Green synthesis of zinc oxide nanoparticles using ethanolic extract of Gliricidia sepium (Jacq.) kunth. Ex. Walp., stem: Characterizations and their gastroprotective effect on ethanol-induced gastritis in rats.

The study presents a significant advancement in drug delivery and therapeutic efficacy through the successful synthesis of Gliricidia sepium(Jacq.) Kunth. ex. Walp., stem zinc oxide nanoparticles(GSS ZnONPs). The phenolic compounds present in Gliricidia sepium stem (GSS) particularly vanillic acid, apegnin-7-O-glucoside, syringic acid, and p-coumaric acid which were identified by HPLC. These compounds shown antioxidant and anti-inflammatory properties. GSS ZnONPs demonstrate pronounced gastroprotective effects against ethanol-induced gastritis, evidenced by the reduction in gastric lesions and mucosal injury upon its treatment. Histopathological evaluation and immunohistochemical analysis of nuclear factor erythroid 2-related factor 2 (Nrf2) expression further validate these results, revealing the amelioration of ethanol-induced gastritis and improved gastric tissue condition due to their treatment. Noteworthy is the dose-dependent response of GSS ZnONPs, showcasing their efficacy even at lower doses against ethanol-induced gastritis which is confirmed by different biomarkers. These findings have substantial implications for mitigating dosage-related adverse effects while preserving therapeutic benefits, offering a more favorable treatment approach. This study aims to investigate the potential gastroprotective activity of GSS ZnONPs against gastritis.

Promising Cytotoxic butenolides from the Soybean endophytic fungus Aspergillus terreus: a combined molecular docking and in-vitro studies.

AIM: This study aimed to use one strain many compounds approach (OSMAC) to investigate the cytotoxic potential of Aspergillus terreus associated with soybean versus several cancer cell lines, by means of in-silico and in vitro approaches. METHODS AND RESULTS: Fermentation of the isolated strain was done on five media. The derived extracts were investigated for their inhibitory activities against three human cancer cell lines; mammary gland breast cancer (MCF-7), colorectal adenocarcinoma (Caco-2), and hepatocellular carcinoma (HepG2) using MTT Assay. The fungal mycelia fermented in Modified Potato Dextrose Broth (MPDB) was the most cytotoxic extract against HepG2, MCF-7, and Caco-2 cell lines with IC50 4.2 ± 0.13, 5.9 ± 0.013 and 7.3 ± 0.004 µg mL-1, respectively. MPDB extract was scaled up resulting in the isolation of six metabolites; three fatty acids (1, 2, and 4), one sterol (3) and two butenolides (5 and 6) by column chromatography. The isolated compounds (1-6) were screened through a molecular docking approach for their binding aptitude to various active sites. butyrolactone-I (5) revealed a significant interaction within the CDK2 active site, while aspulvinone E (6) showed promising binding affinity to FLT3 and EGFR active sites that was confirmed by in vitro CDK2, FLT3 and EGFR inhibitory activity. Finally, the in vitro cytotoxic activities of butyrolactone-I (5) and aspulvinone E (6) revealed the antiproliferative activity of butyrolactone-I (5), against HepG2 cell line (IC50 = 17.85 ± 0.32 µM). CONCLUSION: Molecular docking analysis and in vitro assays suggested the CDK2/A2 inhibitory potential of butyrolactone-I (5) in addition to the promising interaction abilities of aspulvinone E (6) with EGFR and FLT3 active sites as a possible mechanism of their biological activities.

Network pharmacology and molecular docking study for biological pathway detection of cytotoxicity of the yellow jasmine flowers.

