Insights into the effects of extractable phenolic compounds and Maillard reaction products on the antioxidant activity of roasted wheat flours with different maturities.

Experiments were performed to determine the effect of roasting whole wheat flours at 80 °C, 100 °C and 120 °C for 30 min on four forms of phenolics, Maillard reaction products (MRPs), and the DPPH scavenging activity (DSA) at 15, 30 and 45 days after flowering (15-DAF, 30-DAF, and 45-DAF). Roasting increased the phenolic content and antioxidant activity of the wheat flours, which were the dominant contributions to the formation of Maillard reaction products. The highest total phenolic content (TPC) and total phenolic DSA (TDSA) were determined in the DAF-15 flours at 120 °C/30 min. The DAF-15 flours exhibited the highest browning index and fluorescence of free intermediate compounds and advanced MRPs, suggesting that a substantial quantity of MRPs were formed. Four forms of phenolic compounds were detected with significantly different DSAs in the roasted wheat flours. The insoluble-bound phenolic compounds exhibited the highest DSA, followed by the glycosylated phenolic compounds.

Bioaccessibility of terebinth (Pistacia terebinthus L.) coffee polyphenols: Influence of milk, sugar and sweetener addition.

In this study, terebinth coffee formulations were prepared with whole or skimmed milk with or without sugar/sweetener in order to study the matrix effect on the bioaccessibility of terebinth polyphenols. Quercetin glycosides and catechin were the major flavonoids identified in the terebinth formulations, whereas gallic, protocatechuic, syringic and ellagic acids were determined as the non-flavonoid compounds. The in vitro gastrointestinal digestion model results revealed that addition of whole milk to terebinth coffee increased the total bioaccessible flavonoids significantly (45%) (p < 0.05), whereas skim milk addition did not result in any significant change. Furthermore, antioxidant capacity results measured with CUPRAC assay showed that addition of milk alone or together with sugar/sweetener increases the bioaccessibility of terebinth coffee antioxidants (36-70%) (p < 0.05). Overall, terebinth coffee + whole milk + sugar formulation was found to contain the highest amount of bioaccessible flavonoid and non-flavonoid compounds (42.71-47.07 mg/100 g).

Inhibition of the SARS-CoV-2 3CLpro main protease by plant polyphenols.

The abundance of polyphenols in edible plants makes them an important component of human nutrition. Considering the ongoing COVID-19 pandemic, a number of studies have investigated polyphenols as bioactive constituents. We applied in-silico molecular docking as well as molecular dynamics supported by in-vitro assays to determine the inhibitory potential of various plant polyphenols against an important SARS-CoV-2 therapeutic target, the protease 3CLpro. Of the polyphenols in initial in-vitro screening, quercetin, ellagic acid, curcumin, epigallocatechin gallate and resveratrol showed IC50 values of 11.8 µM to 23.4 µM. In-silico molecular dynamics simulations indicated stable interactions with the 3CLpro active site over 100 ns production runs. Moreover, surface plasmon resonance spectroscopy was used to measure the binding of polyphenols to 3CLpro in real time. Therefore, we provide evidence for inhibition of SARS-CoV-2 3CLpro by natural plant polyphenols, and suggest further research into the development of these novel 3CLpro inhibitors or biochemical probes.

Phoenix dactylifera L. date tree pollen fertility effects on female rats in relation to its UPLC-MS profile via a biochemometric approach.

Date palm (Phoenix dactylifera L.) is among the most ancient cultivated crops, of special value owing to its fruits high nutritive and economic benefits. Asides, date palm pollen is a high energy material that has been used traditionally used for fertility enhancement. In this study, effects of date palm pollen crude extract and its fractions viz., petroleum ether, methylene chloride, ethyl acetate and n-butanol on the female reproductive system were evaluated for the first time in relation to its metabolite fingerprint. Fertility activity was evaluated in immature female rats by assessing their FSH-, LH- and estrogen- activities. To pinpoint active hormonal agents in crude pollen extract and fractions, UPLC- MS analysis was employed for metabolites profiling, and in correlation to extract/fraction bioassays using multivariate OPLS analysis. Results revealed that both polar n-butanol and non-polar petroleum ether fractions exhibited the strongest activities; with a significant increase in FSH (25.7 mIU/ml in n-butanol group), estradiol (414.7 pg/ml in petroleum ether group) and progesterone levels (122.4 pg/ml in n-butanol group). Correlation between UPLC-MS and fraction bioassays was attempted using multivariate OPLS analysis to reveal for bioactive hits in these fractions. This study provides the first report on the fertility effect of date palm pollen in female rats and in relation to its metabolite fingerprint.

