Search Results (14)

Background/Objectives: Andiroba oil, extracted from Carapa guianensis seeds, possesses therapeutic properties including anti-inflammatory and wound healing effects. This study aimed to develop and characterize a nanoemulsion formulation containing andiroba oil (NeAnd) and to evaluate its cytotoxicity and wound healing potential in vitro. Methods: The oil was evaluated for acidity, antioxidant activity, and fatty acid composition. NeAnd was produced by ultrasonication and characterized using FTIR (Fourier transform infrared spectroscopy), Raman spectroscopy, dynamic light scattering, and transmission electron microscopy. Results: NeAnd exhibited a spherical shape and stable physicochemical properties, with an average hydrodynamic diameter (HD) of 205.7 ± 3.9 nm, a polydispersity index (PdI) of 0.295 ± 0.05, a negative zeta potential of −4.16 ± 0.414 mV, and pH of approximately 6.5. These nanodroplets remained stable for 120 days when stored at 4 °C and maintained their parameters even under pH variations. FTIR and Raman analyses confirmed the presence of functional groups and the organization of fatty acid chains in NeAnd. Cell viability assays revealed no statistically significant differences in cytotoxicity at various concentrations (90–360 µg/mL) after 24 and 48 h. In scratch wound healing assays, NeAnd significantly enhanced wound closure (88.9%) compared to the PBS control (38%) and free andiroba oil (68.6%) in keratinocytes (p < 0.05). Conclusions: These promising findings indicate NeAnd as a potential nanophytomedicine for wound healing and tissue regeneration treatments. Full article

Brown seaweeds of the Fucus genus represent a rich source of natural antiviral products. In this study, a Fucus ceranoides hydroalcoholic extract (FCHE) was found to inhibit 74.2 ± 1.3% of the proteolytic activity of the free SARS-CoV-2 3CL protease (3CLpro), an enzyme that plays a pivotal role in polyprotein processing during coronavirus replication and has been identified as a relevant drug discovery target for SARS- and MERS-CoVs infections. To purify and identify 3CLpro ligands with potential inhibitory activity using a one-step approach, we immobilized the enzyme onto magnetic microbeads (3CLpro-MPs), checked that the enzymatic activity was maintained after grafting, and used this bait for a ligand-fishing strategy followed by a high-resolution mass spectrometry analysis of the fished-out molecules. Proof of concept for the ligand-fishing capacity of the 3CLpro-MPs was demonstrated by doping the FCHE extract with the substrate peptide TSAVLQ-pNA, resulting in the preferential capture of this high-affinity peptide within the macroalgal complex matrix. Ligand fishing in the FCHE alone led to the purification and identification via high-resolution mass spectrometry (HRMS) of seven hepta-, octa-, and decapeptides in an eluate mix that significantly inhibited the free 3CLpro more than the starting FCHE (82.7 ± 2.2% inhibition). Molecular docking simulations of the interaction between each of the seven peptides and the 3CLpro demonstrated a high affinity for the enzyme’s proteolytic active site surpassing that of the most affine peptide ligand identified so far (a co-crystallographic peptide). Testing of the corresponding synthetic peptides demonstrated that four out of seven significantly inhibited the free 3CLpro (from 46.9 ± 6.4 to 76.8 ± 3.6% inhibition at 10 µM). This study is the first report identifying peptides from Fucus ceranoides with high inhibitory activity against the SARS-CoV-2 3CLprotease which bind with high affinity to the protease’s active site. It also confirms the effectiveness of the ligand-fishing strategy for the single-step purification of enzyme inhibitors from complex seaweed matrices. Full article

The high frequency of infectious diseases has spurred research into effective tactics to combat microorganisms that are resistant to several drugs. The overproduction of the transmembrane efflux pump protein NorA, which may export hydrophilic fluoroquinolones, is a common mechanism of resistance in S. aureus strains. This work evaluated the antimicrobial activity of the ethanolic extract from the leaves of Croton heliotropiifolius (EECH) against different bacterial and fungal strains, as well as investigating its modulating effect on the resistance to norfloxacin in a Staphylococcus aureus SA1199B overproducing the NorA efflux pump. Microdilution assays were used to assess the EECH’s antibacterial efficacy. The MIC of norfloxacin or ethidium bromide (EtBr) against the SA1199B strain was determined in the presence or absence of the EECH in order to assess the modifying influence on drug resistance. The EECH showed no activity against the Gram-positive and Gram-negative bacterial strains tested. The EECH also showed no antifungal activity against Candida albicans ATCC 10231. On the other hand, the extract reduced the MIC values for norfloxacin against SA1199B at subinhibitory concentrations. In addition, the EECH also reduced the MIC values of EtBr at subinhibitory concentrations, suggesting the occurrence of phytochemicals that inhibit efflux pumps. Molecular docking showed that retusin, a flavonoid found in the extract, could compete with norfloxacin at the orthosteric site of the NorA, indicating that it could be a potential efflux pump inhibitor. However, isolated retusin did not enhance the activity of norfloxacin or EtBr and it did not inhibit the EtBr efflux, showing that it is not a NorA inhibitor. Even though C. heliotropiifolius is a source of phytochemicals that function as adjuvants for norfloxacin, isolated retusin cannot be used in conjunction with norfloxacin to treat infections brought on by S. aureus that overproduces NorA. Full article

