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1.
Phytother Res ; 37(10): 4304-4320, 2023 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-37433745

RESUMEN

The prevalence of obesity is steadily rising, making safe and more efficient anti-obesity treatments an urgent medical need. Growing evidence correlates obesity and comorbidities, including anxiety and depression, with the development of a low-grade inflammation in peripheral and central tissues. We hypothesized that attenuating neuroinflammation might reduce weight gain and improve mood. We investigated the efficacy of a methanolic extract from Helichrysum stoechas (L.) Moench (HSE), well-known for its anti-inflammatory properties, and its main constituent arzanol (AZL). HPLC-ESI-MS2 and HPLC-UV were used to characterize the extract. HSE effects on mood and feeding behavior was assessed in mice. The mechanism of action of HSE and AZL was investigated in hippocampus samples and SH-SY5Y cells by western blotting and immunofluorescence. Oral administration of HSE for 3 weeks limited weight gain with no significant decrease in food intake. HSE produced an anxiolytic-like and antidepressant-like phenotype comparable to diazepam and amitriptyline, respectively, in the absence of locomotor and cognitive impairments and induced neuroprotective effects in glutamate-exposed SH-SY5Y cells. A dose-dependent reduction of SIRT1 expression was detected in SH-SY5Y cells and in hippocampal samples from HSE-treated mice. The inhibition of the SIRT1-FoxO1 pathway was induced in the hypothalamus. Molecular docking studies proposed a mechanism of SIRT1 inhibition by AZL, confirmed by the evaluation of inhibitory effects on SIRT1 enzymatic activity. HSE limited weight gain and comorbidities through an AZL-mediated SIRT1 inhibition. These activities indicate HSE an innovative therapeutic perspective for obesity and associated mood disorders.

2.
Curr Top Med Chem ; 23(8): 589-617, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-36617707

RESUMEN

A sedentary lifestyle has evoked a high risk of cardiovascular (CV) disease, diabetes, and obesity, all of them with high morbimortality rates and with a common denominator, hypertension. Numerous pharmacological drugs have been used for the treatment of hypertension. However, the side effects associated with the use of existing pharmacological therapies have triggered a demand for plant-based medications. In this connection, the aim of this review was to provide an in-depth analysis of the use of plant-derived bioactives for the effective management of hypertension. Phytoconstituents from leaves, bark, stem, roots, seeds, and fruits of medicinal plants grown in our different regions of the globe have been highly searched. Among them, polyphenols (e.g., flavonoids as quercetin, anthocyanins as cyanidin, tannins as ellagic acid, stilbenes as resveratrol, lignans as honokiol and others as hydroxytyrosol or curcumin), organosulfur compounds (e.g. s-allyl cysteine and allicin), fatty acids (e.g. α-lipoic acid, DHA and oleic acid), alkaloids (e.g. berberine or tetrandrine) and some terpenes have been intensively investigated for the management of hypertension, with effective ability being stated in controlling high blood pressure and related health problems both in vivo and in vitro studies. Some of the activities presented by these bioactive compounds are reducing oxidative stress, renin-angiotensin system control, SIRT1 activation, regulating platelet aggregation and COX activity, anti-atherogenic effects, anti-inflammatory properties, vasorelaxation and other results that translate into the prevention or control of hypertension. The knowledge of these bioactive compounds is important in developing countries where traditional medicine is the majority, but it can also give rise to new approaches in hypertension therapy.


Asunto(s)
Enfermedades Cardiovasculares , Hipertensión , Lignanos , Humanos , Antocianinas , Hipertensión/tratamiento farmacológico , Polifenoles/farmacología , Resveratrol/uso terapéutico , Flavonoides/uso terapéutico , Enfermedades Cardiovasculares/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico
3.
Cancer Cell Int ; 22(1): 407, 2022 Dec 13.
Artículo en Inglés | MEDLINE | ID: mdl-36514100

RESUMEN

Colorectal cancer (CRC) is the third most revalent type of cancer in the world and the second most common cause of cancer death (about 1 million per year). Historically, natural compounds and their structural analogues have contributed to the development of new drugs useful in the treatment of various diseases, including cancer. Essential oils are natural odorous products made up of a complex mixture of low molecular weight compounds with recognized biological and pharmacological properties investigated also for the prevention and treatment of cancer. The aim of this paper is to highlight the possible role of essential oils in CRC, their composition and the preclinical studies involving them. It has been reviewed the preclinical pharmacological studies to determine the experimental models used and the anticancer potential mechanisms of action of natural essential oils in CRC. Searches were performed in the following databases PubMed/Medline, Web of science, TRIP database, Scopus, Google Scholar using appropriate MeSH terms. The results of analyzed studies showed that EOs exhibited a wide range of bioactive effects like cytotoxicity, antiproliferative, and antimetastatic effects on cancer cells through various mechanisms of action. This updated review provides a better quality of scientific evidence for the efficacy of EOs as chemotherapeutic/chemopreventive agents in CRC. Future translational clinical studies are needed to establish the effective dose in humans as well as the most suitable route of administration for maximum bioavailability and efficacy. Given the positive anticancer results obtained from preclinical pharmacological studies, EOs can be considered efficient complementary therapies in chemotherapy in CRC.

