RESUMO
Tetraclinis articulata (Vahl) Mast. is native to the Mediterranean area and belongs to Cupressaceae family. The aim of this study were: i) to determine the chemical composition of essential oils (EOs) of T. articulata obtained from its stems, leaves, and cones using GC coupled to GC/MS; II) to evaluate their antioxidant activity using non enzymatic (DPPH, ABTS and FRAP) and enzymatic methods (catalase activity); III) to evaluated their anti-enzymatic activity on enzyme involved in metabolism and Central Nervous System using spectrophotometric assays. α-Pinene, limonene, and bornyl acetate were the main components of the three EOs. Moreover, the EO from cones showed the best antioxidant activity and was also to increase of catalase activity. All EOs were active against α-amylase in similar way; the EO leaves was more active against α-glucosidase and the EO from cones was more active against cholinesterase. The EOs demonstrated significant inhibition of the mature biofilm of Gram-negative and Gram-positive strains. This highlight the potential uses of T. articulata EOs in the fields of health and agriculture.
RESUMO
The aim of the current study was to compare some biological activities of edible oils enriched with 10 % of cannabidiol (CBD samples) from the Slovak market. In addition, hemp, coconut, argan, and pumpkin pure oils were also examined. The study evaluated the fatty acids content, as well as antibacterial, antifungal, antioxidant, cytotoxic, and phytotoxic activities. The CBD samples presented antimicrobial activity against the tested bacterial strains at higher concentrations (10000 and 5000â mg/L) and antifungal activity against Alternaria alternata, Penicillium italicum and Aspergillus flavus. DPPHâ and FRAP assays showed greater activity in CBD-supplemented samples compared to pure oils and vitamin E. In cell lines (IPEC-J2 and Caco-2), a reduced cell proliferation and viability were observed after 24â hours of incubation with CBD samples. The oils showed pro-germinative effects. The tested activities were linked to the presence of CBD in the oils.
Assuntos
Antioxidantes , Canabidiol , Proliferação de Células , Canabidiol/farmacologia , Canabidiol/química , Humanos , Proliferação de Células/efeitos dos fármacos , Antioxidantes/farmacologia , Antioxidantes/química , Testes de Sensibilidade Microbiana , Células CACO-2 , Sobrevivência Celular/efeitos dos fármacos , Antibacterianos/farmacologia , Antibacterianos/química , Óleos de Plantas/farmacologia , Óleos de Plantas/química , Antifúngicos/farmacologia , Antifúngicos/química , Penicillium/efeitos dos fármacos , Alternaria/efeitos dos fármacos , Aspergillus flavus/efeitos dos fármacosRESUMO
Entanglement of two umbilical cords in a MCMA twin pregnancy.
Assuntos
Pacientes Internados , Gravidez de Gêmeos , Gravidez , Feminino , Humanos , Pacientes Ambulatoriais , Gêmeos Monozigóticos , Cordão UmbilicalRESUMO
Several researchers have demonstrated the health and pharmacological properties of carvacrol and p-cymene, monoterpenes of aromatic plants. This study investigated these compounds' possible anti-cholinesterase, anti-α-amylase, and neuroprotective effects. We evaluated the anti-acetylcholinesterase and anti-α-amylase activities at different concentrations of the compounds. The maximum non-toxic dose of carvacrol and p-cymene against SH-SY5Y neuroblastoma cells was determined using an MTT assay. The neuroprotective effects of the compounds were evaluated on H2O2-induced stress in SH-SY5Y cells, studying the expression of caspase-3 using Western blotting assays. Carvacrol showed inhibitory activities against acetylcholinesterase (IC50 = 3.8 µg/mL) and butyrylcholinesterase (IC50 = 32.7 µg/mL). Instead, the anti-α-amylase activity of carvacrol resulted in an IC50 value of 171.2 µg/mL After a pre-treatment with the maximum non-toxic dose of carvacrol and p-cymene, the expression of caspase-3 was reduced compared to cells treated with H2O2 alone. Carvacrol and p-cymene showed in vitro anti-enzymatic properties, and may act as neuroprotective agents against oxidative stress. Further studies are necessary to elucidate their possible use as coadjutants in preventing and treating AD in diabetic patients.
