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Current treatments for gynecological cancers include surgery, radiotherapy, and chemotherapy. However, these treatments often have significant side effects. Phytochemicals, natural compounds derived from plants, offer promising anticancer properties. Coumarins, a class of benzopyrone compounds found in various plants like tonka beans, exhibit notable antitumor effects. These compounds induce cell apoptosis, target PI3K/Akt/mTOR signaling pathways, inhibit carbonic anhydrase, and disrupt microtubules. Additionally, they inhibit tumor multidrug resistance and angiogenesis and regulate reactive oxygen species. Specific coumarin derivatives, such as auraptene, praeruptorin, osthole, and scopoletin, show anti-invasive, anti-migratory, and antiproliferative activities by arresting the cell cycle and inducing apoptosis. They also inhibit metalloproteinases-2 and -9, reducing tumor cell migration, invasion, and metastasis. These compounds can sensitize tumor cells to radiotherapy and chemotherapy. Synthetic coumarin derivatives also demonstrate potent antitumor and anticancer activities with minimal side effects. Given their diverse mechanisms of action and minimal side effects, coumarin-class phytochemicals hold significant potential as therapeutic agents in gynecological cancers, potentially improving treatment outcomes and reducing side effects. This review will aid in the synthesis and development of novel coumarin-based drugs for these cancers.
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Olea europaea L. (Oleaceae), is rich in phenolic content and has powerful antioxidant and antidiabetic activity. However, there are no medicinal products prepared due to this feature. Therefore, this study aims to characterize an O. europaea extract with strong antioxidant and antidiabetic properties and to prepare nanoformulations containing this extract. To determine the activities of the extracts prepared from the leaves of the plant, DPPH⢠and ABTSâ¢+ scavenging, Fe+3 reducing activity, α-amylase, and α-glucosidase inhibition assays were performed. The oleuropein content of the absolute ethanol extract with the highest activity was analysed by HPLC. The characterized extract was loaded into liposomes and chitosan coated liposomes, and the long-term sustainability of their activity was investigated. The encapsulation efficiency was 65.2% for the liposome and 66.8% for the chitosan-coated liposome formulation. The amounts of the extracts released from the formulations were evaluated to exhibit antioxidant and antidiabetic activity.
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Antioxidantes , Hipoglicemiantes , Lipossomos , Olea , Extratos Vegetais , Lipossomos/química , Antioxidantes/farmacologia , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Olea/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Folhas de Planta/química , Animais , Camundongos , Linhagem Celular TumoralRESUMO
The medicinal plant Satureja cuneifolia Ten. was widely utilized as spice, tea and traditional medicine. The objective of the current study was to examine the chemical composition and in vitro biological activities (LOX, MMP-1, and MMP-12 enzyme inhibition activity and cytotoxicity on A549 cell line) of Satureja cuneifolia extracts and essential oils. The essential oils of the flowering aerial parts were hydro-distilled at four different distillation times (5, 30, 60, and 180 min) using the Clevenger apparatus. The total essential oil and four fragments were compared in terms of the major component, yield, and distillation time. Volatile compounds of the infusion were extracted by using HS-SPME. Ethanolic extract had the strongest inhibition activity on the LOX enzyme (84.50%), while the essential oils exhibited more cytotoxic activity on the A549 cell line than the extracts. The oils and the infusion were analyzed using GC-MS and the primary chemicals identified by LC-MS/MS.
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Óleos Voláteis , Satureja , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Satureja/química , Cromatografia Líquida , Espectrometria de Massas em Tandem , Cromatografia Gasosa-Espectrometria de Massas , Extratos Vegetais/farmacologia , Extratos Vegetais/químicaRESUMO
The study's objective is to clarify the probable mechanisms underlying the wound-healing properties of Helianthemum canum L. (Cistaceae), a traditional anti-inflammatory and wound-healing medicine. LC/MS-MS was used to perform phytochemical analyses on a 70 % methanol extract of the plant's aerial parts. In vivo, linear incision and circular excision models were used to evaluate the wound healing activity. For anti-inflammatory effect, inâ vivo acetic acid capillary permeability assay and inâ vitro Interleukinâ 1, Interleukinâ 6, and Interferon É£ levels in LPS-induced FR skin fibroblast cell line were also evaluated. The extract significantly improved wound healing in experimental models, with tensile strength values of 27.8 % and a contraction value of 35.09 %. Histopathological examinations, hydroxyproline estimation, hyaluronidase, collagenase, and elastase enzyme inhibitory assays confirmed wound healing potential. Inflammatory cytokines were significantly inhibited in the LPS-induced FR cell line, with the highest effect seen on IL-6 (34.5±2.12â pg/mL). This study offered the first concrete proof that H. canum can be used to treat wounds by suggesting that the myricetin and quinic acid content identified by LCMS-MS analysis may be accountable for the effect of H. canum on wound contraction and hydroxyproline production.