4.
Int J Mol Sci ; 23(22)2022 Nov 20.
Artículo en Inglés | MEDLINE | ID: mdl-36430899

RESUMEN

Functional gastrointestinal diseases (FGID) are worldwide prevalent conditions. Pharmacological treatments can be ineffective, leading the population to turn to herbal or traditional remedies. Helichrysum stoechas (L.) Moench is a medicinal plant traditionally used in the Iberian Peninsula to treat digestive disorders, but its effects on gastrointestinal motility have not been scientifically demonstrated. The aim of this work was to evaluate the antispasmodic effect of a polyphenolic extract of H. stoechas (HSM), its mechanism of action and its antioxidant activity. Isometric myography studies were performed in rat ileum, and malondialdehyde (MDA) and 4-hydroxyalkenals (4-HDA) levels were measured in rat jejunum. HSM reduced the integrated mechanical activity of spontaneous contractions. In Ca2+-free medium, HSM reduced the concentration-response curve of CaCl2 similarly to verapamil. Pre-incubation with the extract blocked the contraction induced by Bay K8644, KCl and carbachol. L-NAME, ODQ, Rp-8-Br-PET-cGMPS, KT-5823, apamin, TRAM-34 and charybdotoxin reduced the relaxant effect of the extract on spontaneous contractions. MDA+4-HDA levels in LPS-treated tissue were reduced by the extract, showing antioxidant activity. In conclusion, HSM showed antispasmodic activity through inhibition of Ca2+ influx, activation of the NO/PKG/cGMP pathway and opening of Ca2+-activated K+ channels. The results suggest that H. stoechas could help in the prevention or treatment of FGIDs.


Asunto(s)
Helichrysum , Animales , Ratas , Parasimpatolíticos , Antioxidantes/farmacología , Flores , Transducción de Señal , Extractos Vegetales/farmacología
5.
Antioxidants (Basel) ; 11(6)2022 May 31.
Artículo en Inglés | MEDLINE | ID: mdl-35739989

RESUMEN

Helichrysum stoechas (L.) Moench (H. stoechas) is a medicinal plant traditionally used in the Iberian Peninsula to treat different disorders such as arterial hypertension. The aim of this study was to investigate the vascular effects of a polyphenolic methanolic extract of H. stoechas, which has high antioxidant activity, and its mechanism of action. Isometric myography studies were performed in an organ bath with rat aortic rings with intact endothelium. The H. stoechas extract produced vasorelaxation in the aortic rings that were precontracted by phenylephrine or KCl. L-NAME and Rp-8-Br-PET-cGMPS but not indomethacin or H-89; it also reduced the relaxant response evoked by H. stoechas extract on the phenylephrine-induced contractions. H. stoechas extract reduced the response to CaCl2 similar to verapamil and reduced the phenylephrine-induced contractions comparable with heparin. TRAM-34, apamin and glibenclamide reduced relaxation induced by the H. stoechas extract. The combination of L-NAME+TRAM-34+apamin almost completely inhibited the H. stoechas-induced effect. In conclusion, the relaxant effect of the H. stoechas extract is partially mediated by endothelium through the activation of the NO/PKG/cGMP pathway and the opening of Ca2+-activated K+ channels. Furthermore, the decrease in the cytosolic Ca2+ by the inhibition of Ca2+ influx through the L-type Ca2+ channels and by the reduction of Ca2+ release from the sarcoplasmic reticulum via the IP3 pathway is also involved.

6.
Oxid Med Cell Longev ; 2021: 1131280, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34471461

RESUMEN

Autism spectrum disorder (ASD) is a neurodevelopmental disorder, where social and communication deficits and repetitive behaviors are present. Plant-derived bioactives have shown promising results in the treatment of autism. In this sense, this review is aimed at providing a careful view on the use of plant-derived bioactive molecules for the treatment of autism. Among the plethora of bioactives, curcumin, luteolin, and resveratrol have revealed excellent neuroprotective effects and can be effectively used in the treatment of neuropsychological disorders. However, the number of clinical trials is limited, and none of them have been approved for the treatment of autism or autism-related disorder. Further clinical studies are needed to effectively assess the real potential of such bioactive molecules.


