Evaluation of Anti-inflammatory, Antinociceptive, and Antipyretic Activities of Prunus persica var. nucipersica (Nectarine) Kernel.

Nectarine (Prunus persica var. nucipersica) is a worldwide appreciated edible subspecies, with a high nutritional value and benefits on human health due to its phenolic content. Despite the large consumption of the fruit, the potential use of its kernel is poorly studied. Herein, the potential pharmacological activities and the phenolic constituents of an alcoholic extract of kernel nectarine fruits were investigated. Administering nectarine kernel extract (50 and 100 mg/kg, respectively) in rats reduced paw edema after carrageenan injection by 11 and 47% in 1 h, 24 and 33% in 2 h, and 23 and 32% in 4 h, when compared to the controls. At the higher dose (100 mg/kg), nectarine kernel extract increased the reaction time in the hot-plate model and produced a significant decrease in the rectal temperature of the pyretic rats, while both doses produced 52 and 59% of writhing inhibition compared to the control group. Total polyphenolic (55.91 ± 5.78 mg/g) and flavonoid (29.89 ± 0.55 mg/g) content indicated that the extract is a promising source of these constituents. HPLC-ESI-MS/MS analysis demonstrated the presence of flavonoids, such as naringenin and apigenin glycosides. The cyanogenic glycosides amigdalin and prunasin were also detected. These results highlight the anti-inflammatory, analgesic, and antipyretic activities of nectarine kernel alcoholic extract, together with significant phenolic content, promoting its exploitation as a source of bioactive molecules.

Phytochemical Profile, Antioxidant and Antidiabetic Activities of Adansonia digitata L. (Baobab) from Mali, as a Source of Health-Promoting Compounds.

Background: Adansonia digitata L. (Malvaceae), also known as baobab, is a tree attracting recent interest especially due to the high nutritional value of the fruit pulp. However, few studies are reported on the secondary metabolite content, showing high variability depending on the geographic region. METHODS: In this study, the chemical profiles of Malian commercial baobab fruits and leaves, focused on phenolic content, were investigated by HPLC coupled with a photodiode array (PDA)/UV and an electrospray ionization (ESI) mass spectrometer (MS) and gas chromatography (GC)/MS. In addition, the extracts of fruit pulps obtained from three different markets (Fruits 1, 2, and 3) were evaluated for their total phenolic content (TPC), antioxidant activity and α-glucosidase inhibition. RESULTS: Baobab fruit pulps were found to be rich in procyanidins and flavonol glycosides, with tiliroside as the major constituent. The baobab leaves showed a similar profile respect to the fruits, but with more detected phenolics. All fruit pulp extracts exerted antioxidant activity (highest for Fruit 3) and higher α-glucosidase inhibition than acarbose used as standard. CONCLUSIONS: This study confirmed the variability of baobab with different origins and indicated Malian species baobab as a promising source of health-promoting substances.

Cannabis sativa L. essential oil: chemical characterisation and antimicrobial activity against methicillin-resistant Staphylococcus pseudintermedius.

Cannabis sativa L. essential oil has attracted the interest of the scientific community thanks to its numerous biological activities. Several studies have evaluated EOs as alternative therapeutic approaches to limit the use of antibiotics; the present study aimed to evaluate the in vitro inhibitory and bactericidal activity of the essential oils obtained from the leaves and inflorescences of two hemp genotypes against twenty-one multidrug-resistant, methicillin-resistant Staphylococcus pseudintermedius strains isolated from canine clinical samples. Both EOs were mainly represented by sesquiterpene hydrocarbons, with a prevalence of ß-caryophyllene and α-humulene. However, different relative amounts of phytocannabinoids were also detected. Microbiological results evidenced better outcomes for the EO characterised by the highest content of phytocannabinoids, which in turn showed no differences among the tested strains. Nevertheless, both the EOs showed better inhibitory and bactericidal activities than their main constituent, ß-caryophyllene, tested individually, highlighting the presence of synergistic effects among the EO compounds.

Production of bioactive and aroma volatile compounds of Lawsonia inermis L. cultivated under different growth conditions.