Assuntos
Neuroblastoma , Fármacos Neuroprotetores , Humanos , Acetilcolinesterase/metabolismo , Amilases/metabolismo , Butirilcolinesterase/metabolismo , Caspase 3/metabolismo , Linhagem Celular Tumoral , Inibidores da Colinesterase/farmacologia , Peróxido de Hidrogênio/toxicidade , Neuroblastoma/tratamento farmacológico , Fármacos Neuroprotetores/farmacologia , Estresse Oxidativo , alfa-Amilases/antagonistas & inibidores , ColinesterasesRESUMO
This study was conducted to examine the chemical composition of the essential oils (EOs) from six Tunisian Eucalyptus species and to evaluate their anti-enzymatic and antibiofilm activities. The EOs were obtained through hydro-distillation of dried leaves and subsequently analyzed using GC/MS. The main class of compounds was constituted by oxygenated monoterpenes, particularly prominent in E. brevifolia (75.7%), E. lehmannii (72.8%), and E. woollsiana (67%). Anti-enzymatic activities against cholinesterases, α-amylase, and α-glucosidase were evaluated using spectrophotometric methods. Notably, the E. brevifolia, E. extensa, E. leptophylla, E. patellaris, and E. woollsiana EOs displayed potent acetylcholinesterase (AChE) inhibition (IC50: 0.25-0.60 mg/mL), with E. lehmannii exhibiting lower activity (IC50: 1.2 mg/mL). E. leptophylla and E. brevifolia showed remarkable α-amylase inhibition (IC50: 0.88 mg/mL), while E. brevifolia and E. leptophylla significantly hindered α-glucosidase (IC50 < 30 mg/mL), distinguishing them from other EOs with limited effects. Additionally, the EOs were assessed for their anti-biofilm properties of Gram-positive (Staphylococcus aureus and Listeria monocytogenes) and Gram-negative (Acinetobacter baumannii, Pseudomonas aeruginosa and Escherichia coli) bacterial strains. The E. extensa EO demonstrated the main antibiofilm effect against E. coli and L. monocytogenes with an inhibition > 80% at 10 mg/mL. These findings could represent a basis for possible further use of Eucalyptus EOs in the treatment of human microbial infections and/or as a coadjutant in preventing and treating Alzheimer's disease and/or diabetes mellitus.
Assuntos
Eucalyptus , Óleos Voláteis , Humanos , Eucalyptus/química , Escherichia coli , Tunísia , Acetilcolinesterase/farmacologia , alfa-Glucosidases/farmacologia , Antibacterianos/farmacologia , Antibacterianos/química , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Óleo de Eucalipto/farmacologia , alfa-Amilases , Testes de Sensibilidade MicrobianaRESUMO
Several foods are used in both the nutraceutical and health sectors; vegetable oils, for example, can prevent the onset of numerous diseases. The properties of these oils are related to their chemical composition and primarily to the presence of fatty acids. The present work aimed to determine the chemical profiles of Argania spinosa, Pinus halepensis, and Pistacia altantica oils, used in traditional Tunisian foods, and to evaluate some biological properties. We evaluated their antioxidant, anti-enzymatic, antimicrobial, and anti-inflammatory properties. Linoleic acid was the main component of the three oils. P. atlantica oil showed more significant inhibitory activity against the enzymes studied than A. spinosa and P. halepensis. All three oils showed similar antioxidant and anti-inflammatory activity. Furthermore, A. spinosa and P. halepensis oils showed antibiofilm activity against P. aeruginosa, with 30-40% inhibition. These results focus on the possible use of these oils in the nutraceutical and healthcare sectors.