In this study, four Moroccan plants, Halimium antiatlanticum, Adenocarpus artemisiifolius, Pistacia lentiscus and Leonotis nepetifolia, were evaluated for their phytoconstituents and biological activities. Methanolic extracts of these plants were obtained by Soxhlet apparatus, phytochemical screening was performed, and the total phenolic and flavonoid contents were determined. Then, the antioxidant and dermocosmetic activities of the methanolic extracts were evaluated. The obtained results revealed that the leaves and/or aerial parts contained tannins, polyphenols, flavonoids, coumarins, carotenoids, terpenoids and saponins. The higher total phenolic content values were recorded on Pistacia lentiscus and Halimium antiatlanticum with 396.64 ± 30.79 and 304.96 ± 55.61 mgGAE/gDW, respectively. The antioxidant activity was measured by DPPH, ABTS and FRAP assays, and showed that Pistacia lentiscus and Halimium antiatlanticum were the most active extracts, with, respectively, IC50 values of 3.705 ± 0.445 and 5.037 ± 0.122 µg/mL for DPPH. The same results were observed for the FRAP and ABTS assays. Those extracts also showed a strong collagenase inhibitory activity at 200 µg/mL, with 78.51 ± 2.27% for Pistacia lentiscus and 73.10 ± 8.52% for Halimium antiatlanticum. Adenocarpus artemisiifolius showed the highest elastase inhibition rate, with 76.30 ± 5.29%. This study disclosed the dermocosmetic potential of Halimium antiatlanticum and Adenocarpus artemisiifolius, two Moroccan endemic plants that can be traditionally used by local populations or exploited by the cosmetic industry. Full article

For more than 40 years, marine microorganisms have raised great interest because of their major ecological function and their numerous applications for biotechnology and pharmacology. Particularly, Archaea represent a resource of great potential for the identification of new metabolites because of their adaptation to extreme environmental conditions and their original metabolic pathways, allowing the synthesis of unique biomolecules. Studies on archaeal carotenoids are still relatively scarce and only a few works have focused on their industrial scale production and their biotechnological and pharmacological properties, while the societal demand for these bioactive pigments is growing. This article aims to provide a comprehensive review of the current knowledge on carotenoid metabolism in Archaea and the potential applications of these pigments in biotechnology and medicine. After reviewing the ecology and classification of these microorganisms, as well as their unique cellular and biochemical characteristics, this paper highlights the most recent data concerning carotenoid metabolism in Archaea, the biological properties of these pigments, and biotechnological considerations for their production at industrial scale. Full article

Morus nigra L. is a species popularly known in the Northeast of Brazil as “amora miúra”. This species is a source of flavonoids with antioxidant activity. Antioxidants play an important role in the preservation of cosmetic formulations, and they neutralize free radicals. The objective of this study was to develop a topical emulsion containing leaf extract of Morus nigra L., as well as to evaluate the stability, antioxidant and antibacterial activities of the formulations. A crude hydroalcoholic (70%) extract of M. nigra leaves (MnCE) was submitted to high-performance liquid chromatography with diode-array detection (HPLC–DAD) analysis and incorporated into an anionic base emulsion. Antioxidant activity was evaluated according to the DPPH (2,2-diphenyl-1-picrylhydrazyl) method, and the stability of the formulation was assessed for 90 days, submitting the emulsion to storage at 4, 20, and 37 °C. Microdilution techniques evaluated the antibacterial activity and a challenge test assessed the microbiological stability. Analysis by HPLC–DAD identified the flavonoids rutin and isoquercetin in the M. nigra extract. The emulsion and plant extract presented antioxidant activity, and the stability of the emulsion was preserved in terms of pH value and viscosity—which did not show significant changes, except for the spreadability, which was affected by the temperature. The antioxidant activity did not change significantly, except for the sample under 4 °C, which showed a considerable decrease in activity. The crude hydroalcoholic extract and formulation showed antimicrobial activity and the emulsion was considered stable in terms of organoleptic, physicochemical, and microbiological properties. Full article

