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Benzylamine (Bza) oral administration delays the onset of hyperglycemia in insulin-resistantTo extend the antihyperglycemic properties of oral benzylamine to a model of insulin-deficient type 1 diabetes.Male Swiss mice were rendered diabetic by streptozotocin treatment (STZ) and divided in two groups: one received 0.5% Bza as drinking solution for 24 d (STZ Bza-drinking) while the other was drinking waterSTZ diabetic mice presented typical features of insulin-deficient diabetes: reduced body mass and increased blood glucose levels. These altered parameters were not normalized in the Bza-drinking group in spite of restored food and water intake. Bza consumption could not reverse the severe fat depot atrophy of STZ diabetic mice. In the nondiabetic mice, no difference was found between control and Bza-drinking mice for any parameter. In isolated adipocytes, hexose uptake was partially activated by 0.1 mmol/L Bza in a manner that was obliteratedBza supplementation could not normalize the altered glucose handling of STZ diabetic mice with severe WAT atrophy. Consequently, its antidiabetic potential in obese and diabetic rodents does not apply to lipoatrophic type 1 diabetic mice.

Functional gastrointestinal diseases (FGID) are worldwide prevalent conditions. Pharmacological treatments can be ineffective, leading the population to turn to herbal or traditional remedies.

Abstract: 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. Phyto-constituents from leaves, bark, stem, roots, seeds, and fruits of medicinal plants grown in our differ-ent 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 tetran-drine) 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, vasorelaxa-tion 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.

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.

Jasonia glutinosa (L.) DC., also known in Spain as "te 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.

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.

Thymoquinone (TQ) is a secondary metabolite found in abundance in very few plant species including Nigella sativa L., Monarda fistulosa L., Thymus vulgaris L. and Satureja montana L. Preclinical pharmacological studies have shown that TQ has many biological activities, such as anti-inflammatory, antioxidant and anticancer. Both in vivo and in vitro experiments have shown that TQ acts as an antitumor agent by altering cell cycle progression, inhibiting cell proliferation, stimulating apoptosis, inhibiting angiogenesis, reducing metastasis and affecting autophagy. In this comprehensive study, the evidence on the pharmacological potential of TQ on pancreatic cancer is reviewed. The positive results of preclinical studies support the view that TQ can be considered as an additional therapeutic agent against pancreatic cancer. The possibilities of success for this compound in human medicine should be further explored through clinical trials. © 2022 The Authors

Caffeine is a plant alkaloid present in food and beverages consumed worldwide. It has high lipid solubility with recognized actions in the central nervous system and in peripheral tissues, notably the adipose depots. However, the literature is scant regarding caffeine’s influence on adipocyte functions other than lipolysis, such as glucose incorporation into lipids (lipogenesis) and amine oxidation. The objective of this study was to explore the direct effects of caffeine and of isobutylmethylxanthine (IBMX) on these adipocyte functions. Glucose transport into fat cells freshly isolated from mice, rats, or humans was monitored by determining [3H]-2-deoxyglucose (2-DG) uptake, while the incorporation of radiolabeled glucose into cell lipids was used as an index of lipogenic activity. Oxidation of benzylamine by primary amine oxidase (PrAO) was inhibited by increasing doses of caffeine in human adipose tissue preparations with an inhibition constant (Ki) in the millimolar range. Caffeine inhibited basal and insulin-stimulated glucose transport as well as lipogenesis in rodent adipose cells. The antilipogenic action of caffeine was also observed in adipocytes from mice genetically invalidated for PrAO activity, indicating that PrAO activity was not required for lipogenesis inhibition. These caffeine inhibitory properties were extended to human adipocytes: relative to basal 2-DG uptake, set at 1.0 ± 0.2 for 6 individuals, 0.1 mM caffeine tended to reduce uptake to 0.83 ± 0.08. Insulin increased uptake by 3.86 ± 1.11 fold when tested alone at 100 nM, and by 3.21 ± 0.80 when combined with caffeine. Our results reinforce the recommendation of caffeine’s potential in the treatment or prevention of obesity complications.