BACKGROUND: The yellow jasmine flower (Jasminum humile L.) is a fragrant plant belonging to the Oleaceae family with promising phytoconstituents and interesting medicinal uses. The purpose of this study was to characterize the plant metabolome to identify the potential bioactive agents with cytotoxic effects and the underlying mechanism of cytotoxic activity. METHODS: First, HPLC-PDA-MS/MS was used to identify the potential bioactive compounds in the flowers. Furthermore, we assessed the cytotoxic activity of the flower extract against breast cancer (MCF-7) cell line using MTT assay followed by the cell cycle, DNA-flow cytometry, and Annexin V-FITC analyses alongside the effect on reactive oxygen species (ROS). Finally, Network pharmacology followed by a molecular docking study was performed to predict the pathways involved in anti-breast cancer activity. RESULTS: HPLC-PDA-MS/MS tentatively identified 33 compounds, mainly secoiridoids. J. humile extract showed a cytotoxic effect on MCF-7 breast cancer cell line with IC50 value of 9.3 ± 1.2 µg/mL. Studying the apoptotic effect of J. humile extract revealed that it disrupts G2/M phase in the cell cycle, increases the percentage of early and late apoptosis in Annexin V-FTIC, and affects the oxidative stress markers (CAT, SOD, and GSH-R). Network analysis revealed that out of 33 compounds, 24 displayed interaction with 52 human target genes. Relationship between compounds, target genes, and pathways revealed that J. humile exerts its effect on breast cancer by altering, Estrogen signaling pathway, HER2, and EGFR overexpression. To further verify the results of network pharmacology, molecular docking was performed with the five key compounds and the topmost target, EGFR. The results of molecular docking were consistent with those of network pharmacology. CONCLUSION: Our findings suggest that J. humile suppresses breast cancer proliferation and induces cell cycle arrest and apoptosis partly by EGFR signaling pathway, highlighting J. humile as a potential therapeutic candidate against breast cancer.

Integration of LC/MS, NMR and Molecular Docking for Profiling of Bioactive Diterpenes from Euphorbia mauritanica L. with in Vitro Anti-SARS-CoV-2 Activity.

In spite of tremendous efforts exerted in the management of COVID-19, the absence of specific treatments and the prevalence of delayed and long-term complications termed post-COVID syndrome still urged all concerned researchers to develop a potent inhibitor of SARS-Cov-2. The hydromethanolic extracts of different parts of E. mauritanica were in vitro screened for anti-SARS-Cov-2 activity. Then, using an integrated strategy of LC/MS/MS, molecular networking and NMR, the chemical profile of the active extract was determined. To determine the optimum target for these compounds, docking experiments of the active extract's identified compounds were conducted at several viral targets. The leaves extract showed the best inhibitory effect with IC50 8.231±0.04 µg/ml. The jatrophane diterpenes were provisionally annotated as the primary metabolites of the bioactive leaves extract based on multiplex of LC/MS/MS, molecular network, and NMR. In silico studies revealed the potentiality of the compounds in the most active extract to 3CLpro, where compound 20 showed the best binding affinity. Further attention should be paid to the isolation of various jatrophane diterpenes from Euphorbia and evaluating their effects on SARS-Cov-2 and its molecular targets.

A new firewall in the fight against breast cancer: in-vitro and in-silico studies correlating chemistry to apoptotic activity of Otostegia fruticosa.

Breast cancer is the most devastating disease for women. There is a great demand for new sources to treat this disease. Medicinal plants are an indispensable source of bioactive compounds with wide range of pharmacological activities. In-vitro cytotoxic activity of Otostegia fruticosa methanolic extract against human breast cancer was studied using MCF-7 cell line. The extract showed mildly potent activity (IC50 = 51 ± 9.836 µg/mL) in comparison to the standard anticancer doxorubicin (IC50 = 7.467 ± 1.05 µg/mL). Potential compounds responsible for activity have been identified using Molecular Operating Environment (MOE) module on the major compounds detected by HPLC-MS/MS technique against estrogen alpha receptor (ERα+: PDB ID 2JF9). 3,5-di-O-dicaffeoylquinic acid, hyperoside and rutin showed similar binding and antagonistic interaction with the estrogen alpha receptor as tamoxifen in several poses. The retrieved results confirm that we can add this plant to a powerful arsenal that combats this insidious disease.

Phytochemical profiling and anti-fibrotic activities of Plumbago indica L. and Plumbago auriculata Lam. in thioacetamide-induced liver fibrosis in rats.

