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Summary: Herein, an ultra‐high performance liquid chromatography coupled to a diode array detector (UHPLC‐DAD) based quantification method has been developed for the simultaneous determination of 21 bioactive phenolic compounds present abundantly in food products. The developed method was validated in terms of parameters such as linearity, detection and quantification limits, intra‐day and inter‐day precision and recovery showing ideal results. Further, the developed method was applied for the quantitative analysis of phenolics in commercially procured dietary samples such as spices, green tea, black tea and dark chocolate. The major phenolics quantified in dry weight of different samples were epigallocatechin gallate (425.5 mg/10 g), epicatechin gallate (111.9 mg/10 g) in green tea; gallocatechin (286.8 mg/10 g) in dark chocolate; and naringin (93.9 mg/10 g) in star anise etc. Overall, the UHPLC‐DAD‐based method was found to be reliable, simple and specific for the estimation of phenolics in different targeted food samples. [ABSTRACT FROM AUTHOR]

This study investigates the differential browning mechanisms among various cultivars of apples. The biochemical mechanism responsible for browning activities in apples involves a group of enzymes known as polyphenol oxidases (PPO). These enzymes facilitate the reaction between polyphenolic substrates (PPS) and oxygen in the production of benzoquinones, a compound that auto-polymerizes to form melanin, the primary browning agent in apples. In this study, both the PPO and PPS were extracted from five distinct apple cultivars, namely Fuji, Red Delicious, Gold Rush, Ruby Frost, and Mutsu. To identify the types of PPO in each subspecies, the reactivity of the extracted enzyme from each cultivar was quantified in the presence of three known substrates, catechol, catechin, and chlorogenic acid using UV-vis absorption spectrophotometry. The reactivity of the PPO extract with each substrate was compared across the five apple cultivars to identify the specificity of PPO to type(s) of PPS present and to quantify the concentration of PPO present in each species. Browning activity directly affects the longevity of fruits and vegetables, which is a consistent problem in the agricultural industry. If the biochemical mechanism of browning activity is better understood, it could lead to improvements in future food production, storage, and transportation methods. [ABSTRACT FROM AUTHOR]

Nanotechnology offers promising avenues for enhancing drug delivery systems, particularly in HIV‐1 treatment. This study investigates a nanoemulsified formulation combining epigallocatechin gallate (EGCG) with dolutegravir (DTG) for managing HIV‐1 infection. The combinatorial interaction between EGCG and DTG was explored through cellular, enzymatic, and molecular studies. In vitro assays demonstrated the potential of a dual drug‐loaded nanoemulsion, NE‐DTG‐EGCG, in inhibiting HIV‐1 replication, with EGCG serving as a supplementary treatment containing DTG. In silico molecular interaction studies highlighted EGCG's multifaceted inhibitory potential against HIV‐1 integrase and reverse transcriptase enzymes. Further investigations are needed to validate the formulation's efficacy across diverse contexts. Overall, by integrating nanotechnology into drug delivery systems, this study represents a significant advancement in managing HIV‐1 infection. [ABSTRACT FROM AUTHOR]

This research presents a new, eco-friendly, and swift method combining solid-phase extraction and hydrophobic deep eutectic solvents (DES) with high-performance liquid chromatography (SPE-DES-HPLC) for extracting and quantifying catechin and epicatechin in Shanxi aged vinegar (SAV). The parameters, such as the elution solvent type, the XAD-2 macroporous resin dosage, the DES ratio, the DES volume, the adsorption time, and the desorption time, were optimized via a one-way experiment. A central composite design using the Box–Behnken methodology was employed to investigate the effects of various factors, including 17 experimental runs and the construction of three-dimensional response surface plots to identify the optimal conditions. The results show that the optimal conditions were an HDES (tetraethylammonium chloride and octanoic acid) ratio of 1:3, an XAD-2 macroporous resin dosage of 188 mg, and an adsorption time of 11 min. Under these optimal conditions, the coefficients of determination of the method were greater than or equal to 0.9917, the precision was less than 5%, and the recoveries ranged from 98.8% to 118.8%. The environmentally friendly nature of the analytical process and sample preparation was assessed via the Analytical Eco-Scale and AGREE, demonstrating that this method is a practical and eco-friendly alternative to conventional determination techniques. In summary, this innovative approach offers a solid foundation for the assessment of flavanol compounds present in SAV samples. [ABSTRACT FROM AUTHOR]

