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Cornus species are widely distributed in central and southern Europe, east Africa, southwest Asia, and America. Several species are known for edible fruits, especially Cornus mas and Cornus officinalis. These delicious fruits, characterized by their remarkable nutritional and biological values, are widely used in traditional medicine. In contrast to the other edible Cornus species, C. mas and C. officinalis are the most studied for which little information is available on the main phytochemicals and their biological activities. Fruits are characterised by several classes of secondary metabolites, such as flavonoids, phenolic acids, lignans, anthocyanins, tannins, triterpenoids, and iridoids. The available phytochemical data show that the different classes of metabolites have not been systematically studied. However, these edible species are all worthy of interest because similarities have been found. Thus, this review describes the traditional uses of Cornus species common in Europe and Asia, a detailed classification of the bioactive compounds that characterize the fruits, and their beneficial health effects. Cornus species are a rich source of phytochemicals with nutritional and functional properties that justify the growing interest in these berries, not only for applications in the food industry but also useful for their medicinal properties.
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Edible flowers consumption has increased in recent years due to their rich content of healthy phytochemicals. The aim of this study was to analyse the chemical profile of Cucurbita pepo L. flowers, and to explore their antioxidant and hypoglycaemic properties. Moreover, in order to assess in vivo effects, biochemical analysis, Reactive Oxygen Metabolites (d-ROMs) and Biological Antioxidant Potential (BAP) tests were performed on mice serum. High Performance Liquid Chromatography-Diode Array Detection (HPLC-DAD) analyses revealed the presence of (+)-catechin, (-)-epicatechin, rutin, and syringic acid as main constituents. 2,2'-Azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) and Ferric Reducing Antioxidant Power (FRAP) tests showed interesting results. The extract exhibited the strongest inhibitory effect on α-glucosidase (IC50 of 144.77 µg/mL). In vivo results confirmed the hypoglycaemic effects, also affecting lipid metabolism but did not revealed benefits on ROS production. These results may add some information supporting the use of C. pepo flowers as functional foods and/or nutraceuticals.
Asunto(s)
Antioxidantes/farmacología , Cucurbita , Animales , Antioxidantes/aislamiento & purificación , Cucurbita/química , Flores/química , Ratones , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Extractos Vegetales/farmacologíaRESUMEN
Salvia officinalis L. (sage) is one of the most appreciated plants for its plethora of biologically active compounds. The objective of our research was a comparative study, in the Mediterranean context, of chemical composition, anticholinesterases, and antioxidant properties of essential oils (EOs) from sage collected in three areas (S1-S3) of Southern Italy. EOs were extracted by hydrodistillation and analyzed by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory properties were investigated by employing Ellman's method. Four in vitro assays, namely, 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric-reducing ability power (FRAP), and ß-carotene bleaching tests, were used to study the antioxidant effects. Camphor (16.16-18.92%), 1,8-cineole (8.80-9.86%), ß-pinene (3.08-9.14%), camphene (6.27-8.08%), and α-thujone (1.17-9.26%) are identified as the most abundant constituents. However, the content of these constituents varied depending on environmental factors and pedoclimatic conditions. Principal component analysis (PCA) was performed. Based on Relative Antioxidant Capacity Index (RACI), S2 essential oil exhibited the highest radical potential with an IC50 value of 20.64 µg/mL in ABTS test and presented the highest protection of lipid peroxidation with IC50 values of 38.06 and 46.32 µg/mL after 30 and 60 min of incubation, respectively. The most promising inhibitory activity against BChE was found for S3 sample (IC50 of 33.13 µg/mL).
