RESUMEN
Amyloidoses represent a group of pathological conditions characterized by amyloid fibrils accumulating in the form of deposits in intra- or extracellular space, leading to tissue damage. The lysozyme from hen egg-white (HEWL) is often used as a universal model protein to study the anti-amyloid effects of small molecules. The in vitro anti-amyloid activity and mutual interactions of green tea leaf constituents: (-)-epigallocatechin gallate (EGCG), (-)-epicatechin (EC), gallic acid (GA), caffeine (CF) and their equimolar mixtures were studied. The inhibition of HEWL amyloid aggregation was monitored by a Thioflavin T fluorescence assay and atomic force microscopy (AFM). The interactions of the analyzed molecules with HEWL were interpreted by ATR-FTIR and protein-small ligand docking studies. EGCG was the only substance efficiently inhibiting amyloid formation (IC50 â¼193 µM), slowing the aggregation process, reducing the number of fibrils and partially stabilizing the secondary structure of HEWL. Compared to EGCG alone, EGCG-containing mixtures displayed lower overall anti-amyloid efficacy. The decrease in efficiency results from (a) the spatial interference of GA, CF and EC with EGCG while binding to HEWL, (b) the propensity of CF to form a less active adduct with EGCG, which participates in interactions with HEWL in parallel with pure EGCG. This study confirms the importance of interaction studies, revealing the possible antagonistic behavior of molecules when combined.
Asunto(s)
Amiloide , Muramidasa , Amiloide/química , Muramidasa/química , Proteínas Amiloidogénicas , Cafeína/farmacología , Té , Hojas de la Planta/metabolismo , Agregado de ProteínasRESUMEN
The worldwide prevalence of gastrointestinal diseases is about 40%, with standard pharmacotherapy being long-lasting and economically challenging. Of the dozens of diseases listed by the Rome IV Foundation criteria, for five of them (heartburn, dyspepsia, nausea and vomiting disorder, constipation, and diarrhoea), treatment with herbals is an official alternative, legislatively supported by the European Medicines Agency (EMA). However, for most plants, the Directive does not require a description of the mechanisms of action, which should be related to the therapeutic effect of the European plant in question. This review article, therefore, summarizes the basic pharmacological knowledge of synthetic drugs used in selected functional gastrointestinal disorders (FGIDs) and correlates them with the constituents of medicinal plants. Therefore, the information presented here is intended as a starting point to support the claim that both empirical folk medicine and current and decades-old treatments with official herbal remedies have a rational basis in modern pharmacology.
Asunto(s)
Enfermedades Gastrointestinales , Plantas Medicinales , Estreñimiento , Enfermedades Gastrointestinales/tratamiento farmacológico , Medicina Tradicional , FitoterapiaRESUMEN
Fibroblasts are actively involved in the formation of granulation tissue and/or tumor stroma. These cells possess the potential to differentiate into myofibroblasts acquiring a highly contractile phenotype characterized by the expression of α-smooth muscle actin (SMA). Considering TGF-ß1 as the main inducer of myofibroblast differentiation and horse chestnut extract (HCE) as an effective modulator of the wound healing, we have new evidence to demonstrate canonical TGF-ß1/SMAD and non-canonical/non-SMAD signaling in normal fibroblasts, isolated from healthy human skin (human dermal fibroblasts - HDFs), and their malignant counterparts (CAFs) isolated from basal cell carcinoma (BCC) and squamous cell carcinoma (SCC) using western blot and immunofluorescence. Our study revealed that HCE stimulated the deposition of fibronectin by BCC fibroblasts (BCCFs), an effect not seen in other studied fibroblasts. Moreover, HCE in combination with TGF-ß1 showed a synergic effect on the presence of polymerized SMA-stress fibers, particularly visible in CAFs. Interestingly, the TGF-ß1 exposure led to activation of the canonical SMAD signaling in HDFs and BCCFs, whereas treatment of SCC fibroblasts (SCCFs) resulted in activation of the non-canonical AKT and/or ERK1/2 signaling. In conclusion, we observed specific differences in signaling between HDFs and CAFs that should be considered when developing new therapeutic approaches targeting wound/tumor microenvironments.
