361 research outputs found
Phytochemical Investigation of Egyptian Riverhemp: A Potential Source of Antileukemic Metabolites
As part of our research group\u27s continuous efforts to find alternative treatments for cancer, the aqueous ethanol extract of Sesbania sesban L. Merr. (SS, Egyptian riverhemp) demonstrated an antileukemic activity against K562 cell line. Bioguided fractionation of SS leaves hydroethanolic extract resulted in the isolation of one new compound (33) named as hederatriol 3-O-β-D-glucuronic acid methyl ester as well as 34 known compounds. Seven compounds ((34), (22), (20), (24), (21), (19), and (35)) showed high antiproliferative effects (IC50 = 22.3, 30.8, 31.3, 33.7, 36.6, 37.5, and 41.5 μM, respectively), while four compounds ((32), (5), (29), and (1)) showed milder activities (IC50 = 56.4, 67.6, 83.3, and 112.3 μM, respectively). A mechanistic study was further carried out on a molecular genetics level against several transcription factors signaling pathways that are incorporated in the incidence of cancer. The results showed that compounds (22) and (21) demonstrated a specific inhibition of Wnt pathway (IC50 = 3.8 and 4.6 μM, respectively), while compound (22) showed a specific inhibition of Smad pathway (IC50 = 3.8 μM). Compound (34) strongly altered the signaling of Smad and E2F pathways (IC50 = 5 μM). The bioactive metabolites were further investigated in silico by docking against several targets related to K562 cell line. The results showed that compounds (22) and (34) exhibited a strong binding affinity towards topoisomerase (docking score = -7.81 and -9.30 Kcal/Mole, respectively). Compounds (22) and (34) demonstrated a strong binding affinity towards EGFR-tyrosine kinase (docking score = -7.12 and -7.35 Kcal/Mole, respectively). Moreover, compound (34) showed a strong binding affinity towards Abl kinase (docking score = -7.05 Kcal/Mole)
Phytochemical Investigation of Egyptian Spinach Leaves, a Potential Source for Antileukemic Metabolites: In Vitro and In Silico Study
Spinacia oleracea L., Amaranthaceae, leaves cultivated in Egypt demonstrated a potential antileukemic activity against the chronic myeloid leukemia, K562 cell line. Thus, the aim of this study is to carry out a phytochemical investigation of S. oleracea leaves as well as the isolation of its antileukemic phytoconstituents. Phytochemical investigation of S. oleracea leaves resulted in the isolation of seventeen known compounds. The biological study revealed that compounds hexaprenol, phytol, and 18-[(1-oxohexadecyl) oxy]-9-octadecenoic acid exhibited a remarkable antiproliferative activity against K562 cells in vitro. A mechanistic in silico study showed that hexaprenol, phytol, and 18-[(1-oxohexadecyl) oxy]-9-octadecenoic acid exhibited a strong binding affinity towards topoisomerase (docking score −12.50, −9.19, and −13.29 kcal/mol, respectively), and showed as well a strong binding affinity towards Abl kinase (docking score −11.91, −9.35, and −12.59 kcal/mol, respectively). Molecular dynamics study revealed that 18-[(1-oxohexadecyl) oxy]-9-octadecenoic acid produced stable complexes with both topoisomerase and Abl kinase with RMSD values of 1.81 and 1.85 Å, respectively. As a result of our findings, we recommend more in vivo and preclinical studies to confirm the potential benefit of spinach leaves for chronic myeloid leukemia patients. Graphical Abstract: [Figure not available: see fulltext.
