Anticholinesterase activity of selected phenolic acids and flavonoids – interaction testing in model solutions

[b][/b][b]Introduction[/b]. Alzheimer’s disease is a progressively developing neurodegenerative disorder of the central nervous system. The only present treatment of this disease is the use of acetyl- and butyrylcholinesterase inhibitors. Previously, the neuroprotection of phenolic acids and flavonoids in the brain has been indicated. [b]Materials and method.[/b] This study measured anticholinesterase activities of 9 phenolic acids and 6 flavonoids, singly or in combination. The synergy/antagonism/zero interaction between compounds was evaluated taking into consideration the statistical significance. Ellman’s modified spectrophotometric method was used with the simultaneous measurement of the false-positive effect of compounds. [b]Results[/b]. The anti-acetylcholinesterase activity of phenolic acids was as follows: homogentisic acid > 4-hydroxyphenylpyruvic acid > nordihydroguaiaretic acid > rosmarinic acid > caffeic acid > gallic acid = chlorogenic acid > homovanillic acid > sinapic acid. p-Hydroxyphenylpyruvic, caffeic, chlorogenic, gentisic, homogentisic, nordihydroguaiaretic and rosmarinic acids in pairs exhibited, in most cases, a lower inhibitory activity (at p>0.05), than the sum of the activities of single compounds. Also, phenolic acids in pairs with flavonoids (cyanidin, delphinidin, kaempferol, myricetin, phloridzin, pelargonidin or quercetin) presented, in most cases, a lower inhibitory activity than could be calculated for both compounds singly (at p>0.05). Only in the case of a few samples was the inhibitory activity of two compounds higher than the sum of inhibitions exerted by the same compounds tested singly (either at p>0.05 or p<0.05). The lack of synergy of pairs of inhibitors suggests one small binding site, making impossible to accommodate both inhibitors adjacent to one another

Anticholinesterase activity of selected phenolic acids and flavonoids – interaction testing in model solutions

[b][/b][b]Introduction[/b]. Alzheimer’s disease is a progressively developing neurodegenerative disorder of the central nervous system. The only present treatment of this disease is the use of acetyl- and butyrylcholinesterase inhibitors. Previously, the neuroprotection of phenolic acids and flavonoids in the brain has been indicated. [b]Materials and method.[/b] This study measured anticholinesterase activities of 9 phenolic acids and 6 flavonoids, singly or in combination. The synergy/antagonism/zero interaction between compounds was evaluated taking into consideration the statistical significance. Ellman’s modified spectrophotometric method was used with the simultaneous measurement of the false-positive effect of compounds. [b]Results[/b]. The anti-acetylcholinesterase activity of phenolic acids was as follows: homogentisic acid > 4-hydroxyphenylpyruvic acid > nordihydroguaiaretic acid > rosmarinic acid > caffeic acid > gallic acid = chlorogenic acid > homovanillic acid > sinapic acid. p-Hydroxyphenylpyruvic, caffeic, chlorogenic, gentisic, homogentisic, nordihydroguaiaretic and rosmarinic acids in pairs exhibited, in most cases, a lower inhibitory activity (at p>0.05), than the sum of the activities of single compounds. Also, phenolic acids in pairs with flavonoids (cyanidin, delphinidin, kaempferol, myricetin, phloridzin, pelargonidin or quercetin) presented, in most cases, a lower inhibitory activity than could be calculated for both compounds singly (at p>0.05). Only in the case of a few samples was the inhibitory activity of two compounds higher than the sum of inhibitions exerted by the same compounds tested singly (either at p>0.05 or p<0.05). The lack of synergy of pairs of inhibitors suggests one small binding site, making impossible to accommodate both inhibitors adjacent to one another

Anticholinesterase activity of selected phenolic acids and flavonoids -interaction testing in model solutions

