/g, and flavonoids were 7.2 mg QE/g. The extract was fractionated through liquid-liquid partitioning, and the trypanocidal potential of the samples was evaluated using the epimastigote forms of the Y strain of T. cruzi. In this process, one compound was characterized by MS, 1H, and 13C NMR and identified as vestitol. Cytotoxicity was evaluated employing MRC-5 fibroblasts and H9C2 cardiomyocytes, showing cytotoxic concentrations above 15.62 µg/mL and 31.25 µg/mL, respectively. In silico analyses were applied, and the data suggested that the substance had a membrane-permeation-enhancing effect, which was confirmed through an in vitro assay. Finally, a molecular docking analysis revealed a higher affinity of vestitol with farnesyl diphosphate synthase (FPPS). The identified isoflavan appears to be a promising lead compound for further development to treat Chagas disease.

Anti-Inflammatory, Antimicrobial, Antioxidant and Photoprotective Investigation of Red Propolis Extract as Sunscreen Formulation in Polawax Cream.

Many activities have been described for propolis, including, antiviral, antibacterial, antifungal, anti-inflammatory, immunoregulatory, antioxidant and wound healing properties. Recently, propolis has been highlighted due to its potential application in the pharmaceutical and cosmetic industries, motivating a better understanding of its antioxidant and anti-inflammatory activities. Propolis and its main polyphenolic compounds presented high antioxidant activity, and effectiveness as broad spectrum UVB and UVA photoprotection sunscreens. Through a qualitative phytochemical screening, the ethanolic red propolis extracts (EEPV) (70% at room temperature and 70% at a hot temperature) presented a positive result for flavonoids and terpenoids. It presented an antioxidant activity for reducing 50% of DPPH of 17 and 12 µg/mL for extraction at room temperature and at a hot temperature, respectively. The UPLC-QTOF-MS/MS analysis allowed the annotation of 40 substances for EEPV-Heated and 42 substances for EEPV-Room Temperature. The IC50 results of the ABTS scavenging activity was 4.7 µg/mL for both extractions, at room temperature and at a hot temperature. Additionally, we also evaluated the cytotoxic profile of propolis extracts against macrophage (RAW 264.7 cells) and keratinocytes (HaCaT cells), which showed non-cytotoxic doses in cell viability assays even after a long period of exposure. In addition, propolis extracts showed antibacterial activity for Gram-positive bacteria (Staphylococcus aureus and Staphylococcus epidermidis), demonstrating potential biological activity for the creation of formulations aimed at disease control and prevention.

Brazilian essential oils as source for the discovery of new anti-COVID-19 drug: a review guided by in silico study.

The emergence of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in China and its spread worldwide has become one of the biggest health problem due to the lack of knowledge about an effective chemotherapy. Based on the current reality of the SARS-CoV-2 pandemic, this study aimed to make a review literature about potential anti-coronavirus natural compounds guided by an in silico study. In the first step, essential oils from native species found in the Brazilian herbal medicine market and Brazilian species that have already shown antiviral potential were used as source for the literature search and compounds selection. Among these compounds, 184 showed high antiviral potential against rhinovirus or picornavirus by quantitative structure-activity relationship analysis. (E)-α-atlantone; 14-hydroxy-α-muurolene; allo-aromadendrene epoxide; amorpha-4,9-dien-2-ol; aristochene; azulenol; germacrene A; guaia-6,9-diene; hedycaryol; humulene epoxide II; α-amorphene; α-cadinene; α-calacorene and α-muurolene showed by a molecular docking study the best result for four target proteins that are essential for SARS-CoV-2 lifecycle. In addition, other parameters obtained for the selected compounds indicated low toxicity and showed good probability to achieve cell permeability and be used as a drug. These results guided the second literature search which included other species in addition to native Brazilian plants. The majority presence of any of these compounds was reported for essential oils from 45 species. In view of the few studies relating essential oils and antiviral activity, this review is important for future assays against the new coronavirus. SUPPLEMENTARY INFORMATION: The online version contains supplementary material available at 10.1007/s11101-021-09754-4.

Herbal medicines to the treatment of skin and soft tissue infections: advantages of the multi-targets action.