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Cistaceae , Extratos Vegetais , Ratos , Animais , Extratos Vegetais/química , Ratos Sprague-Dawley , Hidroxiprolina/metabolismo , Lipopolissacarídeos/farmacologia , Cicatrização , Compostos Fitoquímicos/farmacologia , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Cistaceae/metabolismoRESUMO
Most human infectious diseases are caused by microorganisms growing as biofilms. These three-dimensional self-organized communities are embedded in a dense matrix allowing microorganisms to persistently inhabit abiotic and biotic surfaces due to increased resistance to both antibiotics and effectors of the immune system. Consequently, there is an urgent need for novel strategies to control biofilm-associated infections. Natural products offer a vast array of chemical structures and possess a wide variety of biological properties; therefore, they have been and continue to be exploited in the search for potential biofilm inhibitors with a specific or multi-locus mechanism of action. This review provides an updated discussion of the major bioactive compounds isolated from several natural sources - such as plants, lichens, algae, microorganisms, animals, and humans - with the potential to inhibit biofilm formation and/or to disperse established biofilms by bacterial pathogens. Despite the very large number of bioactive products, their exact mechanism of action often remains to be clarified and, in some cases, the identity of the active molecule is still unknown. This knowledge gap should be filled thus allowing development of these products not only as novel drugs to combat bacterial biofilms, but also as antibiotic adjuvants to restore the therapeutic efficacy of current antibiotics.
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Bactérias , Produtos Biológicos , Animais , Humanos , Biofilmes , Antibacterianos/química , Produtos Biológicos/farmacologiaRESUMO
This work aimed to create an extract of Melissa officinalis L. with strong antiradical efficacy, characterize it, and enhance its long-term efficacy by developing an ethosomal formulation. DPPH and ABTS assays were used to test the antiradical activity of extracts with different ethanol ratios obtained from the aerial part. Phytochemical characterization of the extract with the highest activity, ethyl acetate fraction of 60% ethanol extract, was analyzed by HPLC. The active ethyl acetate fraction was loaded into ethosomes, and characterization and release studies of the formulation were performed. The released extract from the formulation exhibited substantial antiradical action as well as inhibition of collagenase (71.5%) and elastase (75.5%) enzymes. The toxicity of the active extract and the formulation was determined in the mouse fibroblast cell line. This study successfully developed a long-term antioxidant and enzyme inhibitor formulation containing M. officinalis, which stands out for its medicinal properties.
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Antioxidantes , Melissa , Animais , Camundongos , Antioxidantes/farmacologia , Antioxidantes/química , Extratos Vegetais/toxicidade , Extratos Vegetais/química , Melissa/química , EtanolRESUMO
BACKGROUND: The current research centers on exploring the antioxidant, antimicrobial, and antidiabetic features of Schinus molle L. grown in Turkey. METHODS: Quantitative analysis of chlorogenic acid, caffeic acid, and hyperoside levels in leaf, ripe fruit, and raw fruit extracts was conducted using High-Performance Liquid Chromatography (HPLC) in a 70% methanol-water mixture. Among the extracts, the methanol extract from ripe fruits displayed the highest chlorogenic acid concentration, measuring at 2.040% ± 0.172% standard deviation (SD). Moreover, analysis of their total phenolic and flavonoid contents was carried out. Antioxidant power was assessed through different chemical assays, together with their antimicrobial and anti-diabetic properties. RESULTS: The results of DPPH (2,2-Diphenyl-1-picrylhydrazyl), ABTS (2,2'-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), and reducing power assays showed that leaf and ripe fruit alcoholic extract exhibited peak performance. While the MIC ( minimum inhibitory concentration) values of the extracts were determined to have moderate bactericidal effects on Staphylococcus aureus, Escherichia coli, and Candida albicans it was observed that none of the extracts displayed biofilm inhibition. The inhibition percentage of α-glucosidase enzyme activity for the methanol extract of raw fruits was determined to be 99.11 ± 1.61. In diabetic ß-TC cells, glucose level was measured as 129 ± 2.03 mg/dL, and insulin amount was measured as 37.2 ± 0.02 mg/dL. CONCLUSIONS: The findings of our study seem to have important implications for future research, as Schinus molle L. may be a potential pharmaceutical candidate with important pharmacological activities.
