Search

Interest in developing coffee substitutes is on the rise, to minimizing its health side effects. In the Middle East, date palm (Phoenix dactylifera L.) pits are often used as a coffee substitute post roasting. In this study, commercially-roasted date pit products, along with unroasted and home-prepared roasted date pits, were subjected to analyses for their metabolite composition, and neuropharmacological evaluation in mice. Headspace SPME-GCMS and GCMS post silylation were employed for characterizing its volatile and non-volatile metabolite profile. For comparison to roasted coffee, coffee product was also included. There is evidence that some commercial date pit products appear to contain undeclared additives. SPME headspace analysis revealed the abundance of furans, pyrans, terpenoids and sulfur compounds in roasted date pits, whereas pyrroles and caffeine were absent. GCMS-post silylation employed for primary metabolite profiling revealed fatty acids&rsquo, enrichment in roasted pits versus sugars&rsquo, abundance in coffee. Biological investigations affirmed that date pit showed safer margin than coffee from its LD50, albeit it exhibits no CNS stimulant properties. This study provides the first insight into the roasting impact on the date pit through its metabolome and its neuropharmacological aspects to rationalize its use as a coffee substitute.

FLAVONOIDS have demonstrated neuroprotective activity. Hesperidin, the major flavonoid in the hydroalcoholic extract of Citrus trifoliata L. fruits was quantified quantitatively using HPLC. The calibration curve obtained by plotting different concentrations of hesperidin standard versus the area under the curve revealed that hesperidin content was up to 30 mg/g. Hesperidin was isolated and identified using 1H and 13C NMR. Self-nano-emulsifying drug delivery system (SNEDDS) was prepared to improve the physical characteristics and optimize the activity of the extract. Monoamine oxidase enzyme (MAO-B) inhibitory effects of the SNEDDS, the extract, and the isolated hesperidin were evaluated. They showed significant decrease in the IC50 up to 129.9008, 252.7341, and 707.7631 ng/ml, respectively, compared with selegiline, with IC50 of 133.8403 ng/ml. The SNEDDS showed the highest activity, whereas the hydroalcoholic extract showed higher activity than the pure hesperidin, which could be attributed to synergistic effect of other flavonoids in extract. Hesperidin molecular docking studies were carried out. The ability of hesperidin to interact with the key amino acids in MAO-B binding site rationalizes this pronouncing activity as proven by its docking pattern and docking score compared with that of the known MOA-B inhibitor, safinamide.

Phoenix dactylifera L. (date palm) is one of the most valued crops worldwide for its economical and nutraceutical applications of its date fruit (pericarp). Currently date pits, considered as a waste product, is employed as coffee substitute post roasting. Whereas, pollen represents another valuable by-product used as a dietary supplement. In this study, a large-scale comparative metabolomics approach was performed for the first characterization and standardization of date palm by-products viz., date pits and pollen. Moreover, roasting impact on date pit metabolite composition was also assessed. Metabolites profiling of pits and pollen was determined via a multiplex approach of UPLC–MS and NMR, coupled to multivariate analysis, in relation to its antioxidant activities. Chemical analyses led to the identification of 67 metabolites viz., phenolic acids, flavonols, fatty acids, sphingolipids, steroids and saponins of which 10 are first time to be reported. The enrichment of steroids in date pollen accounts for its fertility promoting properties, whereas date pit was found a rich source for antioxidant polyphenols using metabolomics.

Development of natural nano-based plant-protection formulations represents an emerging phenomenon that has been widely improved for crops protection and for enhancing the efficiency and safety of pesticides. In the present study we isolated the essential oil from the fruits of Citrus trifoliata L. and investigated it using gas chromatography-mass spectrometry analysis. Limonene (78.46%) was the major component followed by β-Myrcene (7.94%) and Caryophyllene (4.20%). Citrus trifoliata essential oil (CTEO) loaded nano-cubosomes were successfully prepared by the emulsification technique. The insecticidal and fungicidal activities of formulated CTEO nano-cubosomes and unformulated CTEO were tested. While both of them exhibited substantial activities, CTEO nano-cubosomes were more effective than unformulated oil. It is the first time to formulate CTEO in nano-cubosomes and examine their insecticidal and fungicidal activities. In light of the current study, CTEO as it is or as nano-cubosomes is recommended as a promising candidate for pest and fungal pathogens control.