Assuntos
Pinus , Pistacia , Sapotaceae , Óleos de Plantas/farmacologia , Ácidos Graxos/farmacologia , Tunísia , Antioxidantes/farmacologia , Suplementos Nutricionais , Pseudomonas aeruginosa , Anti-InflamatóriosRESUMO
Plants with medicinal benefits are a crucial source of compounds for developing drugs. This study was designed to determine the chemical composition, antibacterial, antibiofilm, antioxidant, and anti-enzymatic activities of Pulicaria incisa (Lam.) DC. We also reported the molecular interaction between identified molecules and several receptors associated with antimicrobial and antibiofilm activities. A total of seventeen and thirteen compounds were identified in aqueous and methanolic extracts of P. incisa, respectively. The methanolic extract yielded a higher total content of polyphenols and flavonoids of about 84.80 ± 2.8 mg GAE/g and 28.30 ± 1.2 mg QE/g, respectively. Significant antibacterial activity was recorded for both extracts, with minimum inhibitory concentration (MIC) values ranging from 30 to 36 µg/mL, and the result was comparable to the reference antibiotic control. Antibiofilm assays revealed that both extracts were able to reduce the attachment of bacterial cells to 96-well plates, but the highest antibiofilm activity was recorded against Staphylococcus aureus. The methanolic extract also showed anti-enzymatic potency and high antioxidant activity, as demonstrated by all assays used, including DPPH, FRAP, and ABTS. These results were further validated by in silico approaches, particularly the molecular interaction of the identified compounds with the targeted receptors. These findings present P. incisa as a significant source of antibacterial, antibiofilm, antioxidant, and anti-enzymatic molecules.
Assuntos
Antioxidantes , Pulicaria , Antioxidantes/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Antibacterianos/farmacologia , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/química , MetanolRESUMO
Developing new prophylactic and therapeutic agents with broad-spectrum antiviral activities is urgently needed to combat emerging human severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Since no available clinically antiviral drugs have been approved to eradicate COVID-19 as of the writing of this report, this study aimed to investigate bioactive short peptides from Allium subhirsutum L. (Hairy garlic) extracts identified through HR-LC/MS analysis that could potentially hinder the multiplication cycle of SARS-CoV-2 via molecular docking study. The obtained promising results showed that the peptides (Asn-Asn-Asn) possess the highest binding affinities of -8.4 kcal/mol against S protein, (His-Phe-Gln) of -9.8 kcal/mol and (Gln-His-Phe) of -9.7 kcal/mol towards hACE2, (Thr-Leu-Trp) of -10.3 kcal/mol and (Gln-Phe-Tyr) of -9.8 kcal/mol against furin. Additionally, the identified peptides show strong interactions with the targeted and pro-inflammatory ranging from -8.1 to -10.5 kcal/mol for NF-κB-inducing kinase (NIK), from -8.2 to -10 kcal/mol for phospholipase A2 (PLA2), from -8.0 to -10.7 kcal/mol for interleukin-1 receptor-associated kinase 4 (IRAK-4), and from -8.6 to -11.6 kcal/mol for the cyclooxygenase 2 (COX2) with Gln-Phe-Tyr model seems to be the most prominent. Results from pharmacophore, drug-likeness and ADMET prediction analyses clearly evidenced the usability of the peptides to be developed as an effective drug, beneficial for COVID-19 treatment.
Assuntos
Allium , Tratamento Farmacológico da COVID-19 , Antivirais/química , Antivirais/farmacologia , Humanos , Simulação de Acoplamento Molecular , SARS-CoV-2RESUMO
Due to the emergency and uncontrolled situation caused by the COVID-19 pandemic that arising in the entire world, it is necessary to choose available drugs that can inhibit or prevent the disease. Therefore, the repurposing of the commercial antibiotic, dirithromycin has been screened for the first time against fifteen receptors and compared to the azithromycin using a molecular docking approach to identify possible SARS-CoV-2 inhibitors. Our docking results showed that dirithromycin fit significantly in the Furin catalytic pocket having the lowest binding score (-9.9 Kcal/mol) with respect to azithromycin (-9.4 Kcal/mol) and can interact and block both Asp154 and Ser368 residues by Van der Walls interaction as well as bound to His194 and Ser368 residues via hydrogen bonds. Good results were also obtained with the Tmprss-2 receptor. A Molecular Dynamic simulation was assessed to confirm this interaction. Additionally, detailed receptor-ligand interactions with SARS-CoV-2 and pro-inflammatory mediators were investigated suggesting more target information with interesting results. The findings of this study are very efficient and provide a basis for the development of dirithromycin for clinical trial applications to be efficient in treating SARS-CoV-2 infections.