This study aimed at investigating the chemical composition and the hepatoprotective activities of Plumbago indica L. and P. auriculata Lam. LC-MS/MS analyses for the hydroalcoholic extracts of the aerial parts of the two Plumbago species allowed the tentative identification of thirty and twenty-five compounds from P. indica and P. auriculata, respectively. The biochemical and histopathological alterations associated with thioacetamide (TAA)-induced liver fibrosis in rats were evaluated in vivo where rats received the two extracts at three different dose levels (100, 200 and 400 mg/kg p.o, daily) for 15 consecutive days with induction of hepatotoxicity by TAA (200 mg/kg/day, i.p.) at 14th and 15th days. Results of the present study showed a significant restoration in liver function biomarkers viz. alanine transaminase (ALT), aspartate transaminase (AST), gamma glutamyl transferase and total bilirubin. The liver homogenates exhibited increased levels of antioxidant biomarkers: reduced glutathione (GSH) and catalase (CAT), accompanied with decline in malondialdehyde (MDA). Furthermore, treated groups exhibited a significant suppression in liver inflammatory cytokines: tumor necrosis factor-α (TNF-α) and interlukin-6 (IL-6), and fibrotic biomarker: alpha smooth muscle relaxant. Histopathological examination of the liver showed normality of hepatocytes. Noteworthy, P. indica extract showed better hepatoprotective activity than P. auriculata, particularly at 200 mg/kg. To sum up, all these results indicated the hepatoprotective properties of both extracts, as well as their antifibrotic effect was evidenced by reduction in hepatic collagen deposition. However, additional experiments are required to isolate their individual secondary metabolites, assess the toxicity of the extracts and explore the involved mechanism of action.

Anti-androgenic potential of the fruit extracts of certain Egyptian Sabal species and their genetic variability studies: a metabolomic-molecular modeling approach.

This work aimed to evaluate the anti-androgenic activity of S. blackburniana Glazebrook, S. causiarum (O. F. Cook) Becc, and S. palmetto (Walter) Lodd. Ex Schult fruit extracts in rats using Hershberger assay. Furthermore, to annotate secondary metabolites using LC-HRMS technique, to investigate underlying mechanisms responsible for 5-α-reductase inhibitory activity in silico and to compare cytotoxic effects in vitro against human prostatic stromal myofibroblast (WPMY-1) and human benign prostatic hyperplasia (BPH-1) cell lines using MTT, 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (spectrophotometrically). The results showed significant anti-androgenic implications with varying degrees, markedly decreased sex organ weights, reduction in testosterone and increase in LH and FSH serum levels. Genetic diversity study ensured the correct genotype and revealed outperformance of SCoT compared with CBDP markers to interpret polymorphism among selected species. S. blackburniana exhibited selective cytotoxic activity against BPH-1 compared to finasteride. Molecular docking of 59 dereplicated metabolites belonging to various chemical classes revealed that helasaoussazine, pinoresinol and tetra-O-caffeoylquinic acid are the top inhibitors of 5-α-reductase-2. Our study provides an insight into the anti-androgenic activity of selected species of Egyptian Sabal supported by docking study for the first time, demonstrates safety toward liver and kidney and highlights a new potential therapeutic candidate for anti-androgenic related disease such as benign prostatic hyperplasia.

A new arsenal of polyphenols to make Parkinson's disease extinct: HPLC-MS/MS profiling, very interesting MAO-B inhibitory activity and antioxidant activity of Otostegia fruticosa.