The present study aimed to investigate the influence of different growing conditions on the amount of leaf pigments (chlorophylls, carotenoids), bioactive metabolites, such as polyphenols, flavonoids, lawsone and volatile organic compounds (VOCs) of Lawsonia inermis L. (henna) plants. Young henna plants were cultivated for two months in a growth chamber (GC) and in open-air conditions during summer under the Mediterranean climate (OF), and leaves were analysed to evaluate their adaptive responses. The different growth conditions modified the carbon allocation priorities, increasing antioxidant metabolites (e.g. phenolic and flavonoid compounds) while decreasing lawsone in GC conditions. Quali-quantitative changes were observed for VOCs. This study revealed that GC conditions permit an alternative use of Lawsonia cultivation, because of the increase in the endogenous content of bioactive secondary metabolites with many potential biological activities.

Comparing Metabolomic and Essential Oil Fingerprints of Citrus australasica F. Muell (Finger Lime) Varieties and Their In Vitro Antioxidant Activity.

Comparative chemical analyses among peel and pulp essential oils (EOs) and methanolic extracts of four Citrus australasica varieties (Red, Collette, Pink Ice, and Yellow Sunshine), and the hybrid Faustrime, were performed using GC-MS and UHPLC-DAD-HR-Orbitrap/ESI-MS. Peel and pulp extracts were also analysed for their in vitro antioxidant activity on a Balb/3T3 clone A31 mouse embryo fibroblast cell line. The results of peel and pulp EOs were mainly characterised by monoterpenes and sesquiterpenes, respectively. All peels displayed a higher total phenol content (TPC) than pulps, and consequently a greater antioxidant activity. Collette peels and Pink Ice pulps showed the highest amount of identified flavonoids (e.g., luteolin, isosakuranetin, and poncirin derivatives). Collette and Red peels were rich in anthocyanins (delphinidin and petunidin glycosides), exhibiting the maximum protective activity against induced oxidative damage. In conclusion, finger lime fruits are good sources of health-promoting phytocomplexes, with the Red, Collette, and Pink Ice varieties being the most promising.

Hydrosols from Rosmarinus officinalis, Salvia officinalis, and Cupressus sempervirens: Phytochemical Analysis and Bioactivity Evaluation.

The present work evaluates the aromatic waters of rosemary (Salvia rosmarinus Spenn. syn. Rosmarinus officinalis L.), sage (Salvia officinalis L.), and cypress (Cupressus sempervirens L.) obtained as innovative commercial products of a hydrodistillation process. All extracts were exhaustively analysed by GC-MS, 1H-NMR, and LC-MS in order to evaluate potential metabolite fingerprint differences. GC-MS appears to be the most exhaustive technique for the qualitative identification of the single constituents, although in this case, the use of 1H-NMR and LC-MS techniques allowed some useful considerations in semi-quantitative terms. Antimycotic effects were studied against Tricophyton, Candida, and Arthroderma species, resulting in weak activity. The toxicological impact was partly evaluated in vitro by means of allelopathy and brine shrimp lethality. Cytotoxicity was investigated in human colon cancer cells (HCT116) and in hypothalamic cells (Hypo-E22) challenged with hydrogen peroxide. Sage and rosemary hydrosols were the most effective antimycotics, whereas all hydrosols displayed antiradical effects. Cytotoxic effects against HCT116 cells (at 500 µL/mL) were related in silico to the endovanilloid TRPM8 and TRPV1 receptors. At lower concentrations (5-50 µL/mL), the hydrosols protected hypothalamic neurons Hypo-E22 cells from hydrogen peroxide-induced toxicity. The overall experience indicates that hydrolates are an important source of relevant phytochemicals with significant pharmacological potential.

Salinity-Induced Changes of Photosynthetic Performance, Lawsone, VOCs, and Antioxidant Metabolism in Lawsonia inermis L.

