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Despite intensified efforts to develop an effective antibiotic, S. aureus is still a major cause of mortality and morbidity worldwide. The multidrug resistance of bacteria has considerably increased the difficulties of scientific research and the concomitant emergence of resistance is to be expected. In this study we have investigated the in vitro activity of 15 ethanol extracts prepared from Moroccan medicinal plants traditionally used for treatment of skin infections. Among the tested species I. viscosa, C. oxyacantha, R. tinctorum, A. herba alba, and B. hispanica showed moderate anti-staphylococcal activity. However, R. alaternus showed promising growth-inhibitory effects against specific pathogenic bacteria especially methicillin-susceptible Staphylococcus aureus Panton-Valentine leucocidin positive (MSSA-PVL) and methicillin-resistant S. aureus (MRSA). The bioguided fractionation of this plant using successive chromatographic separations followed by nuclear magnetic resonance (NMR) and mass spectrometry (MS) including EIMS and HREIMS analysis yielded the emodin (1) and kaempferol (2). Emodin being the most active with MICs ranging between 15.62 and 1.95 µg/mL and showing higher activity against the tested strains in comparison with the crude extract, its mechanism of action and the structure-activity relationship were interestingly discussed. The active compound has not displayed toxicity toward murine macrophage cells. The results obtained in the current study support the traditional uses of R. alaternus and suggest that this species could be a good source for the development of new anti-staphylococcal agents.
Assuntos
Antibacterianos , Staphylococcus aureus Resistente à Meticilina/crescimento & desenvolvimento , Compostos Fitoquímicos , Rhamnus/química , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Toxinas Bacterianas , Exotoxinas , Leucocidinas , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologiaRESUMO
Vitamin D (VD) production-based microalgae biosynthesis presents various benefits including sustainability, fast expansion, and the capacity to generate substantial quantities. However, this approach suffers from serious challenges that require effective cultivation methods and extraction processes. Indeed, further researches are of significant interest to understand the biosynthesis pathways, enhance the processes, and ensure its viability. In this context, the present review focuses on an in-depth understanding of the chemistry of VD and its analogues and provides a comprehensive explanation of the biosynthesis pathways, precursors, and production methods. In addition, this work discusses the state of the art reflecting the recent advances researches and the global market of microalgae as a potential source of VD. In sum, this paper demonstrates that microalgae can efficiently biosynthesize various forms of VD, presenting a sustainable alternative for VD production.
Assuntos
Metaboloma , Microalgas , Vitamina D , Microalgas/metabolismo , Vitamina D/metabolismo , Vitamina D/biossíntese , Biotecnologia/métodosRESUMO
American cutaneous leishmaniasis is a disease caused by protozoa of the genus Leishmania. Currently, meglumine antimoniate is the first-choice treatment for the disease. The limited efficacy and high toxicity of the drug results in the necessity to search for new active principles. Nanotechnology is gaining importance in the field, since it can provide better efficacy and lower toxicity of the drugs. The present study aimed to synthesize, characterize, and evaluate the in vitro leishmanicidal and antileukemic activity of bismuth nanoparticles (BiNPs). Promastigotes and amastigotes of L. (V.) guyanensis and L. (L.) amazonensis were exposed to BiNPs. The efficacy of the nanoparticles was determined by measurement of the parasite viability and the percentage of infected cells, while the cytotoxicity was characterized by the colorimetry. BiNPs did not induce cytotoxicity in murine peritoneal macrophages and showed better efficacy in inhibiting promastigotes (IC50 < 0.46 nM) and amastigotes of L. (L.) amazonensis. This is the first report on the leishmanicidal activity of Bi-based materials against L. (V.) guayanensis. BiNPs demonstrated significant cytotoxic activity against K562 and HL60 cells at all evaluated concentrations. While the nanoparticles also showed some cytotoxicity towards non-cancerous Vero cells, the effect was much lower compared to that on cancer cells. Treatment with BiNPs also had a significant effect on inhibiting and reducing colony formation in HL60 cells. These results indicate that bismuth nanoparticles have the potential for an inhibitory effect on the clonal expansion of cancer cells.