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Aceites Volátiles/química , Aceites Volátiles/farmacología , Fitoquímicos/química , Fitoquímicos/farmacología , Salvia officinalis/química , Antiinfecciosos/química , Antiinfecciosos/farmacología , Antioxidantes/química , Antioxidantes/farmacología , Inhibidores de la Colinesterasa/química , Inhibidores de la Colinesterasa/farmacología , Relación Dosis-Respuesta a Droga , Cromatografía de Gases y Espectrometría de Masas , Italia , Estructura Molecular , Extractos Vegetales/química , Extractos Vegetales/farmacología , Relación Estructura-ActividadRESUMEN
Natural compounds have always played a key role in drug discovery. Anthocyanins are secondary metabolites belonging to the flavonoids family responsible for the purple, blue, and red colour of many vegetables and fruits. These phytochemicals have attracted the interest of researchers for their important implications in human health and for their use as natural colorants. Many in vitro and in vivo studies demonstrated the potential effects of anthocyanins and anthocyanins-rich foods in the prevention and/or treatment of diabetes, cancer, and cardiovascular and neurodegenerative diseases. This review reports the recent literature data and focuses on the potential role of anthocyanins in drug discovery. Their biological activity, analysis of structure-activity relationships, bioavailability, metabolism, and future prospects of their uses are critically described.
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Antocianinas/farmacología , Descubrimiento de Drogas , Extractos Vegetales/farmacología , Antocianinas/química , Antocianinas/uso terapéutico , Disponibilidad Biológica , Enfermedades Cardiovasculares/tratamiento farmacológico , Diabetes Mellitus/tratamiento farmacológico , Frutas/química , Humanos , Neoplasias/tratamiento farmacológico , Enfermedades Neurodegenerativas/tratamiento farmacológico , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico , Relación Estructura-Actividad , Verduras/químicaRESUMEN
The present study aimed to determine the chemical composition, antioxidant effects and antitumor properties of a methanol extract of Anchusa azurea Mill. (Boraginaceae) aerial parts against four tumour cell lines (MCF-7, MDA-MB-231, RKO, and R2C). The antioxidant effects were assessed by using ß-carotene bleaching, 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and ferric reducing ability power (FRAP) tests. HPLC analyses revealed chlorogenic acid, catechin, caffeic acid, and astragalin as the most abundant compounds. Interesting results were obtained in the ß-carotene bleaching test with IC50 values of 7.6 and 27.5 µg mL-1 after 30 and 60 min of incubation, respectively. Furthermore, the A. azurea extract protects 3T3-L1 mouse cells from oxidative stress induced by menadione and exhibits good antitumor activity, with very low toxicity. Our data indicate that the antitumor properties are due to the ability to induce programmed cancer cell death through caspase 3/7 and 9 activation and interference with the cytoskeleton dynamics.
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Antineoplásicos/farmacología , Apoptosis/efectos de los fármacos , Boraginaceae/química , Citoesqueleto/efectos de los fármacos , Componentes Aéreos de las Plantas/química , Extractos Vegetales/farmacología , Animales , Antioxidantes/farmacología , Benzotiazoles , Compuestos de Bifenilo , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Ratones , Estrés Oxidativo/efectos de los fármacos , Fitoquímicos/química , Fitoquímicos/farmacología , Picratos , Especies Reactivas de Oxígeno , Ácidos SulfónicosRESUMEN
In this study, we investigated for the first time the anti-proliferative and antioxidant properties of D. mezereum and D. striata. The aerial parts were extracted by maceration with n-hexane, dichloromethane, and methanol. MPLC, GC, and GC-MS were used for the phytochemical study. The anti-proliferative activity was tested against MCF-7, A549, LNCaP, ACHN, and C32 cancer human cells. The antioxidant activity was measured by employing ß-carotene bleaching, ABTS, DPPH, and FRAP tests. The Relative Antioxidant Capacity Index (RACI) was applied from the perspective of statistics. D. mezereum dichloromethane extract showed a remarkable anti-proliferative with an IC50 of 6.08 µg/mL against LNCaP cells. Experimental data indicate that Daphne species have interesting anti-proliferative and antioxidant properties that deserve more investigations to develop novel antineoplastic drugs.
