Rojasdyer2412
Our previous studies had shown that watermelon seed antioxidant peptides (WSAPs P1-P5) possessed good activities. However, the structure-activity relationship of P1 is still unclear. Quantum chemistry and molecular docking were used to investigate the antioxidant mechanism of P1. The active site of P1 is located at C6H14 on Arg. P1 can bind to DPPH/ABTS through hydrogen bond and hydrophobic interaction. Compared with P2-P4, P1 has the strongest antioxidant capacity. The molecular simulation showed that P1 could enhance the stability of Keap1 by interacting with Asn382, Arg380 and Tyr 334 in the active sites. Compared with the model group, the expression of Keap1 was down-regulated (p less then 0.05), while the expression of Nrf2 and HO-1 was up-regulated (p less then 0.05) after P1 treatment. P1 has the potential ability to activate the signaling pathway Keap1-Nrf2 and improve the antioxidant defense system. This study provides a new perspective for the rational design and mechanism of antioxidant peptides.In this work, we investigated the degradation of moringin (4-[(α-l-rhamnosyloxy)benzyl]-isothiocyanate), a major bioactive isothiocyanate (ITC) found in moringa seeds (Moringa oleifera Lam), at various food processing conditions. Moringin degrades rapidly to several water-soluble products via a pseudo-first-order kinetics. By analyzing the reaction products, the degradation mechanism was found to be through hydrolyzing to (A) 1-O-(4-hydroxymethylphenyl) α-l-rhamnopyranoside (rhamnobenzyl alcohol RBA) or (B) rhamnobenzylamine. The formed amine further reacts with moringin to form N,N'-bis4-[(α-l-rhamnosyloxy)benzyl]thiourea (di-rhamnobenzyl thiourea, DRBTU). In addition, moringin isomerizes to 4-[(α-l-rhamnosyloxy)benzyl]thiocyanate (RBTC), which further reacts with moringin to form S,N-bis4-[(α-l-rhamnosyloxy)benzyl]-dithiocarbamate (DRBDTC). Furthermore, pH was found to have an effect on the degradation of moringin. RBA and RBTC were major degraded products in neutral and acidic conditions while thiourea (DRBTU) was in alkaline condition. Although moringin showed higher cytotoxicity to cancer cells, its degraded products showed very weak or no activities, suggesting that the isothiocyanate group of ITCs is essential for their cancer chemoprevention activities.Melamine is a compound commonly used in the manufacturing of plastic and flame retardant products, but due to its solubility on water and high nitrogen content, it is also used to adulterate milk to mask adulteration by dilution in protein content tests. This work proposes a quick method using excitation-emission matrix (EEM) fluorescence spectroscopy and second-order calibration methods (PARAFAC and U-PLS/RBL) for the identification and quantification of melamine in milk. The proposed method uses a single clean-up step with acetic acid, resulting in a quick, low-cost, and environmentally friendly procedure, in agreement with green chemistry principles. Both PARAFAC and U-PLS/RBL were capable of detecting melamine in milk above 120.6 and 146.5 ppm respectively, adequate for adulterations above 2% in volume, with RMSEPs of 68.6 and 81.9 ppm, respectively.This study investigated whether a ready-to-use extract obtained using a natural deep eutectic solvent (NADES) affects the pharmacokinetic profile of blueberry phenolic compounds compared to organic solvent (SORG)-extracted compounds. SORG extract was administered as an aqueous solution after solvent removal. Wistar rats received a single dose of crude extract of blueberry obtained using NADES (CE-NADES) or SORG (CE-SORG), followed by LC-DAD-MS/MS analysis of blood and cecal feces. Non-compartmental pharmacokinetic analysis revealed that CE-NADES increased the bioavailability of anthocyanins by 140% compared to CE-SORG. CE-NADES increased the stability of phenolic compounds during in vitro digestion by delaying gastric chyme neutralization. These results suggest that besides being an eco-friendly solvent for the extraction of phytochemicals, choline chlorideglycerolcitric acid-based NADES can be used as a ready-to-use vehicle for increasing oral absorption of bioactive compounds such as anthocyanins.Microwave is a new pretreatment technology, and microwave processing time of camellia seeds is a factor affecting the flavor of camellia seed oil (CSO). Therefore, this study on the characteristic volatile compounds of CSO from microwaved seeds with different processing time was carried out by electronic nose (E-nose), headspace-solid phase microextraction-gas chromatography-mass spectrometry (HS-SPME-GC-MS) and headspace-gas chromatography-ion mobility spectrometry (HS-GC-IMS). The results of E-nose show that W1W, W2W and W5S were the main sensors to distinguish the flavor profile of CSOs. Through HS-SPME-GC-MS and odor activity value analysis, 80 volatile compounds were detected and 22 key aroma compounds were screened in CSOs. Compared with HS-SPME-GC-MS, 44 volatile compounds were detected by HS-GC-IMS, including 9 identical compounds and 35 different compounds. In general, the volatile compounds of 0, 2 and 3 min CSOs were mainly alcohols and esters, while the 4, 5 and 6 min CSOs were mainly heterocycles and aldehydes.The protozoan parasite Trypanosoma cruzi is the causative agent of Chagas disease, the most important parasitic infection in Latin America. The only treatments currently available are nitro-derivative drugs that are characterised by high toxicity and limited efficacy. Therefore, there is an urgent need for more effective, less toxic therapeutic agents. We have previously identified the potential for Mannich base derivatives as novel inhibitors of this parasite. To further explore this family of compounds, we synthesised a panel of 69 new analogues, based on multi-parametric structure-activity relationships, which allowed optimization of both anti-parasitic activity, physicochemical parameters and ADME properties. Additionally, we optimized our in vitro