62 research outputs found

    Synthesis of carboxylic acid derivatives of 2-pyrazolines

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    The medicinal halophyte frankenia laevis l. (Sea Heath) has in vitro antioxidant activity, α-glucosidase inhibition, and cytotoxicity towards hepatocarcinoma cells

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    This work explored the medicinal halophyte Frankenia laevis L. (sea heath) as a potential source of bioactive natural products. In this sense, methanol and dichloromethane extracts were prepared from aerial organs containing flowers, leaves and stems, and were profiled for their chemical composition using high-performance liquid chromatography coupled with electrospray ionization mass spectrometry (HPLC-ESI-MS/MS). The extracts were evaluated for their in vitro antioxidant capacity using five complementary methods: enzyme inhibitory effects on enzymes related with neurodegeneration (acetyl (AChE) and butyrylcholinesterase (BuChE)), Type 2 diabetes (α-glucosidase and α-amylase), hyperpigmentation/food oxidation (tyrosinase), and cytotoxicity towards human hepatocarcinoma (HepG2) cells. Fifty-one molecules were identified in the extracts, including several derivatives of phenolic acids, lignans and flavonoids, monoterpenes, and hydroxylated derivatives of linoleic acid. The methanol extract was effective in DPPH and ABTS radical scavenging (EC50 = 0.25 and 0.65 mg/mL, respectively), copper chelation (EC50 = 0.78 mg/mL), and iron reduction (EC50 = 0.51 mg/mL) activities, whereas the dichloromethane extract had high iron chelating ability (EC50 = 0.76 mg/mL). Both extracts showed the capacity to inhibit α-glucosidase, especially the dichloromethane (EC50 = 0.52 mg/mL). This extract also exerted a significant selective cytotoxicity towards HepG2 cells (EC50 = 52.1 µg/mL, SI > 1.9). In conclusion, extracts from the aerial parts of sea heath were shown to be a promising source of natural products for pharmaceutical and/or food additive applications due to their high antioxidant, anti-diabetic, and cytotoxic properties.info:eu-repo/semantics/publishedVersio

    HPLC-MS analysis of the active ingredients of chamomile (Matricaria chamomilla) bee feeding syrup

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    Apiarists let prepare by bee honey products containing medicinal drugs. Our aim was to prove that the active ingredients originated from the herbs are also present in the bee products. This publication focuses only to the chamomile (Matricaria chamomilla) containing feeding syrup and the difference between the various syrup phases. To fulfil this task, we developed a method analysing the non-volatile components of the syrup using the flowers of chamomile. The method involves a filtration followed by HPLC-MS analysis. The analyses and the data evaluations proved that the non-volatile components of the herb were transferred to syrup. As the characteristic components of certain herbs could be identified also in the syrup, it is obvious that the components responsible for the medicinal effects are also transferred

    Role of physical activity and diet in incidence of hypertension: a population-based study in Portuguese adults

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    Background/Objectives: To evaluate longitudinally the role of physical activity (PA) (type and intensity) and diet (measured using DASH score, nutrients and food intake) in hypertension incidence. Subjects/Methods: As part of the EPIPorto study, 549 participants (X40 years), resident in Porto, Portugal, at risk of developing hypertension, were evaluated. Blood pressure (BP) measurements were obtained twice (1999–2003 and 2005–2008), with a median interval of 3.8 years. Hypertension was defined as systolic BP>=140mmHg and/or diastolic BP>=90mmHg, and/or if the subjects were under anti-hypertensive therapy. Validated questionnaires were used to assess usual PA and dietary intake during the previous year. Poisson regression was used to calculate the incident rate ratios (IRRs) and respective 95% confidence intervals (95% CIs). Results: In our population, the crude incidence rate (95% confidence interval (CI)) per 100 person-years of hypertension was 6.23 (5.26–7.20). After adjustment for several confounders, an inverse, though not significant, association was found across increasing tertiles of leisure-time PA and IRR (95% CI): 1 (reference); 0.77 (0.51–1.16); and 0.74 (0.48–1.11). No significant associations between the DASH score and hypertension incidence were observed. However, potassium intake (mg/1000 kcal) was shown to be inversely associated with hypertension development (upper tertile: >1863.0 for women and >1657.2 for men) vs first tertile (IRR=0.65 (0.44–0.96), P for trend=0.025). Additionally, in multivariate analysis, a significantly inverse association between the consumption of fruits/vegetables/pulses and hypertension incidence was found (upper vs first tertile: IRR=0.61 (0.40–0.93), P for trend=0.024). Conclusions: In Portuguese adults, after adjustment for several confounders, the development of hypertension was inversely associated with potassium and fruits/vegetables/pulses intake. A dose–response is inherent to these inverse associations

    Nutritional anti-nutritional chemical composition and antioxidant activities of the leaves of the sea cliff dwelling species Limonium spathulatum (Desf.) Kuntze