Assuntos
Tratamento Farmacológico da COVID-19 , SARS-CoV-2 , Antivirais/química , Antivirais/farmacologia , Antivirais/uso terapêutico , Azitromicina/química , Azitromicina/farmacologia , Azitromicina/uso terapêutico , Eritromicina/análogos & derivados , Humanos , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Pandemias , Proteínas não Estruturais Virais/química , Proteínas não Estruturais Virais/metabolismoRESUMO
The Eucalyptus genus (Myrtaceae) is characterized by a richness in essential oils (EO) with multiple biological activities. This study reports the chemical composition and the phytotoxic and antimicrobial activities of the EOs from Tunisian E.occidentalis, E.striaticalyx and E.stricklandii. The EOs were analyzed using GC/MS and their phytotoxicities were assessed against the germination and seedling growth of Sinapis arvensis, Trifolium campestre and Lolium rigidum. Antimicrobial activity was investigated against both Gram-negative (Pseudomonas aeruginosa, Escherichia coli and Acinetobacter baumannii) and Gram-positive (Staphylococcus aureus and Listeria monocytogenes) bacteria. The inhibition of biofilm formation and its metabolism was determined at different times. All EOs were rich in oxygenated monoterpenes (36.3-84.8%); the EO of E.occidentalis was rich in sesquiterpenes, both oxygenated and hydrocarbon (40.0% and 15.0%, respectively). Eucalyptol was the main constituent in all samples. The EOs showed phytotoxic activity on seed germination and seedling growth, depending both on chemical composition and weed. The EOs show a remarkable antibacterial potential resulting in a significant inhibition of the formation of bacterial biofilm and its metabolism, depending on the EO and the strain, with activity on the mature biofilm as well. Therefore, these Eucalyptus EOs could have potential applications both in the food and health fields.
Assuntos
Eucalyptus , Óleos Voláteis , Sesquiterpenos , Antibacterianos/química , Antibacterianos/farmacologia , Biofilmes , Escherichia coli , Eucaliptol , Eucalyptus/química , Testes de Sensibilidade Microbiana , Monoterpenos/farmacologia , Óleos Voláteis/química , Óleos Voláteis/farmacologiaRESUMO
This study was carried out to characterize the chemical composition of the essential oils from seven Eucalyptus species (E. griffithsii, E. hemiphloia, E. lesouefii, E. longicornis, E. pyriformis, E. viminalis, and E. wandoo), as well as their phytotoxic and antibacterial activities. The essential oils were analyzed by GC/MS and the potential in vitro phytotoxicity was evaluated against germination and radical elongation of Raphanus sativus, Lolium multiflorum, and Sinapis arvensis seeds. The antibiofilm activity was studied against both Gram-negative (Pseudomonas aeruginosa, Escherichia coli and Acinetobacter baumannii) and Gram-positive (Staphylococcus aureus and Listeria monocytogenes) bacteria. The inhibition of biofilm formation and its metabolism was determined at different times. Eucalyptol was the most abundant component in all essential oils studied (ranging from 40.8% for E. lesouefii EO to 73.6% for E. wandoo) except for that of E. pyriformis where it was present but at 15.1%. E. pyriformis was the most active against both germination and radical elongation of S. arvensis. The action of all essential oils proved to be highly effective in inhibiting the bacterial adhesion process of the five strains considered. In light of these results, these essential oils could have potential applications both in the agricultural and health fields.