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Nowadays, the combination of molecules influences their biological effects, and interesting outcomes can be obtained from different component interactions. Using a mixture design method, this research seeks to simulate the efficacy of essential oil combinations against various bacteria and forecast the ideal combination. The chemical compositions of Myrtus communis, Artemisia herba-alba and Thymus serpyllum essential oils were analyzed using CG/MS. Then, the combined antibacterial effects were evaluated by testing mixture design formulations using the microdilution bioassay. The main compounds detected for M. communis essential oil were myrtenyl acetate (33.67%), linalool (19.77%) and 1,8-cineole (10.65%). A. herba-alba had piperitone as a chemotype, representing 85%. By contrast, the T. serpyllum oil contained thymol (17.29%), γ-terpinene (18.31%) and p-cymene (36.15%). The antibacterial effect of the essential oils studied, and the optimum mixtures obtained were target strain-dependent. T. serpyllum alone ensured the optimal inhibition against S. aureus and E. coli, while a ternary mixture consisting of 17.1%, 39.6% and 43.1% of M. communis, A. herba-alba and T. serpyllum respectively, was associated with optimal inhibitory activity against B. subtilis. The outcome of this research supports the idea of the boosting effect of essential oil combinations toward better activities, giving better understanding of the usefulness of mixture designs for food, cosmetics, and pharmaceutical applications.
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Natural compounds are endowed with a broad spectrum of biological activities, including protection against Toxins. Most of them are known for their antioxidant and radical scavenging activities. However, the synergistic combination of these natural molecules is not well studied. Therefore, the present study aims first to investigate the effect of four potent natural molecules [rosmarinic acid (Ros-A), ellagic acid (Ella-A), curcumin (Cur), and syringic acid (Syr-A)] on H2O2 -induced cell cytotoxicity and oxidative stress on the human monocytes (THP-1) and then to evaluate their combined action effect. Optimal combinations of these molecules were predicted using an augmented mixture design approach. In the first, as preliminary antioxidant activities screening, two in vitro assays were adopted to assess the single radicals scavenging activity of these natural compounds, DPPH⢠and ABTS⢠+ tests. Based on the results obtained, the multitude of optimal formulas proposed by the mixture design study led to choosing four potent compositions (comp) in addition to ellagic acid, proposed as the most efficient when applied alone. The different molecules and mixtures were used to assess their cytoprotective effect on THP-1 cells in the presence and absence of H2O2. The most potent Comp-4, as well as the molecules forming this mixture, were exploited in a second experiment, aiming to understand the effect on oxidative stress via antioxidant enzyme activities analysis in the H2O2-induced oxidative stress in the THP-1 cell line. Interestingly, the natural molecules used for THP-1 cells treatment exhibited a significant increase in the antioxidant defense and glyoxalase system as well as suppression of ROS generation evaluated as MDA content. These results indicate that the natural compounds tested here, especially the synergistic effect of Cur and Ros-A (Comp-4), could serve as cytoprotective and immunostimulant agents against H2O2-induced cytotoxicity THP-1 cells, which makes them interesting for further investigations on the molecular mechanisms in preclinical animal models.
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Several studies have demonstrated the possible synergistic effect as an effective strategy to boost the bioactivity of essential oils. Using this framework, this study was conducted to effectively establish the ideal combination of six essential oils from different plants (Origanum compactum, Origanum majorana, Thymus serpyllum, Mentha spicata, Myrtus communis, and Artemisia herba-alba) that would express the best antioxidant activity. Each mixture was optimized using a mixture design approach to generate the most effective blend. The 2,2-diphenyl-1-picrylhydrazyl radical scavenging method was used as a reference method to assess the antioxidant activity. Each essential oil's composition was identified using the GC/MS method. The single essential oil activities demonstrated variable antioxidant effects, and following the mixture design approach, the optimal antioxidant blend was revealed, as two mixtures demonstrated the best antiradical activity with 79.46% obtained with the mixture of O. majorana (28%) and M. spicata (71%) and 78.8% obtained with the mixture O. compactum (64%), O. majorana (13%), and T. serpyllum (21%). This study proposes a practical way to elaborate mixtures in the search for a boosting effect that can be oriented for the food or pharmaceutical industry.