One new (1) together with four known sterols (2 - 5) and a sesquiterpene (6) were isolated from a polar extract of the Red Sea soft coral Lobophytum crassum. The compounds were identified as 24-methylenecholest-5-ene-lα,3β,1lα-triol 1-acetate (1), 24-methylenecholest-5-ene-la,3β,llα-triol (2), 24- methylenecholest-5-ene-3β-ol (3), 24-methylenecholestane-la,3β,5α,6β,I la-pentol (4), 24-methylenecholestane-3β,5α,6β-triol (5) and alismoxide (6) based on extensive NMR analysis. The cytotoxicity of compounds 1 - 6 was evaluated in vitro using three human cancer cell lines viz., HepG2, Hep-2 and HCT-I 16. Compound 1 showed selective cytotoxic activity against HepG2, while 3 exhibited cytotoxicity against all tested cell lines.

A bioactivity-guided investigation of the ethanolic extract (70%) of the stem bark of Pterocarpus dalbergioides Roxb. ex DC revealed that the butanol fraction possessed potent antihyperglycemic and anti-inflammatory activities at a dose of 100 mg/kg b.wt. compared to metformin (150 mg/kg b.wt.) and indomethacin (20 mg/kg b.wt.) respectively. Two phenolic acids viz: gentisic (1) and gallic (3) acids and isoflavone genistin (2) were isolated for the first time from the studied plant adopting a bioactivity-guided fractionation. Identification of the isolated compounds was achieved using physical, chemical and spectroscopic data.

Different extracts of Nigella sativa L. seed waste; aqueous (AE) 200 mg/kg, ethanol 70% (EE) 250 mg/kg and hexane (HE) 10 mg/kg, were evaluated for their hepatoprotective activities. They were administered orally, once daily, for 5 consecutive days. On day 5, liver injury was induced in animals by a single i.p. injection of carbon tetrachloride (10 mg/kg b. w. of 0.25% (v/v). Hepatoxicity produced, was evaluated by both biochemical and histopathological investigations. The aqueous extract attenuated the CCl(4) -induced liver damage likely due to the decrease of proinflammatory cytokines and T-cell proliferation. This was noticed by a significant decrease in both serum and tissue cytokines; tumor necrosis factor-alpha (TNF-α), interferon-gamma (INF-γ) and interlukin-beta (IL-1β), in the markers of liver functions; bilirubin and glutamic pyruvic transaminase (GPT) and in the oxidative stress markers; malondialdehyde (MDA) and glutathione content (GSH). Fractionation of this extract was performed and its component, protein, saponin, and polyphenol fractions were evaluated by appropriate analytical procedures. The crude protein of the seed waste reached 36.85% while protein fingerprint showed four bands ranging from 91.97 KD and 29.00 KD. The saponin content was evaluated through the determination of the haemolytic index and reached 15.56 mg/g dry powder. Finally, Folin Ciocalteu method was used for the determination of the total polyphenols. The same biochemical and histopathological studies were again performed on the different fractions of the aqueous extract; protein fraction (PF) 10 mg/kg, saponin fraction (SF) 5 mg/kg and polyphenol fraction (FF) 10 mg/kg. The biochemical changes were improved only by the protein fraction (PF) of the seed waste of Nigella sativa. This was manifested by a significant reduction in both serum and tissue cytokines in the liver markers and in the oxidative stress markers. Moreover, liver histopathology showed that (PF) reduced the incidence of liver lesions including hepatic cells cloudy swelling, lymphocytes infiltration, hepatic necrosis and fibrous connective tissue proliferation induced by CCl(4) in mice. From this study, it is concluded that the protein fraction of the aqueous extract of Nigella sativa seed waste exhibited a promising hepatoprotective effect in the management of different liver disorders.