Asunto(s)
Trastorno del Espectro Autista/dietoterapia , Plantas/química , Humanos
7.
Biology (Basel) ; 10(7)2021 Jul 08.
Artículo en Inglés | MEDLINE | ID: mdl-34356488

RESUMEN

Nature is an inexhaustible source of bioactive compounds and products with interesting medicinal properties and technological applications [...].

8.
Biology (Basel) ; 10(5)2021 May 18.
Artículo en Inglés | MEDLINE | ID: mdl-34069854

RESUMEN

In traditional medicine, Jasonia glutinosa (L.) DC or rock tea (RT) has been mainly used to treat digestive and respiratory pathologies but also as an antimicrobial or an antidepressant herbal remedy. An ethanolic extract of RT has been demonstrated to have antioxidant and anti-inflammatory effects, which may be explained by its phytochemical profile, rich in polyphenols and pigments. The aim of this study is to investigate the neuroprotective potential of RT. For this purpose, the ethanolic extract of RT is assayed in Caenorhabditis elegans (C. elegans) as an in vivo model, and through in vitro assays using monoamine oxidase A, tyrosinase and acetylcholinesterase as enzymes. The RT extract reduces juglone-induced oxidative stress in worms and increases the lifespan and prevents paralysis of C. elegans CL4176, a model of Alzheimer's disease; the extract is also able to inhibit enzymes such as acetylcholinesterase, monoamine oxidase A and tyrosinase in vitro. Together these results demonstrate that Jasonia glutinosa is a good candidate with antioxidant and neuroprotective potential for the development of new products with pharmaceutical interests.

9.
Pharmaceuticals (Basel) ; 13(12)2020 Dec 17.
Artículo en Inglés | MEDLINE | ID: mdl-33348565

RESUMEN

The long-term use of anxiolytic and antidepressant drugs can cause a plethora of side effects and the use of complementary and alternative medicine, which is generally considered safer than conventional medicine, is consistently increasing. Helichrysum stoechas (L.) Moench methanolic extract (HSE) has shown MAO-A inhibitory properties in previous studies. With the aim of obtaining innovative and safer therapies for mood disorders, this study investigated the potential activity of HSE in the management of anxiety- and depression-related symptoms. HSE showed dose-dependent (30-100 mg/kg p.o.) anxiolytic-like activity in the light dark box and marble burying tests, without any antidepressant-like activity, as shown by the results of the tail suspension test. Additionally, HSE did not have any effect on the modulation of pain, which highlights its selectivity in the control of anxiety-related behavior. At active doses, HSE did not produce any sedative effect or result in impaired motor coordination and memory functions. Western blotting experiments showed the ability of HSE to counteract the reduction in the phosphorylation of ERK44/42, to restore brain-derived neurotrophic factor (BDNF) expression and to return cyclic AMP response element binding (CREB) levels to basal levels in noradrenergic hippocampal neurons of mice exposed to an anxiety-related environment, which indicates a protective role against anxiety behavior. These results suggest that oral administration of HSE might represent an interesting opportunity for the management of anxiety disorders.

10.
Food Funct ; 11(10): 8931-8938, 2020 Oct 21.
Artículo en Inglés | MEDLINE | ID: mdl-32996952

RESUMEN

Jasonia glutinosa (L.) DC., also known in Spain as "té de roca" (rock tea, RT), is an endemic plant species of the Iberian Peninsula and Southern France. Traditionally, it is used in infusions, prepared with the flowering aerial parts, as a digestive and anti-inflammatory herbal tea. Despite the traditional knowledge of this plant as a digestive after meals, there are hardly any scientific studies that support its use. The aim of this study is to assess the effects of RT extract on physiological targets related to metabolic diseases such as obesity. For this purpose, enzyme inhibition bioassays of lipase, α-glucosidase and fatty acid amide hydrolase were carried out in cell-free systems. Similarly, adipocytes derived from 3T3-L1 cells were employed to study the effects of the extract on adipocyte differentiation and triglyceride (TG) accumulation. RT extract was able to inhibit lipase, α-glucosidase and fatty acid amide hydrolase. Furthermore, the extract displayed anti-adipogenic properties in a dose-dependent manner as it significantly reduced TG accumulation during adipocyte differentiation. These results may explain from a molecular perspective the beneficial effects of RT in the prevention of metabolic-associated disorders such as obesity, diabetes and related complications.