Asunto(s)
Aesculus , Fibroblastos Asociados al Cáncer , Carcinoma Basocelular , Carcinoma de Células Escamosas , Carcinoma de Células Escamosas/tratamiento farmacológico , Diferenciación Celular , Células Cultivadas , Fibroblastos , Humanos , Miofibroblastos , Extractos Vegetales/farmacología , Factor de Crecimiento Transformador beta1 , Microambiente TumoralRESUMEN
Medicinal plants are rich sources of valuable molecules with various profitable biological effects, including antimicrobial activity. The advantages of herbal products are their effectiveness, relative safety based on research or extended traditional use, and accessibility without prescription. Extensive and irrational usage of antibiotics since their discovery in 1928 has led to the increasing expiration of their effectiveness due to antibacterial resistance. Now, medical research is facing a big and challenging mission to find effective and safe antimicrobial therapies to replace inactive drugs. Over the years, one of the research fields that remained the most available is the area of natural products: medicinal plants and their metabolites, which could serve as active substances to fight against microbes or be considered as models in drug design. This review presents selected flavonoids (such as apigenin, quercetin, kaempferol, kurarinone, and morin) and tannins (including oligomeric proanthocyanidins, gallotannins, ellagitannins, catechins, and epigallocatechin gallate), but also medicinal plants rich in these compounds as potential therapeutic agents in oral infectious diseases based on traditional usages such as Agrimonia eupatoria L., Hamamelis virginiana L., Matricaria chamomilla L., Vaccinium myrtillus L., Quercus robur L., Rosa gallica L., Rubus idaeus L., or Potentilla erecta (L.). Some of the presented compounds and extracts are already successfully used to maintain oral health, as the main or additive ingredient of toothpastes or mouthwashes. Others are promising for further research or future applications.
Asunto(s)
Antiinfecciosos , Enfermedades Transmisibles , Plantas Medicinales , Taninos/metabolismo , Flavonoides/uso terapéutico , Extractos Vegetales , Plantas Medicinales/metabolismo , Taninos Hidrolizables/metabolismo , Antiinfecciosos/farmacología , Antiinfecciosos/uso terapéuticoRESUMEN
Bacterial infections of skin and wounds may seriously decrease the quality of life and even cause death in some patients. One of the largest concerns in their treatment is the growing antimicrobial resistance of bacterial infectious agents and the spread of resistant strains not only in the hospitals but also in the community. This trend encourages researchers to seek for new effective and safe therapeutical agents. The pharmaceutical industry, focusing mainly on libraries of synthetic compounds as a drug discovery source, is often failing in the battle with bacteria. In contrast, many of the natural compounds, and/or the whole and complex plants extracts, are effective in this field, inactivating the resistant bacterial strains or decreasing their virulence. Natural products act comprehensively; many of them have not only antibacterial, but also anti-inflammatory effects and may support tissue regeneration and wound healing. The European legislative is in the field of natural products medicinal use formed by European Medicines Agency (EMA), based on the scientific work of its Committee on Herbal Medicinal Products (HMPC). HMPC establishes EU monographs covering the therapeutic uses and safe conditions for herbal substances and preparations, mostly based on folk medicine, but including data from scientific research. In this review, the medicinal plants and their active constituents recommended by EMA for skin disorders are discussed in terms of their antibacterial effect. The source of information about these plant products in the review is represented by research articles listed in scientific databases (Science Direct, PubMed, Scopus, Web of Science, etc.) published in recent years.
