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1.
Plants (Basel) ; 13(6)2024 Mar 08.
Artículo en Inglés | MEDLINE | ID: mdl-38592845

RESUMEN

Withania somnifera (L.) Dunal is a medicinal plant belonging to the traditional Indian medical system, showing various therapeutic effects such as anti-cancer, anti-inflammatory, anti-microbial, anti-diabetic, and hepatoprotective activity. Of great interest is W. somnifera's potential beneficial effect against neurodegenerative diseases, since the authorized medicinal treatments can only delay disease progression and provide symptomatic relief and are not without side effects. A systematic search of PubMed and Scopus databases was performed to identify preclinical and clinical studies focusing on the applications of W. somnifera in preventing neurodegenerative diseases. Only English articles and those containing the keywords (Withania somnifera AND "neurodegenerative diseases", "neuroprotective effects", "Huntington", "Parkinson", "Alzheimer", "Amyotrophic Lateral Sclerosis", "neurological disorders") in the title or abstract were considered. Reviews, editorials, letters, meta-analyses, conference papers, short surveys, and book chapters were not considered. Selected articles were grouped by pathologies and summarized, considering the mechanism of action. The quality assessment and the risk of bias were performed using the Cochrane Handbook for Systematic Reviews of Interventions checklist. This review uses a systematic approach to summarize the results from 60 investigations to highlight the potential role of W. somnifera and its specialized metabolites in treating or preventing neurodegenerative diseases.

2.
Phytochemistry ; 206: 113518, 2023 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-36423749

RESUMEN

Over many years, natural products have been a source of healing agents and have exhibited beneficial uses for treating human diseases. The Gentiana genus is the biggest genus in the Gentianaceae, with over 400 species distributed mainly in alpine zones of temperate countries around the world. Plants in the Gentiana genus have historically been used to treat a wide range of diseases. Still, only in the last years has particular attention been paid to the biological activities of Gentiana lutea Linn., also known as yellow Gentian or bitterwort. Several in vitro/vivo investigations and human interventional trials have demonstrated the promising activity of G. lutea extracts against oxidative stress, microbial infections, inflammation, obesity, atherosclerosis, etc.. A systematic approach was performed using Pubmed and Scopus databases to update G. lutea chemistry and activity. Specifically, this systematic review synthesized the major specialized bitter metabolites and the biological activity data obtained from different cell lines, animal models, and human interventional trials. This review aims to the exaltation of G. lutea as a source of bioactive compounds that can prevent and treat several human illnesses.


Asunto(s)
Gentiana , Animales , Humanos , Gentiana/química , Gentiana/metabolismo , Extractos Vegetales/farmacología
3.
J Food Sci ; 87(10): 4688-4702, 2022 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-36112567

RESUMEN

Few studies have investigated at the same time how physicochemical, volatile, and sensory characteristics affect coffee liking. The aim of this study is to evaluate the influence of geographical origin and variety on physicochemical parameters and volatile compounds composition of mono-origin and mono-variety coffees. Check-all-that-apply (CATA) method was used with the aim of identifying the drivers of coffee liking. Moisture content, bulk density, solubility index, color parameters, and phenols and caffeine content were useful parameters for discriminating Robusta from Arabica variety, but not samples from different origins. The hierarchical cluster and principal component analyses performed on the headspace compositions showed a quite sharp ability to group the samples based on their variety. Based on CATA results, roasted attribute, related to the presence of pyrazines, was considered a positive driver of coffee liking unlike grassy and acidic attributes (associated to the presence of acids and aldehydes, respectively). Findings from this study can be a useful tool for coffee manufacturers for a winning market strategy, helping them in the choice of the most suitable raw materials and process conditions in order to produce a well-balanced beverage by enhancing all the possible positive drivers of acceptability and reducing the negative ones.