Asunto(s)
Hipolipemiantes/farmacología , Extractos Vegetales/farmacología , Polifenoles/farmacología , Té/química , Triglicéridos/metabolismo , Células 3T3-L1 , Adipocitos/efectos de los fármacos , Adipogénesis/efectos de los fármacos , Animales , Diferenciación Celular/efectos de los fármacos , Ratones , Obesidad/prevención & control
11.
Biology (Basel) ; 9(7)2020 Jul 13.
Artículo en Inglés | MEDLINE | ID: mdl-32668697

RESUMEN

Matthiola incana (L.) R. Br. (Brassicaceae) is widely cultivated for ornamental purposes and utilized as a medicinal plant. In the present work, the hydroalcoholic extract from the aerial parts of this species has been evaluated in different bioassays in order to detect potential pharmacological applications. The cytotoxic capacity against the human colorectal adenocarcinoma (CaCo-2) and breast cancer (MCF-7) cell lines was tested using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. The extract was investigated as a neuroprotective inhibitor of central nervous system (CNS) enzymes such as monoamine oxidase A, tyrosinase, acetylcholinesterase, and as a natural enzyme inhibitor of α-glucosidase and lipase involved in some metabolic disorders such as obesity or type 2 diabetes. The antioxidant ability was also evaluated in an enzymatic system (xanthine/xanthine oxidase assay). Results showed that the M. incana extract displayed moderate to low cytotoxicity vs. CaCo-2 cells. The extract acted as a superoxide radical scavenger and enzymatic inhibitor of monoamine oxidase A, tyrosinase, α-glucosidase, and lipase. The best results were found in the α-glucosidase assay, as M. incana hydroalcoholic extract was able to inhibit the enzyme α-glucosidase up to 100% without significant differences, compared to the antidiabetic drug acarbose. Matthiola incana has been demonstrated to exert different biological properties. These are important in order to consider this species as a source of bioactive compounds.

12.
Curr Pharm Des ; 26(16): 1790-1798, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-31985367

RESUMEN

Anthocyanins are plant pigments present in flowers, leaves or fruits with polyphenolic structure belonging to the group of flavonoids. From a nutritional approach, they are the most abundant flavonoids in dietary sources responsible for the antioxidant properties of those foods. In addition, the food and pharma industries have used anthocyanins as food additives or excipients due to its colorant properties. However, beyond its antioxidant effects, anthocyanins may also act as therapeutic agents due to neuroprotective, antidiabetic and cardioprotective properties. There is a growing body of evidence suggesting the role of these compounds in the Central Nervous System (CNS). Previous in vitro and animal studies have suggested neuroprotective benefits, but we here review human interventions made with anthocyanins in relation to cognition, insomnia, anxiety or depression. Due to the link between oxidative stress and neurodegenerative disorders, human studies conducted on healthy volunteers evaluating oxidative stress parameters have also been included. As reviewed here, very few human studies (only ten) have been performed in the area of CNS; however, considering the obtained outcomes in those trials together with human interventions in relation with oxidative stress as well as data showing neuroprotective effects from preclinical experiments, we suggest that anthocyanins may have potential benefits for the CNS.


Asunto(s)
Antocianinas , Ingredientes Alimentarios , Animales , Antocianinas/farmacología , Antioxidantes/farmacología , Sistema Nervioso Central/química , Sistema Nervioso Central/metabolismo , Ensayos Clínicos como Asunto , Frutas , Humanos , Estrés Oxidativo
13.
Inflammopharmacology ; 28(6): 1717-1734, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-31410747

