RESUMO
The pharmacological activation of the GPR39 receptor has been proposed as a novel strategy for treating seizures; however, this hypothesis has not been verified experimentally. TC-G 1008 is a small molecule agonist increasingly used to study GPR39 receptor function but has not been validated using gene knockout. Our aim was to assess whether TC-G 1008 produces anti-seizure/anti-epileptogenic effects in vivo and whether the effects are mediated by GPR39. To obtain this goal we utilized various animal models of seizures/epileptogenesis and GPR39 knockout mice model. Generally, TC-G 1008 exacerbated behavioral seizures. Furthermore, it increased the mean duration of local field potential recordings in response to pentylenetetrazole (PTZ) in zebrafish larvae. It facilitated the development of epileptogenesis in the PTZ-induced kindling model of epilepsy in mice. We demonstrated that TC-G 1008 aggravated PTZ-epileptogenesis by selectively acting at GPR39. However, a concomitant analysis of the downstream effects on the cyclic-AMP-response element binding protein in the hippocampus of GPR39 knockout mice suggested that the molecule also acts via other targets. Our data argue against GPR39 activation being a viable therapeutic strategy for treating epilepsy and suggest investigating whether TC-G 1008 is a selective agonist of the GPR39 receptor.
Assuntos
Epilepsia , Pentilenotetrazol , Animais , Camundongos , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Epilepsia/induzido quimicamente , Epilepsia/genética , Epilepsia/metabolismo , Hipocampo/metabolismo , Camundongos Knockout , Pentilenotetrazol/metabolismo , Receptores Acoplados a Proteínas G/genética , Receptores Acoplados a Proteínas G/metabolismo , Peixe-Zebra/metabolismoRESUMO
The influence of UV radiation on skin discoloration, skin aging and the development of skin cancer is widely known. As a part of this study, the effect of extracts from three varieties of Cornus mas L. (C. mas L.) on skin cells exposed to UVA radiation was assessed. The analyses were performed on both normal and cancer skin cells. For this purpose, the potential photoprotective effects of the obtained extracts (aqueous and ethanolic) was assessed by performing two cytotoxicity tests (Alamar blue and Neutral red). Additionally, the antioxidant capacity was compared using three different assays. The 2',7'-dichlorodihydrofluorescein diacetate (H2DCFDA) probe was used to evaluate the intracellular level of free radicals in cells exposed to the simultaneous action of UVA radiation and dogwood extracts. Additionally, the ability to inhibit excessive pigmentation was determined by assessing the inhibition of melanin formation and tyrosinase activity. The obtained results confirmed the strong antioxidant properties of dogwood extracts and their photoprotective effect on normal skin cells. The ability to inhibit the viability of melanoma cells was also observed. Additionally, a reduction in oxidative stress in skin cells exposed to UVA radiation and a strong inhibition of melanin formation and tyrosinase activity have been demonstrated. This study shows that dogwood extract could be a valuable cosmetic raw material that can play both a photoprotective and antihyperpigmentation role in cosmetic preparations.
Assuntos
Antioxidantes , Cornus , Extratos Vegetais , Raios Ultravioleta , Raios Ultravioleta/efeitos adversos , Humanos , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Cornus/química , Antioxidantes/farmacologia , Melaninas/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Estresse Oxidativo/efeitos da radiação , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos da radiação , Linhagem Celular Tumoral , Células HaCaT , Fibroblastos/efeitos dos fármacos , Fibroblastos/efeitos da radiação , Fibroblastos/metabolismo , Monofenol Mono-Oxigenase/metabolismo , Monofenol Mono-Oxigenase/antagonistas & inibidoresRESUMO
In the cosmetics industry, the extract from Raphanus sativus L. is fermented using specific starter cultures. These cosmetic ingredients act as preservatives and skin conditioners. Kombucha is traditionally made by fermenting sweetened tea using symbiotic cultures of bacteria and yeast and is used in cosmetic products. The aim of this study was to evaluate the cosmetic properties of radish leaf and root extract fermented with the SCOBY. Both unfermented water extracts and extracts after 7, 14, and 21 days of fermentation were evaluated. The analysis of secondary plant metabolites by UPLC-MS showed higher values for ferments than for extracts. A similar relationship was noted when examining the antioxidant properties using DPPH and ABTS radicals and the protective effect against H2O2-induced oxidative stress in fibroblasts and keratinocytes using the fluorogenic dye H2DCFDA. The results also showed no cytotoxicity to skin cells using Alamar Blue and Neutral Red tests. The ability of the samples to inhibit IL-1ß and COX-2 activity in LPS-treated fibroblasts was also demonstrated using ELISA assays. The influence of extracts and ferments on bacterial strains involved in inflammatory processes of skin diseases was also assessed. Additionally, application tests were carried out, which showed a positive effect of extracts and ferments on TEWL and skin hydration using a TEWAmeter and corneometer probe. The results obtained depended on the concentration used and the fermentation time.