Fifteen compounds belong to phenolic acids, derivatives of phenolic acids, iridoids, xanthones and flavonoids were characterized in the methanolic extract of Otostegia fruticosa leaves using HPLC-MS/MS. Extract has been also investigated for its MAO-B inhibitory activity, antioxidant activity, total phenolic and total flavonoid content. The extract exhibited interesting MAO-B inhibitory activity (IC50; 2.24 ± 0.08) compared to the reference compound selegiline (0.55 ± 0.02 µg/mL). It also showed a potent antioxidant activity proven in both DPPH and ORAC assay methods. The extract showed an IC50 of 3.64 ± 1.22 µg/mL in the DPPH test which was significantly lower than that of the standard ascorbic acid which attained an IC50 of 18.3 ± 1.41 µg/mL. Moreover, in the oxygen radical absorbance capacity assay (ORAC) the extract showed a decline in the IC50 to 3.48 ± 1.16 µg/mL as compared to the standard Trolox which exhibited an IC50 of 27.0 ± 13.41.

The role of active metabolites isolated from Jasminum multiflorum flowers against hepatitis C virus infection and related hepatocellular carcinoma.

Jasminum multiflorum Burm. f. (J. multiflorum) is an ornamental plant with traditional medicinal importance. This study aims to evaluate the activity of J. multiflorum isolated compounds against hepatocellular carcinoma cells infected with hepatitis C virus (HCV) in vitro. The in vitro anti-viral and anti-oncogenic-related activity were validated by anchorage-independent assay plus transwell migration/invasion and spreading assay. In addition to chromatographic isolation of the active metabolites. The flower extract demonstrated a significant antiviral potential through reducing active viral replication by more than 90%. Study results credit this to specific reduction of viral NS5A and cellular EphA2 protein levels. Molecular docking analysis proved the role of the isolated compounds especially multifloroside, jasfloroside A and jasfloroside B as possible anti HCV molecules.

Phytochemical constituents and anti-tyrosinase activity of Macadamia integrifolia leaves extract.

Macadamia integrifolia Maiden & Betche is cultivated around the world for its highly valued nuts (macadamia nuts). Although the chemical composition of the edible macadamia oil has been repeatedly investigated, other plant organs have not been phytochemically or biologically assessed. In this study, ethanolic extract of M. integrifolia leaves was phytochemically investigated which led to the isolation of 6 compounds. Two functional galactolipids, i.e., monogalactosyl diacylglycrol 36:4 (MGDG 36:4), digalactosyl monoacylglycerol 18:2 (DGMG 18:2), gallic acid and protocatechuic acid were identified in the genus Macadamia for the first time, in addition to the cyanogenic glycoside dhurrin and ß-sitosterol. Additionally, anti-tyrosinase activity of the extract, its fractions and isolated compounds was investigated and a good tyrosinase inhibitory activity was observed for the extract, IC50=85 µg/mL and its polar fractions (ethyl acetate at 60 µg/mL and n-butanol at 75 µg/mL), with gallic acid showing strong anti-tyrosinase activity at IC50 56 µg/mL.

Antiviral Activity of Zinc Oxide Nanoparticles Mediated by Plumbago indica L. Extract Against Herpes Simplex Virus Type 1 (HSV-1).

INTRODUCTION: Plumbago indica L. is considered a valuable source in the Plumbaginaceae family for various types of active compound such as alkaloids, phenolics and saponins. To promote the usage of P. indica in the bionanotechnology field, zinc oxide nanoparticles (ZnONPs) were biosynthesized by using its alcoholic extract. The inhibitory effects of ZnONPs and the plant extract were also evaluated against HSV-1. METHODS: ZnONPs were described by the following techniques, UV-visible spectroscopy, Fourier transform infrared spectroscopy (FTIR), dynamic light scattering (DLS), zeta potential, scanning electron microscopy (SEM), transmission electron microscopy (TEM) and x-ray diffraction (XRD). The phenolic and flavonoid contents of P. indica extract, which are accountable for bioreduction, formation and stabilization of the nanoparticles, were analyzed by HPLC technique. The antiviral assessment was implemented on both agents by using Vero cell lines. RESULTS: DLS revealed that the average size of ZnONPs was 32.58 ± 7.98 nm and the zeta potential was -20.8 mV. The observation of TEM analysis revealed that the particle size of ZnONPs varied from 2.56 to 8.83 nm. The XRD analysis verified the existence of pure crystals of hexagonal shapes of nanoparticles of ZnO with a main average size of 35.28 nm that is approximating to the values of particle size acquired by SEM analysis (19.64 and 23.21 nm). The HPLC analysis of P. indica ethanolic extract showed that gallic acid, chlorogenic acid and rutin were the major compounds, with concentrations equal to 8203.99, 2965.95 and 1144.99 µg/g, respectively. Regarding the antiviral assessment, the synthesized uncalcinated ZnONPs were found to exhibit a promising activity against HSV-1, with CC50 and IC50 values equal to 43.96 ± 1.39 and 23.17 ± 2.29 µg/mL, respectively. CONCLUSION: The green synthesized ZnONPs are considered promising adjuvants to enhance the efficacy of HSV-1 drugs.