The research for new treatments of skin and soft tissue infections (SSTIs) is important due to their high prevalence and number of hospitalizations. The purpose of this review is to address the pathophysiology of SSTIs to highlight the advantages of herbal medicines to their treatment, showing examples of species and compounds with multi-targets action. SSTIs have a complex physiopathology involving the microorganism, as well as inflammation and difficult healing. Therefore, antimicrobial, anti-inflammatory, antioxidant and healing activities are an approach possible for their treatment. Herbal medicines have a wide diversity of biological compounds, mainly phenolic compounds that may act on different targets and also have synergism between them. Therefore, a single medicine may have the four key activities that allied allow eliminating the infection, control the inflammation process and accelerating the healing process, preventing complications with chronic infections.

Antibacterial substances from leaves of Protium spruceanum (Burseraceae): in vitro and in silico evaluation

Due to the increase of bacterial resistance, the search for new antibiotics is necessary and the medicinal plants represent its most important source. The aim of this study was to evaluate the antibacterial property of extract and fractions from Protium spruceanum leaves, against pathogenic bacteria. By means of diffusion and microdilution assays, the crude extract was active against the nine bacteria tested being the hydromethanolic fraction the most active. During phytochemical procedures, procyanidin (1) and catechin (2) were identified as the main antibacterial constituents of this fraction. In silico results obtained using PASSonline tool indicated 1 and 2 as having good potential to interact with different targets of currently used antibiotics. These results no indicated potential to none DNA effect and indicated the cell wall as mainly target. Electrophoresis result supported that had no DNA damage. Cell wall damage was confirmed by propidium iodide test that showed increased membrane permeability and by cell surface deformations observed in scanning electronic microscopy. The in vitro assays together with the in silico prediction results establish the potential of P. spruceanum as source of antibacterial compounds that acts on important bacterial targets. These results contribute to the development of natural substances against pathogenic bacteria and to discovery of new antibiotics.

Anti-inflammatory activity of Protium spruceanum (Benth.) Engler is associated to immunomodulation and enzymes inhibition.

ETHNOPHARMACOLOGICAL RELEVANCE: Protium spruceanum (Burseraceae) is used in Brazilian traditional medicine as anti-inflammatory, but the factors involved in this activity were not yet characterized. AIMS OF THE STUDY: analyze the aspects involved in the anti-inflammatory activity of polar fractions obtained from extracts of leaves and branches. MATERIALS AND METHODS: Hydromethanolic fraction was obtained by liquid-liquid partition from crude ethanolic extract and its compounds were identified by LC-DAD-MS. Activity tests were performed using LPS + IFN-γ stimulated J774A.1 macrophages. Cytokines were evaluated by CBA kit, NO by Griess method, ROS by DCFH-DA, N-acetylglucosaminidase (NAG) activity by spectrophotometric method, matrix-metalloproteinase (MMP-9) activity by zymography, inducible nitric oxide synthase (iNOS) expression by immunofluorescence and cyclooxygenase (COX-2) expression by Western blot. RESULTS: Fractions induced an increase of IL-6 and IL-10 which leads to the control of pro-inflammatory cytokines levels. The treatment with the fractions also reduced NO production at all concentrations tested in all evaluated periods. ROS production by the macrophages was inhibited by the treatment and the leaves fraction showed the best results with a lower concentration than that observed for the branches. The enzymes assays showed that leaves fraction inhibited NAG and MMP-9 activities, as well as, iNOS and COX-2 expression. These activities can be associated with the presence of procyanidin, catechin, rutin, quercitrin, isoquercitrin and kaempferol-3-O-rhamnoside, major compounds that were identified in the fraction. CONCLUSIONS: Anti-inflammatory activity of P. spruceanum is associated to an immunomodulatory effect that leads to inhibition of ROS, NO, NAG, MMP-9, COX-2 and iNOS.

Antibacterial activity of extract and fractions from branches of Protium spruceanum and cytotoxicity on fibroblasts.

The crude ethanol extract (CEE) and fractions from branches of Protium spruceanum were subjected to antibacterial and cytotoxicity assays. Compounds of the most active fraction were identified by GC-MS and LC-MS. CEE was active against 19 bacteria and the ethyl acetate fraction (EAF) showed the lowest minimum bactericidal concentration (MBC 0.3-80.0 mg/mL). Through time-kill assay was observed that EAF induced rapid bactericidal effect against Staphylococcus saprophyticus. The cytotoxicity tests against L929 fibroblasts showed great potential of EAF on the treatment of infections caused by five bacteria (MBC < IC50). The results provide in vitro scientific support to the possible application of branches of P. spruceanum as antimicrobial agent that may contribute for treatment of infections.