Assuntos
Eucalyptus , Óleos Voláteis , Eucalyptus/química , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Eucaliptol/farmacologia , Bactérias , Antibacterianos/farmacologia , Antibacterianos/química , Tunísia , Testes de Sensibilidade MicrobianaRESUMO
The composition, herbicidal, larvicidal, and toxic activities of Juniperus horizontalis Moench essential oil and sabinene, its main component, were evaluated. The seed germination percentage and root length of eight different plant species (crops and weeds) were measured for in vitro herbicidal activity tests. Different doses (100, 50, 10, 5, 1, 0.5 µg/mL) of the samples were applied to seeds for 120 h. The same doses were applied to test the toxicity of the samples on Tubifex tubifex (sludge worm) and Chironomus aprilinus (blood worm). Four doses (435, 652.5, 870, and 1740) of samples were in a larvicidal test on Tenebrio molitor L. (mealworm), and bioassays were checked after 24 and 48 h. The analysis of the oil allowed for the identification of dominant components as sabinene (38.7%), α-pinene (10.0%), elemol (8.6%), γ-terpinene (8.3%), limonene (7.8%) and α-thujene (5.3%). The results showed that the effect of oil on root length inhibition was significant in all crop species. The doses which affected root growth were not toxic to Tubifex tubifex and Chironomus aprilinus. Finally, the obtained results in the larvicidal bioassay indicate that the potential of J. horizontalis in yellow mealworm survivorship limitation can be a starting point for future research.
Assuntos
Herbicidas , Inseticidas , Juniperus , Óleos Voláteis , Juniperus/química , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Inseticidas/farmacologia , Inseticidas/químicaRESUMO
Alzheimer's disease (AD) is a neurodegenerative disorder leading to cognitive deficits and cognitive decline. Since no cure or preventing therapy is currently available to counteract AD, natural-derived compounds are investigated to find new potential neuroprotective agents for its treatment. In the present study, we tested the neuroprotective effect of lavender and coriander essential oils (EOs) and their main active constituent linalool, against the neurotoxicity elicited by Aß1-42 oligomers, a key molecular factor in the neurodegeneration of AD. Importantly, our findings on neuronally differentiated PC12 cells exposed to Aß1-42 oligomers are in accordance with previous in vivo studies reporting the neuroprotective potential of lavender and coriander EOs and linalool. We found that lavender and coriander EOs at the concentration of 10 µg/mL as well as linalool at the same concentration were able to improve viability and to reduce nuclear morphological abnormalities in cells treated with Aß1-42 oligomers for 24 hours. Lavender and coriander EOs and linalool also showed to counteract the increase of intracellular reactive oxygen species production and the activation of the pro-apoptotic enzyme caspase-3 induced by Aß1-42 oligomers. Our findings provide further evidence that these EOs and their main constituent linalool could be natural agents of therapeutic interest against Aß1-42 -induced neurotoxicity.
Assuntos
Peptídeos beta-Amiloides/toxicidade , Coriandrum/química , Lavandula/química , Fármacos Neuroprotetores/farmacologia , Óleos Voláteis/farmacologia , Fragmentos de Peptídeos/toxicidade , Monoterpenos Acíclicos/farmacologia , Doença de Alzheimer , Animais , Transtornos Cognitivos/induzido quimicamente , Disfunção Cognitiva , Células PC12 , Óleos de Plantas/farmacologia , Ratos , Espécies Reativas de Oxigênio/metabolismoRESUMO
The present study evaluated the therapeutic potential of myricitrin (Myr), a glycosyloxyflavone extracted from Myrica esculenta bark, against diabetic nephropathy. Myr exhibited a significant hypoglycemic effect in high fat-fed and a single low-dose streptozotocin-induced type 2 diabetic (T2D) rats. Myr was found to improve glucose uptake by the skeletal muscle via activating IRS-1/PI3K/Akt/GLUT4 signaling in vitro and in vivo. Myr significantly attenuated high glucose (HG)-induced toxicity in NRK cells and in the kidneys of T2D rats. In this study, hyperglycemia caused nephrotoxicity via endorsing oxidative stress and inflammation resulting in the induction of apoptosis, fibrosis, and inflammatory damages. Myr was found to attenuate oxidative stress via scavenging/neutralizing oxidative radicals and improving endogenous redox defense through Nrf-2 activation in both in vitro and in vivo systems. Myr was also found to attenuate diabetes-triggered renal inflammation via suppressing NF-κB activation. Myr inhibited hyperglycemia-induced apoptosis and fibrosis in renal cells evidenced by the changes in the expressions of the apoptotic and fibrotic factors. The molecular docking predicted the interactions between Myr and different signal proteins. An in silico absorption, distribution, metabolism, excretion, and toxicity (ADMET) study predicted the drug-likeness character of Myr. Results suggested the possibility of Myr to be a potential therapeutic agent for diabetic nephropathy in the future.