RESUMEN

Jasonia glutinosa (L.) DC., known as rock tea (RT), is traditionally used in Spain as a digestive due to its beneficial properties in bowel disorders. The pharmacological nature of these properties has not been established yet. The aim of this work was to evaluate the therapeutic utility of RT in experimental colitis and to identify chemical constituents with anti-inflammatory and/or anti-oxidative properties. RT extract was prepared with ethanol in a Soxhlet apparatus and analysed by HPLC-DAD. Superoxide radical scavenging properties, xanthine oxidase and lipoxygenase (5-LOX) inhibitory activity, and capability to lower nitric oxide (NO) and tumor necrosis factor α (TNF-α) levels were measured in cell-free and cell-based assays. In the 2.5%-dextran-sodium sulphate (DSS) injury-repair model of ulcerative colitis (UC), mice were daily treated with sulfasalazine (SSZ, as reference drug, 100 mg/kg bw), RT (5, 25 and 50 mg/kg bw, p.o.), or vehicle over 20 days. Colitis was scored daily. Colon samples were examined macroscopically and histopathologically. Protein levels of myeloperoxidase (MPO), interleukins 6, and 10 (IL-6, IL-10), inducible NO synthase (iNOS), and cyclooxygenase-2 (COX-2) were studied as markers of oxidative stress and inflammatory activity. The integrity of the apical epithelial layer was assessed by immunofluorescence staining of zonula ocludens-1 (ZO-1). Finally, intestinal contractility was also evaluated by isometric myography. Fifteen phenolic compounds and three pigments were identified and quantified, of which caffeoylquinic acids, and the flavonoid, quercetin-3-O-galactoside, were the most abundant. RT extract significantly scavenged superoxide radicals, inhibited 5-LOX activity, and lowered NO and TNF-α levels. DSS-treated mice receiving RT scored clinically lower than controls during the first 3 days of DSS treatment and during the recovery period. SSZ was less effective than RT. Anatomical and histological examination of colon samples revealed that RT significantly prevented colon shortening, increased colon thickness, and lowered the macroscopic damage score. RT also significantly prevented the increase of MPO activity, IL-6 levels, iNOS and COX-2 expression, the loss of ZO-1 apical expression, and normalized contractility disturbances. In conclusion, daily administration of RT showed therapeutic properties in the DSS-model of UC. The benefits of RT can likely be attributed to its anti-inflammatory and antioxidant phenolic and flavonoid constituents.


Asunto(s)
Colitis Ulcerosa/tratamiento farmacológico , Colon/efectos de los fármacos , Inflamación/tratamiento farmacológico , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/farmacología , Plantas Medicinales/química , Sustancias Protectoras/farmacología , Animales , Antiinflamatorios/farmacología , Biomarcadores/metabolismo , Células Cultivadas , Colitis Ulcerosa/inducido químicamente , Colitis Ulcerosa/metabolismo , Colon/metabolismo , Sulfato de Dextran/farmacología , Modelos Animales de Enfermedad , Medicina de Hierbas/métodos , Inflamación/metabolismo , Mediadores de Inflamación/metabolismo , Masculino , Medicina Tradicional/métodos , Ratones , Ratones Endogámicos C57BL , Fitoterapia/métodos
14.
Molecules ; 24(14)2019 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-31311079

RESUMEN

Developing effective and eco-friendly antiparasitic drugs and insecticides is an issue of high importance nowadays. In this study, we evaluated the anthelminthic and insecticidal potential of the leaf essential oil obtained from Origanum syriacum against the L3 larvae of the parasitic nematode Anisakis simplex and larvae and adults of the mosquito Culex quinquefasciatus. Tests on A. simplex were performed by standard larvicidal and penetration assays, while mosquito toxicity was assessed relying on larvicidal, tarsal contact, and fumigation tests. To shed light on the possible mode of action, we analyzed the oil impact as acetylcholinesterase (AChE) inhibitor. This oil was particularly active on L3 larvae of A. simplex, showing a LC50 of 0.087 and 0.067 mg mL-1 after 24 and 48 h treatment, respectively. O. syriacum essential oil was highly effective on both larvae and adults of C. quinquefasciatus, showing LC50 values of 32.4 mg L-1 and 28.1 µg cm-2, respectively. Its main constituent, carvacrol, achieved larvicidal LC50(90) of 29.5 and 39.2 mg L-1, while contact toxicity assays on adults had an LC50(90) of 25.5 and 35.8 µg cm-2, respectively. In fumigation assays, the LC50 was 12.1 µL L-1 after 1 h and decreased to 1.3 µL L-1 in 24 h of exposure. Similarly, the fumigation LC50 of carvacrol was 8.2 µL L-1 after 1 h of exposure, strongly decreasing to 0.8 µL L-1 after 24 h of exposure. These results support the folk usage of Lebanese oregano as an antiparasitic agent, providing new insights about its utilization for developing new effective and eco-friendly nematocidal and insecticidal products.


Asunto(s)
Anisakis/efectos de los fármacos , Inhibidores de la Colinesterasa/farmacología , Culex/efectos de los fármacos , Aceites Volátiles/farmacología , Origanum/química , Animales , Inhibidores de la Colinesterasa/química , Cimenos/farmacología , Larva/efectos de los fármacos , Mosquitos Vectores/efectos de los fármacos , Aceites Volátiles/química , Hojas de la Planta/química , Aceites de Plantas/química , Aceites de Plantas/farmacología
15.
Food Funct ; 10(8): 4953-4965, 2019 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-31343012