Clinicians often have to face infections caused by microorganisms that are difficult to eradicate due to their resistance and/or tolerance to antimicrobials. Among these pathogens, Pseudomonas aeruginosa causes chronic infections due to its ability to form biofilms on medical devices, skin wounds, ulcers and the lungs of patients with Cystic Fibrosis. In this scenario, the plant world represents an important reservoir of natural compounds with antimicrobial and/or antibiofilm properties. In this study, an extract from the leaves of Combretum micranthum G. Don, named Cm4-p, which was previously investigated for its antimicrobial activities, was assayed for its capacity to inhibit biofilm formation and/or to eradicate formed biofilms. The model strain P. aeruginosa PAO1 and its isogenic biofilm hyperproducer derivative B13 were treated with Cm4-p. Preliminary IR, UV-vis, NMR, and mass spectrometry analyses showed that the extract was mainly composed of catechins bearing different sugar moieties. The phytocomplex (3 g/L) inhibited the biofilm formation of both the PAO1 and B13 strains in a significant manner. In light of the obtained results, Cm4-p deserves deeper investigations of its potential in the antimicrobial field. [ABSTRACT FROM AUTHOR]

Catechins, renowned for their antioxidant properties and health benefits, are commonly present in beverages, particularly tea and wine. An efficient and cost‐effective salting‐out assisted liquid–liquid extraction (SALLE) method has been developed and validated for the simultaneous determination of six catechins and caffeine in tea and wine samples using high‐performance liquid chromatography–ultraviolet (HPLC–UV). This method demonstrates outstanding performance: linearity (1–120 µg/mL, r2 > 0.999), accuracy (96.5%–103.4% recovery), and precision (≤14.7% relative standard deviation), meeting validation requirements set by the US Food and Drug Administration. The reduced sample size (0.1 g) minimizes matrix interferences and costs without compromising sensitivity. All analytes were detected in Camellia sinensis teas, with green tea displaying the highest total catechin content (47.5–100.1 mg/mL), followed by white and black teas. Analysis of wine samples reveals the presence of catechin in all red and white wines, and epigallocatechin gallate in all red wine samples, highlighting the impact of winemaking processes on catechin content. The SALLE–HPLC–UV approach represents a green alternative by eliminating organic waste, surpassing conventional dilution methods in specificity and sensitivity for catechin determination. AGREEprep assessment emphasizes the strengths of the SALLE procedure, including material reusability, throughput efficiency, minimal sample requirements, low energy consumption, and the absence of organic waste generation. [ABSTRACT FROM AUTHOR]

Introduction: The CXCR4 chemokine receptor is a G protein-coupled receptor that plays a role in many physiological processes and diseases, such as cancer metastasis, HIV infection, and immune response. Because of this, it may be possible to target it therapeutically. In addition, the active ingredient of Phaseolus vulgaris L (PVL) has been reported to have anti-inflammatory, antioxidant, and anticancer properties. Novel CXCR4 antagonists from natural resources can be a promising drug development product using a computational approach. This study aims to explore the active compound in PVL that has the responsibility to inhibit CXCR4 using molecular docking and dynamics simulation. Materials and methods: Pharmacokinetic analysis were performed using the pkCSM, OSIRIS for toxicity risk analysis, and the PerMM for membrane permeability assessment. Molecular docking was performed using PyRx software to determine the interaction between the CXCR4 target protein from the PDB database and the active component of PVL from the PubChem database. A molecular dynamics (MD) simulation was performed to determine the stability of the interaction using the WEBGRO Macromolecular Simulations online server. The analysis were performed by comparing the results with plerixafor as a control ligand. Results and discussion: The pharmacokinetic analysis of quercetin, kaempferol, myricetin, catechin, 3,4-dihydroxybenzoic acid, and daidzin in PVL showed that they met the drug-like criteria. These chemicals were expected to have medium-risk effects on mutagenesis and tumorigenesis, with the exception of catechin, which has no risk of toxicity, and daidzin, which has high-risk effects on mutagenesis and reproduction. Molecular docking identified that quercetin (− 6.6 kcal/mol), myricetin (− 6.6 kcal/mol), catechin (− 6.5 kcal/mol), and 3,4-dihydroxybenzoic acid (− 5.4 kcal/mol) bind to CXCR4 with the highest affinity compared to plerixafor (− 5.0 kcal/mol) and can bind to the same binding pocket with key residues Asp187, Asp97, and Glu288. The MD simulation analysis showed that quercetin has a similar stability interaction compared to the control. Conclusions: Considering the pharmacokinetic analysis, molecular docking, and MD simulations, quercetin, myricetin, and 3,4-dihydroxybenzoic acid have the potential to become CXCR4 agonists with their good oral bioavailability and safety properties for the novel drug candidates. Future studies are needed to consider the molecular docking result. [ABSTRACT FROM AUTHOR]