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Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Daphne/química , Extractos Vegetales/farmacología , Antineoplásicos Fitogénicos/química , Antioxidantes/química , Línea Celular Tumoral , Evaluación Preclínica de Medicamentos , Ensayos de Selección de Medicamentos Antitumorales , Cromatografía de Gases y Espectrometría de Masas , Humanos , Componentes Aéreos de las Plantas/química , Extractos Vegetales/análisis , Extractos Vegetales/químicaRESUMEN
Tyrosinase is a multifunctional copper-containing oxidase which catalyses the oxidation of tyrosine to produce melanin. The alteration in melanin biosynthesis occurs in many diseases. The pigment has a protecting role against skin photo-carcinogenesis, but anomalous melanin pigmentation is an aesthetic problem in human beings. Moreover, the formation of neuromelanin in human brain could contribute to the neurodegeneration associated with Parkinson's disease. Finally, tyrosinase is also responsible for undesired browning in fruits and vegetables. These topics encouraged the search for new inhibitors of this enzyme for pharmaceutical, cosmetic and foods industries. This review is to report recent trends in the discovery of tyrosinase inhibitors from plant sources, to provide a rationale for the continued study of natural tyrosinase inhibitors, and to recognise the potential therapeutic rewards associated with the identification of these agents.
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Productos Biológicos , Inhibidores Enzimáticos , Monofenol Monooxigenasa/antagonistas & inhibidores , Enfermedad de Parkinson/tratamiento farmacológico , Extractos Vegetales/química , Plantas/química , Animales , Productos Biológicos/química , Productos Biológicos/farmacología , Productos Biológicos/uso terapéutico , Evaluación Preclínica de Medicamentos , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/farmacología , Inhibidores Enzimáticos/uso terapéutico , Humanos , Melaninas/química , Melaninas/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéuticoRESUMEN
AIMS: The bioactivities of Santolina corsica Jord. & Fourr. n-hexane (EHS) and methanol (EMS) extracts were evaluated in relation to their chemical profile. MAIN METHODS: EHS and EMS were analysed by gas chromatography-mass spectrometry () and high performance liquid chromatography-diode array detection (HPLC-DAD), respectively. Antioxidant activity was determined by ß-carotene bleaching, Ferric Reducing Activity Power (FRAP), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and 2,2'-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS) tests. Nitric oxide (NO) production was assessed in LPS-stimulated RAW 264.7 cells. Anti-proliferative activity was evaluated by MTT assay on A549, HeLa, PC3, MCF-7, MDA-MB-231 cancer cells, and non-tumorigenic MCF10 A cells. Cell motility, migration and invasion were assessed by wound-healing scratch, migration and invasion assays, respectively. DNA fragmentation was tested by TUNEL assay. Cells morphology was studied by phase-contrast microscopy. Procaspase-8, -9, poly (ADP-ribose) polymerase and COX-2 expression levels were evaluated by immunoblotting analysis. KEY FINDINGS: Kaempferol-3-O-glucoside (5878.67 mg/100 g of extract), chlorogenic acid (746.11 mg/100 g), and rosmarinic acid (550.16 mg/100 g) were the dominant EMS constituents. EHS showed myrcene (18.86%) as the main compound, followed by palmitic acid methyl and ethyl esters (9.35 and 9.16%, respectively), ß-phellandrene (8.48%), and ar-curcumene (5.63%). Both extracts showed promising anti-proliferative activity on all tested cancer cells, without inducing cytotoxicity in non-tumorigenic cells MCF-10 A. Moreover, extracts inhibited motility, migration, and invasion of MDA-MB-231 cells, inducing apoptosis. EHS decreased NO production, showing anti-inflammatory activity. SIGNIFICANCE: S. corsica extracts might be potentially useful in cancer treatment, since reduce invasive and migratory potential of MDA-MB-231 cells triggering apoptosis.