Assuntos
Diabetes Mellitus Experimental , Nefropatias Diabéticas , Flavonoides , Hipoglicemiantes , Myrica/química , Estresse Oxidativo/efeitos dos fármacos , Casca de Planta/química , Animais , Linhagem Celular , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Experimental/patologia , Nefropatias Diabéticas/tratamento farmacológico , Nefropatias Diabéticas/metabolismo , Nefropatias Diabéticas/patologia , Flavonoides/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Inflamação/patologia , Masculino , Ratos , Ratos WistarRESUMO
The phytotoxicity and eco-compatibility of essential oils (EOs) from Eucalyptus gunnii (EG) and E. pulverulenta 'Baby Blue' (EP), cultivated in Italy for their cut foliage, were investigated. Leaf micromorphology, EOs phytochemical characterization, and phytotoxicity were analysed. EP revealed a significantly higher oil gland density and a higher EO yield with respect to EG. In both EOs, 1,8-cineole was the major compound (~75%), followed by α-pinene in EG (13.1%) and eugenol in EP (7.5%). EO phytotoxicity was tested on both weeds (Lolium multiflorum, Portulaca oleracea) and crops (Raphanus sativus, Lactuca sativa, Lepidium sativum, Solanum lycopersicum, Pisum sativum, Cucumis sativus). EG EO inhibited germination of P. oleracea, R. sativus, and S. lycopersicum seeds (ranging from 61.5 to 94.6% for the higher dose used), while affecting only radical elongation in S. lycopersicum (ranging from 66.7 to 82.6%). EP EO inhibited germination of P. oleracea and R. sativus (ranging from 41.3 to 74.7%) and affected radical elongation of L. sativum and L. multiflorum (ranging from 57.4 to 76.0%). None of the EOs affected the germination and radical growing of L. sativa, P. sativum, and C. sativus. Moreover, EP EO was more active than EG EO in inhibiting α-amylase, a key enzyme for seed growth regulation. Brine shrimp lethality assay showed that both EOs are safe for aquatic organisms, suggesting their high eco-compatibility. The data collected provide useful information for future applications of these EOs in agriculture as safe and selective bioherbicides.
Assuntos
Produtos Agrícolas/efeitos dos fármacos , Eucalyptus/química , Herbicidas/farmacologia , Óleos Voláteis/farmacologia , Compostos Fitoquímicos/farmacologia , Plantas Daninhas/efeitos dos fármacos , Animais , Artemia , Germinação/efeitos dos fármacos , Herbicidas/química , Herbicidas/isolamento & purificação , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificaçãoRESUMO
The aim of the study was to investigate the micromorphology of Mentha pulegium leaves and flowers harvested in three different Sicilian (Italy) areas with peculiar pedo-climatic conditions, and to characterize the phytochemical profile, the phytotoxic activity, and the eco-compatibility of their essential oils (EOs) for potential use as safe bioherbicides. Light microscopy (LM) and scanning electron microscopy (SEM) highlighted that M. pulegium indumentum consists of non-glandular and glandular trichomes of different types. Peltate trichomes of plants from the different sites showed few significant differences in dimension and abundance, but they were characterized by a surprisingly high number of secretory cells both in leaves and flowers. Phytochemical analyses showed that oxygenated monoterpenes were the most abundant class in all the EOs investigated (92.2-97.7%), but two different chemotypes, pulegone/isomenthone and piperitone/isomenthone, were found. The complex of morphological and phytochemical data indicates that soil salinity strongly affects the expression of the toxic metabolite pulegone, rather than the EO yield. Phytotoxicity tests showed a moderate activity of EOs against the selected species as confirmed by α-amylase assay. Moreover, the low toxicity on brine shrimp provided a rationale for the possible use of investigated EOs as eco-friendly herbicides.