RESUMEN

Date (Phoenix dactylifera L.) seeds are a valuable and abundant by-product with various potential food applications and a source of functional and bioactive ingredients. In this study, date seeds from eight cultivars (Ourous "OUR", Tazizaout "TAZ", Tazarzeit "TAR", Tazoughart "TAG", Ouaouchet "OUC", Oukasaba "OUK", Delat "DEL" and Tamezwertn'telet "TWT") cultivated in the M'zab oasis (south of Algeria) were analyzed for their chemical and phytochemical compositions, antioxidant capacities and in vitro inhibition of some enzymes. Variations in chemical compositions were observed in the studied date seeds. The greatest contents of total phenolic compounds (476 mg GAE per g dw), total flavonoids (6.52 mg QE per g dw), anthocyanins (1.26 mg Q3GE per g dw), flavonols (3.36 mg Q3GE per g dw), proanthocyanidins (85.13 mg CE per g dw), and ascorbic acid were detected in the seeds of the TAG cultivar. All extracts manifested good antioxidant activities tested by ORAC and FRAP assays. The OUC and OUR extracts displayed the most potent antioxidant capacity against DPPH˙ free radicals (IC50 = 37.30 µg ml-1) and ABTS˙+ cation radicals (IC50 = 13.89 µg ml-1), respectively. The antioxidant activity evaluated through a xanthine/xanthine oxidase system demonstrated that the TAZ extract was more efficient as a superoxide radical scavenger (IC50 = 9.08 µg ml-1). Date seed extracts (DSE) exhibited inhibitory activities on enzymes, showing substantial potential as skin-whitening, neuroprotective, anti-hyperglycemic or anti-hyperlipidemic agents; the inhibitory potential was tested using tyrosinase (TYR), acetylcholinesterase (AChE), α-glucosidase (α-GLU) and lipase. All date seed cultivars were able to inhibit tyrosinase and α-glucosidase in a dose-dependent manner reaching the maximum inhibition.


Asunto(s)
Antioxidantes/química , Inhibidores de Glicósido Hidrolasas/química , Phoeniceae/química , Extractos Vegetales/química , Acetilcolinesterasa/química , Antioxidantes/aislamiento & purificación , Inhibidores de Glicósido Hidrolasas/aislamiento & purificación , Extractos Vegetales/aislamiento & purificación , Semillas/química , Residuos/análisis , alfa-Glucosidasas/química
16.
Front Pharmacol ; 10: 472, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31143116

RESUMEN

Low treatment efficacy represents an important unmet need in neuropathic pain patients and there is an urgent need to develop a more effective pharmacotherapy. An increasing number of patients choose complementary medicine to relieve pain. Lavender essential oil (LEO) is approved by the European Medicines Agency as herbal medicine to relieve anxiety and stress. However, the capability of LEO to relieve other nervous system disorders such as neuropathic pain has never been established. Our work aimed to evaluate the antineuropathic properties of lavender on a spared nerve injury (SNI) model of neuropathic pain in mice. An acute oral administration of LEO (100 mg/kg) alleviated SNI-induced mechanical allodynia, evaluated in the von Frey test, with an intensity comparable to the reference drug pregabalin. Investigations into the mechanism of action showed that LEO markedly decreased the phosphorylation of ERK1, ERK2, and JNK1, and decreased the levels of iNOS in the spinal cord; involvement of the endocannabinoid system was also detected using in vitro inhibition of the FAAH and MALG enzymes as well as in vivo experiments with the CB1 antagonist. Conversely, no effect on P38 phosphorylation and NF-kB activation was detected. These antihyperalgesic effects appeared at the same dose able to induce antidepressant-like, anxiolytic-like, and anorexic effects. In addition, gavage with LEO did not significantly alter animals' gross behavior, motor coordination, or locomotor activity, nor impaired memory functions. Oral administration of LEO could represent a therapeutic approach in the management of neuropathic pain states.