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Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Asteraceae/química , Extractos Vegetales/farmacología , Animales , Antineoplásicos Fitogénicos/aislamiento & purificación , Antioxidantes/aislamiento & purificación , Apoptosis/efectos de los fármacos , Línea Celular , Línea Celular Tumoral , Movimiento Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Cromatografía Líquida de Alta Presión/métodos , Fragmentación del ADN/efectos de los fármacos , Cromatografía de Gases y Espectrometría de Masas , Humanos , Etiquetado Corte-Fin in Situ , Invasividad Neoplásica/prevención & control , Neoplasias/tratamiento farmacológico , Neoplasias/patología , Solventes/químicaRESUMEN
Glycyrrhiza glabra cultivation and harvesting produces substantial quantities of aerial parts as waste. With the aim to prospect an innovative valorization of these byproducts, the aerial parts were harvested in May and October and analyzed for their chemical profile, antioxidant properties, and effects on viability of five cancer cell lines. Pinocembrin was the main constituent. A significant protection of lipid peroxidation was observed with the May total extract (IC50 of 4.2 ± 0.4 µg/mL at 30 min of incubation). The effects on viability of HeLa, MCF-7, MDA-MB-231, Caco-2, and PC3 human cancer cells were investigated. All samples shown a remarkable activity with IC50 values below 25 µg/mL. Samples from plants harvested in May exhibited greater activity than those harvested in October. MCF-7 and HeLa were the most sensitive cells with IC50 in the range 2.73-3.01 and 3.28-5.53 µg/mL, respectively. G. glabra aerial parts represent a good source of valuable products.
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Antioxidantes/farmacología , Supervivencia Celular/efectos de los fármacos , Flavanonas/farmacología , Glycyrrhiza/química , Extractos Vegetales/farmacología , Verduras/química , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Línea Celular Tumoral , Flavanonas/química , Flavanonas/aislamiento & purificación , Humanos , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Residuos/análisisRESUMEN
BACKGROUND: Salvia species are known for their biological properties in many countries and might potentially provide novel therapeutic agents. This review provides an overview of the available literature on the anti-inflammatory and antioxidant effects of Salvia species. METHODS: Using bibliographic databases, particularly PubMed, this review aims to add new information to the list of Salvia species, including S. ceratophylla, S. chloroleuca, S. fruticosa, S. lachostachys, S. lavandulifolia, S. miltiorrhiza, S. mirzayanii, S. officinalis, S. plebeia, S. verbenaca, and S. virgata, and their main constituents as promising antiinflammatory and antioxidant agents, highlighting their mode of action. RESULTS: Salvia species are sources of health-promoting phytochemicals that comprise polyphenols, flavonoids, terpenes and several other constituents. Many studies have indicated that plants from the Salvia genus reduce the oxidative stress and may be able to prevent and/or to treat inflammatory diseases. These potential beneficial effects have been attributed to the presence of compounds that show antioxidant properties and that demonstrated to inhibit the molecular targets of pro-inflammatory mediators in inflammatory responses. CONCLUSION: Salvia species and their secondary metabolites may be potential agents to improve the quality of life in patients with inflammatory diseases.
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Antiinflamatorios/farmacología , Antioxidantes/farmacología , Extractos Vegetales/farmacología , Salvia , Animales , Antiinflamatorios/química , Antioxidantes/química , Humanos , Fitoquímicos/análisis , Fitoquímicos/farmacología , Extractos Vegetales/química , Salvia/químicaRESUMEN
Sechum edule peel, leaves and pulp were investigated for their chemical composition (total phenol, flavonoid, carotenoid and vitamin C content), and for antioxidant activity and carbohydrate-hydrolysing enzymes (α-amylase and α-glucosidase) inhibition. In order to evaluate the incidence of cooking process on retention of healthy phytochemicals, the pulp was subjected to different treatments (grill roasting, domestic oven baking, microwave cooking, blanching and steaming). Cooking processes reduced the total phenol content (58.5 mg/g extract for fresh pulp vs 26.3 and 29.3 mg/g extract for roasted and steamed samples, respectively). Pulp was found to be the most active in 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) (IC50 of 0.1 mg/mL), whereas peel showed the highest activity in 2,2-diphenyl-1-picrylhydrazyl (DPPH) test (IC50 of 0.4 mg/mL). Moreover, peel exhibited the highest inhibitory activity against α-amylase with an IC50 of 0.2 mg/mL, except for steamed cooking process, which drastically influenced the bioactivity against both enzymes.