Antioxidant, Anti-Inflammatory and Cytotoxic Activities of Jasminum multiflorum (Burm. F.) Andrews Leaves towards MCF-7 Breast Cancer and HCT 116 Colorectal Cell Lines and Identification of Bioactive Metabolites.

BACKGROUND: The plants of high phenolic contents are perfect antioxidant and anti-inflammatory agents and participate in biological studies as effective agents towards different cancer cell lines. OBJECTIVE: To investigate the antioxidant, anti-inflammatory, and cytotoxic activities of the hydromethanolic leaf extract of Jasminum multiflorum (Burm. f.) Andrews. (J. multiflorum), and phenolic profiling of the extract. METHODS: The antioxidant activity for the extract was estimated using ß-Carotene-linoleic and Ferric Reducing Antioxidant Power (FRAP) assays. The anti-inflammatory activity was evaluated by histamine release assay. Cytotoxicity of J. multiflorum was performed using a neutral red uptake assay towards breast cancer (MCF-7) and colorectal cancer (HCT 116) cell lines. Phenolic profiling of the leaves was characterized using high performance liquid chromatography coupled to photodiode array detector-mass spectroscopy-mass spectroscopy (HPLC-PDA-MS/MS), and chromatographic isolation and identification of the isolated compounds were performed using spectroscopic and NMR data, and virtual docking was performed to the isolated compounds against HSP90 (HEAT SHOCK PROTEIN 90). RESULTS: At a concentration of 75 µg mL-1, J. multiflorum extract showed high antioxidant power; 68.23±0.35 % inhibition and 60.30±0.60 a TEAC (µmol Trolox g-1) for ß-Carotene-linoleic assay and FRAP assay; respectively, and possessed anti-inflammatory activity with IC50 67.2 µg/ml. J. multiflorum showed high cytotoxic activity with IC50 of 24.81 µg/ml and 11.38 µg/ml for MCF-7 and HCT 116 cell lines, respectively. HPLC-PDA-MS/MS analysis tentatively identified 39 compounds; major compounds are secoiridoid glycosides, kaempferol, and quercetin glycosides, in addition to simple phenylethanoid compounds. Isolation of active metabolites was performed and led to the isolation and identification of four compounds. On the basis of docking study using HSP90 legend, kaempferol neohesperidoside showed a high cytotoxic potential supported by a high affinity score towards HSP90 legend protein. CONCLUSION: Jasminum multiflorum is a good candidate to isolate cytotoxic agents.

Green synthesis of magnesium nanoparticles mediated from Rosa floribunda charisma extract and its antioxidant, antiaging and antibiofilm activities.

