Identification of bioactive metabolites from Ficus carica and their neuroprotective effects of Alzheimer's disease

Neurodegenerative disease including Alzheimer’s disease is a major cause of long-term disability. Oxidative stress is frequently implicated as one of the key contributing factors to neurodegenerative diseases. Protection against neuronal damage remains a great challenge for researchers. Ficus carica (commonly known as fig) is a species of great antioxidant nutritional value comprising a protective mechanism against innumerable health disorders related to oxidative stress as well as Alzheimer’s disease. The purpose of this work was to characterize the non-polar active metabolites in Ficus carica endocarp, mesocarp, and exocarp. Crude extracts were prepared using several extraction solvents, which included 1:1 water: ethylacetate, acetone and methanol. The dried extracts were then solvent partitioned between equivalent amounts of water and ethylacetate. Purification and fractionation were accomplished by high-throughput chromatography. The isolated metabolites were tested on their effect on human neuroblastoma cell line by cell viability test and cell cytotoxicity assay with acrolein. Molecular weights of the active metabolites were determined via LC–HRESIMS and GC-EIMS. Metabolomic profiling was performed to identify the active metabolites by using differential expression analysis software (Mzmine) and SIMCA for multivariate analysis. Structural elucidation and identification of the interested active metabolites were studied by 1-D and 2-D NMR. Significant differences in bioactivity against a concentration-dependent assay on acrolein radicals were observed between the three fruit parts. However, metabolites obtained from mesocarp and the endocarp demonstrated bioactivity to scavenge ROS radical. NMR profiling demonstrated that aliphatic compounds such as γ-sitosterol tend to induce neuronal bioactivity and exhibited bioactivity on the cell viability assay. γ-Sitosterol was found in higher concentrations in the mesocarp and was considered as one of the major phytosterol in Ficus carica

The association between diabetes medication and weight change in a non‐surgical weight management intervention: an intervention cohort study

Aim: To compare weight change in a lifestyle‐based weight management programme between participants taking weight‐gaining, weight‐neutral/loss and mixed diabetes medications. Methods: Electronic health records for individuals (≥ 18 years) with Type 2 diabetes who had been referred to a non‐surgical weight management programme between February 2008 and May 2014 were studied. Diabetes medications were classified into three categories based on their effect on body weight. In this intervention cohort study, weight change was calculated for participants attending two or more sessions. Results: All 998 individuals who took oral diabetes medications and attended two or more sessions of weight management were included. Some 59.5% of participants were women, and participants had a mean BMI of 41.1 kg/m2 (women) and 40.2 kg/m2 (men). Of the diabetes medication combinations prescribed, 46.0% were weight‐neutral/loss, 41.3% mixed and 12.7% weight‐gaining. The mean weight change for participants on weight‐gaining and weight‐neutral/loss diabetes medications respectively was −2.5 kg [95% confidence interval (CI) −3.2 to −1.8) and −3.3 kg (95% CI −3.8 to −2.9) (P = 0.05) for those attending two or more sessions (n = 998). Compared with those prescribed weight‐neutral medications, participants prescribed weight‐gaining medication lost 0.86 kg less (95% CI 0.02 to 1.7; P = 0.045) in a model adjusted for age, sex, BMI and socio‐economic status. Conclusions: Participants on weight‐neutral/loss diabetes medications had a greater absolute weight loss within a weight management intervention compared with those on weight‐gaining medications. Diabetes medications should be reviewed ahead of planned weight‐loss interventions to help ensure maximal effectiveness of the intervention

P43 The isolation and purification of bioactive metabolites from Ficus carica and their neuroprotective effects in Alzheimer's disease

Neurodegenerative disease including Alzheimer’s disease (AD) is a major cause of long-term disability. Incidence of Alzheimer’s disease increases with age. According to a recent report by WHO, there are approximately 47.5 million people suffering from dementia, with 7.7 million new cases each year. Acrolein is one of the key contributing factors to accelerate oxidative stress which then implicated AD. However, protection against neuronal damage remains a great challenge for researchers. Ficus carica (commonly known as fig) is a species of great antioxidant nutritional value comprising a protective mechanism against innumerable health disorders related to oxidative stress as well as AD. The purpose of this work was to characterise the bioactive metabolites in Ficus carica mesocarp against oxidative stress related AD. Crude extracts were prepared using several extraction methods to achieve non-polar layer. The isolated metabolites were tested on their effect on human neuroblastoma SHSY5Y cell line by a cell viability test. Molecular weights of the active metabolites were determined via LC-HRESIMS, GC-EIMS, and multivariate analysis via SIMCA was performed. Structural elucidation and identification of the interested active metabolites were studied by 1-D and 2-D NMR. NMR profiling demonstrated that aliphatic compounds such as γ-sitosterol were found to induce neuronal bioactivity

Overcoming the imatinib-resistant BCR-ABL mutants with new ureidobenzothiazole chemotypes endowed with potent and broad-spectrum anticancer activity

AbstractThe design of kinase inhibitors targeting the oncogenic kinase BCR-ABL constitutes a promising paradigm for treating chronic myeloid leukaemia (CML). Nevertheless, the efficacy of imatinib, the first FDA-approved targeted therapy for CML, is curbed by the emergence of resistance. Herein, we report the identification of the 2-methoxyphenyl ureidobenzothiazole AK-HW-90 (2b) as a potent pan-BCR-ABL inhibitor against imatinib-resistant mutants, particularly T315I. A concise array of six compounds 2a–f was designed based on our previously reported benzothiazole lead AKE-5l to improve its BCR-ABLT315I inhibitory activity. Replacing the 6-oxypicolinamide moiety of AKE-5l with o-methoxyphenyl and changing the propyl spacer with phenyl afforded 2a and AK-HW-90 (2b) with IC50 values of 2.0 and 0.65 nM against BCR-ABLT315I, respectively. AK-HW-90 showed superior anticancer potency to imatinib against multiple cancer cells (NCI), including leukaemia K-562. The obtained outcomes offer AK-HW-90 as a promising candidate for the treatment of CML and other types of cancer