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Antioxidantes/farmacología , Metabolismo de los Hidratos de Carbono/efectos de los fármacos , Cucurbitaceae/enzimología , Extractos Vegetales/farmacología , Hojas de la Planta/enzimología , Antioxidantes/análisis , Ácido Ascórbico/análisis , Carotenoides/análisis , Culinaria , Flavonoides/análisis , Hidrólisis , Modelos Lineales , Fenoles/análisis , Fitoquímicos/análisis , Fitoquímicos/farmacología , Extractos Vegetales/análisis , alfa-Amilasas/metabolismo , alfa-Glucosidasas/metabolismoRESUMEN
Citrus × limon cv. Femminello Comune (Rutaceae) from Rocca Imperiale (Italy), one of the six Protected Geographical Indication (PGI) Italian lemon crops, has been recently received renewed interest. In this work, fresh and dried peels and leaves were extracted by hydrodistillation, supercritical fluid extraction (SFE), and Soxhlet apparatus. Chemical profile was assessed by gas chromatography (GC) and gas chromatography/mass spectrometry (GC/MS). Except for leaves extracts obtained by Soxhlet apparatus, the monoterpene hydrocarbons fraction dominated. Limonene, γ-terpinene, and ß-pinene were the main identified compounds. The antioxidant activity was investigated using different in vitro assays namely 2,2-diphenyl-1-picrylhydrazyl (DPPH), ABTS, ferric reducing ability power (FRAP), and ß-carotene bleaching test. In DPPH test, the essential oil obtained by hydrodistillation of fresh peel exhibited the highest activity (IC50 of 1.17 mg/ml). Leaves extracted by SFE showed a good activity in both DPPH and ß-carotene bleaching test with IC50 values of 2.20 and 6.66 mg/ml, respectively. Monoterpene hydrocarbons fraction exhibited a positive Pearson's correlation coefficient with all antioxidant assays. Leaves, often considered waste material, should be considered from a different point because they represent a matrix of indisputable interest.
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Antioxidantes/química , Citrus/química , Aceites Volátiles/química , Extractos Vegetales/química , Rutaceae/química , Antioxidantes/aislamiento & purificación , Cromatografía de Gases , Italia , Espectrometría de Masas , Aceites Volátiles/aislamiento & purificación , Extractos Vegetales/aislamiento & purificaciónRESUMEN
Dementia is becoming a major public health problem worldwide. The most common form of dementia is Alzheimer's disease (AD), characterized by a deficient cholinergic transmission, deposition of amyloid plaques and neurofibrillary tangles, and neuro-inflammation that result in progressive degeneration and/or death of nerve cells and cognitive impairment. At present, AD cannot be prevented or cured, so the symptomatic relief obtainable by the use of acetylcholinesterase (AChE) inhibitors is one of the therapeutic strategies. Accumulated evidence suggests that naturally occurring compounds may potentially improve memory and cognitive function, and prevent neurodegeneration. Even today the search for new neuroprotective agents of natural origin is very active. The neuroprotective effects of medicinal plants covering studies of the last years will be summarized and discussed in this review choosing a family classification with particular emphasis on extracts and isolated compounds as promising new drugs. The search of a multifunctional potential anti-AD agent able to act on different crucial targets, such as galanthamine, quercetin and timosaponin AIII, could be a useful approach to recognizing therapeutics against AD.