Physiological and biochemical analyses shed light on the response of <i>Sargassum vulgare</i> to ocean acidification at different time scales
Studies regarding macroalgal responses to ocean acidification (OA) are mostly limited to short-term experiments in controlled conditions, which hamper the possibility to scale up the observations to long-term effects in the natural environment. To gain a broader perspective, we utilized volcanic CO2 vents as a “natural laboratory” to study OA effects on Sargassum vulgare at different time scales. We measured photosynthetic rates, oxidative stress levels, antioxidant contents, antioxidant enzyme activities, and activities of oxidative metabolic enzymes in S. vulgare growing at a natural acidified site (pH 6.7) compared to samples from a site with current pH (pH 8.2), used as a control one. These variables were also tested in plants transplanted from the control to the acidified site and vice-versa. After short-term exposure, photosynthetic rates and energy metabolism were increased in S. vulgare together with oxidative damage. However, in natural populations under long-term conditions photosynthetic rates were similar, the activity of oxidative metabolic enzymes was maintained, and no sign of oxidative damages was observed. The differences in the response of the macroalga indicate that the natural population at the acidified site is adapted to live at the lowered pH. The results suggest that this macroalga can adopt biochemical and physiological strategies to grow in future acidified oceans
EFFECT OF ANAEROBIC PROBIOTIC AND/OR BIOLOGICAL ANTITOXIN SUPPLEMENTATIONS ON PRODUCTIVE AND REPRODUCTIVE PERFORMANCE OF LACTATING COWS
Forty-eight lactating Holstein Friesian cows were utilized to assess impact of supplementing probiotic ZAD (mixture of live bacterial cells and enzymes) compared with T5X (antitoxins product) on some productive, reproductive and antitoxins activity parameters. we have divided the animals to three experimental categories (16 each). The first category, control treatment, was fed basal diet without any supplements. The second category, ZAD treatment, was fed basal diet supplemented with ZAD probiotic (1.1 L/ton). The third category, T5X treatment, was fed basal diet supplemented with T5X antitoxins product (1.1 Kg/ton). Milk yield was recorded. we have collected and analyzed milk samples, blood samples and feed samples in order to constitutes. Time-interval between calving and fertilizing artificial insemination and pregnancy rate were recorded. The gained outcomes demonstrated that milk yield was significantly raised by ZAD treatment than other treatment. Milk components yield were significantly raised by ZAD probiotic and T5X treatments than control. Blood serum total protein, albumin, globulin, glucose, urea and total lipids were not significantly influenced by treatments. Total aflatoxins in concentrate mixture and aflatoxin M1 in milk were significantly diminished by ZAD and T5X than control. Number of days between calving and fertilized artificial insemination were diminished by treatments than control. Pregnancy rate was significantly raised by ZAD probiotic than T5X and control treatments, respectively. The overall conclusion of this study illustrated that Probiotic ZAD, potentially, has antitoxins activity leading to reinforcing the productive and reproductive performance of lactating cows
Physiological and biochemical analyses shed light on the response of sargassum vulgare to ocean acidification at different time scales
Studies regarding macroalgal responses to ocean acidification (OA) are mostly limited to short-term experiments in controlled conditions, which hamper the possibility to scale up the observations to long-term effects in the natural environment. To gain a broader perspective, we utilized volcanic CO2 vents as a “natural laboratory” to study OA effects on Sargassum vulgare at different time scales. We measured photosynthetic rates, oxidative stress levels, antioxidant contents, antioxidant enzyme activities, and activities of oxidative metabolic enzymes in S. vulgare growing at a natural acidified site (pH 6.7) compared to samples from a site with current pH (pH 8.2), used as a control one. These variables were also tested in plants transplanted from the control to the acidified site and vice-versa. After short-term exposure, photosynthetic rates and energy metabolism were increased in S. vulgare together with oxidative damage. However, in natural populations under long-term conditions photosynthetic rates were similar, the activity of oxidative metabolic enzymes was maintained, and no sign of oxidative damages was observed. The differences in the response of the macroalga indicate that the natural population at the acidified site is adapted to live at the lowered pH. The results suggest that this macroalga can adopt biochemical and physiological strategies to grow in future acidified oceans