Flower based nanoparticles has gained a special attention as a new sustainable eco-friendly avenue. Rosa floribunda charisma belongs to modern roses with bright yellow, red flowers with marvellous rose scent. Different methods were used for the extraction of its floral scent such as hexane, microwave, and solid-phase micro-extraction. The latter was the most efficient method for the extraction of phenyl ethyl alcohol, the unique scent of roses. In the current study, magnesium nanoparticles (RcNps) have been synthesized using Rosa floribunda charisma petals that have privileges beyond chemical and physical routs. RcNps formation was confirmed using UV-Visible (UV-Vis) Spectroscopy, Fourier Transform Infrared Spectroscopy (FTIR), High Resolution-Transmission Electron Microscope (HR-TEM), Field Emission-Scanning Electron Microscope (FE-SEM), Energy dispersive X-ray (EDX), X-ray Diffractometer (XRD), and X-ray photoelectron spectroscopy (XPS). HR-TEM images detected the polyhedral shape of RcNps with a diverse size ranged within 35.25-55.14 nm. The resulting RcNps exhibited a high radical scavenging activity illustrated by inhibition of superoxide, nitric oxide, hydroxyl radical and xanthine oxidase by by IC50 values 26.2, 52.9, 31.9 and 15.9 µg/ml respectively as compared to ascorbic acid. Furthermore, RcNps at concentration of 100 µg/ml significantly reduced xanthine oxidase activity (15.9 ± 0.61 µg/ml) compared with ascorbic acid (12.80 ± 0.32 µg/ml) with p < 0.05. Moreover, RcNps showed an excellent antiaging activity demonstrated by inhibition of collagenase, elastase, hyaluronidase and tyrosinase enzymes in a dose-dependent manner with IC50 values of 58.7 ± 1.66 µg/ml, 82.5 ± 2.93 µg/ml, 191.4 ± 5.68 µg/ml and 158.6 ± 5.20 µg/ml as compared to EGCG respectively. RcNps also, exhibited a promising antibacterial activity against three skin pathogens delineate a significant threat to a public health, as Staphylococcus epidermidis, Streptococcus pyogenes, and Pseudomonas aeruginosa with MIC of 15.63, 7.81, 31.25 µg/ml as compared to ciprofloxacin (7.81, 3.9 and 15.63 µg/ml). Moreover, RcNps suppressed the formation of biofilms with minimum biofilm inhibitory concentrations 1.95, 1.95, 7.81 µg/ml against the fore mentioned strains, respectively. Overall, our findings indicate that Rosa floribunda nanoparticles could be used as a leading natural source in skin care cosmetic industry.

Anti-Alzheimer chemical constituents of Morus macroura Miq.: chemical profiling, in silico and in vitro investigations.

Herein, we investigated both fruits and leaves of Morus macroura Miq. as a potential source of bioactive compounds against Alzheimer's disease (AD). LC-HRMS-assisted chemical profiling of its extracts showed that they are a rich source of diverse phytochemicals. Among the 29 identified compounds in both the fruit and leaf extracts, moracin D, chrysin, resveratrol, and ferulic acid were predicted to pass the human blood-brain barrier (BBB), and hence, reach their therapeutic targets in the brain. Subsequently, these compounds were subjected to a comprehensive pharmacophore-based screening for their protein targets relevant to AD using two independent software programs (i.e. Swiss Target Prediction and PharmMapper). The results of this initial virtual screening were further refined by a number of docking and molecular dynamic simulation experiments to suggest a number of crucial AD-related proteins (e.g. acetylcholine esterase, ß-secretase, and monoamine oxidase) as potential targets for these compounds. Finally, in vitro testing was performed to validate the in silico investigation's results, where chrysin, resveratrol, and ferulic acid were found to inhibit the predicted AD-related enzymes with IC50 values comparable with those of the reference inhibitors. Additionally, they were able to inhibit the aggregation of amyloid-beta, one of the hallmarks in AD pathogenesis, and to exhibit considerable antioxidant capacity. Our results highlighted Morus macroura compounds as future anti-Alzheimer chemical leads.

Metabolic profiling of cytotoxic metabolites from five Tabebuia species supported by molecular correlation analysis.