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Inhibidores de la Colinesterasa/aislamiento & purificación , Inhibidores de la Colinesterasa/uso terapéutico , Demencia/tratamiento farmacológico , Fármacos Neuroprotectores/aislamiento & purificación , Fármacos Neuroprotectores/uso terapéutico , Plantas Medicinales/química , Animales , Inhibidores de la Colinesterasa/química , Humanos , Fármacos Neuroprotectores/químicaRESUMEN
This study aimed to investigate the antidiabetic, antilipidaemic and antioxidant activities of Citrus medica cv Diamante (Rutaceae) hydroalcoholic (CD) peel extract in Zucker diabetic fatty (ZDF) rats. The ability of CD to protect against oxidative stress was investigated by using different in vitro assays and in vivo by using the reactive oxygen metabolites-derived compounds (d-ROMs) test and the biological antioxidant potential test (BAP). Two different doses of CD extract (300 and 600 mg/kg/die) were administered at ZDF rats for 4 weeks. CD reduced cholesterol and triglycerides levels. A dose-dependent effect on body weight and serum glucose levels was observed. A decrease of d-ROMs and an increase of BAP were recorded by using the dose of 600 mg/kg. The extract inhibited lipid peroxidation (IC50 value of 0.23 mg/ml). These findings suggest as an efficient phytotherapeutic approach in combating hyperlipidaemic and hyperglycaemic disorders.
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Glucemia/metabolismo , Citrus/química , Diabetes Mellitus Experimental/sangre , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/farmacología , Animales , Masculino , Ratas , Ratas ZuckerRESUMEN
Edible flowers are receiving renewed interest as rich sources of bioactive compounds. Ethanol extracts of eight edible flowers were phytochemically characterized and investigated for their bioactivity. Rutin, quercetin, luteolin, kaempferol, and myricetin were selected as standards and quantified by HPLC. The fatty acid profile was analyzed by GC and GC-MS. Antioxidant properties were evaluated by using different in vitro tests. The hypoglycemic effects were investigated via the inhibition of α-amylase and α-glucosidase. Sambucus nigra exhibited the highest radical-scavenging activity (IC50 of 1.4 µg/mL), followed by Hedysarum coronarium (IC50 of 1.6 µg/mL). Both species contained high quercetin and rutin contents. S. nigra extract exerted the highest activity in preventing lipid oxidation. Malva sylvestris extract inhibited both α-amylase and α-glucosidase with IC50 values of 7.8 and 11.3 µg/mL, respectively. These findings support the consumption of edible flowers as functional foods and their use as sources of natural antioxidants by the food industry.
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Antioxidantes/análisis , Flores/química , Inhibidores de Glicósido Hidrolasas/análisis , Hipoglucemiantes/análisis , Fitoquímicos/análisis , Antioxidantes/química , Antioxidantes/farmacología , Compuestos de Bifenilo/química , Compuestos de Bifenilo/farmacología , Cromatografía Líquida de Alta Presión , Ácidos Grasos/análisis , Flavonoides/análisis , Cromatografía de Gases y Espectrometría de Masas , Inhibidores de Glicósido Hidrolasas/química , Inhibidores de Glicósido Hidrolasas/farmacología , Hipoglucemiantes/química , Hipoglucemiantes/farmacología , Concentración 50 Inhibidora , Quempferoles/análisis , Luteolina/análisis , Fenoles/análisis , Fitoquímicos/química , Fitoquímicos/farmacología , Picratos/química , Picratos/farmacología , Plantas Medicinales/química , Quercetina/análisis , Quercetina/metabolismo , Rutina/análisis , Sambucus nigra/química , alfa-Amilasas/antagonistas & inhibidores , alfa-Amilasas/metabolismoRESUMEN
BACKGROUND: The aim of this study is to evaluate, for the first time, the chemical profile, antioxidant properties and cholinesterase inhibitory activity of dried fruits and honey of Ficus carica (fig) cultivars Dottato, Citrullara, and San Francesco. RESULTS: Gas chromatography-mass spectrometry (GC-MS) analysis of fig extracts identified terpenes, sterols and fatty acids as major constituents. The aroma profile of honey obtained from a mixture of the three cultivars was investigated by solid-phase micro-extraction/GC-MS. 5-(Hydroxymethyl)-2-furancarboxaldehyde, 2,3-dihydro-3,5-dihydroxy-6-methyl-4H-pyran-4-one and 1,3-dihydroxy-2-propanone were the main compounds. Total phenol, flavonoid and anthocyanin content are also reported. The San Francesco cultivar is characterised by the highest phenol and flavonoid content, while Dottato showed the major anthocyanin content. The Dottato cultivar exhibited the best radical scavenging activity against both 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) and 2,2-diphenyl-1-picrylhydrazyl radicals (IC50 values of 5.4 and 22.6 µg mL(-1) , respectively). This cultivar also showed the highest inhibitory activity against both acetylcholinesterase and butyrylcholinesterase, with IC50 values of 26.9 and 31.8 µg mL(-1) , respectively. CONCLUSION: Dried figs are a convenient source of bioactive compounds that demonstrated potential neuroprotection and antioxidant effects. Therefore, the addition of figs to the human diet should be recommended by dieticians and nutritionists.