Multi-response optimal hot pressurized liquid recovery of extractable polyphenols from leaves of maqui (Aristotelia chilensis [Mol.] Stuntz).

Multi-response optimization of hot pressurized liquid extraction (HPLE) was applied for the first time to obtain maqui (Aristotelia chilensis [Mol.] Stuntz) leaf extracts. The total polyphenol content (TPC), the antioxidant capacity (AC) as well as the total polyphenol purity of the maqui leaf extracts were accurately predicted (RSD < 8%) at the evaluated extraction scales. The optimum HPLE conditions that prioritized TPC and AC equally (OPT1) recovered ~3 times more TPC (205.14 mg GAE/g leaves) than maqui leaf extracts obtained by maceration, while the extract that prioritized purity over TPC and AC presented the highest purity (36.29%) and an EC50 ~3 times lower than currently reported values. It was found by multi-response optimization that maqui leaves and HPLE are among the best natural sources and extraction techniques, respectively, to recover protocatechuic acid, quercetin, and catechin.

Future prospects of ketoprofen in improving the safety of the gastric mucosa.

INTRODUCTION: Ketoprofen (K) was synthesized in 1968. K belongs to nonsteroidal anti-inflammatory drugs (NSAIDs) and has analgesic, anti-inflammatory and antipyretic properties. K is commonly used due to rapid absorption, simple metabolism, high antinociceptive activity and fast blood brain barrier crossing. However, this substance causes various side effects which are the major factors affecting its' popularity. Many researchers have modified this drug to discover an improved and safe NSAID. AIM: The aim of the review was to find in recent publications data bout future prospects of K of improved safety for the gastric mucosa after oral administration. METHOD: Systematic literature review was conducted in March 2021 (2015 onwards). We selected 22 articles from PubMed, Google Scholar, Medline Complete databases. RESULTS AND DISCUSSION: Many studies aimed at obtaining K with lower ulcerogenic properties. This article describes K with lysine, new K delivery systems, K in form of hydrogels, prodrugs and codrugs of K, K as ATB-352, K with zinc, K encapsulated as proliposomal powders and several substances that reduce the gastric side effects of K described after 2015. CONCLUSION: Our review confirms that modifications of K maintain its' desirable actions and decrease ulcer producing side effect. Some new forms of K were also found to have better activity profile compared to the parent drug.

Edible flowers from Theobroma speciosum: Aqueous extract rich in antioxidant compounds.

Theobroma speciosum, known as "cacauí" in Brazil, is considered a prominent unconventional food plant. The objective of this work was to evaluate the chemical profiles, antioxidant capacity and minerals of the aqueous extract and fractions from its flowers. The identified compounds were sugars, organic acids and phenolics compounds such as citric, malic and protocatechuic acids, quercetin, quercetin pentoside and quercetin-3-O-glucoside. The extract was rich in phenolic compounds (640 mg GAE g-1). Furthermore, fractions also presented phenolic compounds from 170.7 to 560.7 mg GAE g-1 (mainly protocatechuic acid, quercetin and derivatives), which influenced on the high antioxidant capacity in DPPH, ABTS, FRAP and co-oxidation ß-carotene/linolenic acid assays. Flowers presented potassium (115 ± 2 µg mL-1), magnesium (18.4 ± 0.2 µg mL-1), phosphorus (7.0 ± 0.0 µg mL-1) and calcium (3.1 ± 0.1 µg mL-1). Moreover, the flowers aqueous extract represents a new promising food source rich in antioxidant compounds.

Phenolic composition, antioxidant capacity and α-glucosidase inhibitory activity of raw and boiled Chilean Araucaria araucana kernels.