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Anti-Infecciosos , Antioxidantes , Antioxidantes/farmacologia , Antioxidantes/química , Frutas/química , Schinus , Ácido Clorogênico/análise , Hipoglicemiantes/farmacologia , Metanol , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Anti-Infecciosos/farmacologia , Fenóis/farmacologia , Folhas de Planta/químicaRESUMO
In this study, BALB/c mice with Ehrlich solid tumors were used to examine the effect of Achillea millefolium L. (AM) extract on the Ehrlich ascites tumor (EAT) model, which is one of the experimental cancer models. Also known as yarrow and plant, AM has antioxidant, anti-inflammatory, antibacterial and antitumor properties. In our study, 57 male BALB/c type mice, 8-10 weeks old, weighing 25-30 g, were used. Mice were divided into two groups. Ehrlich Solid Tumor group: Negative Control Group (ENC), Positive Control Group (EPC), and Treatment Group (TG) (TNCAM-200 mg/kg, TPCAM-400 mg/kg). EPC and TG were given to EAT cells. Each EAT contained 1 × 106 (will be 6 out of 10: so:000000) EAT cells, 0.1 ml of phosphate-buffered saline (PBS) was administered subcutaneously (s.c.) to the nape of mice. Then It was awaited for solid tumor formation. AM extract was administered intraperitoneally (i.p.) to TG for 17 days to mice. AM extract was found to have a curative effect on areas of inflammation, bleeding, and necrosis in treatment groups treated with AM extract alone. The treatment groups showed nearly normal histological results compared to the positive control group. According to the results, the TPCAM-400 mg/kg group had a more significant histological impact than the TNCAM-200 mg/kg group. In terms of tumor growth, tumor length, tumor volume, and tumor weight, AM extract did not show significant effects. However, in the light of histological findings, promising results of AM were observed in mice in which Ehrlich Solid Tumor was formed.
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Neoplasias , Animais , CamundongosRESUMO
Among various cancers, breast cancer is the most prevalent type in women throughout the world. Breast cancer treatment is challenging due to complex nature of the etiology of disease. Cell division cycle alterations are often encountered in a variety of cancer types including breast cancer. Common treatments include chemotherapy, surgery, radiotherapy, and hormonal therapy; however, adverse effects and multidrug resistance lead to complications and noncompliance. Accordingly, there is an increasing demand for natural products from medicinal plants and foods. This review summarizes molecular mechanisms of signaling pathways in breast cancer and identifies mechanisms by which natural compounds may exert their efficacy in the treatment of breast cancer.