Asunto(s)
Cafeína , Café , Café/química , Cafeína/análisis , Fenoles/análisis , Aldehídos/análisis , Pirazinas/análisis
4.
Food Chem ; 393: 133401, 2022 Nov 01.
Artículo en Inglés | MEDLINE | ID: mdl-35689927

RESUMEN

The present study investigated the potential antioxidant applications of Humulus lupulus L. as raw extract and nanoformulated in liposomes. H. lupulus is commonly used as a food ingredient, but it is also a promising source of specialized metabolites with health-promoting effects. In the extract obtained by hydroalcoholic maceration, 24 compounds were characterized using liquid chromatography-mass spectrometry analyses. The extract exhibited an interesting antioxidant activity in in vitro spectrophotometric and cell assays. The extract was nanoformulated into liposomes to exploit and improve its beneficial proprieties. The in vitro assays revealed that, after incorporation into liposomes, the extract's antioxidant activity was preserved and even improved. Moreover, a lower dose of the extract was required to prevent reactive oxygen species overproduction when included in the nanoformulation. These results confirm the advantages of nanoformulating herbal extract to maximize its health-promoting effects for a potential pharmaceutical application.


Asunto(s)
Humulus , Antioxidantes/química , Cromatografía Liquida , Humulus/química , Liposomas , Extractos Vegetales/química
5.
Fitoterapia ; 158: 105164, 2022 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-35217120

RESUMEN

Fourteen flavones (1-14) including twelve polymethoxylated flavones, two A-type proanthocyanidins (oligomeric flavonoids) (15, 16), one benzoyl glucoside (17), one triterpenoid (18), and one phenylpropanoid (19) were isolated from the leaves of the South Asian medicinal plant Ceriscoides campanulata (Roxb.) Tirveng (Rubiaceae). The structures of the compounds were identified based on their spectroscopic and spectrometric data and in comparison with literature data. Isolated compounds were tested in vitro against inflammatory enzymes (COX-2, iNOS), pro-inflammatory cytokines (IL-1ß, IL-6, TNF-α), esophageal squamous carcinoma cell line (TE13), and carbohydrate digestion enzymes (α-amylase, α-glucosidase). Proanthocyanidins 15 and 16 significantly attenuated the LPS-induced inflammatory response of COX-2, iNOS, IL-1ß, IL-6, TNF-α in RAW 264.7 cells. Proanthocyanidins also satisfactorily inhibited the regrowth (64%), migration (51%), and formation of tumor-spheres (48%) in ESCC cell line TE13 at 50% toxic concentration. Compounds 15 and 16 showed the most potent effect against mammalian α-amylase (IC50 8.4 ± 0.3 µM and 3.5 ± 0.0 µM, respectively) compared to reference standard acarbose (IC50 5.9 ± 0.1 µM). As yeast α-glucosidase inhibitors, compounds 15 and 16 also displayed significant activities (IC50 6.2 ± 0.3 and 4.7 ± 0.1 µM, respectively), while compounds 1-6 displayed weaker α-glucosidase inhibitory activities, ranging from 49 to 142 µM, compared to acarbose (IC50 665 ± 42 µM). In an anticholinesterase assay, compounds 1, 2, 6 (IC50 51 ± 2, 53 ± 7, 64 ± 5 µM, respectively), and 4 (IC50 44 ± 1 µM) showed moderate inhibitory activities against acetylcholinesterase and butyrylcholinesterase, respectively. Furthermore, molecular docking and molecular dynamic simulation analyses of compounds 15 and 16 were performed against human pancreatic α-amylase and human lysosomal acid α-glucosidase to elucidate the interactions of these compounds in the respective enzymes' active sites.