Among the dietary amines present in foods and beverages, tyramine has been widely studied since its excessive ingestion can cause catecholamine release and hypertensive crisis. However, tyramine exerts other actions than depleting nerve endings: it activates subtypes of trace amine associated receptors (TAARs) and is oxidized by monoamine oxidases (MAO). Although we have recently described that tyramine is antilipolytic in human adipocytes, no clear evidence has been reported about its effects on glucose transport in the same cell model, while tyramine mimics various insulin-like effects in rodent fat cells, such as activation of glucose transport, lipogenesis, and adipogenesis. Our aim was therefore to characterize the effects of tyramine on glucose transport in human adipocytes. The uptake of the non-metabolizable analogue 2-deoxyglucose (2-DG) was explored in adipocytes from human subcutaneous abdominal adipose tissue obtained from women undergoing reconstructive surgery. Human insulin used as reference agent multiplied by three times the basal 2-DG uptake. Tyramine was ineffective from 0.01 to 10 µM and stimulatory at 100 µM-1 mM, without reaching the maximal effect of insulin. This partial insulin-like effect was not improved by vanadium and was impaired by MAO-A and MAO-B inhibitors. Contrarily to benzylamine, mainly oxidized by semicarbazide-sensitive amine oxidase (SSAO), tyramine activation of glucose transport was not inhibited by semicarbazide. Tyramine effect was not dependent on the Gi-coupled receptor activation but was impaired by antioxidants and reproduced by hydrogen peroxide. In all, the oxidation of high doses of tyramine, already reported to inhibit lipolysis in human fat cells, also partially mimic another effect of insulin in these cells, the glucose uptake activation. Thus, other MAO substrates are potentially able to modulate carbohydrate metabolism.

Nature is an inexhaustible source of bioactive compounds and products with interest- ing medicinal properties and technological applications. Although natural products can be found in plants, animals, microorganisms and minerals, the vast majority of them come from plants ...

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.

Diabetes mellitus is a chronic metabolic disease characterized by high blood glucose concentration. Nowadays, type 2 diabetes or insulin resistant diabetes is the most common diabetes, mainly due to unhealthy lifestyle. Healthy habits like appropriate nutritional approaches or the consumption of certain natural products or food supplements have been suggested as non-pharmacological strategies for the treatment and prevention of type 2 diabetes. Some of the main bioactive compounds from plant foods are polyphenols, important mainly for their antioxidant capacity in oxidative stress conditions and ageing. Anthocyanins are polyphenols of the flavonoid group, which act as pigments in plants, especially in fruits such as berries. A search of in vitro, in vivo and human studies in relation with antidiabetic properties of anthocyanins has been performed in different electronic databases. Results of this review demonstrate that these compounds have the ability to inhibit different enzymes as well as to influence gene expression and metabolic pathways of glucose, such as AMPK, being able to modulate diabetes and other associated disorders, as hyperlipidaemia, overweight, obesity and cardiovascular diseases. Additionally, human interventional studies have shown that high doses of anthocyanins have potential in the prevention or treatment of type 2 diabetes; nevertheless, anthocyanins used in these studies should be standardized and quantified in order to make general conclusions about its use and to claim benefits for the human population.

Urolithin A is a metabolite generated from ellagic acid and ellagitannins by the intestinal microbiota after consumption of fruits such as pomegranates or strawberries. The objective of this study was to determine the cytoprotective capacity of this polyphenol in Neuro-2a cells subjected to oxidative stress, as well as its direct radical scavenging activity and properties as an inhibitor of oxidases. Cells treated with this compound and H2O2 showed a greater response to oxidative stress than cells only treated with H2O2, as mitochondrial activity (MTT assay), redox state (ROS formation, lipid peroxidation), and the activity of antioxidant enzymes (CAT: catalase, SOD: superoxide dismutase, GR: glutathione reductase, GPx: glutathione peroxidase) were significantly ameliorated, additionally, urolithin A enhanced the expression of cytoprotective peroxiredoxins 1 and 3. Urolithin A also acted as a direct radical scavenger, showing values of 13.2 &mu, M Trolox Equivalents for Oxygen Radical Absorbance Capacity (ORAC) and 5.01 &micro, M and 152.66 &micro, M IC50 values for superoxide and 2,2-diphenyss1-picrylhydrazyl (DPPH) radicals, respectively. Finally, inhibition of oxidizing enzymes, such as monoamine oxidase A and tyrosinase, was also detected in a dose-dependent manner. The cytoprotective effects of urolithin A could be attributed to the improvement of the cellular antioxidant battery, but also to its role as a direct radical scavenger and enzyme inhibitor of oxidases.

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 &alpha, 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, &alpha, glucosidase, and lipase. The best results were found in the &alpha, glucosidase assay, as M. incana hydroalcoholic extract was able to inhibit the enzyme &alpha, 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.

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&ndash, 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.

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 a (TNF-a) 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-a 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.

AIM To study complete dose-dependent effects of obestatin on lipolytic and glucose transport activities in human adipocyte preparations highly responsive to insulin. METHODS Adipocytes were prepared by liberase digestion from subcutaneous abdominal adipose tissue obtained from overweight subjects undergoing plastic surgery. The index of lipolytic activity was the glycerol released in the incubation medium, while glucose transport was assessed by [3H]-2-deoxyglucose uptake assay. RESULTS When tested from 0.1 nmol/L to 1 μmol/L, obestatin did not stimulate glycerol release; it did not inhibit the lipolytic effect of isoprenaline and did not alter the insulin antilipolytic effect. Obestatin hardly activated glucose transport at 1 μmol/L only. Moreover, the obestatin stimulation effect was clearly lower than the threefold increase induced by insulin 100 nmol/L. CONCLUSION Low doses of obestatin cannot directly influence lipolysis and glucose uptake in human fat cells.