Assuntos
Economia , Mentha pulegium/química , Animais , Artemia , Flores/anatomia & histologia , Flores/ultraestrutura , Geografia , Itália , Mentha pulegium/anatomia & histologia , Mentha pulegium/ultraestrutura , Óleos Voláteis/análise , Óleos Voláteis/economia , Compostos Fitoquímicos/toxicidade , Folhas de Planta/anatomia & histologia , Folhas de Planta/ultraestrutura , Sus scrofa , Testes de Toxicidade , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismoRESUMO
In this study, we investigated the bioactive potential (antibacterial and antioxidant), anticancer activity and detailed phytochemical analysis of Selaginellarepanda (S. repanda) ethanolic crude extract for the very first time using different in vitro approaches. Furthermore, computer-aided prediction of pharmacokinetic properties and safety profile of the identified phytoconstituents were also employed in order to provide some useful insights for drug discovery. S. repanda, which is a rich source of potent natural bioactive compounds, showed promising antibacterial activity against the tested pathogenic bacteria (S. aureus, P. aeruginosa, E. coli and S. flexneri). The crude extract displayed favorable antioxidant activity against both 2,2-diphenyl-1-picrylhydrazyl (DPPH) (IC50 = 231.6 µg/mL) and H2O2 (IC50 = 288.3 µg/mL) molecules. S. repanda also showed favorable and effective anticancer activity against all three malignant cancer cells in a dose/time dependent manner. Higher activity was found against lung (A549) (IC50 = 341.1 µg/mL), followed by colon (HCT-116) (IC50 = 378.8 µg/mL) and breast (MCF-7) (IC50 = 428.3 µg/mL) cancer cells. High resolution-liquid chromatography-mass spectrometry (HR-LC-MS) data of S. repanda crude extract revealed the presence of diverse bioactive/chemical components, including fatty acids, alcohol, sugar, flavonoids, alkaloids, terpenoids, coumarins and phenolics, which can be the basis and major cause for its bioactive potential. Therefore, achieved results from this study confirmed the efficacy of S. repanda and a prospective source of naturally active biomolecules with antibacterial, antioxidant and anticancer potential. These phytocompounds alone with their favorable pharmacokinetics profile suggests good lead and efficiency of S. repanda with no toxicity risks. Finally, further in vivo experimental investigations can be promoted as probable candidates for various therapeutic functions, drug discovery and development.
Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Selaginellaceae/química , Antibacterianos/química , Antibacterianos/farmacocinética , Antibacterianos/farmacologia , Antibacterianos/toxicidade , Antineoplásicos/farmacocinética , Antineoplásicos/toxicidade , Antioxidantes/química , Antioxidantes/farmacocinética , Antioxidantes/farmacologia , Antioxidantes/toxicidade , Neoplasias da Mama/patologia , Linhagem Celular Tumoral , Neoplasias Colorretais/patologia , Humanos , Neoplasias Pulmonares/patologia , Extratos Vegetais/farmacocinética , Extratos Vegetais/toxicidadeRESUMO
Cesarean scar pregnancy (CSP) is a rare form of ectopic pregnancy which represents a consequence of a previous cesarean section. It is associated with major maternal morbidity and mortality and has potential implications on future fertility. Because of possible serious complications, CSP should be swiftly diagnosed and treated. There is no management protocol for this rare, life-threatening condition, and each patient should be evaluated individually. Several types of conservative treatment have been used to treat cesarean scar pregnancy: dilation and curettage (D&C), excision of trophoblastic tissues, local or systemic administration of methotrexate, bilateral hypogastric artery ligation, and selective uterine artery embolization with curettage and/or methotrexate administration. In our study we present a cesarean scar pregnancy of a 40-year-old woman who was treated with angiographic uterine artery embolization (UAE) followed by hysteroscopic diode laser resection. Our combined UAE-hysteroscopic laser surgery appears to offer an effective, safe, and minimally invasive surgical treatment.