The present study aimed to elucidate the salinity influence on the bioactive metabolites of Lawsonia inermis L. (henna) plants. Young henna plants were cultivated under salinity stress with two NaCl concentrations (75 mM and 150 mM) in controlled environmental conditions and the leaves were investigated to check their adaptative responses. The modulation of photosynthetic performance to salinity stress was demonstrated by gas exchange and chlorophyll fluorescence parameters. The partial stomatal closure triggered an enhanced water-use efficiency, and a proline accumulation was observed, leading to an osmotic adjustment. The increased capacity to dissipate the excess excitation energy at photosystem II as heat was associated with changes in chlorophylls, anthocyanins, and carotenoids. The higher antioxidant activity at 150 mM salt level suggested its scavenger role on reactive oxygen species (ROS) dissipation and photoprotection. The reduced CO2 uptake and the higher metabolic costs necessary to sustain the henna tolerance mechanism against high NaCl concentration negatively affected lawsone production. Leaf volatile organic compounds (VOCs) showed changes in the amount and composition of VOCs with increasing salinity level. Overall, this study revealed efficient physiological and biochemical adaptations of henna leaves to salt stress despite an altered production of important economic metabolites such as lawsone.

Metronomic vinorelbine is directly active on Non Small Cell Lung Cancer cells and sensitizes the EGFRL858R/T790M cells to reversible EGFR tyrosine kinase inhibitors.

Metronomic vinorelbine (mVNR) has been described primarily as an antiangiogenic therapy, and no direct effects of mVNR on Non Small Cell Lung Cancer (NSCLC) cells has yet been demonstrated. The aims of this study were i) to establish the direct activity of mVNR on NSCLC cells either EGFR wt or EGFRL858R/T790M, and ii) to quantify the synergism of the combination with reversible EGFR tyrosine kinase inhibitors (TKIs), investigating the underlying mechanism of action. Proliferation assays were performed on A-549 (wt EGFRhigh), H-292 (EGFR-wt), H-358 (EGFR-wt), H-1975 (EGFRL858R/T790M) NSCLC cell lines exposed to mVNR, its active metabolite deacetyl-VNR (D-VNR), gefitinib and erlotinib for 144 h treatments. The synergism between mVNR and EGFR TKIs was determined by the combination index (CI) in EGFR-wt and H-1975 NSCLC cells. Cyclin-D1 and ABCG2 genes expression and protein levels were measured by RT-PCR and ELISA assays, as well as the phosphorylation of ERK1/2 and Akt. Intracellular concentrations of EGFR TKIs and VNR were investigated with a mass spectrometry system. mVNR, and its active metabolite D-VNR, were extremely active on NSCLC cells, in particular on H-1975 (IC50 = 13.56 ±â€¯2.77 pM), resistant to TKIs. mVNR inhibited the phosphorylation of ERK1/2 and Akt and significantly decreased the expression of both cyclin-D1 and ABCG2 m-RNA and protein. The simultaneous combination of VNR and reversible EGFR TKIs showed a strong synergism on EGFR-wt NSCLC cells and on H-1975 cells (e.g. CI = 0.501 for 50% of affected cells), increasing the intracellular concentrations of EGFR TKIs (e.g. +50.5% vs. gefitinib alone). In conclusions, mVNR has direct effects on NSCLC cells and sensitizes resistant cells to EGFR TKIs, increasing their intracellular concentrations.

Response to metal stress of Nicotiana langsdorffii plants wild-type and transgenic for the rat glucocorticoid receptor gene.

Recently our findings have shown that the integration of the gene coding for the rat gluco-corticoid receptor (GR receptor) in Nicotiana langsdorffii plants induced morphophysiological effects in transgenic plants through the modification of their hormonal pattern. Phytohormones play a key role in plant responses to many different biotic and abiotic stresses since a modified hormonal profile up-regulates the activation of secondary metabolites involved in the response to stress. In this work transgenic GR plants and isogenic wild type genotypes were exposed to metal stress by treating them with 30ppm cadmium(II) or 50ppm chromium(VI). Hormonal patterns along with changes in key response related metabolites were then monitored and compared. Heavy metal up-take was found to be lower in the GR plants. The transgenic plants exhibited higher values of S-abscisic acid (S-ABA) and 3-indole acetic acid (IAA), salicylic acid and total polyphenols, chlorogenic acid and antiradical activity, compared to the untransformed wild type plants. Both Cd and Cr treatments led to an increase in hormone concentrations and secondary metabolites only in wild type plants. Analysis of the results suggests that the stress responses due to changes in the plant's hormonal system may derive from the interaction between the GR receptor and phytosteroids, which are known to play a key role in plant physiology and development.