ABSTRACT
Cadmium ions (Cd2+) penetrate the blood-brain barrier and can, among other effects, influence intracellular calcium metabolism, leading to neurodegeneration. In the presented work, we estimated the effect of Cd2+ on the expression of calretinin in the neurons of the rat hippocampus and analyzed the reverse effect of freshly pressed beetroot/carrot juice in this context. In the 12-week lasting experiment, 32 8-week-old male Wistar rats were divided into four experimental groups (n = 8): the control group (C) received pure tap water; the Cd group (Cd)-received Cd2+ dissolved in tap water (5 mg Cd2+/kg b.w.); and two groups received beetroot/carrot juice: the BCJ group was administered only juice, and the Cd + BCJ group received juice with the addition of Cd2+ (5 mg Cd2+/kg b.w.). The exposition to low doses of Cd2+ caused a significant decrease in calretinin-immunoreactive (Cr-IR) neurons compared to the non-exposed groups. Moreover, the addition of Cd2+ to tap water reduced the numbers and length of Cr-IR nerve fibers. The negative effect of Cd2+ was significantly attenuated by the simultaneous supplementation of beetroot/carrot juice (Cd + BCJ). The study showed that the bioactive compounds in the beetroot/carrot juice can modulate Ca2+ levels in neurons, and thus, potentially act as a neuroprotective factor against neuronal damage.
ABSTRACT
In coffee beans, especially roasted, a significant part of hydroxycinnamic acid (HCAs) and their esters chlorogenic acids (CHAs) is attached to melanoidins through both covalent and non-covalent bonds. Bound and, to a greater extent, unbound HCAs, including those released from the polymerized material during digestion, can be pivotal in preventing of many chronic civilization diseases. The aim of the study was to determine the amount of free CHAs and those released from coffee extracts during in vitro digestion in various sections of the gastrointestinal tract, in the presence and absence of probiotic bacteria. The concentration of free CHAs was the lowest in the stomach and achieved the highest levels in the large intestine. Probiotic bacteria caused significant release of CHAs, and in the colon their concentration was the highest. The studies with Caco-2 and HT-29 cell lines showed that digested coffee extracts had cytoprotective potential against tert-BOOH induced oxidative stress.
Subject(s)
Coffee , Probiotics , Antioxidants/analysis , Caco-2 Cells , Chlorogenic Acid/analysis , Coffee/chemistry , Coumaric Acids/chemistry , Digestion , HT29 Cells , Hot Temperature , Humans , Plant Extracts/chemistry , Plant Extracts/pharmacologyABSTRACT
The aim of the study was to present the fingerprint of different Lepidium peruvianum tuber extracts showing glucosinolates-containing substances possibly playing an important role in preventinting dementia and other memory disorders. Different phenotypes of Lepidium peruvianum (Brassicaceae) tubers were analysed for their glucosinolate profile using a liquid chromatograph coupled with mass spectrometer (HPLC-ESI-QTOF-MS/MS platform). Qualitative analysis in 50% ethanolic extracts confirmed the presence of ten compounds: aliphatic, indolyl, and aromatic glucosinolates, with glucotropaeolin being the leading one, detected at levels between 0-1.57% depending on phenotype, size, processing, and collection site. The PCA analysis showed important variations in glucosinolate content between the samples and different ratios of the detected compounds. Applied in vitro activity tests confirmed inhibitory properties of extracts and single glucosinolates against acetylcholinesterase (AChE) (15.3-28.9% for the extracts and 55.95-57.60% for individual compounds) and butyrylcholinesterase (BuChE) (71.3-77.2% for the extracts and 36.2-39.9% for individual compounds). The molecular basis for the activity of glucosinolates was explained through molecular docking studies showing that the tested metabolites interacted with tryptophan and histidine residues of the enzymes, most likely blocking their active catalytic side. Based on the obtained results and described mechanism of action, it could be concluded that glucosinolates exhibit inhibitory properties against two cholinesterases present in the synaptic cleft, which indicates that selected phenotypes of L. peruvianum tubers cultivated under well-defined environmental and ecological conditions may present a valuable plant material to be considered for the development of therapeutic products with memory-stimulating properties.