Szwajgier D. Anticholinesterase activity of selected phenolic acids and flavonoids: interaction testing in model solutions. Ann Agric Environ Med. 2015; 22(4): 690-694. doi: 10.5604/12321966.1185777 Abstract Introduction. Alzheimer's disease is a progressively developing neurodegenerative disorder of the central nervous system. The only present treatment of this disease is the use of acetyl-and butyrylcholinesterase inhibitors. Previously, the neuroprotection of phenolic acids and flavonoids in the brain has been indicated. Materials and method. This study measured anticholinesterase activities of 9 phenolic acids and 6 flavonoids, singly or in combination. The synergy/antagonism/zero interaction between compounds was evaluated taking into consideration the statistical significance. Ellman's modified spectrophotometric method was used with the simultaneous measurement of the false-positive effect of compounds. Results. The anti-acetylcholinesterase activity of phenolic acids was as follows: homogentisic acid > 4-hydroxyphenylpyruvic acid > nordihydroguaiaretic acid > rosmarinic acid > caffeic acid > gallic acid = chlorogenic acid > homovanillic acid > sinapic acid. p-Hydroxyphenylpyruvic, caffeic, chlorogenic, gentisic, homogentisic, nordihydroguaiaretic and rosmarinic acids in pairs exhibited, in most cases, a lower inhibitory activity (at p>0.05), than the sum of the activities of single compounds. Also, phenolic acids in pairs with flavonoids (cyanidin, delphinidin, kaempferol, myricetin, phloridzin, pelargonidin or quercetin) presented, in most cases, a lower inhibitory activity than could be calculated for both compounds singly (at p>0.05). Only in the case of a few samples was the inhibitory activity of two compounds higher than the sum of inhibitions exerted by the same compounds tested singly (either at p>0.05 or p<0.05). The lack of synergy of pairs of inhibitors suggests one small binding site, making impossible to accommodate both inhibitors adjacent to one another

The Neuroprotective Effects of Phenolic Acids: Molecular Mechanism of Action

The neuroprotective role of phenolic acids from food has previously been reported by many authors. In this review, the role of phenolic acids in ameliorating depression, ischemia/reperfusion injury, neuroinflammation, apoptosis, glutamate-induced toxicity, epilepsy, imbalance after traumatic brain injury, hyperinsulinemia-induced memory impairment, hearing and vision disturbances, Parkinson’s disease, Huntington’s disease, anti-amyotrophic lateral sclerosis, Chagas disease and other less distributed diseases is discussed. This review covers the in vitro, ex vivo and in vivo studies concerning the prevention and treatment of neurological disorders (on the biochemical and gene expression levels) by phenolic acids

The Role of Beetroot Ingredients in the Prevention of Alzheimer’s Disease

Beets (Beta vulgaris L.) are a source of numerous bioactive compounds, including betalain pigments, phenols, and saponins. The bioactive compounds show neuroprotective properties due to their antioxidant activity (they protect cells against oxidative stress caused by the overaccumulation of reactive oxygen species), anti-inflammatory effects, and the ability to lower the activity of acetylcholinesterase. The most common pigment present in beetroot is betanin. Scientists have repeatedly demonstrated the antioxidant activity of this compound, which is capable of protecting the cell membrane of neurons against peroxidation. The phenolic compounds present in the root showed the same effect. Phenolic acids are the most prevalent group of such compounds, including gallic, ferulic, and vanillic acids. It has been shown that neurodegenerative diseases induced artificially (e.g., with sodium fluoride or trimethyltin chloride) are reversed by the administration of betanin. A similar protective effect has been demonstrated in streptozotocin-induced disease models. For example, the administration of vanillic acid improved spatial learning ability. Hence, processed beetroot (juices, jams, etc.) can offer viable benefits in preventing neurodegenerative diseases such as Alzheimer’s disease (AD). The following review presents a detailed summary of the current state of knowledge regarding the most important bioactive compounds present in beetroots and their applicability in AD prevention and support therapy

Some Plant Food Products Present on the Polish Market Are a Source of Vitamin B12

Cyanocobalamin is the most widespread form of vitamin B12, which is sufficient for humans. Vitamin B12 is mainly found in animal products. However, supplementation does not have to be necessary because certain amounts of vitamin B12 are present in plant products. Previous studies showed significant contents of cyanocobalamin in sea buckthorn and in sauerkraut. In this study, selected products such as sea-buckthorn jam and fermented plant products (obtained by lactic acid fermentation) were tested in a search for vitamin B12. Bacteria involved in this type of fermentation have the potential to produce cyanocobalamin. Popular fermented plant products on the Polish market were selected, namely sauerkraut and pickled cucumbers, as well as parsley juice, beetroot juice and white borscht. The analysis was carried out using HPLC-UV. Most of the analyzed products did not contain significant levels of vitamin B12. Only sea-buckthorn jam and pickled parsley juice can provide the amount of vitamin B12 needed to prevent deficiency

Influence of different heat treatments on the content of phenolic acids and their derivatives in selected fruits