The argan tree (Argania spinosa (L.) Skeels) is one of the most important floristic resources in Morocco. This Moroccan endemic tree is known for its numerous therapeutic and medicinal uses. In addition to some medicinal and cosmetic uses, argan fruit pulp and press cake are traditionally used by the Berber population for heating and feeding livestock. Molecular docking is an in silico approach that predicts the interaction between a ligand and a protein. This approach is mainly used in chemistry and pharmacology of natural products as a prediction tool with the purpose of selecting plant extracts or fractions for in vitro tests. The aim of this research is to study the evaluation of potential tyrosinase, collagenase, and elastase inhibitory activities of argan fruit press-cake and pulp extracts. Extracts were evaluated for their total phenolic content (TPC), and the major polyphenols of both press-cake and pulp extracts were submitted to molecular docking in order to determine the mechanisms of action of these compounds. Obtained results revealed that fruit pulp had the strongest dermocosmetic activities, as well as the highest TPC, with values above 55 mg gallic-acid equivalent per gram of dry matter (mg_eq AG/g_DM). Moreover, those results were positively correlated with the docking findings, suggesting that the pulp lead compounds have higher affinity with tyrosinase, collagenase, and elastase action sites. The results here presented are very promising and open new perspectives for the exploitation of argan-tree by-products as cosmetic agents towards the development of new anti-aging products. Full article

Croton rhamnifolioides is used in popular medicine for the treatment of inflammatory diseases. The objective of this study was to characterize and evaluate the anti-inflammatory effect of C. rhamnifolioides essential oil complexed in β-cyclodextrin (COEFC). The physicochemical characterization of the complexes was performed using different physical methods. The anti-inflammatory activity was evaluated in vivo by ear edema, paw edema, cotton pellet-induced granuloma, and vascular permeability by Evans blue extravasation. The mechanism of action was validated by molecular docking of the major constituent into the cyclooxygenase-2 (COX-2 enzyme). All doses of the COEFC reduced acute paw edema induced by carrageenan and dextran, as well as vascular permeability. Our results suggest the lowest effective dose of all samples inhibited the response induced by histamine or arachidonic acid as well as the granuloma formation. The complexation process showed that the pharmacological effects were maintained, however, showing similar results using much lower doses. The results demonstrated an involvement of the inhibition of pathways dependent on eicosanoids and histamine. Complexation of β-cyclodextrin/Essential oil (β-CD/EO) may present an important tool in the study of new compounds for the development of anti-inflammatory drugs. Full article

The relevance of oxidative stress in the pathogenesis of several diseases (including inflammatory disorders) has traditionally led to the search for new sources of antioxidant compounds. In this work, we report the selection of fractions with high antioxidant action from B. tetraphylla (BT) leaf extracts. In vitro methods (DPPH and ABTS assays; determination of phenolic and flavonoid contents) were used to select products derived from B. tetraphylla with high antioxidant action. Then, the samples with the highest potentials were evaluated in a model of injury based on the inoculation of a lethal dose of heat-inactivated Escherichia coli in Tenebrio molitor larvae. Due to its higher antioxidant properties, the methanolic extract (BTME) was chosen to be fractionated using Sephadex LH-20 column-based chromatography. Two fractions from BTME (BTFC and BTFD) were the most active fractions. Pre-treatment with these fractions protected larvae of T. molitor from the stress induced by inoculation of heat-inactivated E. coli. Similarly, BTFC and BTFD increased the lifespan of larvae infected with a lethal dose of enteroaggregative E. coli 042. NMR data indicated the presence of aliphatic compounds (terpenes, fatty acids, carbohydrates) and aromatic compounds (phenolic compounds). These findings suggested that products derived from B. tetraphylla leaves are promising candidates for the development of antioxidant and anti-infective agents able to treat oxidative-related dysfunctions. Full article

Anadenanthera colubrina var cebil (Griseb.) Altschul is a medicinal plant found throughout the Brazilian semi-arid area. This work performed a bioguided purification of active substances present in ethyl acetate extract from A. colubrina leaves. The anti-Staphylococcus aureus and antioxidant actions were used as markers of bioactivity. The extract was subjected to flash chromatography resulting in five fractions (F1, F2, F3, F4, and F5). The fractions F2 and F4 presented the highest antimicrobial action, with a dose able to inhibit 50% of bacteria growth (IN50) of 19.53 μg/mL for S. aureus UFPEDA 02; whereas F4 showed higher inhibitory action towards DPPH radical (2,2-diphenyl-1-picryl-hydrazyl-hydrate) [dose able to inhibit 50% of the radical (IC50) = 133 ± 9 μg/mL]. F2 and F4 were then subjected to preparative high-performance liquid chromatography (HPLC) and nuclear magnetic resonance (NMR), resulting in the identification of p-hydroxybenzoic acid and hyperoside as the major compounds in F2 and F4, respectively. Hyperoside and p-hydroxybenzoic acid presented IN50 values of 250 μg/mL and 500 μg/mL against S. aureus UFPEDA 02, respectively. However, the hyperoside had an IN50 of 62.5 μg/mL against S. aureus UFPEDA 705, a clinical isolate with multidrug resistant phenotype. Among the purified compounds, the proanthocyanidins obtained from F2 exhibited the higher antioxidant potentials. Taken together, these results highlight the potential of A. colubrina leaves as an alternative source of biomolecules of interest for the pharmaceutical, food, and cosmetic industries. Full article