17.
J Ethnopharmacol ; 220: 67-74, 2018 Jun 28.
Artículo en Inglés | MEDLINE | ID: mdl-29604377

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Pomegranate fruit is considered an antidiabetic medicine in certain systems of traditional medicine. In addition, pomegranate polyphenols are known as powerful antioxidants with beneficial effects such as the reduction of oxidative / inflammatory stress and the increase of protective signalling such as antioxidant enzymes, neurotrophic factors and cytoprotective proteins. AIM OF THE STUDY: This work evaluates the effects of pomegranate juice, its main polyphenols known as ellagic acid and punicalagin, as well as its main metabolite urolithin A, on physiological and pharmacological targets of metabolic diseases such as obesity and diabetes. MATERIALS AND METHODS: For this purpose, enzyme inhibition bioassays of lipase, α-glucosidase and dipeptidyl peptidase-4 were carried out in cell-free systems. Similarly, adipocytes derived from 3T3-L1 cells were employed to study the effects of ellagic acid, punicalagin and urolithin A on adipocyte differentiation and triglyceride (TG) accumulation. RESULTS: Pomegranate juice, ellagic acid, punicalagin and urolithin A were able to inhibit lipase, α-glucosidase and dipeptidyl peptidase-4. Furthermore, all tested compounds but significantly the metabolite urolithin A displayed anti-adipogenic properties in a dose-dependent manner as they significantly reduced TG accumulation and gene expression related to adipocyte formation such as adiponectin, PPARγ, GLUT4, and FABP4 in 3T3-L1 adipocytes. CONCLUSION: These results may explain from a molecular perspective the beneficial effects and traditional use of pomegranate in the prevention of metabolic-associated disorders such as obesity, diabetes and related complications.


Asunto(s)
Adipogénesis/efectos de los fármacos , Cumarinas/farmacología , Lythraceae/química , Polifenoles/farmacología , Células 3T3-L1 , Adipocitos/efectos de los fármacos , Adipocitos/metabolismo , Adipogénesis/genética , Animales , Cumarinas/administración & dosificación , Cumarinas/aislamiento & purificación , Dipeptidil Peptidasa 4/efectos de los fármacos , Dipeptidil Peptidasa 4/metabolismo , Relación Dosis-Respuesta a Droga , Ácido Elágico/administración & dosificación , Ácido Elágico/aislamiento & purificación , Ácido Elágico/farmacología , Regulación de la Expresión Génica/efectos de los fármacos , Taninos Hidrolizables/administración & dosificación , Taninos Hidrolizables/aislamiento & purificación , Taninos Hidrolizables/farmacología , Lipasa/metabolismo , Ratones , Polifenoles/administración & dosificación , Polifenoles/aislamiento & purificación , Triglicéridos/metabolismo , alfa-Glucosidasas/efectos de los fármacos , alfa-Glucosidasas/metabolismo
18.
Food Funct ; 8(5): 1775-1784, 2017 May 24.
Artículo en Inglés | MEDLINE | ID: mdl-28418429

RESUMEN

Cotoneaster pannosus (Rosaceae) is a semievergreen shrub, producing globose dark red pomes, native to China and widely used as an ornamental plant all over the world. Despite its extensive cultivation, little information is available on the chemical composition and biological activities of its fruits. In this work, the analysis of the chemical composition of C. pannosus fruits, in terms of phenolic components, carotenoids and ascorbic acid by HPLC/DAD, HPLC/ESI-MS and MS/MS as well as in terms of macro- and micro-nutrients was performed. The fruits proved to be a good source of shikimic acid and caffeoylquinic acids, whereas ß-carotene, pelargonidin-3-O glucoside and cyanidin-3,5-rutinoside gave an important contribution to the color of the fruit. Both the polar and apolar fruit extracts showed noteworthy radical scavenger activity and inhibitory effects against monoamine oxidase A (MAO-A), tyrosinase (TYR) and α-glucosidase, making C. pannosus red pomes a promising candidate ingredient in functional foods and dietary supplements.


Asunto(s)
Inhibidores Enzimáticos/química , Depuradores de Radicales Libres/química , Frutas/química , Extractos Vegetales/química , Rosaceae/química , Cromatografía Líquida de Alta Presión , Cinética , Monofenol Monooxigenasa/antagonistas & inhibidores , Monofenol Monooxigenasa/química , Espectrometría de Masa por Ionización de Electrospray , alfa-Glucosidasas/química
19.
Rev. esp. enferm. dig ; 108(12): 785-789, dic. 2016. tab, graf
Artículo en Español | IBECS | ID: ibc-159626

RESUMEN

Antecedentes: Jasonia glutinosa es una planta utilizada en la Península Ibérica y en el sur de Francia por su efecto espasmolítico, pero sin evidencia científica sobre ello. Objetivo: examinar el efecto espasmolítico de un extracto de té de roca. Métodos: estudiamos el efecto de dicho extracto sobre las contracciones espontáneas en duodeno de rata in vitro y sobre el tránsito gastrointestinal en el ratón in vivo. Resultados: el extracto de té de roca redujo las contracciones espontáneas en el músculo liso longitudinal del duodeno de rata, inhibió las contracciones inducidas por KCl, bloqueó la contracción causada por la entrada de Ca2+ extracelular y la contracción inducida por el Bay K8644, agonista de los canales de Ca2+ tipo L. El efecto inhibitorio del extracto de té de roca fue similar al del verapamilo, inhibidor de los canales de Ca2+ tipo L. El té de roca no modificó el tránsito gastrointestinal total en ratones sanos. Sin embargo, tras el tratamiento con dextrano sulfato de sodio, un inductor de colitis, el extracto de té de roca revirtió el aumento del tránsito gastrointestinal asociado a dicho tratamiento. Conclusión: el extracto de té de roca relajó el músculo liso duodenal a través de canales de Ca2+ tipo L y normalizó el tránsito gastrointestinal en un modelo de colitis. Estos resultados validan el uso tradicional de Jasonia glutinosa en alteraciones digestivas. Así, el té de roca podría ser utilizado como espasmolítico en el tratamiento de diversas patologías gastrointestinales (AU)