screening approaches against all three developmental forms of the parasite, allowing us to discard the least effective and trypanostatic derivatives at an early stage. We ultimately identified derivative 3c, which demonstrated excellent trypanocidal properties, and a synergistic mode of action against trypomastigotes in combination with the reference drug benznidazole. Both its druggability and low-cost production make this derivative a promising candidate for the preclinical, in vivo assays of the Chagas disease drug-discovery pipeline.A series of novel 1-(4-(piperazin-1-yl)phenyl)pyridin-2(1H)-one derivatives were synthesized and evaluated for their serotonin (5-HT) reuptake inhibitory activity. GSK 3 inhibitor The results in vitro indicated that most of the evaluated compounds displayed potent 5-HT reuptake inhibition. The most promising compound A20 was stable in human liver microsomes and possessed good pharmacokinetic properties. Antidepressant study in vivo of the compound A20 showed that A20 could potently antagonize the p-chloroamphetamine (PCA)-induced depletion of serotonin in hypothalamus and reduce immobility times in the rat forced swimming test (FST).Urban health is shaped by a system of factors spanning multiple levels and scales, and through a complex set of interactions. Building on causal loop diagrams developed via several group model building workshops, we apply the cross-impact balance (CIB) method to understand the strength and nature of the relationships between factors in the food and transportation system, and to identify possible future urban health scenarios (i.e., permutations of factor states that impact health in cities). We recruited 16 food and transportation system experts spanning private, academic, non-government, and policy sectors from six Latin American countries to complete an interviewer-assisted questionnaire. The questionnaire, which was pilot tested on six researchers, used a combination of questions and visual prompts to elicit participants' perceptions about the bivariate relationships between 11 factors in the food and transportation system. Each participant answered questions related to a unique set of relationships within their domain of expertise. Using CIB analysis, we identified 21 plausible future scenarios for the system. In the baseline model, 'healthy' scenarios (with low chronic disease, high physical activity, and low consumption of highly processed foods) were characterized by high public transportation subsidies, low car use, high street safety, and high free time, illustrating the links between transportation, free time and dietary behaviors. In analyses of interventions, low car use, high public transport subsidies and high free time were associated with the highest proportion of factors in a healthful state and with high proportions of 'healthy' scenarios. High political will for social change also emerged as critically important in promoting healthy systems and urban health outcomes. The CIB method can play a novel role in augmenting understandings of complex urban systems by enabling insights into future scenarios that can be used alongside other approaches to guide urban health policy planning and action.Drawing on 40 in-depth interviews with Chinese breast cancer patients who participated in the breast cancer biobank at a hospital in Beijing, China, this paper explores these patients' perceptions of privacy. The analysis indicates that these patients primarily perceived privacy as informational privacy; they were concerned about the disclosure of contact information, cancer diagnosis, and genetic testing results; further, their views on disclosing different kinds of personal information were dynamic and heterogeneous in various relationships and contexts, which differs from the stereotypical beliefs of privacy in China. This paper provides situated understanding of why these patients had such privacy perceptions and what strategies they adopted to cope with their privacy. It then discusses the international similarities and differences in the disclosure of cancer and genetic testing results.People living with dementia (PLWD) are almost always admitted to the acute hospital for reasons unrelated to their dementia, finding themselves in the unfamiliar environment of a Health Care of Older Persons acute ward. The effect of this environment creates a challenge not just for a PLWD themselves, but also for the staff who care for them. Concerns have been raised by both policy makers and staff about the quality of communication between hospital staff and PLWD. Using conversation analysis, we examined 41 video recordings of healthcare professional (HCP)/PLWD interactions collected across three acute inpatient wards in a large teaching hospital in the UK. In this paper, we focus our analysis on hard-to-interpret talk (talk where there are problems in hearing, speaking and/or understanding), and the ways in which healthcare professionals respond to this. Repair of hard- to- interpret talk is common in ordinary interaction, but we find that HCPs in this setting use a range of approaches to avoid direct repair. These approaches are the use of non-committal responses and continuers such as 'yeah' or nods; the use of repetitions or partial repetitions; responding to the emotional tone displayed in the PLWD's utterance; closing the current topic and shifting to the next; and treating the PLWD's talk as related to the task at hand. We suggest that the use of these approaches may be one way in which HCPs manage respecting the personhood of the PLWD, by preserving face and enabling a continuation of an interaction in which the PLWD can take an active part. Our paper provides an empirical demonstration of the high level of interactional skill involved in dementia care work. It also illustrates how these skills can be described and specified, and hence incorporated into the recommendations and tips that are produced for communication with PLWD.