Ximenia americana L. (Olacaceae) is used in ethnomedicine as cicatrizant and for the treatment of gastric disorders. This study identified the chemical constituents of the aqueous extract of X. americana (XaAE) and evaluated its antiulcerogenic activity. After lyophilization, XaAE was analyzed by liquid chromatography-mass spectrometry (LC-MS) and its antiulcerogenic effect was evaluated in acute gastric lesions induced by ethanol, acidified ethanol, and indomethacin. Antisecretory action, mucus production and the participation of sulfhydryl groups (–SH) and nitric oxide (NO) were also investigated. The chromatographic analysis identified procyanidins B and C and catechin/epicatechin as major compounds. Oral administration of XaAE (100, 200 and 400 mg/kg) inhibited the gastric lesions induced by ethanol (76.1%, 77.5% and 100%, respectively), acidified ethanol (44.9%, 80.6% and 94.9%, respectively) and indomethacin (56.4%, 52.7% and 64.9%, respectively). XaAE reduced gastric contents and acidity (51.4% and 67.7%, respectively) but did not alter the production of gastric mucus. The reduction of the -SH and NO groups promoted by N-ethylmaleimide (NEM) and Nω-nitro-l-arginine-methyl-ester (L-NAME) respectively, reduced the gastroprotective effect of XaAE. In conclusion, XaAE has gastroprotective activity mediated in part by -SH, NO and antisecretory activity. This antiulcer action was initially correlated to its major constituents, procyanidins B and C and catechin/epicatechin. Full article

Extensive regional droughts are already a major problem on all inhabited continents and severe regional droughts are expected to become an increasing and extended problem in the future. Consequently, extended use of available drought resistant food plants should be encouraged. Bromelia laciniosa, Neoglaziovia variegata and Encholirium spectabile are excellent candidates in that respect because they are established drought resistant edible plants from the semi-arid Caatinga region. From a food safety perspective, increased utilization of these plants would necessitate detailed knowledge about their chemical constituents. However, their chemical compositions have previously not been determined. For the first time, the non-polar constituents of B. laciniosa, N. variegata and E. spectabile have been identified. This is the first thorough report on natural products from N. variegata, E. spectabile, and B. laciniosa. Altogether, 20 non-polar natural products were characterized. The identifications were based on hyphenated gas chromatography-high resolution mass spectrometry (GC-HRMS) and supported by 1D and 2D Nuclear Magnetic Resonance (NMR) plant metabolomics. Full article

Medicinal plants have been widely used in the treatment of chronic pain. In this study, we describe the antinociceptive effect of the essential oil from Croton conduplicatus (the EO 25, 50, and 100 mg/kg, i.p.), a medicinal plant native to Brazil. Antinociceptive activity was investigated by measuring the nociception induced by acetic acid, formalin, hot plate and carrageenan. A docking study was performed with the major constituents of the EO (E-caryophyllene, caryophyllene oxide, and camphor). The EO reduced nociceptive behavior at all doses tested in the acetic acid-induced nociception test (p < 0.05). The same was observed in both phases (neurogenic and inflammatory) of the formalin test. When the hot-plate test was conducted, the EO (50 mg/kg) extended the latency time after 60 min of treatment. The EO also reduced leukocyte migration at all doses, suggesting that its antinociceptive effect involves both central and peripheral mechanisms. Pretreatment with glibenclamide and atropine reversed the antinociceptive effect of the EO on the formalin test, suggesting the involvement of K_ATP channels and muscarinic receptors. The docking study revealed a satisfactory interaction profile between the major components of the EO and the different muscarinic receptor subtypes (M2, M3, and M4). These results corroborate the medicinal use of C. conduplicatus in folk medicine. Full article

Phytochemical investigation of Anaxagorea dolichocarpa Sprague & Sandwith led to isolation of three azaphenanthrene alkaloids: eupolauramine, sampangine and imbiline 1. Their chemical structures were established on the basis of spectroscopic data from IR, HR-ESI-MS, NMR (including 2D experiments) and comparison with the literature. Sampangine and imbiline 1 are being described in the Anaxagorea genus for the first time. Eupolauramine and sampangine show concentration-dependent antitumoral activity in leukemic cells K562 with IC₅₀ of 18.97 and 10.95 µg/mL, respectively. Full article