Assuntos
Antibacterianos , Anti-Inflamatórios , Antioxidantes , Fermentação , Extratos Vegetais , Folhas de Planta , Raízes de Plantas , Raphanus , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Folhas de Planta/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Raphanus/química , Antibacterianos/farmacologia , Antibacterianos/química , Humanos , Antioxidantes/farmacologia , Antioxidantes/química , Raízes de Plantas/química , Fibroblastos/efeitos dos fármacos , Fibroblastos/metabolismo , Chá de Kombucha , Ciclo-Oxigenase 2/metabolismo , Interleucina-1beta/metabolismo , Estresse Oxidativo/efeitos dos fármacosRESUMO
Plant extracts can be a valuable source of biologically active compounds in many cosmetic preparations. Their effect depends on the phytochemicals they contain and their ability to penetrate the skin. Therefore, in this study, the possibility of skin penetration by phenolic acids contained in dogwood extracts of different fruit colors (yellow, red, and dark ruby red) prepared using different extractants was investigated. These analyses were performed using a Franz chamber and HPLC-UV chromatography. Moreover, the antioxidant properties of the tested extracts were compared and their impact on the intracellular level of free radicals in skin cells was assessed. The cytotoxicity of these extracts towards keratinocytes and fibroblasts was also analyzed and their anti-inflammatory properties were assessed using the enzyme-linked immunosorbent assay (ELISA). The analyses showed differences in the penetration of individual phenolic acids into the skin and different biological activities of the tested extracts. None of the extracts had cytotoxic effects on skin cells in vitro, and the strongest antioxidant and anti-inflammatory properties were found in dogwood extracts with dark ruby red fruits.
Assuntos
Anti-Inflamatórios , Antioxidantes , Cornus , Extratos Vegetais , Pele , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Cornus/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Antioxidantes/farmacologia , Antioxidantes/química , Pele/metabolismo , Pele/efeitos dos fármacos , Humanos , Queratinócitos/efeitos dos fármacos , Queratinócitos/metabolismo , Fibroblastos/efeitos dos fármacos , Fibroblastos/metabolismo , Hidroxibenzoatos/farmacologia , Hidroxibenzoatos/química , Frutas/química , Animais , Cromatografia Líquida de Alta PressãoRESUMO
Cornus mas L. is a rich source of vitamin C and polyphenols. Due to their health-benefit properties, C. mas L. extracts have been used in, e.g., dermatology and cosmetology, and as a food supplement. Peroxisome proliferator-activated receptor gamma (PPARγ) and its co-activator (PGC-1α) are now suspected to be the main target of active substances from C. mass extracts, especially polyphenols. Moreover, the PPARγ pathway is involved in the development of different diseases, such as type 2 diabetes mellitus (DM2), cancers, skin irritation, and inflammation. Therefore, the aim of the present study was to evaluate the PPARγ pathway activation by the most popular water and ethanol extracts from specific C. mas L. cultivars in an in vitro model of the human normal fibroblast (BJ) cell line. We analyzed the content of biologically active compounds in the extracts using the UPLC-DAD-MS technique and revealed the presence of many polyphenols, including gallic, quinic, protocatechuic, chlorogenic, and ellagic acids as well as iridoids, with loganic acid being the predominant component. In addition, the extracts contained cyanidin 3-O-galactoside, pelargonidin 3-O-glucoside, and quercetin 3-glucuronide. The water-ethanol dark red extract (DRE) showed the strongest antioxidant activity. Cytotoxicity was assessed in a normal skin cell line, and positive effects of all the extracts with concentrations ranging from 10 to 1000 µg/mL on the cells were shown. Our data show that the studied extracts activate the PPARγ/PGC-1α molecular pathway in BJ cells and, through this mechanism, initiate antioxidant response. Moreover, the activation of this molecular pathway may increase insulin sensitivity in DM2 and reduce skin irritation.