Asunto(s)
Antibacterianos/uso terapéutico , Medicina Tradicional/métodos , Fitoterapia/métodos , Extractos Vegetales/uso terapéutico , Plantas Medicinales/química , Enfermedades Cutáneas Bacterianas/tratamiento farmacológico , Infección de Heridas/tratamiento farmacológico , Humanos , Enfermedades Cutáneas Bacterianas/microbiología , Infección de Heridas/microbiologíaRESUMEN
Exogenous insulin, used as a therapeutic agent for diabetes, forms insoluble deposits containing amyloid fibrillar structures near the administration site. We have analyzed the in vitro anti-amyloid activity of four green tea constituents: (-)-epigallocatechin gallate (EGCG), (-)-epicatechin (EC), gallic acid (GA), caffeine (CF), and their equimolar mixtures. Regarding individually tested compounds, only EGCG inhibited the fibrillization process. The individual EC, GA, and CF molecules were ineffective. The presence of EGCG in equimolar combinations with GA, EC, or CF was required for the inhibitory activity of most mixtures. Molecular docking revealed that EGCG interacts with an essential amyloidogenic region of insulin chain B. Individually inactive GA had a potentiating effect on the activity of EGCG. In contrast, EC and CF had a negative impact on the activity of the mixtures. We have observed diverse morphology and the amount of insulin amyloid aggregates formed in the presence of studied compounds. The distinct types of amyloid aggregates created in vitro in the presence of EGCG and other green tea constituents were characterized. Results indicate that the biological activity of individual molecules is not directly applicable to the pooled samples effects prediction.
Asunto(s)
Amiloide/química , Insulina/química , Agregado de Proteínas/fisiología , Té/química , Amiloide/metabolismo , Sitios de Unión , Cafeína/química , Cafeína/metabolismo , Catequina/análogos & derivados , Catequina/química , Catequina/metabolismo , Ácido Gálico/química , Ácido Gálico/metabolismo , Humanos , Insulina/metabolismo , Cinética , Simulación del Acoplamiento Molecular , Estructura Secundaria de Proteína , Té/metabolismoRESUMEN
The ability of horse chestnut extract (HCE) to induce contraction force in fibroblasts, a process with remarkable significance in skin repair, motivated us to evaluate its wound healing potential in a series of experiments. In the in vitro study of the ability of human dermal fibroblasts to form myofibroblast-like cells was evaluated at the protein level (Western blot and immunofluorescence). The in vivo study was conducted on male Sprague-Dawley rats with inflicted wounds (one open circular and one sutured incision) on their backs. Rats were topically treated with two tested HCE concentrations (0.1% and 1%) or sterile water. The control group remained untreated. The incisions were processed for wound tensile strength (TS) measurement whereas the open wounds were subjected to histological examination. On the in vitro level the HCE extract induced fibronectin-rich extracellular matrix formation, but did not induced α-smooth muscle actin (SMA) expression in dermal fibroblasts. The animal study revealed that HCE increased wound TS and improved collagen organization. In conclusion, the direct comparison of both basic wound models demonstrated that the healing was significantly increased following HCE, thus this extract may be found useful to improve healing of acute wounds. Nevertheless, the use of an experimental rat model warrants a direct extrapolation to the human clinical situation.
Asunto(s)
Aesculus/química , Matriz Extracelular/efectos de los fármacos , Matriz Extracelular/metabolismo , Miofibroblastos/efectos de los fármacos , Miofibroblastos/metabolismo , Extractos Vegetales/farmacología , Cicatrización de Heridas/efectos de los fármacos , Animales , Cromatografía Líquida de Alta Presión , Estructura Molecular , Extractos Vegetales/química , Ratas , Regeneración , Resistencia a la TracciónRESUMEN
The compositions of leaf infusions of three genotypes of Lycopus europaeus L. with origins in central Europe, namely L. europaeus A (LeuA), L. europaeus B (LeuB), and L. europaeus C (LeuC), and one genotype of L. exaltatus (Lex), were examined by LC-MS-DAD (Liquid Chromatography Mass Spectrometry and Diode Array Detection) analysis. This revealed the presence of thirteen compounds belonging to the groups of phenolic acids and flavonoids, with a predominance of rosmarinic acid (RA) and luteolin-7-O-glucuronide (LGlr). The antimicrobial activity of leaf infusions was tested on the collection strains of Gram-positive and Gram-negative bacteria, and on the clinical Staphylococcus aureus strains. We detected higher activity against Gram-positive bacteria, of which the most susceptible strains were those of Staphylococcus aureus, including methicillin-resistant and poly-resistant strains. Furthermore, we examined the antioxidant activity of leaf infusions using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) methods, and on NIH/3T3 cell lines using dichlorodihydrofluorescein diacetate (DCFH-DA). We also studied the mutual interactions between selected infusions, namely RA and/or LGlr. In the mixtures of leaf infusion and RA or LGlr, we observed slight synergism and a high dose reduction index in most cases. This leads to the beneficial dose reduction at a given antioxidant effect level in mixtures compared to the doses of the parts used alone. Therefore, our study draws attention to further applications of the Lycopus leaves as a valuable alternative source of natural antioxidants and as a promising topical antibacterial agent for medicinal use.