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Produtos Biológicos , Neoplasias da Mama , Plantas Medicinais , Produtos Biológicos/farmacologia , Produtos Biológicos/uso terapêutico , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/metabolismo , Neoplasias da Mama/prevenção & controle , Feminino , Humanos , Transdução de SinaisRESUMO
Controlled release systems containing natural compounds have been successfully applied in cosmetics as antiaging products to enhance the penetration of active compounds through the skin. In this study, we aimed to develop novel ethosomal formulations containing a potent antioxidant, epigallocatechin-3-gallate (EGCG), and to evaluate their potential for use in cosmetics by determining their antioxidant and antiaging effects. Ethosomes (ETHs) were prepared via mechanical dispersion and characterized in vitro in terms of particle size (PS), zeta potential (ZP), polydispersity index (PDI), encapsulation efficiency percentage (EE%), and in vitro release. The best ETH formulation was used to prepare the ethosome-based gel (ETHG) by using Carbopol 980 as a gelling agent at a ratio of 1:1 (v/v). The gel formulation was evaluated regarding organoleptic properties, pH values, and viscosity. Stability studies were conducted for three months and changes in characterization parameters and residual EGCG content of ETHs were examined. Besides, for ETHG, organoleptic properties, pH values (every two weeks), and viscosity (first and twelfth week) were determined for three months. The 3-(4,5-dimethyldiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was used to test the cytotoxicity of the formulations and different EGCG solutions on the L929 cell line. The cell permeation properties and inhibitory effects of ETHs and ETHGs on collagenase and elastase enzymes were investigated compared to those of the solution form. Within the scope of antioxidant activity studies, 2,2-diphenyl-1-picrylhydrazyl (DPPHâ¢) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS+â¢) radical scavenging and ß-carotene/linoleic acid co-oxidation inhibitory effects were carried out. The optimized EGCG-loaded ETHs (F3) were within the nanoscale range (238 ± 1.10 nm). The highest encapsulation efficiency and in vitro release values were 51.7 ± 1.15% and 50.8 ± 1.70%, respectively. The ETHG was successfully formulated with F3-coded ETHs and the cytotoxicity test revealed that the formulations and the EGCG solution at different concentrations were nontoxic. In terms of cell permeability, enzyme inhibition, and antioxidant activity, the ethosomal formulations yielded better results compared to the EGCG solution. It was observed that the formulations had a long-term effect due to the stability of EGCG. The findings of the study underline the potential of antioxidant and antiaging effects of the developed ethosomal formulations for use in the cosmetic field.
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Nepeta is one of the largest genera of the Lamiaceae family. Nepeta species are commonly employed in traditional medicine for a variety of ailments, as well as food additives. In addition, they also come to the fore with their rich phytochemical content. In the present study, the quantitative phytochemical content of methanolic extracts and infusions prepared from the aerial parts of 14 Nepeta taxa collected from Turkey and their cytotoxic effects on two breast cancer cell lines, MCF-7 and MDA-MB-231, were investigated by using the MTT (3-(4,5-dimethylthiazol-2-yl))-2,5-diphenyltetrazolium-bromide) test. According to HPLC-PDA analysis, N. racemosa methanolic extract had the highest ursolic acid content with 165.9 mg/g extract. Total sterol, total iridoid, and total triterpenoid content were determined to be greatest in the methanolic extracts of N. meyeri, N. trichocalyx and N. phyllochlamys. The MTT experiment demonstrated that certain Nepeta species suppressed the growth of MCF-7 and MDA-MB-231 cells in a dose-dependent manner. Statistical analysis revealed a strong correlation between the cytotoxic effects of the extracts and their triterpene content. In conclusion, the data obtained from this study are important in terms of forming a basis for advanced anticancer activity studies on breast cancer with Nepeta sp.
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Cancer is one of the important causes of death worldwide. Despite remarkable improvements in cancer research in the past few decades, several cancer patients still cannot be cured owing to the development of drug resistance. Natural sources might have prominence as potential drug candidates. Among the several chemical classes of natural products, anthraquinones are characterized by their large structural variety, noticeable biological activity, and low toxicity. Aloe emodin, an anthraquinone derivative, is a natural compound found in the roots and rhizomes of many plants. This compound has proven its antineoplastic, anti-inflammatory, antiangiogenic, and antiproliferative potential as well as ability to prevent cancer metastasis and potential in reversing multidrug resistance of cancer cells. The anticancer property of aloe emodin, a broad-spectrum inhibitory agent of cancer cells, has been detailed in many biological pathways. In cancer cells, these molecular mechanisms consist of inhibition of cell growth and proliferation, cell cycle arrest deterioration, initiation of apoptosis, antimetastasis, and antiangiogenic effect. In accordance with the strategy of developing potential drug candidates from natural products, aloe emodin's low bioavailability has been tried to be overcome by structural modifications and nanocarrier systems. Consequently, this review summarizes the antiproliferative and anticarcinogenic properties of aloe emodin, as well as the enhanced activity of its derivatives and the advantages of drug delivery systems on bioavailability.