Metabolic syndrome (MetS) is a group of abnormal disorders; hypertension, glucose intolerance, dyslipidemia, proinflammatory, and prothrombotic states, affecting approximately 14 % of the world's population. The potential of grape seeds extract (GSE) supplementation to improve the metabolic disturbances and their related conditions like obesity, type 2 diabetes, and nonalcoholic fatty liver disease was investigated in this study. In-vitro metabolic syndrome assays were investigated through α-amylase, α-glucosidase, lipase, lipoxygenase (LOX), cyclooxygenases (COX-1 and COX-2), renin and angiotensin converting enzyme (ACE) inhibition assays. Additionally, in-vivo rat model of high-fat-high-carbohydrate diet (HFD)-induced MetS was established, where metformin (MT) (200 mg/kg) was used as a reference drug and GSE was given at 100 and 200 mg/kg by oral gavage. GSE was standardized using HPLC analysis for the major reported compound; catechin which should be ≥ 160.76 ± 5.52 μg/mL. Total phenolic content of GSE was 21.12±0.61 µg gallic acid equivalent/1 mg extract and total flavonoid content was 23.81±0.64 µg rutin equivalent/1 mg extract. In-vitro assays revealed the potential of GSE to manage the metabolic syndrome, besides its strong antioxidant capacity. Treatment with GSE (100 mg/kg and 200 mg/kg) markedly (P < 0.05) controlled the weight gain, improved the metabolic pathways (total glucose, cholesterol, triglycerides, AST, and ALT), oxidative stress parameters (MDA, GSH, and catalase) and inflammatory biomarkers in HFD fed rats. GSE downregulated the expression of insulin resistance gene (IR) and some inflammatory related genes (TNF-α and NF-κB), additionally it improved the pathological features of metabolic conditions and upgraded the expression of Nrf2 compared to HFD group. The superior effects were owned to the high dose of GSE, 200 mg/kg b.wt. (P < 0.05, P < 0.001). All results sustenance the beneficial effects of the standardized GSE in the management of metabolic syndrome. [Display omitted] • Grapes (Vitis vinifera L.) as a medicine have been well known since ancient times. • Inhibition assays documented GSE in the management of the metabolic syndrome. • GSE had hypoglycemic, hypolipidemic, hepatoprotective, and anti-inflammatory. • GSE improved the pathological features of metabolic conditions. • Standardization of GSE using HPLC, catechin should be ≥ 160.76 ± 5.52 μg/mL. [ABSTRACT FROM AUTHOR]

Summary: In this study, the effect of germination in changes on total phenol, flavonoid contents, antioxidant capacity, polyphenols and biogenic elements of raw and germinated barley parts (radicle, foliole and germinated grain) was investigated. Total phenolic and flavonoid contents of raw and germinated barley parts were recorded to be between 97.61 (foliole) and 164.44 mgGAE/100 g (radicle) to 38.93 (germinated barley grain) and 371.07 mg/100 g (radicle), respectively. Antioxidant capacity results (DPPH and ABTS assays) were recorded between 3.37 (germinated barley grain) and 4.82 mmol kg−1 (radicle) to 0.79 (germinated barley grain) and 2.28 mmol kg−1 (radicle), respectively. The highest total phenol and flavonoid content as well as antioxidant capacity values were detected in radicle. Catechin and kaempferol values of raw and germinated barley parts (radicle, foliole and germinated barley grain) were recorded between 5.85 (germinated barley grain) and 19.71 mg/100 g (radicle) to 3.91 (germinated barley grain) and 4.62 mg/100 g (foliole), respectively. Gallic acid results of barley samples varied between 0.72 (germinated barley grain) and 10.95 mg/100 g (radicle). The phenolic compounds detected in the highest amounts in raw and germinated barley parts were catechin, kaempferol and gallic acid. P and K results of raw (control) and germinated barley parts were recorded to be between 727.64 (foliole) and 2078.10 mg kg−1 (control) to 955.40 (germinated barley grain) and 3982.63 mg kg−1 (control), respectively. As a micro elements, Fe and Zn results of barley samples were identified between 2.95 (foliole) and 14.30 mg kg−1 (control) to 6.26 (foliole) and 24.84 mg kg−1 (control), respectively. Significant decreases in macro and micro element contents were observed during the germination of barley grain compared to the control. [ABSTRACT FROM AUTHOR]