Asunto(s)
Carcinoma de Células Escamosas , Diabetes Mellitus , Neoplasias Esofágicas , Proantocianidinas , Rubiaceae , Acetilcolinesterasa/metabolismo , Animales , Butirilcolinesterasa/análisis , Butirilcolinesterasa/metabolismo , Simulación por Computador , Células Epiteliales/metabolismo , Neoplasias Esofágicas/tratamiento farmacológico , Inhibidores de Glicósido Hidrolasas/química , Inhibidores de Glicósido Hidrolasas/farmacología , Humanos , Inflamación , Mamíferos/metabolismo , Simulación del Acoplamiento Molecular , Estructura Molecular , Hojas de la Planta/química , Proantocianidinas/análisis , Proantocianidinas/farmacología , alfa-Amilasas , alfa-Glucosidasas/metabolismo
6.
Molecules ; 27(3)2022 Jan 28.
Artículo en Inglés | MEDLINE | ID: mdl-35164160

RESUMEN

Dittrichia graveolens L. Greuter belonging to the Asteraceae family, is an aromatic herbaceous plant native to the Mediterranean region. This plant species has been extensively studied for its biological activities, including antioxidant, antitumor, antimicrobial, antifungal, anti-inflammatory, anticholinesterase, and antityrosinase, and for its peculiar metabolic profile. In particular, bioactivities are related to terpenes and flavonoids metabolites, such as borneol (40), tomentosin (189), inuviscolide (204). However, D. graveolens is also well known for causing health problems both in animals and humans. Moreover, the species is currently undergoing a dramatic northward expansion of its native range related to climate change, now including North Europe, California, and Australia. This review represents an updated overview of the 52 literature papers published in Scopus and PubMed dealing with expansion, chemistry (262 different compounds), pharmacological effects, and toxicology of D. graveolens up to October 2021. The review is intended to boost further studies to determine the molecular pathways involved in the observed activities, bioavailability, and clinical studies to explore new potential applications.


Asunto(s)
Asteraceae/química , Flavonoides/química , Flavonoides/farmacología , Terpenos/química , Terpenos/farmacología , Animales , Antiinfecciosos/química , Antiinfecciosos/farmacología , Antiinflamatorios/química , Antiinflamatorios/farmacología , Antineoplásicos/química , Antineoplásicos/farmacología , Antioxidantes/química , Antioxidantes/farmacología , Descubrimiento de Drogas , Humanos , Extractos Vegetales/química , Extractos Vegetales/farmacología
7.
Phytother Res ; 35(11): 6359-6368, 2021 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-34585449

RESUMEN

Male infertility refers to the inability to conceive a natural pregnancy in a fertile female, and approximately 15% of reproductive-aged couples worldwide face this problem. Several plants were used to treat fertility disorders and, among them, Lepidium meyenii, a folk medicament of Andean regions, is still used to enhance vitality and treat sterility in humans and domestic animals. The aim of the study was to evaluate the effects of L. meyenii Walpers on infertile patients by a randomized, double-blind, placebo-controlled trial. Fifty patients suffering from various reproductive-related problems were enrolled for 16 weeks to evaluate the effect of yellow maca on semen quality and serum hormone levels. Treatment with maca improved the percentage of sperm concentration by 40%, whereas the placebo improved by 76% after 8 and 16 weeks of treatment, but the results were statistically non-significant. No statistically significant change in hormone levels was reported by using maca, except a decrease in the level of free testosterone. Results are not sufficient to assess the efficacy of maca on male fertility. Further investigation and trials are required to obtain conclusive results.


Asunto(s)
Infertilidad Masculina , Lepidium , Adulto , Animales , Humanos , Infertilidad Masculina/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Análisis de Semen , Recuento de Espermatozoides , Testosterona
8.
Artículo en Inglés | MEDLINE | ID: mdl-34257698