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Antraquinonas/uso terapêutico , Sistemas de Liberação de Medicamentos/métodos , Neoplasias/tratamento farmacológico , Antraquinonas/farmacologia , HumanosRESUMO
Sleep disturbances, as well as sleep-wake rhythm disorders, are characteristic symptoms of Alzheimer's disease (AD) that may head the other clinical signs of this neurodegenerative disease. Age-related structural and physiological changes in the brain lead to changes in sleep patterns. Conditions such as AD affect the cerebral cortex, basal forebrain, locus coeruleus, and the hypothalamus, thus changing the sleep-wake cycle. Sleep disorders likewise adversely affect the course of the disease. Since the sleep quality is important for the proper functioning of the memory, impaired sleep is associated with problems in the related areas of the brain that play a key role in learning and memory functions. In addition to synthetic drugs, utilization of medicinal plants has become popular in the treatment of neurological diseases. Curcuminoids, which are in a diarylheptanoid structure, are the main components of turmeric. Amongst them, curcumin has multiple applications in treatment regimens of various diseases such as cardiovascular diseases, obesity, cancer, inflammatory diseases, and aging. Besides, curcumin has been reported to be effective in different types of neurodegenerative diseases. Scientific studies exclusively showed that curcumin leads significant improvements in the pathological process of AD. Yet, its low solubility hence low bioavailability is the main therapeutic limitation of curcumin. Although previous studies have focused different types of advanced nanoformulations of curcumin, new approaches are needed to solve the solubility problem. This review summarizes the available scientific data, as reported by the most recent studies describing the utilization of curcumin in the treatment of AD and sleep deprivation-related consequences.
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Doença de Alzheimer/tratamento farmacológico , Curcumina/uso terapêutico , Idoso , Idoso de 80 Anos ou mais , Doença de Alzheimer/patologia , Curcumina/farmacologia , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Estudos Prospectivos , Privação do Sono/tratamento farmacológicoRESUMO
Psychiatric disorders are frequently encountered in many neurological disorders, such as Alzheimer's and Parkinson diseases along with epilepsy, migraine, essential tremors, and stroke. The most common comorbid diagnoses in neurological diseases are depression and anxiety disorders along with cognitive impairment. Whether the underlying reason is due to common neurochemical mechanisms or loss of previous functioning level, comorbidities are often overlooked. Various treatment options are available, such as pharmacological treatments, cognitive-behavioral therapy, somatic interventions, or electroconvulsive therapy. However oral antidepressant therapy may have some disadvantages, such as interaction with other medications, low tolerability due to side effects, and low efficiency. Natural compounds of plant origin are extensively researched to find a better and safer alternative treatment. Experimental studies have shown that phytochemicals such as alkaloids, terpenes, flavonoids, phenolic acids as well as lipids have significant potential in in vitro and in vivo models of psychiatric disorders. In this review, various efficacy of natural products in in vitro and in vivo studies on neuroprotective and their roles in psychiatric disorders are examined and their neuro-therapeutic potentials are shed light.
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The Lime Basra (Citrus aurantifolia Linn., Rutaceae) plant also known as dried lime, and Limoo Omani, is used both as a spice in meals and as an herbal tea in the treatment of some diseases in the Middle East. It was aimed to determine the biological activity screening of the 70% methanol, ethanol extracts and infusion which were prepared from dried fruits. 1,1-diphenyl-2-picrylhydrazyl (DPPHâ) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS+â) radical scavenging activities, ferric reducing activity, cytotoxicity on A 549, MCF 7 and L929 cell lines and α-amylase inhibitory effects were determined. According to the results, 70% methanol extract was more active in antioxidant activity tests and ethanol extract was more active in cytotoxicity tests. Interestingly both 70% methanol and ethanol extracts were found to have potent hypoglycemic activity. The present findings shed light on the fact that it is important to research and scientifically evaluate plants with traditional medicinal use.
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Antioxidantes/farmacologia , Citrus/química , Alimentos em Conserva , Animais , Antioxidantes/análise , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Etanol/química , Flavonoides/análise , Flavonoides/farmacologia , Alimentos em Conserva/análise , Frutas/química , Humanos , Metanol/química , Fenóis/análise , Fenóis/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , alfa-Amilases/antagonistas & inibidoresRESUMO
The study was aimed to evaluate the effectiveness of rosmarinic acid (RA) loaded ethosomes (ETHs) and liposomes (LPs) when subjected to the transdermal application. RA-loaded ETHs and LPs were prepared, optimised, and characterised. The ex vivo permeation studies of formulations using mouse abdominal skin were performed. Antioxidant activities and the inhibitory effects of formulations on collagenase and elastase enzymes were measured. Optimised ethosomal formulation (F3) was showed nanometric size range (138 ± 1.11 nm) and greatest entrapment (55 ± 1.80%), was selected for further transdermal permeation studies. Skin permeation profile of the nanoformulations analysed by HPLC revealed an enhanced permeation of ETHs. Transdermal flux of ETHs was found to be higher than RA solution and LPs. Enzyme inhibitions of ETHs were the significant difference found between ETHs and LPs (p < 0.05). ETHs were found to be more effective and successful than LPs. Results suggest that ETHs are more effective than LPs for transdermal delivery of RA.