Helichrysum stoechas (L.) Moench is one of the scientific names of everlasting flower, which has traditionally been used as an ornamental, medicinal and food plant. The aim of this study was to identify the main phytochemical constituents as well as to evaluate the potential of this plant in terms of antioxidant, antidiabetic and neuroprotective activities. The phytochemical analysis of the methanolic extract allowed for the identification of ten constituents mainly of phenolic nature and with chemosystematic relevance: two heterodimeric phloroglucinols, arzanol (1) and compound (3), one homodimeric α-pyrone, helipyrone (2), three phenolic acids, p-hydroxybenzoic (4), caffeic (5) and neochlorogenic (6) acids, one polymethoxylated and two glycosidic flavonoids, 5,7-dihydroxy-3,6,8-trimethoxyflavone (7), isoquercitrin (8) and quercetagetin-7-O-glucopyranoside (9) together with santinol B (10). Bioassays showed significant antioxidant and antiproliferative effects and for the first time the potential of Helichrysum stoechas to inhibit the MAO-A, AChE and TYR enzymes, as well as to exert anti-α-glucosidase and anti-dipeptidyl peptidase-4 activities.

Pomegranate juice (PJ) is a beverage with potential beneficial effects due to its high content of polyphenols. The objective of this study is to explore at a molecular level the direct properties of PJ and its two main polyphenolic components, punicalagin and ellagic acid, on adipocyte functions. Increasing doses of PJ were tested using radiometric methods to determine amine oxidase activities in human adipose tissue preparations. The influences on lipogenic and lipolytic activity were also assessed by radiochemical and colorimetric assays. The results showed a dose-dependent capacity of PJ to inhibit the monoamine oxidase and the semicarbazide-sensitive amine oxidase activities present in human adipose tissue. PJ also inhibited lipogenesis and lipolysis in mouse and human adipose cells, while punicalagin and ellagic acid inhibited lipolysis rather than lipogenesis. However, the combination of punicalagin and ellagic acid resulted in a synergistic action in impairing MAO activity or basal glucose incorporation into lipids.

Tyramine is naturally occurring in foods. This biogenic amine is known to induce hypertension, especially when ingested by individuals treated by irreversible inhibitors of monoamine oxidases (MAO). However, in animals, tyramine is also an agonist for trace amine-associated receptors and substrate of semicarbazide-sensitive amine oxidases (SSAO). Though tyramine can alter aminergic transmission by various mechanisms, it was recently reported that prolonged tyramine supplementation does not deteriorate glucose tolerance and does not cause adverse cardiovascular effects in mice. Since previous studies have described insulin-like effects of tyramine in fat cells from diabetic rats, we have further tested tyramine in vitro and in vivo actions on fattening. To this aim, antilipolytic and lipogenic responses to insulin and tyramine were first compared in rat adipocytes while tyramine oxidation was compared in adipose and intestinal tissues. Then, effects of repeated intraperitoneal injections of tyramine (17 µmol/kg/day) on adiposity and on adipocyte functions were studied in young and mature rats. Millimolar doses of tyramine inhibited glycerol release by adipocytes with a maximal antilipolytic effect comparable to that of insulin. Repeated tyramine administration enhanced fat deposition in epididymal white adipose tissue, irrespective of the age of treated rats. This effect was not accompanied by desensitization to lipogenic activation by insulin, tyramine or hydrogen peroxide. Lastly, tyramine was more readily oxidized in adipose than in intestinal tissues when enzymatic activity was expressed per mg of protein. Moreoever, MAO mostly contributed to oxidative deamination in gut while SSAO was predominant in fat. Thus, both short-term and prolonged effects of tyramine were evidencing somewhat insulin-like actions in adipose tissue and led to reconsider the risk/benefit ratio of the dietary intake of this amine.

This study was undertaken to evaluate the nutraceutical potential of the Mela Rosa dei Monti Sibillini (MR), an ancient apple variety of the Sibillini Mountains, central Italy. The chemical profile of the apple&rsquo, s polyphenolic-rich extract (MRE) obtained from first- and second-choice samples using the Amberlite&reg, XAD7HP resin was analyzed by High Performance Liquid Chromatography with Diode-Array and Mass spectrometry (HPLC-DAD-MS) and 21 phytochemicals were quali&ndash, quantitatively determined. For comparative purposes, the polyphenol-rich extract of Annurca (ANE), a southern Italian variety, was analyzed. The antioxidant capacity of MREs was evaluated by Folin&ndash, Ciocalteu, 1, 1-diphenyl-2-picrylhydrazyl (DPPH), and 2, 2&prime, azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) assays. The inhibitory capacity of MREs for the enzymes &alpha, glucosidase, lipase, monoamine oxidase A, tyrosinase, and acetylcholinesterase was also determined. The MREs showed higher polyphenolic and triterpene profiles than the ANE. Their radical scavenging activity was higher than that of ANE and comparable to the reference trolox. The MRE from the second-choice apples displayed higher contents of the 21 phytochemicals investigated. Either MRE from second-choice or first-choice samples showed enzymatic inhibition with IC50 values higher than those of reference inhibitors but worthy of nutraceutical consideration. Taken together, these results show the potential of MRE as a source of bioactive compounds to be used for pharmaceutical, nutraceutical, and cosmeceutical applications has been confirmed.