RESUMEN

Many Bangladeshi medicinal plants have been used to treat Alzheimer's disease and other neurodegenerative diseases. In the present study, the anticholinesterase effects of eight selected Bangladeshi medicinal plant species were investigated. Species were selected based on the traditional uses against CNS-related diseases. Extracts were prepared using a gentle cold extraction method. In vitro cholinesterase inhibitory effects were measured by Ellman's method in 96-well microplates. Blumea lacera (Compositae) and Cyclea barbata (Menispermaceae) were found to have the highest acetylcholinesterase inhibitory (IC50, 150 ± 11 and 176 ± 14 µg/mL, respectively) and butyrylcholinesterase inhibitory effect (IC50, 297 ± 13 and 124 ± 2 µg/mL, respectively). Cyclea barbata demonstrated competitive inhibition, where Blumea lacera showed an uncompetitive inhibition mode for acetylcholinesterase. Smilax guianensis (Smilacaceae) and Byttneria pilosa (Malvaceae) were also found to show moderate AChE inhibition (IC50, 205 ± 31 and 221 ± 2 µg/mL, respectively), although no significant BChE inhibitory effect was observed for extracts from these plant species. Among others, Thunbergia grandiflora (Acanthaceae) and Mikania micrantha (Compositae) were found to display noticeable AChE (IC50, 252 ± 22 µg/mL) and BChE (IC50, 314 ± 15 µg/mL) inhibitory effects, respectively. Molecular docking experiment suggested that compounds 5-hydroxy-3,6,7,3',4'-pentamethoxyflavone (BL4) and kaempferol-3-O-α-L-rhamnopyranosyl-(1⟶6)-ß-D-glucopyranoside (BL5) from Blumea lacera bound stably to the binding groove of the AChE and BChE by hydrogen-bond interactions, respectively. Therefore, these compounds could be candidates for cholinesterase inhibitors. The present findings demonstrated that Blumea lacera and Cyclea barbata are interesting objects for further studies aiming at future therapeutics for Alzheimer's disease.

9.
Toxins (Basel) ; 13(3)2021 03 22.
Artículo en Inglés | MEDLINE | ID: mdl-33809838

RESUMEN

The evolutionary arms race between plants and herbivores has led, over millions of years, to the production of many substances that prevent plants from being over-eaten by plant-feeding animals [...].


Asunto(s)
Extractos Vegetales/farmacología , Plantas Tóxicas/metabolismo , Toxinas Biológicas/farmacología , Animales , Humanos , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/toxicidad , Plantas Tóxicas/toxicidad , Toxinas Biológicas/aislamiento & purificación , Toxinas Biológicas/toxicidad
10.
Curr Neuropharmacol ; 19(7): 1007-1018, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-32442088

RESUMEN

Curcumin is a spice derived nutraceutical which gained tremendous attention because of its profound medicinal values. It alters a number of molecular pathways such as nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB), signal transducer and activator of transcription 3 (STAT3), nuclear factor erythroid 2-related factor 2 (Nrf2) and cyclooxygenases-2 (COX-2), which make it potential therapeutic choice in treating multiple disorders. It also possesses the potential to prevent protein aggregation and thus protect against degeneration of neurons in neurodegenerative disorders including Huntington's disease (HD). HD is an autosomal dominant disorder linked with altered gene expression which leads to an increase in the size of cytosine, adenine and guanine (CAG) trinucleotide repeats, aids in protein aggregation throughout the brain and thus damages neurons. Upstream regulation of oxidative stress and inflammatory cascade are two important factors that drive HD progression. Available therapies just suppress the severity of symptoms with a number of side effects. Curcumin targets multiple mechanisms in treating or preventing HD including antioxidant and anti-inflammatory potential, metal ion chelation, transcriptional alterations and upregulating activity of molecular chaperons, heat shock proteins (HSPs). Having a favorable safety profile, curcumin can be an alternative therapeutic choice in treating neurodegenerative disorders like HD. This review will focus on mechanistic aspects of curcumin in treating or preventing HD and its potential to arrest disease progression and will open new dimensions for safe and effective therapeutic agents in diminishing HD.


Asunto(s)
Curcumina , Enfermedad de Huntington , Encéfalo , Curcumina/farmacología , Curcumina/uso terapéutico , Humanos , Enfermedad de Huntington/tratamiento farmacológico , Neuronas , Estrés Oxidativo
11.
Mol Nutr Food Res ; 65(3): e2000812, 2021 02.
Artículo en Inglés | MEDLINE | ID: mdl-33300660