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Antioxidantes/administração & dosagem , Cinamatos/administração & dosagem , Depsídeos/administração & dosagem , Portadores de Fármacos/química , Inibidores de Metaloproteinases de Matriz/administração & dosagem , Administração Cutânea , Animais , Antioxidantes/farmacocinética , Antioxidantes/farmacologia , Linhagem Celular , Cinamatos/farmacocinética , Cinamatos/farmacologia , Colagenases/metabolismo , Depsídeos/farmacocinética , Depsídeos/farmacologia , Lipossomos/química , Inibidores de Metaloproteinases de Matriz/farmacocinética , Inibidores de Metaloproteinases de Matriz/farmacologia , Camundongos , Elastase Pancreática/antagonistas & inibidores , Elastase Pancreática/metabolismo , Pele/efeitos dos fármacos , Pele/metabolismo , Absorção Cutânea , Envelhecimento da Pele/efeitos dos fármacos , Ácido RosmarínicoRESUMO
The use of microbial cell culture a valuable tool for the biosynthesis of nanoparticles is considered a green technology as it is eco-friendly, inexpensive and simple. Here, the synthesis of nanosilver particle (AgNP) from the yeast, Saccharomyces cerevisiae, gram (+), Bacillus subtilis and gram (-), Escherichia coli was shown. In this field we are the first to study their the antimicrobial effects of the microorganisms mentioned above against pathogens and anticancer activity on MCF-7 cell line. Silver nanoparticles in the size range of 126-323â¯nm were synthesized extracellularly by the microorganisms, which have different cell structures. Optical absorption, scanning electron microscopy, and zetasizer analysis confirmed the silver nanoparticles formation. Antimicrobial activity of AgNPs was evaluated the minimum inhibition concentration and disc diffusion methods. AgNPs inhibited nearly 90% the growth of Gram-positive Listeria monocytogenes, Streptococcus pneumoniae and Gram-negative Haemophilus influenzae, Klebsiella pneumoniae, Neisseria meningitidis bacterial pathogens. Anticancer potentials of AgNPs were investigated by MTT method. The synthesized AgNPs exhibited excellent high toxicity on MCF-7 cells and had a dose-dependent effect on cell viability. Especially AgNP 2 eliminated 67% of the MCF-7 cells at the concentration of 3.125⯵g/mL. We found that extracellular synthesis of nanoparticles from microbial culture may be 'green' alternative to physical and chemical methods from the point of view of synthesis in large amounts and easy process.
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The current study was designed to evaluate the antioxidant, anti-inflammatory and antimicrobial activities of Alchemilla mollis (Buser) Rothm. (Rosaceae) aerial parts extracts. Chemical composition was analyzed by spectrophotometric and chromatographic (HPLC) techniques. The antioxidant properties assessed included DPPH· and ABTS·+ radical scavenging, ß-carotene-linoleic acid co-oxidation assay. Antimicrobial activity was evaluated with disc diffusion and micro dilution method. In order to evaluate toxicity of the extracts, with the sulforhodamine B colorimetric assay L929 cell line (mouse fibroblast) was used. The anti-inflammatory activities of the potent antioxidant extracts (methanol, 70% methanol, and water extracts) were determined by measuring the inhibitory effects on NO production and pro-inflammatory cytokine TNF-α levels in lipopolysaccharide stimulated RAW 264.7 cells. 70% methanol and water extracts which were found to be rich in phenolic compounds (184.79 and 172.60 mg GAE/g extract) showed higher antioxidant activity. Luteolin-7-O-glucoside was the main compound in the extracts. Ethyl acetate and 70% methanol extracts showed higher antibacterial activity against Staphylococcus aureus and Salmonella enteritidis with MIC value of 125 µg/ml. 70% methanol extract potentially inhibited the NO and TNF-α production (18.43 µm and 1556.22 pg/ml, respectively, 6 h).