A hexane extract of the flower-heads of Euryops pectinatus L. (Cass.) was formulated into local anti-inflammatory implantation patches with controlled release. Cross-linked sodium hyaluronate patches (F1-F3) and chitosan patches (F4-F6) were prepared by a casting/solvent evaporation technique. Morphological and mechanical characterizations including the components ratio, surfactant and the loaded amount of the hexane extract (50, 100, and 200 mg/kg b.wt.) were investigated. Release studies were performed during 24 h using a diffusion cell. Films with optimum in vitro release rate have been investigated for testing the anti-inflammatory activity and the sustaining effect of the formulations. The sustained anti-inflammatory effect of the hexane extract of E. pectinatus flower-heads from the selected films was studied by inducing paw edema in rats with 1% (w/v) carrageenan solution. The results indicated the compatibility of hexane extract with both sodium hyaluronate and chitosan patches forming yellowish transparent films. Based on variations in drug release profiles throughout the 24-h among the formulations (F1-F6) studies, F3 and F6 were selected for further investigation. When the films were applied 1 h before the subplantar injection of carrageenan in the hind paw of male Albino rats, formulation (F3) provided its maximum inhibition of paw edema in rats (91.3%) 4 h after edema induction whereas, formulation (F6) showed less inhibition after 4 h (70.6%). The previous two formulations (F3 and F6) produced potent results (95.3 and 89.5%, respectively) after 24 h when compared with a local market preparation containing 25% β-sitosterol used as positive control. Histophathological investigation was conducted for 1, 4, and 12 weeks to study the tissue response for the two formulations (F3 and F6) at the implantation site. Chemical investigation of the hexane extract was achieved for both unsaponifiable matter (USM) and fatty acid methyl esters (FAME) using gas liquid chromatography (GLC). The USM was dominated by n-pentacosane (14.40%), phytosterols (Cholesterol, Campesterol, Stigmasterol, β-sitosterol, α-amyrin) reached 33.44% and the FAME was dominated by Linoleinic (49.97%). Quality control of the local implantation was evaluated by GLC using cholesterol as an analytical marker and phytosterols as an active marker compared to the plain extract.

Passiflora incarnata as well as some other Passiflora species are reported to possess anxiolytic and sedative activity and to treat various CNS disorders. The medicinal use of only a few Passiflora species has been scientifically verified. There are over 400 species in the Passiflora genus worldwide, most of which have been little characterized in terms of phytochemical or pharmacological properties. Herein, large-scale multi-targeted metabolic profiling and fingerprinting techniques were utilized to help gain a broader insight into Passiflora species leaves' chemical composition. Nuclear magnetic resonance spectroscopy (NMR) and mass spectrometry (MS) spectra of extracted components derived from 17 Passiflora accessions and from different geographical origins were analyzed using multivariate data analyses. A total of 78 metabolites were tentatively identified, that is, 20 C-flavonoids, 8 O-flavonoids, 21 C, O-flavonoids, 2 cyanogenic glycosides, and 23 fatty acid conjugates, of which several flavonoid conjugates are for the first time to be reported in Passiflora spp. To the best of our knowledge, this study provides the most complete map for secondary metabolite distribution within that genus. Major signals in (1)H-NMR and MS spectra contributing to species discrimination were assigned to those of C-flavonoids including isovitexin-2″-O-xyloside, luteolin-C-deoxyhexoside-O-hexoside, schaftoside, isovitexin, and isoorientin. P. incarnata was found most enriched in C-flavonoids, justifying its use as an official drug within that genus. Compared to NMR, LC-MS was found more effective in sample classification based on genetic and/ or geographical origin as revealed from derived multivariate data analyses. Novel insight on metabolite candidates to mediate for Passiflora CNS sedative effects is also presented.

Chemical investigation of an ethyl acetate soluble fraction of Sinularia polydactyla (Ehrenberg) led to the isolation of three known terpenoides, two of them sterols, 24-methylcholestane-3β,5α,6β,25-tetrol 25-monoacetate (1), 24-methylcholestane-5-en-3β,25-diol (2), in addition to a cembranoid diterpene, durumolide C (3), for the first time. The cytotoxicity and antimicrobial activities of the ethyl acetate extract and the isolated compounds 1-3 were evaluated in vitro. Durumolide C (3) showed selective cytotoxicity against HepG2 (IC50 1.0 μg/mL), whereas 24-methylcholestane-3β,5α,6β,25-tetrol 25-monoacetate (1) showed IC50 of 6.1 and 8.2 μg/mL against Hep2 and HCT human cancer cell lines, respectively.