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Antioxidantes/farmacología , Inhibidores de la Colinesterasa/farmacología , Ficus/química , Frutas/química , Miel/análisis , Extractos Vegetales/farmacología , Acetilcolinesterasa/metabolismo , Animales , Antocianinas/análisis , Antocianinas/farmacología , Antioxidantes/análisis , Compuestos de Bifenilo/metabolismo , Butirilcolinesterasa/metabolismo , Inhibidores de la Colinesterasa/análisis , Desecación , Dieta , Electrophorus , Ficus/clasificación , Humanos , Lípidos/análisis , Picratos/metabolismo , Extractos Vegetales/química , Polifenoles/análisis , Polifenoles/farmacología , Especificidad de la Especie , Terpenos/análisisRESUMEN
Cardiospermum halicacabum is widely used in traditional medicine. Previous studies have focused on the aerial parts, while the seeds have been poorly investigated. This work aimed to analyse the chemical composition of extracts from aerial parts and seeds obtained using Naviglio and Soxhlet (PN, PS, and SN, SS, respectively), the inhibitory properties against tyrosinase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) and the antioxidant effects. PN total extract showed significant anti-tyrosinase activity (IC50 value of 10.8 µg/mL). After partitioning with n-hexane, an HPLC method for analysing chemical constituents was established. Apigenin, luteolin, and apigenin-7-O-glucoside are the predominant constituents. SN n-hexane fraction was the most active inhibitor of BChE (IC50 of 57.9 µg/mL). Gas chromatography-mass spectrometry analysis revealed fatty acids, including eicosanoic acid, methyl 11-eicosenoate and oleic acid, as the major constituents. These findings suggest the potentiality of both seeds and aerial parts of C. halicacabum in the treatment of neurological disorders.
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Antioxidantes/farmacología , Inhibidores Enzimáticos/farmacología , Enfermedades Neurodegenerativas/tratamiento farmacológico , Fármacos Neuroprotectores/farmacología , Componentes Aéreos de las Plantas/química , Sapindaceae/química , Semillas/química , Acetilcolinesterasa/metabolismo , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Butirilcolinesterasa/metabolismo , Relación Dosis-Respuesta a Droga , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/aislamiento & purificación , Humanos , Monofenol Monooxigenasa/antagonistas & inhibidores , Monofenol Monooxigenasa/metabolismo , Enfermedades Neurodegenerativas/enzimología , Enfermedades Neurodegenerativas/metabolismo , Fármacos Neuroprotectores/química , Fármacos Neuroprotectores/aislamiento & purificación , Relación Estructura-ActividadRESUMEN
OBJECTIVES: This study involves for the first time the evaluation of Berberis aetnensis C. Presl. and Berberis libanotica Ehrenb. ex C.K. Schneid. roots for anticholinesterase and antioxidant properties, with the aim to search compounds possibly useful for the treatment of Alzheimer's disease (AD). METHODS: Samples were evaluated for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The antioxidant activity was assayed by 2,2-diphenyl-1-picrylhydrazyl radical and ß-carotene bleaching tests. Berberine and palmatine were isolated by flash chromatography and identified by spectrometric methods as main constituents. Non-polar compounds were analysed by gas chromatography and gas chromatography-mass spectrometry. KEY FINDINGS: Extracts, fractions and isolated compounds inhibited AChE and BChE to varying degrees. The methanol fractions exhibited the strongest AChE inhibitory activity with inhibitory concentration 50% (IC50 ) of 7.6 and 16.9 µg/ml for B. aetnensis and B. libanotica, respectively. The alkaloid fraction of B. aetnensis inhibited AChE (IC50 of 24.5 µg/ml) and possessed the highest antioxidant activity (IC50 value of 2.2 µg/ml in ß-carotene-bleaching test after 30 min of incubation). Berberine was more potent of palmatine against AChE (IC50 of 2.2 and 7.4 µg/ml, respectively). CONCLUSIONS: These findings raise the possibility of developing B. aetnensis and B. libanotica as a promising candidate for the treatment of AD.