Asunto(s)
Antiinfecciosos/química , Antiinfecciosos/farmacología , Antioxidantes/química , Antioxidantes/farmacología , Lycopus/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Antibacterianos/química , Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Fitoquímicos/químicaRESUMEN
Macarpine is a minor benzophenanthridine alkaloid with interesting biological activities, which is produced in only a few species of the Papaveraceae family, including Eschscholzia californica. Our present study was focused on the enhancement of macarpine production in E. californica suspension cultures using three elicitation models: salicylic acid (SA) (4; 6; 8 mg/L) elicitation, and simultaneous or sequential combinations of SA and L-tyrosine (1 mmol/L). Sanguinarine production was assessed along with macarpine formation in elicited suspension cultures. Alkaloid production was evaluated after 24, 48 and 72 h of elicitation. Among the tested elicitation models, the SA (4 mg/L), supported by L-tyrosine, stimulated sanguinarine and macarpine production the most efficiently. While sequential treatment led to a peak accumulation of sanguinarine at 24 h and macarpine at 48 h, simultaneous treatment resulted in maximum sanguinarine accumulation at 48 h and macarpine at 72 h. The effect of SA elicitation and precursor supplementation was evaluated also based on the gene expression of 4'-OMT, CYP719A2, and CYP719A3. The gene expression of investigated enzymes was increased at all used elicitation models and their changes correlated with sanguinarine but not macarpine accumulation.
Asunto(s)
Benzofenantridinas/biosíntesis , Eschscholzia/efectos de los fármacos , Reguladores del Crecimiento de las Plantas/farmacología , Ácido Salicílico/farmacología , Tirosina/farmacología , Sistema Enzimático del Citocromo P-450/biosíntesis , Sistema Enzimático del Citocromo P-450/genética , Relación Dosis-Respuesta a Droga , Eschscholzia/genética , Eschscholzia/crecimiento & desarrollo , Eschscholzia/metabolismo , Regulación de la Expresión Génica de las Plantas , Hidroponía/métodos , Isoquinolinas , Metiltransferasas/biosíntesis , Metiltransferasas/genética , Proteínas de Plantas/agonistas , Proteínas de Plantas/genética , Proteínas de Plantas/metabolismo , Tirosina/metabolismoRESUMEN
In the previous study, the artichoke leaf extract showed effective inhibition of AKR1B1, the first enzyme of polyol pathway, which reduces high level of glucose to osmotically active sorbitol, important for development of chronic diabetic complications. In the present study, the effect of artichoke leaf extract and of several participating phenols (caffeic acid, chlorogenic acid, quinic acid, and luteolin) was tested on sorbitol level in rat lenses exposed to high glucose ex vivo, on cytotoxicity as well as on oxidative stress in C2C12 muscle cell line induced by high glucose in vitro. The concentration of sorbitol was determined by enzymatic analysis, the cytotoxicity was provided by WST-1 test and intracellular content of reactive oxygen species was determined by fluorescence of 2'-7'-dichlorofluorescein probe. The extract and the compounds tested showed significant protection against toxic effects of high concentration of glucose in both models. On balance, the artichoke leaf extract thus represents a prospective preventive agent of development of chronic diabetic complications, probably due to phenols content, concerning preclinical and clinical studies.