Camellia is an important plant genus that includes well-known species such as C. sinensis, C. oleifera, and C. japonica. The C. sinensis cultivar 'Sangmok', one of Korea's standard types of tea landraces, is a small evergreen tree or shrub. Genome annotation has shown that Korean tea plants have special and unique benefits and superior components, such as catechin. The genome of Camellia sinensis cultivar 'Sangmok' was assembled on the chromosome level, with a length of 2678.62 Mbp and GC content of 38.16%. Further, 15 chromosome-scale scaffolds comprising 82.43% of the assembly (BUSCO completeness, 94.3%) were identified. Analysis of 68,151 protein-coding genes showed an average of 5.003 exons per gene. Among 82,481 coding sequences, the majority (99.06%) were annotated by Uniprot/Swiss-Prot. Further analysis revealed that 'Sangmok' is closely related to C. sinensis, with a divergence time of 60 million years ago. A total of 3336 exclusive gene families in 'Sangmok' were revealed by gene ontology analysis to play roles in auxin transport and cellular response mechanisms. By comparing these exclusive genes with 551 similar catechin genes, 17 'Sangmok'-specific catechin genes were identified by qRT-PCR, including those involved in phytoalexin biosynthesis and related to cytochrome P450. The 'Sangmok' genome exhibited distinctive genes compared to those of related species. This comprehensive genomic investigation enhances our understanding of the genetic architecture of 'Sangmok' and its specialized functions. The findings contribute valuable insights into the evolutionary and functional aspects of this plant species. [ABSTRACT FROM AUTHOR]

Pinus massoniana needles, a traditional herb, were applied to prevent hair loss in China. Studies available mainly focused on pine needle flavonoids with various biological activities. However, there has been no pharmacokinetics study of the flavonoids from Pinus needles extract. A selective and sensitive ultra-high performance liquid chromatography–tandem mass spectrometry (UHPLC-MS/MS) method was developed to simultaneously quantify taxifolin, quercetin and catechin in rat plasma. To separate the three constituents, an Agilent Extend-C18 column (2.1 mm × 100 mm, 1.8 μm) was used with a mobile phrase of (A) 0.1% formic acid and (B) acetonitrile. The analytes were measured by multiple reaction monitoring in the negative ionization mode. There was good linearity in the established UHPLC-MS/MS method, with a coefficient of determination (r 2) of >0.99. The accuracy, intra-day and inter-day precision and recovery were all satisfactory and these 3 compounds were stable under the tested conditions. The validated method in this study was successfully applied to pharmacokinetic study in healthy rats after oral and transdermal administration of Pinus needles extract. The results could provide further research foundation for pine needle extract as external preparations. [ABSTRACT FROM AUTHOR]

This study aimed to explore the effects of different baking treatments on the quality of Yongchuan Xiuya (YCXY) green tea. It was found that a long time baking at low temperature was beneficial to keep green colour, faint scent, mellow and fresh taste quality, whereas baking under high temperature was adverse to the quality. Baking treatments slightly regulated (−)‐epigallocatechin, (−)‐epicatechin, (−)‐gallocatechin gallate, total chlorophyll and carotenoid. As the baking temperature rose, the content of tea polyphenols, gallic acid, catechins, caffeine, soluble sugar and polyphenols/amino acids ratio obviously decreased. A total of 40 kinds of volatiles were detected in these six tea samples. A model for aroma type discrimination was successfully established based on partial least squares‐discriminant analysis (PLS‐DA). Ten kinds of volatile substances were the key characteristic markers for the faint scent, chestnut aroma and high‐fired aroma types of YCXY green tea. 1‐hexanol, hotrienol and dimethyl sulfide were furtherly used to discriminant aroma type based on Fisher discriminant analysis (FDA). [ABSTRACT FROM AUTHOR]