The Araucaria araucana kernels are a traditional food in southern Chile and Argentina. The aim of this work was to determine the composition of the phenolic-enriched extracts (PEEs) of the boiled kernels as well as their antioxidant capacity, inhibitory activity on metabolic syndrome-associated enzymes and effect on postprandial oxidative stress in a simulated gastric digestion model. The PEEs composition was assessed by HPLC-DAD-MS/MS. The main PEEs constituents were catechin and epicatechin in the unbound form, while hydroxybenzoic acids occurred mainly in the bound form. The unbound phenolics from boiled kernels showed significant correlations with DPPH, FRAP, TEAC (Pearson's r of 0.481, 0.331 and 0.417, respectively) and lipid peroxidation (r = 0.381) and were more active than the bound phenolics. The extracts were highly active against α-glucosidase (IC50: 0.33-3.15 µg/mL) and reduced lipoperoxidation. Traditional processing increases the flavan-3-ol content. Our results suggest that this traditional food has potential health promoting properties.

Phytochemical composition and antioxidant activity of Cinnamomum burmannii Blume extracts and their potential application in white chocolate.

This study aims at determining the potentials of cinnamon (Cinnamomun burmannii) extracts to improve the health-promoting properties of white chocolate. LC-HRMS analysis was employed to obtain information regarding the phytochemical content while the phosphomolybdenum, FRAP and DPPH assays were used to determine antioxidant activity of cinnamon extract. Furthermore, the cinnamon extract was loaded into nanoparticles before adding it to white chocolate. The results show that cinnamon extracts contained phenols up to 310 mg EE and possessed antioxidant activity up to 260 mg TAE per gram of dry extract depending on the extraction mode (i.e., traditional and ultrasonic-assisted method) and the solvent type. The cinnamon extract contained catechin, epicatechin, procyanidin B2, quercitrin, 3,4-dihydroxybenzaldehyde, protocatechuic acid and cinnamic acid at levels of 51, 53, 1396, 13, 1138, 228 and 934 µg/g of dry extract, respectively. The encapsulated cinnamon extract increased the phenolic content of white chocolate from 47.6 to 1060.6 µg EE/g.

Evaluation of polyphenol bioaccessibility and kinetic of starch digestion of spaghetti with persimmon (Dyospyros kaki) flours coproducts during in vitro gastrointestinal digestion.

The aim was to study the in vitro starch digestibility, the free and bound polyphenol profile and their bioaccessibility and antioxidant activity during in vitro gastrointestinal digestion of durum wheat semolina spaghetti added with two types of persimmon flour concentrates ("Rojo Brillante" flour and "Triumph" flour) at two concentrations (3 and 6%). Results obtained showed that persimmon flour improves the polyphenol profile of spaghetti by addition gallic acid and coumaric acid-o-hexoside, and increasing 2-fold and around 3-fold its content in spaghetti with 3% and 6% persimmon flours, respectively. Cooked process and digestion affected more to free polyphenol content than bound. Furthermore, 3% persimmon flour enriched spaghetti reduce kinetic of starch digestion, while 6% enriched spaghetti increased it. In conclusion, persimmon flours (Rojo Brillante and Triumph) at low concentrations could be used to develop spaghetti with more polyphenol content and less starch digestibility than traditional spaghetti.

Model-free and model-based analysis of thermo-oxidative response of wolfberries: A new developed mechanistic scheme.

Thermally accelerated oxidative degradation of wolfberry pulp was kinetically monitored using model-free and model-based approaches. Kinetic calculations were performed based on simultaneous thermal analysis measurements in an air at four different heating rates. From kinetic analysis, new developed mechanistic scheme which is responsible for wolfberries anti-oxidative behavior was proposed. It was found that thermo-oxidative process proceeds through multiplestep mechanism including sum of two independent reaction sets, via consecutive and competitive steps. It was established that rutoside degradation pathway to flavonol through hydrolysis reaction is rate-determining step of considered process. Furthermore, it was found that key flavonol compound degraded by competitive reactions mechanism forming such kinetic branches, which lead to compounds responsible for wolfberries antioxidant activity. It was established that flavonol oxidative cleavage reaction and oxidative polymerization are main chemical routes which are very important in a complex antioxidant mechanism for scavenging free radicals in wolfberries oxidative stress response.