Studies in animal models of diabetes and obesity have shown that resveratrol mitigates complications of metabolic diseases, beyond those resulting from oxidative stress. Furthermore, results obtained with cultured preadipocytes have also revealed that prolonged resveratrol treatment impairs adipogenesis. Considering the role of adipocytes in the hypertrophy of fat stores, and keeping in mind that insulin is the main trigger of excessive energy storage during post-prandial periods, the present study aimed to investigate how short-term effects of resveratrol can limit glucose disposal in a gut-adipose tissue axis. We found that resveratrol exhibits a more potent inhibitory capacity towards alpha-glucosidase than pancreatic lipase activity. Resveratrol also rapidly blunts glucose transport in mature fat cells by counteracting the effect of insulin and insulin-like lipogenic agents. Within two hours, resveratrol also inhibited the incorporation of glucose into lipids of adipocytes, which was unaffected by membrane cholesterol depletion. Moreover, the comparison between adipocytes with invalidated semicarbazide-sensitive amine oxidase activity and their control, or between resveratrol and several inhibitors, did not indicate that the recently described interaction of resveratrol with amine oxidases was involved in its antilipogenic effect. Caffeine and piceatannol, previously said to interact with glucose carriers, also inhibit lipogenesis in adipocytes, whereas other antioxidant phytochemicals do not reproduce such an antilipogenic effect. This study highlights the diverse first steps by which resveratrol impairs excessive fat accumulation, indicating that this natural molecule and its derivatives deserve further studies to develop their potential anti-obesity properties., This research received no external funding. Corresponding authors' studies were supported by recurrent funding from the French National Institute of Health (INSERM), and from recurrent funding of the Univ. San Jorge.

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.

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&minus, 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&minus, 1 and 28.1 &micro, g cm&minus, 2, respectively. Its main constituent, carvacrol, achieved larvicidal LC50(90) of 29.5 and 39.2 mg L&minus, 1, while contact toxicity assays on adults had an LC50(90) of 25.5 and 35.8 &micro, 2, respectively. In fumigation assays, the LC50 was 12.1 &micro, L L&minus, 1 after 1 h and decreased to 1.3 &micro, 1 in 24 h of exposure. Similarly, the fumigation LC50 of carvacrol was 8.2 &micro, 1 after 1 h of exposure, strongly decreasing to 0.8 &micro, 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.

The juices of berries or red fruits are appreciated as a source of antioxidants with potential health effects. However, they are rich in carbohydrates, an aspect that could be considered negative in view of diabetes and obesity epidemics. Indeed, it is the high polyphenol content of these beverages that is beneficial. When drinking such natural beverages, the consumers have the feeling of following a diet rich in fruit, recognized to reduce the risk of oxidative stress, cardiovascular injury, cancer, and neurodegenerative disorders. In this chapter, the polyphenol content will be compared between cranberry (Vaccinium macrocarpon), blueberry (Vaccinium myrtillus), sour cherry (Punica granatum), and pomegranate (P. granatum) juices. These juices are not a source of resveratrol, the most known polyphenol found in red wines, but the phenolic compounds they contain (punicalagins, ellagic acid, phenolic acids, and kuromanin) are more than mere antioxidants. These polyphenols exhibit superoxide radical scavenging activity and bacteriostatic properties and are protective for their plant of origin. Once ingested, they interact with various enzymes in human tissues, and with intestinal microbiota. We will focus attention on the interplay between extracts of such juices and monoamine oxidase (MAO) activity. MAO is involved in the metabolism of brain neurotransmitters and is expressed in peripheral tissues such as adipose tissue and produces hydrogen peroxide when degrading dietary amines (e.g., tyramine). We report that lyophilisates of fruit juices and their polyphenols inhibit human MAO. In addition, the red fruit polyphenols inhibit alpha-glucosidase, a key enzyme of glucose metabolism. Thus, polyphenols of red fruits juices should have beneficial effects on consumers not only in terms of antioxidant potential, but also as a consequence of modulation of amine degradation and metabolism, potentially acting on the mood and adiposity of the consumers.