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    This work explored the nutritional and antioxidant properties of the leaves of the halophytic species Limonium spathulatum (Desf.) Kuntze from Tunisian sea cliffs. Furthermore, the analysis of the total phenolics and flavonoids contents and their individual compounds using high-performance liquid chromatography coupled with electrospray ionization mass spectrometry (HPLC-ESI-MS/MS) were also studied. L. spathulatum leaves had high levels of moisture, ash, neutral detergent fiber, and acid detergent fiber, but low concentrations of crude protein, crude fat and acid detergent lignin. It contained low carbohydrates levels, and low energetic values. The most abundant macroelements were Cl, Na and Ca while the microelements detected in the highest levels were Fe and Zn. No relevant alpha-amylase inhibition was observed, and no toxic metals (Pb and Cd) and phytic acid were detected. The ethanol and the hydroethanolic extracts had the highest capacity to scavenge free radicals, to chelate iron and copper and to inhibit lipid peroxidation. The same samples were also the most active towards oxidative haemolysis. These extracts contained high total phenolic and flavonoid contents. HPLC analysis, performed on ethanolic extracts identified 58 individual compounds known for their high antioxidant actvitiy including hydroxybenzoic acids (gallic, syringic acids), hydroxycinnamic acids (caffeic, coumaric, ferulic acids) and flavonoids (catechin, epigallocatechin gallate and naringin).In conclusion, the leaves of Tunisian accession of L. spathulatum were good source of minerals and fibers useful in the human diet for attaining nutritional sufficiency. The high in vitro and ex vitro antioxidant activities associated with high favonoids contents and compounds suggest the possibility to use the extracts of L. spathulatum in herbal products with the aim of improving general health and well-being, and/or as food additives for preventing lipid oxidation of lipid-rich foodinfo:eu-repo/semantics/publishedVersio

    Chemical profiling and biological evaluation of Nepeta baytopii extracts and essential oil: An endemic plant from Turkey

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    Nepeta baytopii is a poorly studied, endemic Nepeta species (Lamiaceae) of Turkey. For the first time, the biological activities (antioxidant, enzyme inhibition, and cytotoxicity properties) of the hexane, ethyl acetate, methanol, water/methanol, and water extracts and essential oil prepared from N. baytopii aerial parts were assessed. Hydro-methanol (41.25 mg gallic acid equivalent (GAE)/g) and water extracts (50.30 mg GAE/g), respectively showed the highest radical scavenging (94.40 and 129.22 mg Trolox equivalent (TE)/g, for 2,2-diphenyl-1-picrylhydrazyl radical and 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid radical scavenging assays) and reducing (229.37 and 129.55 mg TE/g, for ferric-reducing antioxidant power and cupric-reducing antioxidant capacity assays) capacities in vitro. An interestingly high inhibition was observed for ethyl acetate extract against butyrylcholinesterase (10.85 mg galantamine equivalent/g). The methanol extract showed high cytotoxicity (31.7%) against HepG2 cells. Caryophyllene oxide was identified in high concentrations in the essential oil (39.3%). Luteolin and apigenin and their derivatives were identified from the methanol and water extracts. The results obtained from this study highlighted that the abundance of highly bioactive compounds from Nepeta baytopii ensures the multiple biological activities of the tested extracts, and this suggests a potential use in the pharmaceutical and nutraceutical fields, and therefore should be investigated further.info:eu-repo/semantics/publishedVersio

    Towards the Pharmacological Validation and Phytochemical Profiling of the Decoction and Maceration of Bruguiera gymnorhiza (L.) Lam.-A Traditionally Used Medicinal Halophyte

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    Decoctions (leaves and roots) of Bruguiera gymnorhiza (L.) Lam. are traditionally used against diabetes in many countries, including Mauritius. This study endeavoured to evaluate the inhibitory potential of leaves, roots, twigs and fruits extracts (decoction and maceration) of B. gymnorhiza against key enzymes relevant to diabetes. Considering complications related to diabetes, other clinical enzymes, namely, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, elastase and pancreatic lipase, were used. Identification of compounds was carried out using ultra-high-performance liquid chromatography/electrospray ionization tandem mass spectrometry (UHPLC-ESI-MS/MS). Antioxidant capacities were assessed using DPPH, ABTS, FRAP, CUPRAC, phosphomolybdenum, metal chelating. The relationship between mode of extraction, plant parts and biological activities was determined using multivariate analysis. Macerated fruits, rich in phytochemicals (phenolic, flavanol, tannin, and triterpenoid), exhibited substantially high antioxidant capacities related to radical scavenging (DPPH: 547.75 ± 10.99 and ABTS: 439.59 ± 19.13 mg TE/g, respectively) and reducing potential (CUPRAC: 956.04 ± 11.90 and FRAP: 577.26 ± 4.55 mg TE/g, respectively). Additionally, the same extract significantly depressed AChE and BChE (3.75 ± 0.03 and 2.19 ± 0.13 mg GALAE/g, respectively), tyrosinase (147.01 ± 0.78 mg KAE/g), elastase (3.14 ± 0.08 mg OE/g) and amylase (1.22 ± 0.01 mmol ACAE/g) enzymatic activities. Phytochemical results confirmed the presence of 119 compounds in all maceration and 163 compounds in all decoction samples. The screening also revealed important compounds in the extracts, namely, quinic acid, brugierol, bruguierol A, epigallocatechin, chlorogenic acid, to name a few. Multivariate analysis reported that the plant parts of B. gymnorhiza greatly influenced the observed biological activities in contrast to the types of extraction methods employed. Docking calculations have supported the findings of the experimental part through the high binding affinity and strong interactions of some compounds against tyrosinase, AChE, BChE and elastase enzymes. The decocted root and leaf of B. gymnorhiza showed low to moderate antidiabetic activity, thereby partially supporting its traditional uses in the management of diabetes. However, the fruit, the most active organ, can be used as a diet supplement to reduce the risk of diabetes complications after evaluating its cytotoxic effects.Funding: This research was funded by UAEU Program for Advanced Research, grant number 31S398-UPAR to Yusra Al Dhaheri.Scopu
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