Clitoria ternatea L. petal bioactive compounds display antioxidant, antihemolytic and antihypertensive effects, inhibit α-amylase and α-glucosidase activities and reduce human LDL cholesterol and DNA induced oxidation.

The purpose of this study was to use a statistical approach to optimise the experimental conditions regarding the extraction of bioactive compounds, and to analyse the in vitro functional properties of crude lyophilized extracts (CLE) and partially purified (PPE) extracts of Clitoria ternatea petals. The results showed that the factors of temperature and time influenced the extraction of phenolic compounds, antioxidant activity and the physicochemical parameters. Simultaneous optimisation showed that the same levels of bioactive compounds were extracted when using temperatures from 11.7 to 68.3 °C and times from 8.47 to 51.12 min. Principal component analysis revealed the experimental conditions that provided the extraction producing the highest level of phenolic content (40 °C/30 min). The CLE showed antimicrobial activity; protective effect against hemolysis of erythrocytes; inhibition of α-amylase, α-glucosidase and angiotensin-I-converting (ACE-I) enzymes; and inhibition of lipid peroxidation. The CLE and PPE demonstrated oxygen radical absorption capacity; inhibition of DNA strand scission; inhibition of LDL cholesterol oxidation; intracellular antioxidant activity against reactive oxygen species (>100 µg/mL); and no cytotoxicity (IC50, GI50 and LC50 > 900 µg/mL) against A549, HCT8 and IMR90 cell lines.

Letting wine polyphenols functional: Estimation of wine polyphenols bioaccessibility under different drinking amount and drinking patterns.

Effects of drinking amount and patterns of wine on the digestive characteristics and bioaccessibility of wine polyphenols under in vitro gastrointestinal digestion were investigated. Wine polyphenols released well during mouth and stomach digestion, and the release rates in the "serum-available" fraction, "colon-available" fraction, and after the colon were much lower. Red wine showed a higher biological activity than white wine, but white wine had a better bioaccessibility than red wine, especially under binge drinking. The bioaccessibility of most polyphenols decreased as the drinking amount increased, indicating that drinking larger volumes of wine did not increase the bioaccessibility of polyphenols. Additionally, the relevant biological activities did not increase as the drinking amount increased. Drinking after a meal showed significantly better results than drinking before a meal in most of the tests. Hence, in order to let wine polyphenols play its functional for human health, there still need a moderate consumption amount of wine and drinking after meal is better.

Ethnopharmacology, phytochemistry, biological activities, and therapeutic applications of Cedrela serrata Royle: A mini review.

ETHNOPHARMACOLOGICAL RELEVANCE: Cedrela serrata Royle (C. serrata) is a medicinal plant not only used for constructions but also an important conventional medicine for the treatment of various diseases such as; diabetes, jaundice, liver diseases, diarrhea, fever, chronic infantile dysentery, intestinal worms, hypertension, skin and blood diseases. AIMS: This review article documents and critically assesses, for the first time; up to date categorized information about C. serrata including its reported pharmacological activities, cultural uses, active compounds, and botanical description. MATERIALS AND METHOD: s: All provided information about C. serrata was collected using the electronic databases (e.g. Google Scholar, Web of Science, Scopus, PubMed, Science Direct and Springer Link), books (e.g. Trees of Pakistan and Herbalism, Phytochemistry, and Ethnopharmacology) and thesis. RESULTS: Qualitative and quantitative phytochemical studies on C. serrata revealed the presence of important chemical constituents such as; flavonoids, phenolic acids, alkaloids, saponins, tannins, and cardiac glycosides. The phytochemicals showed various in vitro activities like antioxidant, anti-infective, antiglycation, cytotoxic activities. Major areas of research conducted on C. serrata are its antioxidant and anti-infective activities. Few historical uses of C. serrata are supported by modern in vitro pharmacological studies such as; antidiarrheal, antidiabetic, and leishmanicidal activity. CONCLUSION: There were convincing evidence in in vitro studies supporting C. serrata antioxidant, anti-infective, anti-diabetic, anti-glycating, and cytotoxic activities. Nevertheless, all reported pharmacological activities were carried out in vitro and a gap in research i.e. preclinical and clinical investigation still exists. The authors emphasize the need for future in-depth research and clinical trials to investigate C. serrata pharmacological activity, clinical efficacy and safety. The potential chemical compounds with suggestive classes may need to be isolated and pharmacological activities must be established for these compounds. The plant has very limited information about pharmacological activities and the data available for supportive cultural uses needs proper validation.