Tabebuia is the largest genus among the family Bignoniaceae. Tabebuia species are known for their high ornamental and curative value. Here, the cytotoxic potential of extracts from the leaves and stems of five Tabebuia species was analyzed. The highest activity was observed for T. rosea (Bertol.) DC. stem extract against HepG2 cell line (IC50 4.7 µg/mL), T. pallida L. stem extract against MCF-7 cell line (IC50 6.3 µg/mL), and T. pulcherrima stem extract against CACO2 cell line (IC50 2.6 µg/mL). Metabolic profiling of the ten extracts using liquid chromatography-high-resolution mass spectrometry for dereplication purposes led to annotation of forty compounds belonging to different chemical classes. Among the annotated compounds, irridoids represent the major class. Principle component analysis (PCA) was applied to test the similarity and variability among the tested species and the score plot showed similar chemical profiling between the leaves and stems of both T. pulcherrima and T. pallida L. and unique chemical profiling among T. rosea (Bertol.) DC., T. argentea Britton, and T. guayacan (Seem.) Hemsl. leaf extracts and the stem extract of T. rosea (Bertol.) DC. Additionally, a molecular correlation analysis was used to annotate the bioactive cytotoxic metabolites in the extracts and correlate between their chemical and biological profiles.

Anticholinesterase activity and metabolite profiling of Syagrus romanzoffiana (Cham.) Glassman leaves and fruits via UPLC-QTOF-PDA-MS.

The purpose of this study is to provide a complete metabolic profile of the hydroalcoholic extracts of the leaves and fruits of Syagrus romanzoffiana (Cham.) Glassman via UPLC-QTOF-PDA-MS and to evaluate their anticholinesterase activities in a model of Alzheimer disease. The current study has identified 39 metabolites belonging to various chemical classes (i.e. flavonols, phenolic acids, fatty acids, stilbenoids and lignans). While the fatty acids predominated in both leaves and fruits, the stilbenoids were more predominant in leaves. Their neuroprotective effect was comparable to Aricept; the standard drug used in treatment of Alzheimer disease. Both extracts significantly decreased the acetylcholinesterase activity and improved the histopathological changes in the cerebral cortex and cerebellum of rat model of aluminium chloride-induced Alzheimer disease. In light of the current study, Syagrus romanzoffiana (Cham.) Glassman is recommended as promising candidate for palliative treatment in Alzheimer disease through inhibition of the acetylcholinesterase activity.

Phenolic profiling of different Jasminum species cultivated in Egypt and their antioxidant activity.

This study focused on the profiling of phenolic constituents in 80% methanolic extracts of the leaves of some Jasminum species cultivated in Egypt and their antioxidant activities. Phenolic profiling was performed by total phenolic contents, total flavonoid contents and HPLC-DAD for selected species in comparison to authentic standards. DPPH assay was used to estimate the antioxidant activities of Jasminum azoricum L., Jasminum humile L., Jasminum multiflorum (Burm.f.) Andrew, Jasminum officinale L., Jasminum sambac (Ait) L. "Arabian Nights cultivar" and Jasminum sambac (Ait) L. "Grand Duke of Tuscany cultivar". Jasminum multiflorum showed the highest antioxidant activity among selected species with IC50 of 34.8 µg/ml. J. multiflorum showed high concentrations of hydroxytyrosol, protocatechuic acid, hydroxybenzoic acid, kaempferol-3-O- neohesperidoside, and quercetin-3-O-glucoside with concentrations of 977.1 µg/g, 2224.7 µg/g, 714.8 µg/g, 1738.8 µg/g, and 4356.1 µg/g, respectively.

Validation of Antidiabetic Potential of Gymnocarpos decandrus Forssk.

Gymnocarpos decandrus Forssk. is a well-known grazing wild plant. This study targets scientific validation of its claimed antidiabetic activity and exploring its bioactive metabolites. Chromatographic purification of G. decandrus ethanol extract (GDEE) allowed isolation of vitexin (C1), protocatechuic acid (C2) and quercetin (C3). HPLC-PDA-MS/MS enabled identification of nineteen metabolites; 13 flavonoids, 5 saponins, and 1 phenolic acid in G. decandrus and four in the genus Gymnocarpos for the first time. The antidiabetic potential was evaluated via testing the Coxsackie B4 virus and α-glucosidase inhibitory potentials. C3 exhibited its potent antiviral activity through blocking of the virus attachment (96.28%, SI 4.41) and virus inactivation before adsorption (91.47%, SI 4.78). GDEE and C1-C3 showed dose dependent α-glucosidase inhibitory activity with IC50 of 733.9, 293.3, 118.1 and 69.1 µg/mL, respectively. Our study represents the sole complete map for G. decandrus secondary metabolites and presents it as promising drug for diabetes management.