Asunto(s)
Cynara scolymus/química , Glucosa/farmacología , Cristalino/efectos de los fármacos , Extractos Vegetales/farmacología , Hojas de la Planta/química , Sorbitol/metabolismo , Aldehído Reductasa/antagonistas & inhibidores , Animales , Células Cultivadas , Relación Dosis-Respuesta a Droga , Inhibidores Enzimáticos/farmacología , Cristalino/metabolismo , Ratones , Técnicas de Cultivo de Órganos , Estrés Oxidativo/efectos de los fármacos , Ratas , Especies Reactivas de Oxígeno/farmacologíaRESUMEN
Although it has been shown that oestrogen replacement therapy is able to improve wound healing, several side effects of this replacement therapy have precluded its common use in clinical practice. On the other hand, the phytoestrogen genistein (the selective oestrogen receptor modulator belonging to the group of isoflavones) has been introduced into several clinical trials to improve cancer treatment efficiency and experiments suggest its positive effect on wound healing. The main mechanisms of action, which have been elucidated so far, include induction of apoptosis, cell cycle arrest, inhibition of angiogenesis and tyrosine kinase activity as well as cancer chemoprevention and reduction of climacteric symptoms. Unfortunately, all underlying mechanism in the modulation of biological processes involved in wound healing and tumour growth are not yet fully understood. Therefore, the present review summarizes the effects of genistein on biological processes in different wound healing models and selected tumours. Key words: genistein ⢠tissue repair and regeneration ⢠carcinoma ⢠skin.
Asunto(s)
Genisteína/farmacología , Neoplasias/tratamiento farmacológico , Cicatrización de Heridas/efectos de los fármacos , Humanos , Fitoestrógenos/farmacologíaRESUMEN
The basal production of secondary metabolites in medicinal plants is limited. One of the effective approaches that encourages plants to produce a remarkable amount of precious compounds is an application of elicitors. Our work was focused on the elicitation of Eschscholzia californica Cham. suspension cultures using various concentrations of MnCl2 (5; 10; 15 mg/L) with the aim of evaluating its effect on sanguinarine, chelerythrine, and macarpine production and gene expression of enzymes involved in the biosynthesis of mentioned secondary metabolites (BBE, 4'-OMT, CYP80B1) or in defense processes (LOX). Suspension cultures were exposed to elicitor for 24, 48, and 72 h. The content of alkaloids in phytomass was determined on the basis of their fluorescence properties. The relative mRNA expression of selected genes was analyzed using the ΔΔCt value method. PCR products were evaluated by melting curve analysis to confirm the specific amplification. Our results demonstrated that Eschscholzia californica Cham. cell suspension cultures evince sensitivity to the presence of MnCl2 in growth media resulting in the increased production of benzophenanthridine alkaloids and gene expression of selected enzymes. Manganese chloride seems to be a potential elicitor supporting natural biosynthetic properties in plant cell cultures and can be applied for the sustained production of valuable secondary metabolites.
Asunto(s)
Cloruros/metabolismo , Eschscholzia/metabolismo , Compuestos de Manganeso/metabolismo , Alcaloides/biosíntesis , Vías Biosintéticas/efectos de los fármacos , Cloruros/farmacología , Eschscholzia/efectos de los fármacos , Eschscholzia/genética , Compuestos de Manganeso/farmacologíaRESUMEN
Basil (Ocimum L.) species are used as medicinal plants due to their essential oils exhibiting specific biological activity. The present work demonstrated that both the variety and season/conditions of cultivation had a significant effect on (i) the produced amount (extraction yield), (ii) qualitative, as well as (iii) quantitative profile of basil essential oil. Among studied basil varieties, a new variety, 'Mánes', was characterized for the first time. Based on our quantitative evaluation of GC-MS profiles, the following chemotypes and average concentrations of a main component were detected in the studied basil varieties: 'Ohre', 'Lettuce Leaf', 'Purple Opaal', 'Dark Green' (linalool, 5.99, 2.49, 2.34, 2.01 mg/mL, respectively), and 'Mammolo Genovese', 'Mánes', 'Red Rubin' (eucalyptol, 1.34, 0.96, 0.76 mg/mL, respectively). At the same time, when considering other compounds identified in GC-MS profiles, all the studied varieties, except from 'Lettuce Leaf', were methyl eugenol-rich with a strong dependence of the eugenol:methyl eugenol ratio on the seasonal changes (mainly solar irradiation, but also temperature and relative humidity). More complex and/or variable (depending on the season and cultivation) chemotypes were observed with 'Lettuce Leaf' (plus estragole, 2.27 mg/mL), 'Dark Green' (plus eucalyptol, 1.36 mg/mL), 'Mammolo Genovese' (plus eugenol, 1.19 mg/mL), 'Red Rubin' (plus linalool and eugenol, 0.46 and 0.56 mg/mL, respectively), and 'Mánes' (plus linalool and eugenol, 0.58 and 0.40 mg/mL, respectively). When considering superior extraction yield (ca. 17 mL·kg-1, i.e., two to five times higher than other examined varieties) and consistent amounts (yields) of essential oil when comparing inter-seasonal or inter-year data (RSD and inter-year difference in mean yield values Ë2.5%), this new basil variety is very promising for use in the pharmaceutical, food, and cosmetic industries.