Assuntos
Antioxidantes , Cornus , Extratos Vegetais , Antioxidantes/farmacologia , Antioxidantes/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Humanos , Cornus/química , Polifenóis/farmacologia , Polifenóis/química , PPAR gama/metabolismo , Linhagem Celular , Citoproteção/efeitos dos fármacosRESUMO
Osteoporosis stands out as a prevalent skeletal ailment, prompting exploration into potential treatments, including dietary strontium ion supplements. This study assessed the efficacy of supplementation of three strontium forms-strontium citrate (SrC), strontium ranelate (SrR), and strontium chloride (SrCl)-for enhancing bone structure in 50 female SWISS mice, aged seven weeks. In total, 40 mice underwent ovariectomy, while 10 underwent sham ovariectomy. Ovariectomized (OVX) mice were randomly assigned to the following groups: OVX (no supplementation), OVX + SrR, OVX + SrC, and OVX + SrCl, at concentrations equivalent to the molar amount of strontium. After 16 weeks, micro-CT examined trabeculae and cortical bones, and whole-bone strontium content was determined. Results confirm strontium administration increased bone tissue mineral density (TMD) and Sr content, with SrC exhibiting the weakest effect. Femur morphometry showed limited Sr impact, especially in the OVX + SrC group. This research highlights strontium's potential in bone health, emphasizing variations in efficacy among its forms.
Assuntos
Ácido Cítrico , Osteoporose , Estrôncio , Tiofenos , Feminino , Animais , Camundongos , Densidade Óssea , Cloretos , Citratos , Osteoporose/tratamento farmacológico , Halogênios , Modelos Animais de DoençasRESUMO
Isoflavones, belonging to polyphenolic compounds, show structural similarity to natural estrogens, and in this context, they have been extensively studied. Some of them are also applied as cosmetic additives; however, little is known regarding their effects on skin cells. In this investigation, common isoflavones, including genistein, daidzein, glycitein, formononetin, and biochanin A, as well as coumestrol, were evaluated for antioxidant activity and their impact on human skin fibroblasts and keratinocytes. Antioxidant effects were assessed using DPPH, ABTS, and FRAP tests, and the ability to scavenge reactive oxygen species (ROS) was tested in cells with H2O2-provoked oxidative stress. The impact on the activity of antioxidant enzymes (SOD, CAT, GSH) and lipid peroxidation (MDA) was also explored. As shown by Alamar Blue and neutral red uptake assays, the compounds were not toxic within the tested concentration range, and formononetin and coumestrol even demonstrated a stimulatory effect on cells. Coumestrol and biochanin A demonstrated significant antioxidative potential, leading to a significant decrease in ROS in the cells stimulated by H2O2. Furthermore, they influenced enzyme activity, preventing depletion during induced oxidative stress, and also reduced MDA levels, demonstrating protection against lipid peroxidation. In turn, genistein, daidzein, and glycitein exhibited low antioxidant capacity.
Assuntos
Genisteína , Isoflavonas , Humanos , Genisteína/farmacologia , Cumestrol , Espécies Reativas de Oxigênio , Fitoestrógenos , Antioxidantes , Peróxido de Hidrogênio , Isoflavonas/química , Estresse Oxidativo , Queratinócitos , FibroblastosRESUMO
Tiliroside is a natural polyphenolic compound with a wide range of biological activity, and defatted strawberry seeds are its rich source. The goal of this study was to optimize accelerated solvent extraction (ASE) conditions, including temperature, solvent composition, and the number of extraction cycles, using Box-Behnken design to maximize the yield of tiliroside. UPLC-DAD-MS was applied to investigate the polyphenolic composition of the extracts, and preparative liquid chromatography (pLC) was used for isolation. All obtained mathematical models generally showed an increase in the efficiency of isolating polyphenolic compounds with an increase in temperature, ethanol content, and the number of extraction cycles. The optimal established ASE conditions for tiliroside were as follows: a temperature of 65 °C, 63% ethanol in water, and four extraction cycles. This allowed for the obtainment of a tiliroside-rich fraction, and the recovery of isolated tiliroside from plant material reached 243.2 mg from 100 g. Our study showed that ASE ensures the isolation of a tiliroside-rich fraction with high effectiveness. Furthermore, defatted strawberry seeds proved to be a convenient source of tiliroside because the matrix of accompanying components is relatively poor, which facilitates separation.