RESUMEN

SCOPE: Capsicum annuum L. cv Senise is a sweet pepper containing health promoting compounds that can be modified by ripening and drying. This study focuses on finding the peppers with the best antioxidant properties, which are evaluated on an experimental model of obesity. METHODS AND RESULTS: Phytochemical profile and antioxidant activity are evaluated on several peppers obtained from the same cultivar at different ripening stages. Red sweet peppers show the highest content in polyphenols, ß-carotene, lycopene, and capsinoids, and demonstrate the best antioxidant activity in vitro. Mice fed a high fat diet are orally treated with an extract from these peppers (Capsicum annuum extract [CAE]) (1, 10, and 25 mg/kg/day). It promotes weight loss and improves plasma markers related to glucose and lipid metabolisms. CAE also ameliorates obesity-associated systemic inflammation reducing the expression of pro-inflammatory cytokines in adipose and hepatic tissues and improving the expression of different markers involved in the gut epithelial barrier function. These effects are associated with a modulation of the intestinal microbiome, which appears altered. CONCLUSIONS: The extract can be considered a new potential approach for the treatment of obesity, complementary to dietary restrictions.


Asunto(s)
Antioxidantes/farmacología , Capsicum/química , Microbioma Gastrointestinal/efectos de los fármacos , Obesidad/dietoterapia , Extractos Vegetales/farmacología , Animales , Antioxidantes/química , Carotenoides/análisis , Citocinas/metabolismo , Dieta Alta en Grasa/efectos adversos , Prueba de Tolerancia a la Glucosa , Masculino , Ratones Endogámicos C57BL , Obesidad/etiología , Obesidad/microbiología , Extractos Vegetales/química
12.
Future Med Chem ; 12(19): 1779-1803, 2020 10.
Artículo en Inglés | MEDLINE | ID: mdl-33032465

RESUMEN

The natural tridecapeptide neurotensin has been emerged as a promising therapeutic scaffold for the treatment of neurological diseases and cancer. In this work, we aimed to identify the top 100 most cited original research papers as well as recent key studies related to neurotensins. The Web of Science Core Collection database was searched and the retrieved research articles were analyzed by using the VOSviewer software. The most cited original articles were published between 1973 and 2013. The top-cited article was by Carraway and Leeman reporting the discovery of neurotensin in 1973. The highly cited terms were associated with hypotension and angiotensin-converting-enzyme. The conducted analysis reveals the therapeutic potentials of neurotensin, and further impactful research toward its clinical development is warrantied.


Asunto(s)
Antineoplásicos/uso terapéutico , Fármacos del Sistema Nervioso Central/uso terapéutico , Neoplasias/tratamiento farmacológico , Enfermedades del Sistema Nervioso/tratamiento farmacológico , Neurotensina/uso terapéutico , Animales , Antineoplásicos/química , Fármacos del Sistema Nervioso Central/química , Humanos , Neurotensina/química
13.
Molecules ; 25(21)2020 Oct 22.
Artículo en Inglés | MEDLINE | ID: mdl-33105817

RESUMEN

Azorella glabra Wedd. (AG) is traditionally used to treat gonorrhea or kidney's problems. The antioxidant, antidiabetic, anticholinesterase and in vitro antitumor activities of AG extracts were recently reported. The aim of this work was to investigate anti-leukemic properties of AG chloroform fraction (AG CHCl3) and of its ten sub-fractions (I-X) and to identify their possible bioactive compounds. We determined their in vitro antioxidant activity using 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), nitric oxide (NO) and superoxide anion (SO) assays, and their phytochemical profile by spectrophotometric and LC-MS/MS techniques. I-X action on two acute myeloid leukemia (AML) cell lines viability, apoptosis and cell cycle were evaluated by MTS, western blotting and cytofluorimetric assays. Different polyphenol, flavonoid and terpenoid amount, and antioxidant activity were found among all samples. Most of I-X induced a dose/time dependent reduction of cell viability higher than parent extract. IV and VI sub-fractions showed highest cytotoxic activity and, of note, a negligible reduction of healthy cell viability. They activated intrinsic apoptotic pathway, induced a G0/G1 block in leukemic cells and, interestingly, led to apoptosis in patient AML cells. These activities could be due to mulinic acid or azorellane terpenoids and their derivatives, tentatively identified in both IV and VI. In conclusion, our data suggest AG plant as a source of potential anti-AML agents.