Asunto(s)
Cromatografía de Gases y Espectrometría de Masas/métodos , Ocimum basilicum/química , Aceites Volátiles/análisis , Hojas de la Planta/química , Monoterpenos Acíclicos , Derivados de Alilbenceno , Anisoles/análisis , Ciclohexanoles/análisis , Eucaliptol , Eugenol/análogos & derivados , Eugenol/análisis , Monoterpenos/análisis , Ocimum , Aceites de Plantas/análisisRESUMEN
The human intracellular enzyme AKR1B1 belongs to the aldo-keto reductase superfamily. The AKR1B1-catalyzed reduction of aldehydes is part of the intracellular inflammatory pathway leading to the activation of NF-κB and the expression of pro-inflammatory genes. The present study is aimed at determining the inhibition of AKR1B1 brought about by an extract of artichoke leaves (bracts), and the effects of this extract and three participating compounds on the expression of AKR1B1, COX-2, and MMP-2 proteins in THP-1 cells. It seeks to identify the ability of the test substances to modulate the lipopolysaccharide (LPS)-induced activation of NF-κB in cells and the intracellular oxidant effect of test substances after incubation with LPS. Low concentrations of the extract inhibit the enzyme AKR1B1. After stimulation by LPS, the extract attenuated the activity of NF-κB in THP-1 cells, but no changes in the expression of AKR1B1 were recorded. The extract diminished the expression of the inflammation-related enzymes COX-2 and MMP-2, probably by inhibiting the activity of NF-κB. The extract significantly diminished the intracellular reactive oxygen species after a brief LPS incubation, which may also have reduced intracellular inflammation. The diminished activity of NF-κB in the cells could be linked to the inhibition of the activity of AKR1B1. Copyright © 2017 John Wiley & Sons, Ltd.
Asunto(s)
Aldehído Reductasa/antagonistas & inhibidores , Cynara scolymus/química , Leucemia/patología , Extractos Vegetales/farmacología , Hojas de la Planta/química , Aldehído Reductasa/genética , Aldehído Reductasa/metabolismo , Animales , Células Cultivadas , Ciclooxigenasa 2/metabolismo , Regulación hacia Abajo/efectos de los fármacos , Regulación de la Expresión Génica/efectos de los fármacos , Humanos , Inflamación/inducido químicamente , Inflamación/genética , Inflamación/metabolismo , Leucemia/genética , Leucemia/metabolismo , Lipopolisacáridos , Metaloproteinasa 2 de la Matriz/genética , Metaloproteinasa 2 de la Matriz/metabolismo , Ratas , Transducción de Señal/efectos de los fármacos , Transducción de Señal/genética , Factor de Transcripción ReIA/antagonistas & inhibidores , Factor de Transcripción ReIA/metabolismoRESUMEN
This overview paper describes in its introductory part bitter-tasting herbal drugs in the context of their traditional use in the loss of appetite and digestive disorders. Then, it mentions current knowledge on signals origin in bitter taste receptors leading to different, unexpected physiological processes. Newly observed biological effects of bitter tastants are correlated with modern trends of their complex study with an aim to develop new drugs primarily acting on bitter taste receptors.Key words: T2R bitter taste receptors GPCR bitters glucose homeostasis asthma ghrelin GLP-1 solitary chemosensory cells.