Assuntos
Fragaria , Extratos Vegetais , Polifenóis , Sementes , Solventes , Fragaria/química , Polifenóis/química , Polifenóis/isolamento & purificação , Sementes/química , Solventes/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Cromatografia Líquida de Alta Pressão/métodos , Flavonoides/química , Flavonoides/isolamento & purificação , Fracionamento Químico/métodosRESUMO
Osteoarthritis (OA) is one of the most prevalent diseases of the osteoarticular system. Progressive destruction of joints is accompanied by development of pathological changes in the muscle tissue, i.e., weakening, atrophy, and remodelling (sarcopenia). The aim of the present study is to assess the impact of physical activity on the musculoskeletal system in an animal model of early degenerative lesions in the knee joint. The study involved 30 male Wistar rats. The animals were allocated to three subgroups of 10 animals each. Each animal from the three subgroups received sodium iodoacetate by injection into the patellar ligament of the right knee joint, whereas saline was administered through the patellar ligament in the left knee joint. The rats in the first group were stimulated to exercise on a treadmill. The animals in the second group were allowed to lead a natural lifestyle (no treadmill stimulation). In the third group, all parts of the right hind limb muscle were injected with Clostridium botulinum toxin type A. The study demonstrated that, compared to the active rats, bone density in the immobilised rats decreased, as indicated by the densitometric assessment of the whole body and the examination of rats' hind limbs and knee joints alone. This clearly evidenced the impact of physical activity on bone mineralisation. The weight of both fat and muscle tissues in the physically inactive rats was reduced. Additionally, the adipose tissue had higher weight in the entire right hind limbs, where monoiodoacetic acid was administered to the knee joint. The animal model clearly showed the importance of physical activity in the early stages of OA, as it slows down the process of joint destruction, bone atrophy, and muscle wasting, whereas physical inactivity contributes to progression of generalised changes in the musculoskeletal system.
Assuntos
Osteoartrite do Joelho , Osteoartrite , Ratos , Masculino , Animais , Ratos Wistar , Articulação do Joelho/patologia , Osteoartrite/patologia , Modelos Animais , Ácido Iodoacético , Atrofia Muscular/patologia , Modelos Animais de Doenças , Osteoartrite do Joelho/patologiaRESUMO
Chronic venous disease (CVD) is a condition characterized by functional disturbances in the microcirculation of the superficial and deep veins, affecting up to 30% of the global population. Diosmin, a phlebotropic drug, is commonly used in the treatment of CVD, and its beneficial effects have been described in numerous clinical studies. However, the precise molecular mechanism underlying the activity of diosmin is not yet fully understood. Therefore, the objective of our study was to investigate whether diosmin has an impact on oxygen management, as cardiovascular diseases are often associated with hypoxia. In our study, patients were administered a daily dosage of 2 × 600 mg of diosmin for 3 months, and we evaluated several factors associated with oxygen management, angiogenesis, and inflammation using biochemical assays. Our findings indicate that diosmin reduced the levels of fibroblast growth factors (FGF) and vascular endothelial growth factor (VEGF-C), while increasing endostatin and angiostatin levels, suggesting a potential influence on angiogenesis regulation. Furthermore, diosmin exhibited anti-inflammatory properties by suppressing the levels of tumor necrosis factor-alpha (TNF-α), interleukin 1-beta (IL-1ß), and interleukin 6 (IL-6), while promoting the production of interleukin 12 (IL-12). Additionally, diosmin significantly decreased the levels of hypoxia-inducible factor (HIF), anion gap (AG), and lactate, indicating its potential influence on the hypoxia-inducible factor pathway. These findings suggest that diosmin may play a crucial role in modulating oxygen management and inflammation in the context of chronic venous disease.