Introduction: Jasonia glutinosa is an endemic plant species of the Iberian Peninsula and Southern France traditionally used in infusions as a spasmolytic; this plant is also known as "té de roca" (rock tea) but there is no scientific evidence about the effects of this plant. Aim: To evaluate the spasmolytic effect of rock tea. Methods: We have studied the in vitro effect of a rock tea extract on rat duodenum spontaneous contractions and the in vivo effect on mice gastrointestinal transit. Results: Rock tea extract reduced the spontaneous contractions of rat duodenal smooth muscle, inhibited KCl-induced contractions and blocked the contractions invoked by both extracellular Ca2+ and the agonist of L-type calcium channels Bay K8644. This inhibitory effect was similar to the one observed after the addition of the antagonist of L-type calcium channels verapamil. Rock tea did not modify gastrointestinal transit in healthy mice. However, after the treatment with dextran sulfate sodium, an inducer of colitis, rock tea extract reverted the increase in the gastrointestinal transit associated with this treatment. Conclusion: Rock tea extract relaxed duodenal smooth muscle via L-type calcium channels and normalized gastrointestinal transit in a model of colitis. These results may validate the traditional use of Jasonia glutinosa in patients with gastrointestinal alterations. Thus, rock tea may be used as a spasmolytic agent to treat gastrointestinal disorders (AU)


Asunto(s)
Animales , Masculino , Ratones , Ratas , Parasimpatolíticos/farmacocinética , Parasimpatolíticos/uso terapéutico , , Bloqueadores de los Canales de Calcio/farmacocinética , Bloqueadores de los Canales de Calcio/uso terapéutico , Motilidad Gastrointestinal , Tránsito Gastrointestinal , Asteraceae , Músculo Liso , Medicina Tradicional , Análisis de Varianza , Verapamilo/uso terapéutico , Potasio/uso terapéutico
20.
Rev Esp Enferm Dig ; 108(12): 785-789, 2016 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-27804305

RESUMEN

INTRODUCTION: Jasonia glutinosa is an endemic plant species of the Iberian Peninsula and Southern France traditionally used in infusions as a spasmolytic; this plant is also known as "té de roca" (rock tea) but there is no scientific evidence about the effects of this plant. AIM: To evaluate the spasmolytic effect of rock tea. METHODS: We have studied the in vitro effect of a rock tea extract on rat duodenum spontaneous contractions and the in vivo effect on mice gastrointestinal transit. RESULTS: Rock tea extract reduced the spontaneous contractions of rat duodenal smooth muscle, inhibited KCl-induced contractions and blocked the contractions invoked by both extracellular Ca2+ and the agonist of L-type calcium channels Bay K8644. This inhibitory effect was similar to the one observed after the addition of the antagonist of L-type calcium channels verapamil. Rock tea did not modify gastrointestinal transit in healthy mice. However, after the treatment with dextran sulfate sodium, an inducer of colitis, rock tea extract reverted the increase in the gastrointestinal transit associated with this treatment. CONCLUSION: Rock tea extract relaxed duodenal smooth muscle via L-type calcium channels and normalized gastrointestinal transit in a model of colitis. These results may validate the traditional use of Jasonia glutinosa in patients with gastrointestinal alterations. Thus, rock tea may be used as a spasmolytic agent to treat gastrointestinal disorders.


Asunto(s)
Asteraceae/química , Intestinos/efectos de los fármacos , Parasimpatolíticos/farmacología , Extractos Vegetales/farmacología , Animales , Canales de Calcio Tipo L/efectos de los fármacos , Duodeno/efectos de los fármacos , Tránsito Gastrointestinal/efectos de los fármacos , Técnicas In Vitro , Masculino , Ratones , Ratones Endogámicos C57BL , Contracción Muscular/efectos de los fármacos , Ratas , Ratas Wistar
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