Asunto(s)
Antineoplásicos Fitogénicos/química , Antioxidantes/química , Apiaceae/química , Flavonoides/química , Leucemia Mieloide Aguda/tratamiento farmacológico , Extractos Vegetales/aislamiento & purificación , Polifenoles/química , Terpenos/química , Anciano , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Células Cultivadas , Cloroformo/química , Descubrimiento de Drogas , Femenino , Humanos , Persona de Mediana Edad , Extractos Vegetales/farmacología , Solventes/química , Espectrometría de Masas en Tándem
14.
Antioxidants (Basel) ; 9(8)2020 Aug 04.
Artículo en Inglés | MEDLINE | ID: mdl-32759838

RESUMEN

The leaves of Vitis vinifera L. have been used for a long time in traditional medicine for the treatment of many ailments. Grape polyphenols, indeed, have been demonstrated to be able to defend against oxidative stress, responsible for various disorders such as cancer, diabetes and neurodegenerative diseases. The effects of different extraction techniques, Soxhlet (SOX), Accelerated Solvent (ASE 40, ASE 50) and Ultrasound Assisted Extraction (UAE) were studied in this work to evaluate their impact on the chemical profile and bioactive potential of Vitis vinifera L. (cv. Aglianico) leaf extracts. The phytochemical profile was investigated by HPLC-DAD and 9 phenolic compounds were identified and quantified in the extract. Moreover, the antioxidant, anticholinesterase and antityrosinase activities were evaluated. In detail, the total polyphenol content and antioxidant activity (2,2-diphenyl-1-picrylhydrazyl, Oxygen Radical Absorbance Capacities and ß-Carotene Bleaching assays) were evaluated and compared to assess the Relative Antioxidant Capacity Index (RACI). To test the inhibitory activity of extracts towards cholinesterases, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition assays were performed. SOX and ASE 50 have shown the highest value of RACI, 0.76 and 0.65, respectively. Regarding enzymatic inhibitory activity, ASE 50 (IC50 = 107.16 ± 8.12 µg/mL) and SOX (IC50 = 171.34 ± 12.12 µg/mL) extracts exhibited the highest AChE and BChE inhibitory activity, respectively, while UAE (IC50 = 293.2 ± 25.6 µg/mL, followed by SOX (IC50 = 302.5 ± 38.3 µg/mL) showed the highest tyrosinase inhibition value. Our results demonstrated for the first time that Aglianico leaves are important sources of phenols that could be used to prevent oxidative stress and be potentially helpful in diseases treatable with tyrosinase and cholinesterase inhibitors, like myasthenia gravis or Alzheimer's.

15.
Pharmaceutics ; 12(6)2020 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-32549193

RESUMEN

The purpose of this study was to improve the knowledge on Hura crepitans L., a plant belonging to the Euphorbiaceae family that, on the one hand, is known to be toxic, but on the other, is a source of polyphenols with health-promoting effects. Different green extraction methods were applied, varying solvent, temperature, and duration of extraction, which can influence the phytochemical profile and biological activity of plant extracts, and the extracts were fully characterized. Aqueous extracts exhibited a superior antioxidant activity, as indicated by different spectrophotometric tests, and were cytoprotective to HepG2 cells used as model cells. Liquid chromatography-mass spectrometry analyses were performed to identify the secondary metabolites involved in these effects and demonstrated that solvent, duration, and temperature indeed influenced the extraction of polyphenols. Furthermore, the most promising extract, in terms of antioxidant potential, was incorporated into liposomes with the aim of promoting cell interaction and enhancing the antioxidant activity.