Design, Synthesis and Biological Evaluation of Novel Pyrimido[4,5-d]pyrimidine CDK2 Inhibitors as Anti-Tumor Agents
A series of 2,5,7-trisubstituted pyrimido[4,5-d]pyrimidine cyclin-dependent kinase (CDK2) inhibitors is designed and synthesized. 6-Amino-2-thiouracil is reacted with an aldehyde and thiourea to prepare the pyrimido[4,5-d]-pyrimidines. Alkylation and amination of the latter ones give different amino derivatives. These compounds show potent and selective CDK inhibitory activities and inhibit in vitro cellular proliferation in cultured human tumor cells
Synthesize of bio-based encapsulated nano urea modified hydroxyapatite for controlling release of nitrogen and enhancing green bean yield
The massive rise in the world population requires increasing food production, and the world needs to decrease agricultural inputs like agrochemicals to preserve natural resources. The low nutrient use efficiency of conventional fertilizers has always been a concern because of their impact on the environment, and they are considered a waste of natural resources, which is against sustainability goals. Their low efficiency is attributed to their high solubility and fast release into the soil. Controlled-release fertilizers (CRFs) can reduce nutrient loss, which increases their efficiency and controls environmental pollution. In this study, single- and double-layers coating of biopolymers were applied to encapsulate nano urea-modified hydroxyapatite to control nitrogen release in soil. Hydroxyapatite was synthesized using the wet chemical precipitation method and two different rodlike and mesoporous hydroxyapatites were obtained. Nano-hydroxyapatite that had been synthesized was mixed with urea in two different amounts: 4:1 and 8:1. Biopolymers were then added on top. The current CRF synthesis strategy focuses on using low-cost, widespread biorefinery materials to decrease the manufacturing cost of CRFs. The nitrogen release rate of the synthesized CRFs and commercial urea in water and soil was studied. In field experiments, the impact of CRFs on green bean growth and yield was studied. The results showed that both single and double-coated CRFs reduced the N release rate in the soil and increased the fertilizer's longevity to 24 days, compared to 6 days for conventional urea. The total yield of green beans increased by 48%-120% by applying 75% of the recommended dose compared with that obtained with the full dose of conventional urea (control). Also, applying double-coated CRFs at N level of 25% of the recommended dose gives a green bean yield equal to the control. The recommended treatment is SC-CRF prepared with C-HA applied at N rate of 75% to match the future increase in the required amount of food
Eco-friendly preparation of thyme essential oil nano emulsion: Characterization, antifungal activity and resistance of Fusarium wilt disease of Foeniculum vulgare
Essential oil nanoemulsions have received much attention in the last period for controlling of fungal plant pathogens. In this study, thyme oil nanoemulsion (TONE) was successfully prepared from thyme oil which extracted from Thymus vulgaris (T. vulgaris). The prepared TONE was characterized using DLS, Zeta potential, and TEM analyses. Results revealed that, TONE has spherical shape with size 32.7 nm. Moreover, results illustrated that TONE exhibited promising antifungal activity against Fusarium oxysporum (F. oxysporum) with minimum fungicidal concentration (MFC) 5 mg/ml. Additionally, TONE concentrations 1, 2, 3 and 4 mg/ml reduced the growth of F. oxysporum with percentages 7.78, 31.1, 52.2 and 67.8 % respectively. Disease index (DI) of Fusarium wilt reached the maximum rate by (85 %) in the Foeniculum vulgare (F. vulgare) plant infected with F. oxysporum. Application of TONE treatment on infected plants led to a decrease in DI to (17.5%) and an increase in the percentage of protection to (79.4%). Furthermore, DI was decrease to 42.5% with protection percentage 50% in the case of infected plant with TOE. Moreover, TOE, TONE played an important role in improving plant immunity by increasing phenol, proline, and antioxidant enzymes (POD&PPO) activities, as well as reducing oxidative stress by reducing (MDA & H2O2). Results revealed that TONE led to significant increase in free proline in compared to TOE. We can conclude that TOE, TONE are considered eco-friendly safe strong inducers of F. vulgare plant immunity alternatives to difenoconazole against fusarial wilt disease to preserve plant, soil, and human health
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