Assuntos
Cesárea , Gravidez Ectópica , Adulto , Artérias , Cesárea/efeitos adversos , Cicatriz/complicações , Feminino , Humanos , Lasers Semicondutores , Metotrexato/uso terapêutico , Gravidez , Gravidez Ectópica/diagnóstico por imagem , Gravidez Ectópica/cirurgia , Doenças Raras , Estudos Retrospectivos , Resultado do TratamentoRESUMO
Diabetes mellitus is a life-threatening metabolic syndrome. Over the past few decades, the incidence of diabetes has climbed exponentially. Several therapeutic approaches have been undertaken, but the occurrence and risk still remain unabated. Several plant-derived small molecules have been proposed to be effective against diabetes and associated vascular complications via acting on several therapeutic targets. In addition, the biocompatibility of these phytochemicals increasingly enhances the interest of exploiting them as therapeutic negotiators. However, poor pharmacokinetic and biopharmaceutical attributes of these phytochemicals largely restrict their clinical usefulness as therapeutic agents. Several pharmaceutical attempts have been undertaken to enhance their compliance and therapeutic efficacy. In this regard, the application of nanotechnology has been proven to be the best approach to improve the compliance and clinical efficacy by overturning the pharmacokinetic and biopharmaceutical obstacles associated with the plant-derived antidiabetic agents. This review gives a comprehensive and up-to-date overview of the nanoformulations of phytochemicals in the management of diabetes and associated complications. The effects of nanosizing on pharmacokinetic, biopharmaceutical and therapeutic profiles of plant-derived small molecules, such as curcumin, resveratrol, naringenin, quercetin, apigenin, baicalin, luteolin, rosmarinic acid, berberine, gymnemic acid, emodin, scutellarin, catechins, thymoquinone, ferulic acid, stevioside, and others have been discussed comprehensively in this review.
Assuntos
Composição de Medicamentos , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Nanomedicina Teranóstica , Animais , Diabetes Mellitus/tratamento farmacológico , Diabetes Mellitus/metabolismo , Portadores de Fármacos , Sistemas de Liberação de Medicamentos , Humanos , NanopartículasRESUMO
The present study was carried out to determine some biochemical characteristics, in particular the total polyphenol content and the free radical scavenging activity, of the extracts recovered from bulbs and aerial parts (these last often considered as by-products) of two landraces of A. ampeloprasum var. holmense cultivated in Southern Italy. For the first time, the capacity of the extracts of these landraces to inhibit the formation of biofilm of different Gram-negative and Gram-positive bacteria and to affect the metabolism of the cells present within the bacterial biofilm was evaluated. All extracts exhibited an amount of total polyphenols not lower than 2.86 mg/g of dried product and revealed a noteworthy antioxidant activity, with EC50 values not exceeding 4.95 mg. In both cases, the aerial parts extracts were more effective than the bulb extracts, which also showed a minor amount of total polyphenols. The extracts inhibited mainly the adhesive capability of Pseudomonas aeruginosa and Staphylococcus aureus, by 95.78% and 85.01%, respectively. The extracts demonstrated to inhibit also the metabolism of the bacterial cells reaching levels up to 90%. Finally, as assessed by the assays performed on the 24-h preformed biofilms, all the extracts were also capable to cause a reduction in bacterial biomass and to affect their metabolism.