16.
Sci Rep ; 10(1): 10268, 2020 06 24.
Artículo en Inglés | MEDLINE | ID: mdl-32581267

RESUMEN

The physiological role of the renal ClC-Ka/ClC-K1 channels is to confer a high Cl- permeability to the thin Ascending Limb of Henle (tAL), which in turn is essential for establishing the high osmolarity of the renal medulla that drives water reabsorption from collecting ducts. Here, we investigated by whole-cell patch-clamp measurements on HEK293 cells co-expressing ClC-Ka (tagged with GFP) and the accessory subunit barttin (tagged with m-Cherry) the effect of a natural diuretic extract from roots of Dandelion (DRE), and other compounds activating PKC, such as ATP, on ClC-Ka activity and its membrane localization. Treatment with 400 µg/ml DRE significantly inhibited Cl- currents time-dependently within several minutes. Of note, the same effect on Cl- currents was obtained upon treatment with 100 µM ATP. Pretreatment of cells with either the intracellular Ca2+ chelator BAPTA-AM (30 µM) or the PKC inhibitor Calphostin C (100 nM) reduced the inhibitory effect of DRE. Conversely, 1 µM of phorbol meristate acetate (PMA), a specific PKC activator, mimicked the inhibitory effect of DRE on ClC-Ka. Finally, we found that pretreatment with 30 µM Heclin, an E3 ubiquitin ligase inhibitor, did not revert DRE-induced Cl- current inhibition. In agreement with this, live-cell confocal analysis showed that DRE treatment did not induce ClC-Ka internalization. In conclusion, we demonstrate for the first time that the activity of ClC-Ka in renal cells could be significantly inhibited by the activation of PKC elicited by classical maneuvers, such as activation of purinergic receptors, or by exposure to herbal extracts that activates a PKC-dependent pathway. Overall, we provide both new information regarding the regulation of ClC-Ka and a proof-of-concept study for the use of DRE as new diuretic.


Asunto(s)
Canales de Cloruro/metabolismo , Diuréticos/farmacología , Asa de la Nefrona/metabolismo , Proteína Quinasa C/metabolismo , Adenosina Trifosfato/farmacología , Animales , Membrana Celular/efectos de los fármacos , Membrana Celular/metabolismo , Células HEK293 , Humanos , Microscopía Intravital , Asa de la Nefrona/citología , Masculino , Potenciales de la Membrana/efectos de los fármacos , Ratones , Microscopía Confocal , Naftalenos/farmacología , Técnicas de Placa-Clamp , Extractos Vegetales/farmacología , Raíces de Plantas/química , Proteína Quinasa C/antagonistas & inhibidores , Transducción de Señal/efectos de los fármacos , Taraxacum/química , Acetato de Tetradecanoilforbol/farmacología
17.
Foods ; 9(2)2020 Feb 01.
Artículo en Inglés | MEDLINE | ID: mdl-32024045

RESUMEN

The genus Minthostachys belonging to the Lamiaceae family, and is an important South American mint genus used commonly in folk medicine as an aroma in cooking. The phytochemical-rich samples of the aerial parts of Minthostachys diffusa Epling. were tested for pharmacological and health-promoting bioactivities using in vitro chemical and enzymatic assays. A range of radical scavenging activities of the samples against biological radicals such as nitric oxide and superoxide anion and against synthetic 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radicals, the ferric reducing antioxidant power and the lipid peroxidation inhibition were determined and ranked using the 'relative antioxidant capacity index' (RACI). The ethyl acetate fraction showed the highest RACI of +1.12. Analysis of the various fractions' inhibitory ability against enzymes involved in diabetes (α-amylase and α-glucosidase), and against enzymes associated with Parkinson's or Alzheimer's diseases (acetylcholinesterase and butyrylcholinesterase) also suggested that the ethyl acetate fraction was the most active. Liquid chromatography-tandem mass spectrometry analysis of the ethyl acetate fraction showed more than 30 polyphenolic compounds, including triterpenes. The inhibitory cholinesterase effects of the triterpenes identified from M. diffusa were further analysed by in silico docking of these compounds into 3D-structures of acetylcholinesterase and butyrylcholinesterase. This is the first study on pharmacological activities and phytochemical profiling of the aerial parts of M. diffusa, showing that this plant, normally used as food in South America, is also rich in health-promoting phytochemicals.