Introduction. A considerable number of positive effects after the consumption of fruits has been pointed out in the past: hypolipidemic action, reduction of blood glucose levels, hepatoprotection and improvement of the antioxidant status as well as, inter alia, antioxidant, antiradical, anti-inflammatory, anticancer and anti-adipogenic status. Materials and methods. The changes in the levels of phenolic acids and their derivatives in fresh as well as in processed fruits (chokeberry, wild strawberry, apples var. Idared and Champion, cherry, apricot, peach, raspberry, cranberry, and bilberry) were studied using HPLC with UV detection. Dried fruit homogenates and compotes were produced. Also, fruits were fried to simulate jam production. Results and discussion. Eleven phenolic acids and their derivatives were identified in tested samples: caffeic, chlorogenic, p-coumaric, ferulic, gallic, ellagic, protocatechuic, p-hydroxybenzoic, gentisic, syringic and vanillic acids. In most cases, the thermal processing of fruits caused a decrease in the levels of phenolic acids. In some preserves, the level of selected individual phenolic compounds was unchanged or was significantly increased. Conclusion. It can be concluded that thermal processing can have a differential effect on the levels of phenolic acids in preserves and general conclusions could not be formulated. The fruit composition in which a phenolic acid is present can play a role in this context

Honeys as Possible Sources of Cholinesterase Inhibitors

Alzheimer’s disease (AD) is a progressive neurodegenerative disease characterised by low levels of the neurotransmitter (acetylcholine), oxidative stress, and inflammation of the central nervous system. The only currently available form of treatment entails the administration of AChE/BChE (acetylcholinesterase/butyrylcholinesterase) inhibitors to patients diagnosed with the disease. However, AD prevention is possible by administering the correct inhibitors with food. The aim of this study was to examine 19 types of honey in terms of their contents of cholinesterase inhibitors. The inhibition of AChE and BChE relative to the respective honey samples was evaluated using Ellman’s colorimetric method, including the “false-positive” effect. The highest potential for AChE inhibition was observed in the case of thyme honey (21.17% inhibition), while goldenrod honey showed the highest capacity for BChE inhibition (33.89%). Our study showed that honeys may provide a rich source of cholinesterase inhibitors and, in this way, play a significant role in AD

Determination of the Content of Selected Pesticides in Surface Waters as a Marker of Environmental Pollution

Pesticides are a major problem not only in the food chain but also when considering the protection of our planet. The use of neonicotinoids has been banned in the EU due to their high toxicity to living organisms, in particular honeybees. The presence of neonicotinoids in natural waters poses a threat to pollinating insects and thus hampers organic production. Pesticide residues in the natural waters of agricultural land are monitored within the framework of promoting sustainable rural development to maintain the safety of human and animal health. Chromatographic analyses of selected neonicotinoid pesticides in water samples from agricultural sites in eastern Poland were performed using high performance liquid chromatography (HPLC), which followed a solid-phase extraction (SPE). The research revealed no evidence of neonicotinoids contamination. Water quality in this region can be a good factor in promoting sustainable development. The obtained results complement the existing knowledge on the impact of neonicotinoids on both the sustainable food chain and the environment. Based on the results obtained, it is possible to conclude that they are not being used in rural area under the study

Inhibitory activity of chokeberry, bilberry, raspberry and cranberry polyphenol-rich extract towards adipogenesis and oxidative stress in differentiated 3T3-L1 adipose cells

<div><p>Berries are a rich source of antioxidants and phytochemicals that have received considerable interest for their possible relations to human health. In this study, the anti-adipogenic effect of polyphenol-rich extract obtained from chokeberry <i>Aronia melanocarpa</i> (Michx.) Elliot, raspberry <i>Rubus idaeus</i> L., bilberry <i>Vaccinium myrtillus</i> L. and cranberry <i>Vaccinium macrocarpon</i> Aiton fruits and its underlying molecular mechanisms were investigated in differentiated 3T3-L1 adipose cells. Treatment with the extract (25–100 μg/mL) significantly decreased lipid accumulation and reactive oxygen species generation in adipocytes without showing cytotoxicity. Real-time PCR analysis revealed that the extract at a concentration of 100 μg/mL suppressed adipogenesis and lipogenesis via the down-regulation of <i>PPARγ</i> (67%), <i>C/EBPα</i> (72%), <i>SREBP1</i> (62%), <i>aP2</i> (24%), <i>FAS</i> (32%), <i>LPL</i> (40%), <i>HSL</i> (39%), and <i>PLIN1</i> (32%) gene expression. Moreover, the extract significantly increased the expression of adiponectin (4.4-fold) and decreased leptin expression (90%) and respectively regulated the production of these adipokines in 3T3-L1 adipocytes. The obtained results suggest that the analyzed extract may be a promising source of bioactive compounds that support long-term weight maintenance and promote the effective management of obesity.</p></div