Asunto(s)
Preparaciones de Plantas , Gusto , Humanos , Receptores Acoplados a Proteínas G/efectos de los fármacos , Receptores Acoplados a Proteínas G/fisiologíaRESUMEN
Diabetes mellitus (DM) is frequently diagnosed at a time when patients already suffer from several cardiovascular complications. Our previously published data (Molecules 201520 (11): 20538-50) on the anti-oxidative properties of Agrimonia eupatoria L. (AE) and Cynara cardunculus L. (CC) prompted us to extend the available evidence on their possible protective activities on selected DM-related parameters in a streptozotocin-induced DM rat model and in a series of in vitro experiments. Male rats were divided into four groups: control group, untreated diabetic group, AE and CC treated diabetic groups. During a five-week period, changes in blood glucose and body weight were monitored. Then, rats were sacrificed and subjected to the assessment of changes in the reactivity of aortas and measurement of butyrylcholinesterase activity. To complete the panel of experiments, α-glucosidase activity was assessed in vitro. Our results demonstrate that both tested extracts exert similar anti-diabetic activities. However, better anti-oxidant activity of the A. eupatoria extract indicates its higher clinical potential in the prevention and/or adjuvant therapy of developing cardiovascular complications related to DM and diseases associated with oxidative stress.
Asunto(s)
Agrimonia/química , Cynara/química , Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/administración & dosificación , Extractos Vegetales/administración & dosificación , Animales , Antioxidantes/administración & dosificación , Antioxidantes/farmacología , Glucemia/análisis , Peso Corporal/efectos de los fármacos , Butirilcolinesterasa/metabolismo , Diabetes Mellitus Experimental/metabolismo , Regulación de la Expresión Génica , Humanos , Hipoglucemiantes/farmacología , Extractos Vegetales/farmacología , Ratas , EstreptozocinaRESUMEN
Reactive oxygen species (ROS) are highly considered in the ethiopathogenesis of different pathological conditions because they may cause significant damage to cells and tissues. In this paper, we focused on potential antioxidant properties of two medical plants such as the Agrimonia eupatoria L. and Cynara cardunculus L. Both plants have previously been studied for their pharmacological activities, especially as hepatoprotective and hypoglycemic activities. It has been suggested, that their effects are related to the antioxidant properties of polyphenols, which are dominant compounds of the plants' extracts. In the present study HPLC-MS analysis of water infusion was performed allowing the identification of several phenolic constituents. Furthermore, antioxidant effects of the two extracts were compared showing higher effects for agrimony extract compared to artichoke. Thus, agrimony was selected for the in vivo study using the skin flap viability model. In conclusion, our results provide evidence that the A. eupatoria extract may be a valuable source of polyphenols to be studied for the future development of supplements useful in the prevention of diseases linked to oxidative stress.
Asunto(s)
Agrimonia/química , Antioxidantes/química , Cynara/química , Fenoles/química , Extractos Vegetales/química , Animales , Antioxidantes/farmacología , Catalasa/metabolismo , Línea Celular/efectos de los fármacos , Línea Celular/metabolismo , Supervivencia Celular/efectos de los fármacos , Cromatografía Líquida de Alta Presión , Daño del ADN/efectos de los fármacos , Humanos , Estrés Oxidativo/efectos de los fármacos , Fenoles/farmacología , Extractos Vegetales/farmacología , Ratas , Especies Reactivas de Oxígeno/metabolismo , Superóxido Dismutasa/metabolismoRESUMEN
The aim of this study was to test the effect of Pycnogenol(®) (PYC) mixture and its three fractions (buthanolic, water, ethyl acetate) on heart function in rats with experimental diabetes mellitus (DM) and compare their effects to the diabetic group. Their antioxidant activity "in vitro" was also determined. DM rats (streptozotocin over 3 consecutive days at a dose of 25 mg/kg of body weight) had increased systolic blood pressure, thicker left ventriculi wall (LV) and weaker myocardial contraction, prolonged QT interval in comparison to controls rats. In comparison to the diabetic group, PYC (20 mg/kg b.w./day) suppressed the influence of DM on the LV, improved contraction, increased coronary flow and displayed negative effect on electrical activity of hearts. The most effective of PYC's fractions was the water fraction. It improved biometric parameters and hemodynamic function of the DM hearts, enhanced shortening the QT interval, reduced the amount of dysrhythmias of the DM hearts and had the strongest antioxidant activity. In conclusion, DM damaged isolated rat heart function. Only the water fraction improved the function of the diabetic heart. The different results of three fractions and PYC on myocardial function may be caused by a various lipo- and hydro-philic action of the PYC components.