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Alchemilla/química , Anti-Infecciosos/química , Anti-Inflamatórios/química , Antioxidantes/química , Fenóis/química , Animais , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Ácido Linoleico/química , Camundongos , Óxido Nítrico/imunologia , Oxirredução/efeitos dos fármacos , Fenóis/isolamento & purificação , Fenóis/farmacologia , Células RAW 264.7 , Fator de Necrose Tumoral alfa/imunologia , beta Caroteno/químicaRESUMO
CONTEXT: Pelargonium endlicherianum Fenzl. (Geraniaceae) roots and flowers are traditionally used in Turkey as a decoction treatment against intestinal parasites. Neither the chemical composition nor the potential bioactivity of the plant roots has been studied before. OBJECTIVES: The phenolic content and effects of P. endlicherianum root extracts on antioxidant enzyme levels on A549 cells were studied for the first time. MATERIALS AND METHODS: The chemical composition was analyzed via spectrophotometric and chromatographic (HPLC MS/MS and HPLC) techniques. The antioxidant activity was determined at different concentrations ranging from 0.001 to 2 mg/mL using DPPH⢠and ABTSâ¢+ radical scavenging activity, ß-carotene-linoleic acid co-oxidation assay, protection of 2-deoxyribose and bovine brain-derived phospholipids against a hydroxyl radical-mediated degradation assay. Glutathione peroxidase and superoxide dismutase activities were also studied as well as the effects of the extracts on nitric oxide levels on IL-1ß stimulated A549 cells. RESULTS: The key parameters for the most active ethyl acetate extract included the following: DPPH⢠IC50: 0.23 mg/mL, TEAC/ABTS: 2.17 mmol/L Trolox, reduction: 0.41 mmol/g AsscE, and protection of lipid peroxidation IC50: 0.05 mg/mL. Furthermore, the ethyl acetate extract increased the SOD level significantly compared to control group (4.48 U/mL) at concentrations of 100 and 200 µg/mL SOD, 5.50 and 5.67 U/mL, respectively. Apocynin was identified as the major component, and the ethyl acetate fraction was found to be rich in phenolic compounds. DISCUSSION AND CONCLUSION: Pelargonium endlicherianum root extracts displayed antioxidant activity and increased the antioxidant enzyme levels in IL-1ß stimulated A549 cells, while decreasing the NO levels.
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Antioxidantes/farmacologia , Pelargonium/química , Extratos Vegetais/farmacologia , Células A549 , Animais , Antioxidantes/administração & dosagem , Antioxidantes/isolamento & purificação , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Bovinos , Cromatografia Líquida de Alta Pressão , Relação Dose-Resposta a Droga , Glutationa Peroxidase/metabolismo , Humanos , Concentração Inibidora 50 , Óxido Nítrico/metabolismo , Fosfolipídeos/metabolismo , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Raízes de Plantas , Superóxido Dismutase/metabolismo , Espectrometria de Massas em Tandem , TurquiaRESUMO
Herein, we report the biosynthesis of Ag NPs, for the first time, using identified antimicrobial molecules (gallic acid+apocynin) and (gallic acid+apocynin+quercetin) from the medicinal plant Pelargonium endlicherianum Fenzl. and dramatically enhanced antimicrobial activity. We also investigate the role of each molecule on formation Ag NPs and explain the increase in the antimicrobial activity of identified molecules mediated Ag NPs. The extraction protocols, 11% ethanol and 70% methanol, resulted in identification of different constituents of gallic acid+apocynin (M1) and gallic acid+apocynin+quercetin (M2) with respective concentrations. The M1-Ag and M2-Ag NPs exhibit excellent inhibitory activities towards Gram negative bacteria; Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853 and Gram positive bacteria; Staphylococcus epidermidis ATCC 3699 bacterial using in vitro microdilution method. The minimum inhibitory concentration (MIC) values of M1-Ag and M2-Ag NPs were determined to be 7.81 and 6.25ppm for S. epidermidis, respectively. Surprisingly, MIC value for both Ag NPs was indicated to be identical as 9. 37ppm for P. aeruginosa and E., coli.