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In this work, the chemical composition, the antioxidant, and the antibacterial activities of two Moroccan essential oils less studied, extracted from Pelargonium asperum and Ormenis mixta, were investigated. According to the gas chromatography coupled to mass spectrometry analysis, citronellol (25.07%), citronellyl ester (10.52%), geraniol (10.46%), and buthyl anthranilate (5.93%) were found to be the major components of P. asperum, while O. mixta was mainly composed of D-germacrene (11.46%), 1,8-cineole (10.28%), and cis-methyl isoeugenol (9.04%). Moreover, O. mixta essential oil exhibited an important antioxidant activity being significantly higher than that exhibited by P. asperum oil (P < 0.001). As regards the antimicrobial activity of both essential oils, the zones of growth inhibition and the minimum inhibitory concentration values showed that P. asperum essential oil was more active than that of O. mixta. Thereafter, the impact of the binary combination of essential oils on their antimicrobial effect was investigated against Staphylococcus aureus using the fractional inhibitory concentration index calculation. The results showed a promising synergistic antibacterial interaction between essential oils studied.
Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Asteraceae , Óleos Voláteis/farmacologia , Pelargonium , Antibacterianos/química , Antioxidantes/química , Cromatografia Gasosa-Espectrometria de Massas , Testes de Sensibilidade Microbiana , Óleos Voláteis/química , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/crescimento & desenvolvimentoRESUMO
Phytopharmaceuticals play an essential role in medicine, since the need to investigate highly effective and safe drugs for the treatment of diabetes mellitus disease remains a significant challenge for modern medicine. Arbutus unedo L. root has various therapeutic properties, and has been used widely in the traditional medicine as an antidiabetic agent. The current study aimed to isolate the pharmacologically active compound from A. unedo roots using accelerated solvent extraction technology, to determine its chemical structure using different instrumental analytical methods, and also to evaluate the α-glucosidase inhibitory activity. The roots of A. unedo were exhaustively extracted by high-pressure static extraction using the Zippertex® technology (Dionex-ASE, Paris, France), and the extract was mixed with XAD-16 resin to reach quantifiable amounts of active compounds which were identified by high-pressure liquid chromatography (HPLC), ¹H NMR (300 MHz), and 13C NMR. The antidiabetic activity of the isolated compound was evaluated using the α-glucosidase inhibitory assay. The active compound was isolated, and its structure was identified as catechin using instrumental analysis.The results revealed that the isolated compound has potential α-glucosidase inhibitory activity with an IC50 value of 87.55 ± 2.23 µg/mL greater than acarbose. This was used as a positive control, which has an IC50 value of 199.53 ± 1.12 µg/mL. According to the results achieved, the roots of A. unedo were considered the best source of catechin and the Zippertex® technology method of extraction is the best method for isolation of this therapeutic active compound. In addition, the α-glucosidase inhibitory activity results confirmed the traditional use of A. unedo roots as an antidiabetic agent. Future clinical trials and investigations of antidiabetic and other pharmacological effects such as anticancer are required.
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Biofilm formation on dental biomaterials is implicated in various oral health problems. Thus the challenge is to prevent the formation of this consortium of microorganisms using a safe approach such as antimicrobial and anti-adhesive natural products. Indeed, in the present study, the effects of an antifungal extract of Bacillus sp., isolated from plant rhizosphere, on the surface physicochemical properties of cobalt and nickel based dental alloys were studied using the contact angle measurements. Furthermore, in order to predict the adhesion of Candida albicans to the treated and untreated dental alloys, the total free energy of adhesion was calculated based on the extended Derjaguin-Landau-Verwey-Overbeek approach. Results showed hydrophobic and weak electron-donor and electron-acceptor characteristics of both untreated dental alloys. After treatment with the antifungal extract, the surface free energy of both dental alloys was influenced significantly, mostly for cobalt based alloy. In fact, treated cobalt based alloy became hydrophilic and predominantly electron donating. Those effects were time-dependent. Consequently, the total free energy of adhesion of C. albicans to this alloy became unfavorable after treatment with the investigated microbial extract. A linear relationship between the electron-donor property and the total free energy of adhesion has been found for both dental alloys. Also, a linear relationship has been found between this latter and the hydrophobicity for the cobalt based alloy. However, the exposure of nickel based alloy to the antifungal extract failed to produce the same effect.