Assuntos
Doenças Cardiovasculares , Diosmina , Humanos , Diosmina/farmacologia , Diosmina/uso terapêutico , Fator A de Crescimento do Endotélio Vascular , Interleucina-12 , Fatores de Crescimento de Fibroblastos , Hipóxia , Inflamação , Interleucina-6 , Ácido Láctico , Homeostase , OxigênioRESUMO
Due to the high demand for products that can help treat various skin conditions, the interest in plant extracts, which are a valuable source of phytochemicals, is constantly growing. In this work, the properties of extracts and ferments from Cornus mas L. and their potential use in cosmetic products were compared. For this purpose, their composition, antioxidant properties and cytotoxicity against skin cells, keratinocytes and fibroblasts were assessed in vitro. In addition, the ability to inhibit the activity of collagenase and elastase was compared, which enabled the assessment of their potential to inhibit skin aging. Microbiological analyses carried out on different bacterial strains were made in order to compare their antibacterial properties. The conducted analyses showed that both dogwood extract and ferment have antioxidant and anti-aging properties. In addition, they can have a positive effect on the viability of keratinocytes and fibroblasts and inhibit the proliferation of various pathogenic bacteria, which indicates their great potential as ingredients in skin care preparations. The stronger activity of the ferment compared to the extract indicates the legitimacy of carrying out the fermentation process of plant raw materials using kombucha in order to obtain valuable products for the cosmetics industry.
Assuntos
Antioxidantes , Cornus , Antioxidantes/farmacologia , Fibrinolíticos , Antibacterianos/farmacologia , Extratos Vegetais/farmacologiaRESUMO
The causes and mechanisms underlying adolescent idiopathic scoliosis (AIS) remain unclear, and the available information regarding metabolic imbalances in AIS is still insufficient. This investigation aimed to evaluate the concentrations of specific bone remodeling-related agents in postmenarcheal girls diagnosed with AIS. The study encompassed thirty-six scoliosis patients and eighteen age-matched healthy individuals assigned to the control group. The patients underwent clinical and radiological examinations to assess the degree of the spinal deformity, type of curvature, and skeletal maturity. Blood and urine samples were collected from all participants and serological markers were measured using an enzyme-linked immunosorbent assay. Our study results demonstrated that the balance of phosphate-calcium and parathormone levels seems normal in individuals with AIS. Furthermore, no statistically significant differences were observed in the content of Klotho protein, osteocalcin, osteoprotegerin, C-terminal telopeptide of type I collagen (CTX), sclerostin, and alkaline phosphatase. Nevertheless, the serum levels of vitamin D (25-OH-D) were lowered, while N-terminal propeptide of type I procollagen (PINP), and fibroblast growth factor-23 (FGF23) were increased in the AIS group, with p-values of 0.044, 0.001, and 0.022, respectively. This finding indicates the potential involvement of these factors in the progression of AIS, which necessitates further studies to uncover the fundamental mechanisms underlying idiopathic scoliosis.
Assuntos
Escoliose , Feminino , Humanos , Adolescente , Fosfatase Alcalina , Remodelação Óssea , Colágeno Tipo IRESUMO
The herbivore Cameraria ohridella (kingdom Animalia) and the pathogen Erysiphe flexuosa (kingdom Fungi) are considered pests and biotic stressors of Aesculus hippocastanum (chestnut trees). The impact of both pests on the accumulation of secondary metabolites in chestnut leaves was investigated. Specifically, the interactive effect of both pests on metabolite accumulation and their potential role in enhancing the resistance of chestnut trees to biological stress was the focus of this study. Aesculus hippocastanum leaves with varying degrees of Cameraria ohridella infestation and Erysiphe flexuosa infection were used in this research. Leaf samples were collected during the plant vegetative growth phase and evaluated for pest infection and secondary metabolite content. Eight main polyphenols were identified in the leaves: (1) neochlorogenic acid, (2) (-)-epicatechin, (3) procyanidin trimer A-type, (4) procyanidin tetramer A-type, (5) quercetin-3-O-arabinoside, (6) quercetin-3-O-rhamnoside, (7) kaempferol-3-O-arabinoside, and (8) kaempferol-3-O-rhamnoside. It was found that the accumulation of metabolites, primarily those derived from epicatechin and quercetin, during the initial vegetation phase (up to 11.05 or 09.05), strongly depended on the later degree of pest infection. The differences observed in the metabolite dynamics in the chestnut leaves, depending on the extent of infection, indicate the development of a metabolic response mechanism in chestnut trees to biological stress.