Asunto(s)
Antioxidantes/farmacología , Cardiotónicos/farmacología , Diabetes Mellitus Experimental/fisiopatología , Flavonoides/farmacología , Corazón/efectos de los fármacos , Animales , Antioxidantes/administración & dosificación , Cardiotónicos/administración & dosificación , Flavonoides/administración & dosificación , Corazón/fisiología , Técnicas In Vitro , Masculino , Extractos Vegetales , Distribución Aleatoria , Ratas , Ratas WistarRESUMEN
The purpose of this study was to detect the effectiveness of Cotinus coggygria Scop. leaves methanol extract against planktonic and biofilm growth forms of Staphylococcus aureus. The antimicrobial activity was determined by the broth microdilution test. Minimal inhibitory concentrations and minimal bactericidal concentrations were detected against two collection and ten clinical S. aureus strains. Anti-biofilm activity of the tested extract was detected using 24 h bacterial biofilm on the surface of microtiter plate wells. The biofilm inhibitory activity was evaluated visually after 24 h interaction of extract with biofilm, and the eradicating activity by a regrowth method. The tested extract showed bactericidal activity against all S. aureus strains (methicillin susceptible or methicillin resistant) in concentrations ranging from 0.313 to 0.625 mg·mL(-1). Biofilm inhibitory concentrations were 10-times higher and biofilm eradicating concentrations 100-times higher (8 and 32 mg·mL(-1), respectively). The phytochemical analysis of C. coggygria leaves 60% methanol extract performed by LC-DAD-MS/MS revealed quercetin rhamnoside, methyl gallate, and methyl trigallate as main constituents. Results of our study indicate that C. coggygria, rich in tannins and flavonoids, seems to be a prospective topical antibacterial agent with anti-biofilm activity.
Asunto(s)
Anacardiaceae/química , Antibacterianos/farmacología , Metanol/farmacología , Hojas de la Planta/química , Staphylococcus aureus/efectos de los fármacos , Antibacterianos/química , Biopelículas/efectos de los fármacos , Metanol/química , Metanol/aislamiento & purificación , Pruebas de Sensibilidad Microbiana , Plancton/efectos de los fármacos , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Espectrometría de Masas en TándemRESUMEN
OBJECTIVES: Although the exact underlying mechanisms are still unknown, Plantago lanceolataâ L. (PL) water extracts are frequently used to stimulate wound healing and to drain abscesses. Therefore, in this experimental study the effect of PL water extract on skin wound healing was studied in Sprague-Dawley rats. METHODS: Two excisional and one incisional skin wounds were performed on the back of each rat. Wounds were treated for three consecutive days with two different concentrations of the aqueous extract of PL. Rats were sacrificed 7, 14, and 21 days after surgery. Samples of wounds were processed for macroscopic (excisions - wound contraction measurement), biomechanical (incisions - wound tensile strength (TS) measurement) and histological examination (excisions). KEY FINDINGS: It was shown that open wounds treated with PL extract contained myofibroblasts and demonstrated significantly higher contraction rates. Furthermore, significantly increased wound TSs were recorded in treated rats as a consequence of increased organization of extracellular matrix proteins, such as the collagen type 1. CONCLUSIONS: We demonstrated that PL aqueous extract improves skin wound healing in rats. However, further research need to be performed to find optimal therapeutic concentration, and exact underlying mechanism prior obtained results may be introduced into the clinical practice.