One new (1) together with four known sterols (2 - 5) and a sesquiterpene (6) were isolated from a polar extract of the Red Sea soft coral Lobophytum crassum. The compounds were identified as 24-methylenecholest-5-ene-1α,3 1α,11α-triol 1-acetate (1), 24-methylenecholest-5-ene-1α,3β,11α-triol (2), 24-methylenecholest-5-ene-3β-ol (3), 24-methylenecholestane-1α,3β,5a,6P,1-pentol (4), 24-methylenecholestane-3β,5α,6β-triol (5) and alismoxide (6) based on extensive NMR analysis. The cytotoxicity of compounds 1 - 6 was evaluated in vitro using three human cancer cell lines viz., HepG2, Hep-2 and HCT-116. Compound 1 showed selective cytotoxic activity against HepG2, while 3 exhibited cytotoxicity against all tested cell lines.

Objective: Total investigation of the macro-and micromorphological features of Citrus maxima (Burm.) Merrill. In addition, DNA fingerprinting in this study was to estimate genetic polymorphism and relationships with another citrus viz: Citrus paradise and Citrus sinensis based on RAPD and ISSR markers.Methods: For the establishment of macro-and micromorphological investigation and genetic estimation, this study presents a total investigation of the macro-and micromorphological features of the roots, stems, leaves, flowers, fruits and seeds of the plants through microscopical investigation of the prepared entire, transverse sections and powdered forms of different organs under study. Furthermore, the DNA of the three plants was extracted from leaf samples and two types of DNA markers RAPD and ISSR were assayed.Results: Macro-and micromorphological features of different organs were investigated. On the other hand Genetic polymorphism and relationships among Citrus maxima, Citrus paradisi and Citrus sinensis was revealed. The highest genetic similarity was between Citrus maxima and Citrus paradisi while the lowest similarity was between Citrus paradisi and Citrus sinensis as revealed by RAPD, ISSR and combined data.Conclusion: For the present study, macro and micro-morphological characters, as well as, DNA fingerprinting can be considered as the identifying parameters for authentication of Citrus maxima (Burm.) Merrill.

Aim of the study The present study aimed to evaluate the anti-diabetic activity of Zizyphus spina-christi leaf extract (200 mg/kg b.w.), plain and formulated in STZ-diabetic rats. Percentage yield of extracts, marker yield (christinin-A) and antihyperglycemic potencies, depending on seasonal variation were investigated. The chemical stability, study of storage conditions, shelf life T90 prediction of both plain extract and formulated soft gelatin capsules by accelerated studies were studied. Material and methods Changes in all studied parameters after oral administration of Z. spina-christi extract for 28 days were reported. Seasonal variation affecting yield and activities was studied. Flavonoid contents were HPLC evaluated. The capsules were stored at 30, 40 and 50 °C [75% relative humidity] and their residual christinin-A content was assayed for 24 weeks. Christinin-A chemical degradation was monitored by HPLC stability indicating method previously validated. Possible physical examination was checked by dissolution test of the content of the capsules using dissolution tester USP XXIV. Result Oral administration of Z. spina-christi leaf extract, plain and formulated for 28 days reduced blood glucose level with significant increase in serum insulin and C-peptide levels. Marked elevation in total antioxidant capacity with normalization of percentage of glycated hemoglobin (HbA1C%) was reported. Moreover, they succeeded to reduce the elevated blood lactate level and to elevate the reduced blood pyruvate content of diabetic rats. In line with amelioration of the diabetic state, Zizyphus extract, plain and formulated restored liver and muscle glycogen content together with significant decrease of hepatic glucose-6-phosphatase and increase in glucose-6-phosphate dehydrogenase activities. In vitro experiments showed a dose-dependent inhibitory activity of Zizyphus extract against α-amylase enzyme with (IC 50 ) at 0.3 mg/ml. Such finding has been supported by the in vivo suppression of starch digestion and absorption by Zizyphus extract in normal rats. The flavonoids content of the formulated leaves (collected during June 2009) were found to be 11.5 μg/g of the dry plant material (expressed as quercetin) and 58.8 μg/g of the dry plant material (expressed as rutin). The shelf life for the capsules stored at 30, 40 and 50 °C [75% relative humidity] for plain and formulated extract were calculated to be 66.90 and 70.74 weeks, respectively. Conclusion The current work revealed that Z. spina-christi leaf extract, plain and formulated, improved glucose utilization in diabetic rats by increasing insulin secretion which may be due to both saponin and polyphenols content and controlling hyperglycemia through attenuation of meal-derived glucose absorption that might be attributed to the total polyphenols. Studies showed that leaves are preferably collected from June to October. Finally, the release followed the Higuchi kinetic model, indicating diffusion dominated drug release with no drop in the dissolution values throughout the test period.