Assuntos
Aesculus , Mariposas , Proantocianidinas , Animais , Quempferóis , Quercetina , Mariposas/fisiologia , Folhas de Planta , FenóisRESUMO
In this study, an attempt was made to evaluate the antioxidant, anti-inflammatory and protective effects of the Sambucus nigra fruit extract and its ferment obtained by fermentation with kombucha tea fungus. For this purpose, fermented and non-fermented extracts were compared in terms of their chemical composition by the HPLC/ESI-MS chromatographic method. The antioxidant activity of the tested samples was assessed using DPPH and ABTS assays. Cytotoxicity was also determined using Alamar Blue and Neutral Red tests to assess the viability and metabolism of fibroblast and keratinocyte skin cells. Potential anti-aging properties were determined by their ability to inhibit the activity of the metalloproteinases collagenase and elastase. Tests showed that the extract and the ferment have antioxidant properties and stimulate the proliferation of both cell types. The study also assessed the anti-inflammatory activity of the extract and ferment by monitoring levels of the pro-inflammatory interleukins IL-6, IL-1ß, tumor necrosis factor (TNF-α) and anti-inflammatory IL-10 in lipopolysaccharide (LPS)-treated fibroblast cells. The results indicate that both the S. nigra extract and its kombucha ferment can be effective in preventing free-radical-induced cell damage and have positive effects on skin cell health.
Assuntos
Sambucus nigra , Humanos , Sambucus nigra/química , Antioxidantes/metabolismo , Lipopolissacarídeos/metabolismo , Água/metabolismo , Frutas/química , Anti-Inflamatórios/química , Extratos Vegetais/química , Interleucina-6/metabolismo , Fator de Necrose Tumoral alfa/metabolismo , Fibroblastos/metabolismoRESUMO
The fruits of R. nigrum L., A. melanocarpa Michx., and V. myrtillus L. are well-known natural plant materials with proven antioxidant activity. This work attempts to compare the antioxidant properties of extracts of these plants and ferments obtained during their fermentation using a consortium of microorganisms referred to as kombucha. As part of the work, a phytochemical analysis of extracts and ferments was carried out using the UPLC-MS method and the content of the main components was determined. The antioxidant properties of the tested samples and their cytotoxicity were assessed with the use of DPPH and ABTS radicals. The protective effect against hydrogen peroxide-induced oxidative stress was also assessed. The possibility of inhibiting the increase in the intracellular level of reactive oxygen species was carried out on both human skin cells (keratinocytes and fibroblasts) and the yeast Saccharomyces cerevisiae (wild-type strains and sod1Δ deletion mutants). The conducted analyses showed that the ferments obtained are characterized by a greater variety of biologically active compounds; in most cases they do not cause a cytotoxic effect, show strong antioxidant properties, and can reduce oxidative stress in both human and yeast cells. This effect depends on the concentration used and the fermentation time. The results obtained indicate that the tested ferments can be considered as an extremely valuable raw material protecting cells against the negative effects of oxidative stress.