Pharmacodynamics and pharmacokinetics of Danshen in isoproterenol-induced acute myocardial ischemic injury combined with Honghua.

ETHNOPHARMACOLOGICAL RELEVANCE: Herb pair, the most fundamental and simplest form of herb compatibility, serves as the basic building block of traditional Chinese medicine formulae. The Danshen-Honghua herb pair (DH), composed of Salviae Miltiorrhizae Radix et Rhizoma (Danshen in Chinese) and Carthami Flos (Honghua in Chinese), has remarkable clinical efficacy to cure cardio-cerebrovascular diseases. This study was designed to investigate the pharmacodynamics of DH in comparison with single herbs and pharmacokinetics of DH relative to Danshen in acute myocardial ischemic injury. MATERIALS AND METHODS: Sixty male Wistar rats were divided into control, model and drug treated groups. The acute myocardial ischemia rat model was induced by administering 85 mg/kg/d isoproterenol (ISO) subcutaneously for two consecutive days. For pharmacodynamic study, histopathological and biochemical analysis were performed to assess the anti-myocardial ischemic effects. While for pharmacokinetic study, a UPLC-MS/MS method was developed for determination of nine main active ingredients, namely danshensu, protocatechuic acid, protocatechualdehyde, caffeic acid, lithospermic acid, rosmarinic acid, salvianolic acid B, salvianolic acid A and salvianolic acid C in rat plasma. RESULTS: The histopathological and biochemical analysis revealed that DH exerted enhanced anti-myocardial ischemic effects against the ISO-induced myocardial ischemia compared with single herbs. The pharmacokinetic study indicated that DH could significantly increase the t1/2z of danshensu, Tmax, AUC0-∞ and MRT0-t of protocatechuic acid in comparison with Danshen alone in normal rats, but more importantly elevate systemic exposure level and prolong t1/2z of protocatechualdehyde, caffeic acid, Tmax of danshensu in acute myocardial ischemia rats. CONCLUSIONS: Our findings demonstrated the greater effects of DH after the compatibility in ISO-induced acute myocardial ischemia rats at pharmacodynamic and pharmacokinetic levels and provided valuable information for clinical application of herb pairs.

Identification of acacia honey treated with macroporous adsorption resins using HPLC-ECD and chemometrics.

The adulteration of honey is generally a safety and quality concern for consumers and the industry as a whole. Resin technologies allow harmful substances to enter honey, creating substandard honey, which can enter the market. Thus, it is necessary to identify such illegal products quickly and easily. In this study, HPLC-ECD combined with chemometrics was used to identify raw acacia honey that had been treated with macroporous adsorption resins. The chromatography fingerprints of 46 honey samples were established, and principal component analysis (PCA) and the OPLS-DA identified that differences in some of the chromatographic peaks could be used to distinguish raw from resins-treated raw honeys. 100% correct classification was achieved with test samples, based on the chromatographic peaks identified. These results show that HPLC-ECD, combined with chemometric methods, can identify correctly resins-treated honey and can be applied for the quality control of honey.

Phenolic profiles, antioxidant activities and cytoprotective effects of different phenolic fractions from oil palm (Elaeis guineensis Jacq.) fruits treated by ultra-high pressure.

The present work investigated the phenolic profiles, antioxidant activities, and cytoprotective effects of the free, esterified, and insoluble-bound phenolic fractions from oil palm fruits treated under ultra-high pressure (UHP). Results showed that UHP treatment significantly increased the total phenolic and flavonoid contents of all three phenolic fractions (p < 0.05). A total of 11 and 12 phenolic compounds were detected and quantified in non-treated and UHP-treated fruits, with caffeic acid having the highest concentration in insoluble-bound phenolic fractions with 8.68 and 11.27 mg/g of dry extract, respectively. The antioxidant activities, intracellular reactive oxygen species inhibition, and cytoprotective effects of all three phenolic fractions were dramatically enhanced after UHP pretreatment (p < 0.05). Therefore, UHP-treated oil palm fruits with increased bioactivities could be used in functional food or the nutraceutical industry to enhance their applications and economic value.