Subject(s)
Lepidium , Acetylcholinesterase , Butyrylcholinesterase , Cholinesterase Inhibitors/pharmacology , Glucosinolates/analysis , Lepidium/chemistry , Molecular Docking Simulation , Phenotype , Plant Extracts/chemistry , Plant Extracts/pharmacology , Tandem Mass SpectrometryABSTRACT
The biological activity of an in vitro digested infusion of Epilobium angustifolium (fireweed) was examined in a model system of intestinal epithelial and colon cancer tissues. The content of selected phenolic compounds in the digested aqueous extract of fireweed was determined using HPLC-ESI-QTOF-MS/MS. Biological activity was examined using the human colon adenocarcinoma cell lines HT-29 and CaCo-2 and the human colon epithelial cell line CCD 841 CoTr. Cytotoxicity was assessed by an MTT assay, a Neutral Red uptake assay, May-Grünwald-Giemsa staining, and a label-free Electric Cell-Substrate Impedance Sensing cytotoxicity assay. The effect of the infusion on the growth of selected intestinal bacteria was also examined. The extract inhibited the growth of intestinal cancer cells HT-29. This effect can be attributed to the activity of quercetin and kaempferol, which were the most abundant phenolic compounds found in the extract after in vitro digestion. The cytotoxicity of the fireweed infusion was dose-dependent. The highest decrease in proliferation (by almost 80%) compared to the control was observed in HT-29 line treated with the extract at a concentration of 250 µg/mL. The fireweed infusion did not affect the growth of beneficial intestinal bacteria, but it did significantly inhibit E. coli. The cytotoxic effect of the fireweed extract indicates that it does not lose its biological activity after in vitro digestion. It can be concluded that the fireweed infusion has the potential to be used as a supporting agent in colon cancer therapy.
Subject(s)
Antineoplastic Agents, Phytogenic/chemistry , Epilobium/chemistry , Plant Extracts/chemistry , Polyphenols/chemistry , Antineoplastic Agents, Phytogenic/pharmacology , Caco-2 Cells , Cell Proliferation/drug effects , HT29 Cells , Humans , Neoplasms/drug therapy , Plant Extracts/pharmacology , Polyphenols/pharmacologyABSTRACT
The paper aimed to evaluate the degree of contamination of honey available on the Polish market with cadmium (Cd) and lead (Pb). The analyses involved 49 samples of honey: monofloral (n = 24): linden, raspberry, goldenrod, bean, dandelion, buckwheat and rapeseed honey, multifloral honey (n = 17) and coniferous honeydew honey (n = 8). The content of Cd and Pb was determined using Inductively Coupled Plasma-Optical Emission Spectrometers (ICP-OES). The content of Cd and Pb was confirmed in all the analysed honeys, but in 18% of samples the level of Cd was < LOQ. The analysed honeys contained from < LOQ to ca. 0.09 mg Cd per 1 kg, on average 0.025 mg kg-1. On average, they contained 0.193 mg Pb (range 0.014-1.007) per 1 kg of the raw product. The content of Cd and Pb can be presented as: honeydew honey > multifloral honey > monofloral honey. The content of Cd in monofloral honeys can be presented as follows: linden > other (raspberry, goldenrod, bean, linden + bean) > dandelion = buckwheat = rape, while the content of Pb as linden > other > rapeseed > buckwheat > dandelion honey. It should be emphasised that consuming 19 g of honey a week (mean honey consumption in Poland) is safe for human health, as it results in an intake of Cd at the level of 1.18E-04% PTWI and 0.553% PTWI for children and an intake of Pb at the level of 0.641% BMDL01 for adults and 5.916% BMDL for children. The obtained results lead to a conclusion that the risk of disorders related to chronic exposure to Cd and Pb ingested with honey is very low, which is demonstrated by the fact that both children and adults showed CDI, CR, THQ and HI that were lower than 1.