Assuntos
Antioxidantes , Peróxido de Hidrogênio , Humanos , Antioxidantes/farmacologia , Peróxido de Hidrogênio/farmacologia , Saccharomyces cerevisiae , Frutas/química , Cromatografia Líquida , Espectrometria de Massas em Tandem , Estresse Oxidativo , Extratos Vegetais/farmacologia , PlantasRESUMO
Due to the growing popularity of herbal extract-loaded hydrogels, this study assessed the biological activity of extracts and hydrogels containing three types (water (WE), water-ethanol (EE) and water-glycerin (GE)) of Cornus mas L. (dogwood) extracts. The content of biologically active compounds in the extracts was assessed using the UPLC-DAD-MS technique. Antioxidant properties were assessed by using DPPH and ABTS radicals and measuring the intracellular level of reactive oxygen species. Alamar Blue and Neutral Red tests were used to measure the cytotoxicity of the tested samples on skin cells-fibroblasts and keratinocytes. Cell migration and the anti-aging activity of the tested extracts and hydrogels were assessed. Transepidermal water loss and skin hydration after applying the hydrogels to the skin were also determined. A chromatographic analysis revealed that the extracts contained polyphenols, including gallic, caftaric, protocatechuic, chlorogenic, ellagic and p-coumaroylquinic acids, as well as iridoids, with loganic acid as the predominant component. Additionally, they contained cyanidin 3-O-galactoside, pelargonidin 3-O-glucoside and quinic acid. The obtained results show that the tested extracts and hydrogels had strong antioxidant properties and had a positive effect on the viability of skin cells in vitro. Additionally, it was shown that they stimulated the migration of these cells and had the ability to inhibit the activity of collagenase and elastase. Moreover, the tested hydrogels increased skin hydration and prevented transepidermal water loss. The obtained results indicate that the developed hydrogels may be effective delivery systems for phytochemicals contained in dogwood extracts.
Assuntos
Cornus , Dermatologia , Antioxidantes/química , Cornus/química , Hidrogéis , Água , Extratos Vegetais/farmacologia , Extratos Vegetais/químicaRESUMO
Carlina vulgaris is a little-understood plant with unexplored biological potential, and the papers regarding its chemical composition are scarce. In our study, for the first time, the phytochemical profile of the plant, focusing on polar metabolites, was established using modern chromatographic techniques including LC-HRMS-QTOF-CAD, UHPLC-PDA-MS. Phytochemical analysis revealed that the species is a rich source of polyphenolic components, with the most abundant being chlorogenic acid and C-glycosides of luteolin, including carlinoside, orientin, isoorientin, and C-glycosides of apigenin, schaftoside, isoschaftoside, and vitexin. Furthermore, we assessed the impact of the polyphenolic-rich fraction of C. vulgaris extracts on human skin fibroblasts using the MTT and NR assays. It was found that the extract was non-toxic and exhibited potent antioxidant activity in the cells subjected to induced oxidative stress. Additionally, it effectively protected the cells against H2O2-induced cytotoxicity. Our study contributes to the general trend of searching for new phytotherapeutics with potential applications in pharmacy and medicine. The results indicate that further exploration of C. vulgaris species is worthwhile, as they can serve as valuable plant material for cosmetic use.
Assuntos
Antioxidantes , Peróxido de Hidrogênio , Humanos , Antioxidantes/química , Peróxido de Hidrogênio/farmacologia , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Glicosídeos/farmacologia , Estresse Oxidativo , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análiseRESUMO
Carlina acaulis is highly valued in the traditional medicine of many European countries for its diuretic, cholagogue, anthelmintic, laxative, and emetic properties. Moreover, practitioners of natural medicine indicate that it has anti-cancer potential. However, its phytochemistry is still little known. In the present study, the polyphenolic composition of the plant was investigated using ultra-high-performance liquid chromatography coupled with a high-resolution/quadrupole time-of-flight mass spectrometer (UHPLC-HR/QTOF/MS-PDA). The fractionation of the extract was carried out using liquid-liquid extraction and preparative chromatography techniques. Cytotoxicity was assessed based on neutral red and MTT assays. The obtained data showed that the species is rich in chlorogenic acids and C-glycosides of luteolin and apigenin. The total amount of chlorogenic acids was 12.6 mg/g. Among flavonoids, kaempferol dihexosidipentose and schaftoside were the most abundant, reaching approximately 3 mg/g, followed by isoorientin, vitexin-2-O-rhamnoside, and vicenin II, each with a content of approximately 2 mg/g. Furthermore, the cytotoxic potential of the plant against human colorectal adenocarcinoma (HT29) and human cervical cancer (HeLa) cells was investigated using the normal epithelial colon cell line (CCD 841CoTr) as a reference. It has been demonstrated that the ethyl acetate fraction was the most abundant in polyphenolic compounds and had the most promising anticancer activity. Further fractionation allowed for the obtaining of some subfractions that differed in phytochemical composition. The subfractions containing polyphenolic acids and flavonoids were characterized by low cytotoxicity against cancer and normal cell lines. Meanwhile, the subfraction with fatty acids was active and decreased the viability of HeLa and HT29 with minimal negative effects on CCD 841CoTr. The effect was probably linked to traumatic acid, which was present in the fraction at a concentration of 147 mg/g of dried weight. The research demonstrated the significant potential of C. acaulis as a plant with promising attributes, thus justifying further exploration of its biological activity.