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Enfermedad de Alzheimer/tratamiento farmacológico , Antioxidantes/farmacología , Berberis/química , Inhibidores de la Colinesterasa/farmacología , Extractos Vegetales/farmacología , Alcaloides/aislamiento & purificación , Alcaloides/farmacología , Enfermedad de Alzheimer/metabolismo , Berberina/farmacología , Humanos , Estrés OxidativoRESUMEN
The search for improved cytotoxic agents continues to be an important line in the discovery of modern anticancer drugs. Sarcopoterium spinosum (L.) Spach is mentioned in ethnobotanical surveys as a medicinal plant used for the treatment of cancer. The aim of this study is to investigate and to compare the aerial parts of S. spinosum collected in Italy and Lebanon for their chemical composition and their antiproliferative activity against ACHN, C32, A375, MCF-7, LNCaP and HeLa human cancer cell lines using SRB assay. The main constituent tormentic acid was isolated by MPLC and characterized by spectroscopic techniques (NMR, MS). Non polar compounds were analyzed by GC and GC-MS. S. spinosum showed an interesting antiproliferative activity against ACHN and C32 cell lines with IC(50) values of 2.4 and 2.7 µg/ml for S. spinosum from Italy and Lebanon, respectively. Remarkable results were obtained also against A375 and LNCaP cell lines. The cytotoxicity against ACHN cell line could be partially attributed to tormentic acid that demonstrated a higher cytotoxicity than the positive control vinblastine. Close association between the radical scavenging activity (evaluated by DPPH and ABTS assay) and cytotoxicity was also demonstrated. This investigation demonstrated the potential cytotoxic activity of S. spinosum taking into account also that none of the tested extracts, fractions and isolated compound affected the proliferation of normal cell line 142BR. Tormentic acid, the major constituent isolated from S. spinosum, play an important role in the cytotoxicity exhibited by the extract.
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Componentes Aéreos de las Plantas , Extractos Vegetales/farmacología , Plantas Medicinales , Triterpenos/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/aislamiento & purificación , Depuradores de Radicales Libres/farmacología , Inhibidores de Crecimiento/química , Inhibidores de Crecimiento/aislamiento & purificación , Inhibidores de Crecimiento/farmacología , Células HeLa , Humanos , Neoplasias Renales/tratamiento farmacológico , Neoplasias Renales/patología , Células MCF-7 , Masculino , Melanoma Experimental/tratamiento farmacológico , Melanoma Experimental/patología , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Neoplasias de la Próstata/tratamiento farmacológico , Neoplasias de la Próstata/patología , Triterpenos/química , Triterpenos/aislamiento & purificaciónRESUMEN
The antioxidant and anti-cholinesterase properties of Globularia meridionalis (Podp.) O. Schwarz (Globulariaceae) were investigated. G. meridionalis aerial parts and roots were extracted with methanol, and the total extract successively partitioned with n-hexane. The methanol fraction of the roots showed the highest antioxidant activity with IC50 values of 8.0 and 2.1 microg/mL in the DPPH and beta-carotene bleaching tests, respectively. From this fraction, three flavonoids, namely pectolinarigenin 7-O-beta-glucoside, apigenin 7-O-beta-glucoside and luteolin, and two phenylethanoids, namely acteoside and isoacteoside, were isolated. Potential anti-cholinesterase effects were assessed through the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes inhibition assay. The n-hexane fraction of the roots exhibited the highest activity against both AChE and BChE with IC50 values of 65.5 and 70.4 microg/mL, respectively.