18.
Foods ; 8(10)2019 10 22.
Artículo en Inglés | MEDLINE | ID: mdl-31652576

RESUMEN

The genus Berberis includes about 500 different species and commonly grown in Europe, the United States, South Asia, and some northern areas of Iran and Pakistan. Leaves and fruits can be prepared as food flavorings, juices, and teas. Phytochemical analysis of these species has reported alkaloids, tannins, phenolic compounds and oleanolic acid, among others. Moreover, p-cymene, limonene and ocimene as major compounds in essential oils were found by gas chromatography. Berberis is an important group of the plants having enormous potential in the food and pharmaceutical industry, since they possess several properties, including antioxidant, antimicrobial, anticancer activities. Here we would like to review the biological properties of the phytoconstituents of this genus. We emphasize the cultivation control in order to obtain the main bioactive compounds, the antioxidant and antimicrobial properties in order to apply them for food preservation and for treating several diseases, such as cancer, diabetes or Alzheimer. However, further study is needed to confirm the biological efficacy as well as, the toxicity.

19.
Plants (Basel) ; 8(8)2019 Aug 03.
Artículo en Inglés | MEDLINE | ID: mdl-31382601

RESUMEN

Oxidative stress is involved in different diseases, such as diabetes and neurodegenerative diseases. The genus Azorella includes about 70 species of flowering plant species; most of them are commonly used as food and in particular as a tea infusion in the Andean region of South America in folk medicine to treat various chronic diseases. Azorella glabra Wedd. aerial parts were firstly analyzed for their in vitro antioxidant activity using different complementary assays. In particular, radical scavenging activity was tested against biological neutral radical DPPH; ferric reducing power and lipid peroxidation inhibitory capacity (FRAP and Beta-Carotene Bleaching tests) were also determined. The Relative Antioxidant Capacity Index (RACI) was used to compare data obtained by different assays. Then, the inhibitory ability of samples was investigated against α-amylase and α-glucosidase enzymes involved in diabetes and against acetylcholinesterase and butyrylcholinesterase enzymes considered as strategy for the treatment of Parkinson's or Alzheimer's diseases. Moreover, the phytochemical profile of the sample showing the highest RACI (1.35) and interesting enzymatic activities (IC50 of 163.54 ± 9.72 and 215.29 ± 17.10 µg/mL in α-glucosidase and acetylcholinesterase inhibition, respectively) was subjected to characterization and quantification of its phenolic composition using LC-MS/MS analysis. In fact, the ethyl acetate fraction derived from ethanol extract by liquid/liquid extraction showed 29 compounds, most of them are cinnamic acid derivatives, flavonoid derivatives, and a terpene. To the best of our knowledge, this is the first report about the evaluation of significant biological activities and phytochemical profile of A. glabra, an important source of health-promoting phytochemicals.

20.
Plants (Basel) ; 8(8)2019 Jul 24.
Artículo en Inglés | MEDLINE | ID: mdl-31344952

RESUMEN

An ethnobotanical study was performed to collect information on the use of medicinal plants in Papantla, Veracruz, Mexico. The area has a high number of endemic species, and the social importance of the medicinal plants in the community is essential for public health and the conservation of traditional knowledge. This study identified the medicinal plants currently used, registered traditional knowledge, and documented the patterns of ailments treated in the indigenous communities of Totonacas. A total of 101 medicinal plants belonging to 51 families were described by 85 local informants. Asteraceae was the family with the highest number of plant species identified by these informants. Plant parts are used to treat several ailments, including venomous bites, gastro-intestinal disorders, infectious diseases and other disorders. Informants reported that the most common plant part used was the leaf tissue (55%), and they also took the herbal remedies orally (72%), and decoctions (38%) as well as infusions (29%) were the forms used to prepare these natural remedies. This study provides documentation of medicinal plants used in the Veracruz area of Mexico. Mexican people are still dependent upon medicinal plants, and in order to avoid their loss, certain measures of conservation for medicinal plants are needed.

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