Assuntos
Adenocarcinoma , Antineoplásicos , Neoplasias Colorretais , Neoplasias do Colo do Útero , Humanos , Feminino , Neoplasias do Colo do Útero/tratamento farmacológico , Adenocarcinoma/tratamento farmacológico , Neoplasias Colorretais/tratamento farmacológico , Flavonoides/farmacologia , Extratos Vegetais/farmacologiaRESUMO
Soybeans are commonly known as a valuable source of biologically active compounds including isoflavones as well as allantoin and alpha-hydroxy acids. Since these compounds exhibit skin therapeutic effects, they are widely used in the cosmetic and pharmaceutical industries. The presented paper shows the optimization of three solvent systems (ethanol, water, and 1,3-propanediol) to increase the extraction efficiency of isoflavones (daidzin, genistin, 6â³-O-malonyldaidzin, 6â³-O-malonylglycitin, 6â³-O-malonylgenistin), allantoin, and alpha-hydroxy acids (citric acid, malic acid) from soybean leaves. A simplex centroid mixture design for three solvents with interior points was applied for the experimental plan creation. Based on the obtained results of metabolite extraction yield in relation to solvent composition, polynomial regression models were developed. All models were significant, with predicted R-squared values between 0.77 and 0.99, while in all cases the model's lack of fit was not significant. The optimal mixture composition enabling the maximization of extraction efficiency was as follows: 32.9% ethanol, 53.9% water, and 13.3% propanediol (v/v/v). Such a mixture composition provided the extraction of 99%, 91%, 100%, 92%, 99%, 70%, 92%, and 69% of daidzin, genistin, 6â³-O-malonyldaidzin, 6â³-O-malonylglycitin, 6â³-O-malonylgenistin, allantoin, citric acid, and malic acid, respectively. The solvent mixture composition developed provides a good extraction efficiency of the metabolites from soybean leaves and high antioxidant properties.
Assuntos
Glycine max , Isoflavonas , Glycine max/metabolismo , Alantoína , Isoflavonas/metabolismo , Malatos , Solventes , Etanol , Água , Ácido CítricoRESUMO
Despite the fact that there are many studies related to the adaptogenic and pro-healthy activities of plant-based compounds, there are some adaptogenic plants whose activities are not fully known, especially those coming from the wild regions of Asia, Africa, and South America. The aim of these studies was to examine the contents of non-nutritional compounds, such as polyphenols, flavonoids, and phenolic acids in ten adaptogenic species (Astragalus membranaceus (AM), Uncaria rhynchophylla (UR), Polygonum multiflorum (PM), Angelica sinensis (AS), Andrographis paniculatea (AP), Tinospora cordifolia (TC), Uncaria tomentosa (UT), Pfaffia paniculate (PP), Sutherlandia frutescens (SF), and Rhaponticum carthamoides (RC)). Considering biological activity, their antioxidant (DPPH, ABTS, FRAP, and ferrous-ion-chelating ability assays), anti-acetylcholinesterase, anti-hyaluronidase, and anti-tyrosinase activities were evaluated. The richest in polyphenols, flavonoids, and phenolic acids was UR (327.78 mg GAE/g, 230.13 mg QE/g, and 81.03 mg CA/g, respectively). The highest inhibitions of acetylcholinesterase, hyaluronidase, and tyrosinase were observed for TC, UR, and PM, respectively. In the case of antioxidant properties, extract from PM appeared to most strongly reduce DPPH, extract from UR inhibited ABTS, and extract from SF showed the best chelating properties. It should be noted that a particularly interesting plant was Ulcaria rhynchophylla. The results mean that there were compounds in UR with broad biological activities, and this species should be explored in more detail. Additionally, our results justify the traditional use of these species in the nutripharmacological or ethnopharmacological care systems of different regions.