Identification of Chemopreventive Components from Halophytes Belonging to Aizoaceae and Cactaceae Through LC/MS-Bioassay Guided Approach.

Six halophytes, namely, Aptenia cordifolia var. variegata, Glottiphyllum linguiforme, Carpobrotus edulis, Ferocactus glaucescens, F. pottsii and F. herrerae were investigated for chemopreventive effect. Prioritization of most promising plant for further investigation was carried out through an integrated liquid chromatography-high resolution electrospray ionization mass spectrometry profiling-bioassay guided approach. NAD(P)H: quinone oxidoreductase-1 (NQO-1) induction in cultured murine hepatoma cells (Hepa-1c1c7) and inhibition of nitric oxide (NO) production in lipopolysaccharide-activated macrophages (RAW 264.7) were carried out to investigate chemopreventive effect. Bioassay data revealed that F. herrerae, A. cordifolia, C. edulis and F. glaucescens were the most active with 2-, 1.7-, 1.6- and 1.5-folds induction of NQO-1 activity. Only F. glaucescens exhibited >50% inhibition of NO release. LCMS profiling of the F. glaucescens revealed its high content of flavonoids, a known micheal acceptor with possible NQO-1 induction, as proved by quantitative high-performance liquid chromatography analysis. Thus, the extract of F. glaucescens was subjected to chromatographic fractionation leading to the isolation of four compounds including (i) 2S-naringenin, (ii) trans-dihydrokaempferol (aromadendrin), (iii) 2S-naringenin-7-O-ß-d-glucopyranoside and (iv) kaempferol-7-O-ß-d-glucopyranoside (populnin). The current study through an LCMS dereplication along with bio guided approach reported the activity of populnin as NO inhibitor and NQO-1 inducer with promising chemopreventive potential.

Metabolic profiling and in vivo hepatoprotective activity of Malpighia glabra L. leaves.

Although Malpighia glabra Linn. fruits are well studied for their nutritional and medicinal prominence; little attention has been given to the leaves. Our study intends to investigate the leaves metabolic profile using Q-TOF LC/MS/MS (Quadrupole-Time-of-Flight-Liquid-Chromatography-Mass-Spectrometry), and to explore their in vivo hepatoprotective activity in rats using CCL4 -induced hepatic damage model and silymarin as standard. Fifty metabolites were characterized, belonging to different classes; coumarins (capensine, daphnoretin, and scopoletin), flavonoids (mainly quercetin and apigenin glycosides), phenolic acids (cinnamic acid and quinic acid derivatives) and amino acids (adenosine, homoisoleucine, and phenylalanine).These compounds are detected in the leaves for the first time. The hepatoprotective activity at three doses (200, 400, and 800 mg/kg) was investigated. The dose of 800 mg/Kg showed the highest hepatoprotective effect as it reduced the elevated serum levels of ALT, AST, NO, and TNF-α liver content by 26, 24, 23, and 42%, respectively, it also remarkably increased the serum level of catalase by 102%. All the tested doses showed higher reduction in serum level of TNF-α compared to silymarin which suggests their strong anti-inflammatory potential. M. glabra leaves are revealed to be a rich source of secondary metabolites and proved to possess significant hepatoprotective potential. PRACTICAL APPLICATIONS: The performed analyses in this study shows the richness of Malpighia glabra Linn. leaves in a plethora of beneficial and safe phytochemicals which are well-known to have a pivotal role in protection against different diseases including liver disorders. The carried-out investigations were done using Q-TOF LC/MS/MS analysis which is a reliable technique for the determination, characterization and identification of bioactive metabolites; in addition to evaluation of the hepatoprotective effect of the leaves. Therefore, this study may emphasize that Malpighia glabra Linn. leaves may have the same nutritional and medicinal importance as its fruits, and they could be incorporated into pharmaceuticals and foods instead of discarding them.