Subject(s)
Fagopyrum , Honey , Cadmium , Child , Humans , Lead , PolandABSTRACT
Alzheimer's disease (AD) is a progressive neurodegenerative disease characterized, among others, by abnormally low levels of the neurotransmitter acetylcholine in the brain. Acetylcholinesterase (AChE) plays a significant role in the process through hydrolysis of the acetylcholine neurotransmitter. Currently, the main method for treatment of AD at a symptomatic stage entails administration of AChE inhibitors to patients diagnosed with the disease. However, it is also possible to take certain steps to treat AD by delivering inhibitors with food. There is a growing body of evidence to suggest that tea (Camellia sinensis) shows numerous beneficial properties, including improving cognitive abilities. This is particularly important in the case of AD patients. The study assessed the impact of brewing conditions on the inhibition of AChE activity observed in tea extracts (black, white, or fruit). Our study revealed that neither temperature nor time of brewing influenced the respective infusions' ability to inhibit the activity of AChE. Anticholinesterase activity was observed in most of the different types of tea that were analyzed, with the highest rate of inhibition (30.46%-48.54%) evidenced in the Biofix Tea Wild Strawberry brand. The results of our research show that tea may be used as a rich source of cholinesterase inhibitors which play a significant role in AD treatment.
Subject(s)
Camellia sinensis/chemistry , Cholinesterase Inhibitors , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Tea/chemistry , Alzheimer Disease/therapy , Humans , Phytotherapy , Plant Extracts/therapeutic useABSTRACT
Neurodegenerative diseases are progressive diseases of the nervous system that lead to neuron loss or functional disorders. Neurodegenerative diseases require long-term, sometimes life-long pharmacological treatment, which increases the risk of adverse effects and a negative impact of pharmaceuticals on the patients' general condition. One of the main problems related to the treatment of this type of condition is the limited ability to deliver drugs to the brain due to their poor solubility, low bioavailability, and the effects of the blood-brain barrier. Given the above, one of the main objectives of contemporary scientific research focuses on the prevention of neurodegenerative diseases. As disorders related to the competence of the antioxidative system are a marker in all diseases of this type, the primary prophylactics should entail the use of exogenous antioxidants, particularly ones that can be used over extended periods, regardless of the patient's age, and that are easily available, e.g., as part of a diet or as diet supplements. The paper analyzes the significance of the oxidoreductive balance in the pathogenesis of neurodegenerative diseases. Based on information published globally in the last 10 years, an analysis is also provided with regard to the impact of exogenous antioxidants on brain functions with respect to the prevention of this type of diseases.
Subject(s)
Brain/metabolism , Dietary Supplements , Neurodegenerative Diseases/etiology , Neurodegenerative Diseases/prevention & control , Animals , Antioxidants , Blood-Brain Barrier , Female , Humans , Male , Oxidation-ReductionABSTRACT
BACKGROUND: Cholinesterase inhibitors are routinely applied in the treatment of Alzheimer's disease, and seeking new cholinesterase inhibitors is a priority. OBJECTIVES: Twenty seven compounds were compared, including ones not previously tested. An attempt was undertaken to precisely describe the role of alcohol in the inhibitory activity. This paper underlines the role of a "false positive" blank sample in the routine analysis. METHODS: The inhibition of cholinesterase was measured using Ellman's colorimetric method with a few modifications designed by the authors (including the "false-positive" effect). The inhibitory role of ethanol and methanol was also carefully evaluated. The present and past results were compared taking the source of enzyme and alcohol content into consideration. RESULTS: For the first time, new inhibitors were identified, namely: methyl jasmonate, 1R-(-)-nopol ((anti-acetyl-(AChE) and butyrylcholinesterase (BChE) activity)) and 1,4-cineole, allo-aromadendrene, nerolidol, ß-ionone, and (R)-(+)-pulegone (anti-BChE activity). Oleanolic acid and (+)-ß-citronellene (not previously studied) proved to be inefficient inhibitors. For a number of well-known inhibitors (such as nerol, (-)-menthol, (+)-menthol, isoborneol, (-)-bornyl acetate, limonene, α-pinene, ß-pinene, α- ionone, and eugenol) some serious discrepancies were observed between our findings and the results of previous studies. Ethanol and methanol showed no anti-AChE activity up to 0.29% (v/v) and 0.23% (v/v), respectively. Similarly, ethanol up to 0.33% (v/v) and methanol up to 0.29% (v/v) did not inhibit the activity of BChE. CONCLUSION: It can be stated that the impact of alcohol should be precisely determined and that blank "false-positive" samples should be processed together with test samples. Furthermore, the effect of the enzyme origin on the result of this test must be taken into consideration.