The Influence of a Nanoemulsion of Cardamom Essential Oil on the Growth Performance, Feed Utilization, Carcass Characteristics, and Health Status of Growing Rabbits under a High Ambient Temperature

Recently, nanotechnology approaches have been employed to enhance the solubility, availability, and efficacy of phytochemicals, overcoming some industrial obstacles and natural biological barriers. In this regard, 120 clinically healthy growing V-line rabbits (5 weeks old) reared during the summer season were divided randomly into four equal experimental groups (30 rabbits each). The first group received a basal diet without the supplementation of the nanoemulsion of cardamom essential oil (NCEO) (0 g/kg diet) and served as a control (NCEO 0). The other groups were given diets containing NCEO at levels of 150 (NCEO 150), 300 (NCEO 300), and 600 (NCEO 600) mg/kg diet, respectively. The growth performance (higher LBW and ADG), feed utilization (lower FCR), dressing percentage, and relative weight of the liver were improved significantly in the NCEO-treated groups compared to the control group. Moreover, the dietary treatment significantly decreased the rectum temperature and respiration rate, minimizing the 350 and 325 mg NECO/kg diets. The erythrocyte count, hematocrit, and hemoglobin concentration were significantly increased (p p = 0.0200) in the NCEO300 and NCEO600 groups compared to the control group. Treatment with 300 or 600 mg NCEO/kg significantly increased the blood serum total protein and albumin compared to the control group. Meanwhile, the liver enzymes (AST and ALT), uric acid, and creatinine concentrations decreased significantly in the NCEO300 group compared to the control group. The concentrations of triglycerides and total cholesterol were reduced significantly by the dietary treatment. The total antioxidant capacity, dismutase activity, and glutathione concentration were significantly higher, while the malondialdehyde and protein carbonyl levels were significantly lower in the NCEO300 group than in the control. The inflammatory responses and immunity statuses were improved in the blood serum of the NCEO-treated rabbits compared to the control. Heat-stress-induced pathological perturbations in renal/hepatic tissues and NCEO co-treatment successfully re-established and recovered near-control renal–hepatic morphology. In conclusion, a dietary supplementation of NCEO (300 mg/kg) could effectively enhance growing rabbits’ growth indices, feed efficiency, redox balance, immunity, and inflammatory responses during the summer

Lactoferrin: Antimicrobial impacts, genomic guardian, therapeutic uses and clinical significance for humans and animals

Lactoferrin (LF) is a protein found in several bodily fluids, such as milk. This protein has a diverse range of functions and is evolutionarily conserved. Lactoferrin is a multifunction protein with distinct biological abilities affecting mammals' immune structures. Reports indicated that the daily uptake of LF from dairy products is unsatisfactory in detecting further health-promoting abilities. Research has shown that it protects against infection, mitigates cellular senescence, and improves nutritional quality. Additionally, LF is being studied as a potential treatment for various diseases and conditions, including gastrointestinal issues and infections. Studies have also demonstrated its effectiveness against various viruses and bacteria. In this article, we'll look closer at the structure of LF and its various biological activities, including its antimicrobial, anti-viral, anti-cancer, anti-osteoporotic, detoxifying, and immunomodulatory properties. More specifically, the protective effect of LF against oxidative DNA damage was also clarified through its ability to abolish DNA damaging issues without interfacing with host genetic material. Fortification with LF protects mitochondria dysfunction syndromes via sustaining redox status and biogenesis and suppressing apoptosis and autophagy singling. Additionally, we'll examine the potential benefits of lactoferrin and provide an overview of recent clinical trials conducted to examine its use in laboratory and living models

Foliar Application of Nano, Chelated, and Conventional Iron Forms Enhanced Growth, Nutritional Status, Fruiting Aspects, and Fruit Quality of Washington Navel Orange Trees (Citrus sinensis L. Osbeck)

Iron (Fe) is required for most metabolic processes, including DNA synthesis, respiration, photosynthesis, and chlorophyll biosynthesis; however, Fe deficiency is common in arid regions, necessitating additional research to determine the most efficient form of absorbance. Nano-fertilizers have characteristics that are not found in their traditional equivalents. This research was implemented on Washington navel orange trees (Citrus sinensis L. Osbeck) to investigate the effect of three iron forms—nano (Fe-NPs), sulfate (FeSO4), and chelated (Fe-chelated)—as a foliar spray on the growth, fruiting aspects, and nutritional status of these trees compared to control. The highest values of the tested parameters were reported when the highest Fe-NPs level and the highest Fe-chelated (EDTA) rate were used. Results obtained here showed that the spraying of the Washington navel orange trees grown under similar environmental conditions and horticulture practices adopted in the current experiment with Fe-NPs (nanoform) and/or Fe-chelated (EDTA) at 0.1% is a beneficial application for enhancing vegetative growth, flower set, tree nutritional status, and fruit production and quality. Application of Fe-NPs and Fe-chelated (EDTA, 0.1%) increased yield by 32.0% and 25% and total soluble solids (TSS) by 18.5% and 17.0%, respectively, compared with control. Spraying Washington navel orange trees with nano and chelated iron could be considered a significant way to improve vegetative growth, fruit production, quality, and nutritional status while also being environmentally preferred in the arid regions