Fruit and herbal meads - Chemical composition and antioxidant properties.

The aim of the study was to determine the effect of fruit additives such as syrup from chokeberry or grape seeds, and herbal in the form of a dandelion syrup on the course of the fermentation process of "trójniak" type meads, on their physicochemical and antioxidant properties. The addition of grape seeds allowed for the highest final alcoholic content, which was measured by HPLC, ie 120.73 g/L, and for obtaining a beverage with the highest overall polyphenol content measured by the Folin-Ciocialteu reagent method: 23.18 mg GAE/100 mL, while in the control sample (without additives) it was successively: 91.38 g/L and 12 mg GAE/100 mL. Our research shows that different various of fruit and herbal have a significant impact on the course of the mead fermentation process and on their composition and on the content of biologically active compounds.

UPLC-QqQ-MS/MS-based phenolic quantification and antioxidant activity assessment for thinned young kiwifruits.

For the first time, thinned young kiwifruits (TYK) have been investigated as a source of deserted agriculture resource and evaluated for their phenolic characteristics along with antioxidant capacity. Two batches of TYK in different maturity stages (TYK1 and TYK2) and mature kiwifruits (MK) were sourced from three New Zealand cultivars. Comparing with MK, the TYK, especially TYK1, exhibited significantly higher contents of total phenolics (7.92 fold), total flavonoids (17.56 fold) and total flavanols (10.11 fold) as well as elevated and phenolic-correlated antioxidant capacities. A novel UPLC-QqQ-MS/MS method with low limit of detection (0.010-0.240 mg/L) and high accuracy (RSDs < 6.79%) was established to quantify 15 phenolics in the kiwifruit extracts. Epicatechin was the prevailing antioxidant in both TKY and MK, with the highest level of 2989.23 µg/g FDW present in TYK1 of 'Zesy002' cultivar. These results provide good evidence for the development and utilization of TYK of these cultivars in food and nutraceuticals.

Identification and quantification of free and bound phenolic compounds contained in the high-molecular weight melanoidin fractions derived from two different types of cocoa beans by UHPLC-DAD-ESI-HR-MSn.

The aim of the present study was to establish the profiles of soluble free phenolics (SFPs) and bound phenolics (BPs) in high molecular weight (HMW) melanoidin fractions isolated from raw and roasted beans of two Theobroma cacao L. varieties. Samples were prepared using three methods (saline treatment and acidic and alkaline hydrolysis) to obtain different forms of phenolic compounds. A total of fifteen phenolics, including three flavan-3-ols, seven phenolic acids, one phenolic aldehyde, and four N-phenylpropenoyl-L-amino acids (NPAs), were identified using ultra-high-performance liquid chromatography coupled to diode array detection and electrospray ionization high-resolution mass spectrometry (UHPLC-DAD-ESI-HR-MSn). In HMW fractions from both studied cocoa types, the main SFPs were N-caffeoyl-L-Asp and procyanidin B2, whereas the main BPs were catechin, epicatechin, ellagic acid, protocatechualdehyde, and N-caffeoyl-L-Asp. The concentrations of individual BPs were much higher than the content of total SFPs. It was also found that, as compared to alkaline hydrolysis, acid hydrolysis released a significantly higher amount of BPs from HMW melanoidin fractions. A comprehensive quantitative analysis indicated significant variation in the investigated phenolic compounds depending on the cocoa type and roasting conditions. An increase in treatment temperature from 110 to 150 °C led to a decline in SFPs and an increment in BPs. The HMW fractions of unroasted Criollo beans exhibited the highest content of SFPs and the lowest content of BPs. The highest BP concentrations were obtained for both cocoa bean varieties roasted at 150 °C. The present study revealed that HMW melanoidin fractions from cocoa beans of different varieties roasted at higher temperatures are a good source of phenolic compounds that can be released under both acidic and alkaline conditions.