Purpose: Accumulation of ammonia causes central and peripheral fatigue. This study aimed to investigate the synergistic effect of tea catechins and low-dose ornithine in activating the urea cycle to reduce blood ammonia levels during exercise. Methods: We used hepatocyte-like cells derived from human-induced pluripotent stem (iPS) cells to assess the effect of tea catechins combined with ornithine on urea cycle activity. The urea production and expression of key genes involved in the metabolism of urea were investigated. We then examined the synergistic improvement in ammonia metabolism by tea catechins in combination with ornithine in a human pilot study. Results: Tea catechins combined with ornithine increased urea cycle activity in hepatocyte-like cells derived from human iPS cells. Intake of 538.6 mg of tea catechins with 1592 mg of ornithine for 2 consecutive days during exercise loading suppressed the exercise-induced increase in the blood ammonia concentration as well as stabilized blood glucose levels. Conclusion: Controlling the levels of ammonia, a toxic waste produced in the body, is important in a variety of situations, including exercise. The present study suggests that a heterogeneous combination of polyphenols and amino acids efficiently suppresses elevated ammonia during exercise in humans by a mechanism that includes urea cycle activation. Trial registration: This study was registered in the University Hospital Medical Information Network Clinical Trial Registry (No. UMIN000035484, dated January 8, 2019). [ABSTRACT FROM AUTHOR]

Background: Soil-transmitted helminths (STH) infect more than a quarter of the world's human population. In the absence of vaccines for most animal and human gastrointestinal nematodes (GIN), treatment of infections primarily relies on anthelmintic drugs, while resistance is a growing threat. Therefore, there is a need to find alternatives to current anthelmintic drugs, especially those with novel modes of action. The present work aimed to study the composition and anthelmintic activity of Combretum mucronatum leaf extract (CMLE) by phytochemical analysis and larval migration inhibition assays, respectively. Methods: Combretum mucronatum leaves were defatted with petroleum ether and the residue was extracted by ethanol/water (1/1) followed by freeze-drying. The proanthocyanidins and flavonoids were characterized by thin layer chromatography (TLC) and ultra-high performance liquid chromatography (UPLC). To evaluate the inhibitory activity of this extract, larval migration assays with STH and GIN were performed. For this purpose, infective larvae of the helminths were, if necessary, exsheathed (Ancylostoma caninum, GIN) and incubated with different concentrations of CMLE. Results: CMLE was found to be rich in flavonoids and proanthocyanidins; catechin and epicatechin were therefore quantified for standardization of the extract. Data indicate that CMLE had a significant effect on larval migration. The effect was dose-dependent and higher concentrations (1000 µg/mL) exerted significantly higher larvicidal effect (P < 0.001) compared with the negative control (1% dimethyl sulfoxide, DMSO) and lower concentrations (≤ 100 µg/ml). Infective larvae of Ascaris suum [half-maximal inhibitory concentration (IC50) = 5.5 µg/mL], Trichuris suis (IC50 = 7.4 µg/mL), and A. caninum (IC50 = 18.9 µg/mL) were more sensitive to CMLE than that of Toxocara canis (IC50 = 310.0 µg/mL), while infective larvae of Toxocara cati were largely unaffected (IC50 > 1000 µg/mL). Likewise, CMLE was active against most infective larvae of soil-transmitted ruminant GIN, except for Cooperia punctata. Trichostrongylus colubriformis was most sensitive to CMLE (IC50 = 2.1 µg/mL) followed by Cooperia oncophora (IC50 = 27.6 µg/mL), Ostertagia ostertagi (IC50 = 48.5 µg/mL), Trichostrongylus axei (IC50 = 54.7 µg/mL), Haemonchus contortus (IC50 = 145.6 µg/mL), and Cooperia curticei (IC50 = 156.6 µg/mL). Conclusions: These results indicate that CMLE exhibits promising anthelmintic properties against infective larvae of a large variety of soil-transmitted nematodes. [ABSTRACT FROM AUTHOR]

Purpose: Green tea is a widely consumed beverage. A recent clinical study reported green tea decreased systemic exposure of raloxifene and its glucuronide metabolites by 34–43%. However, the underlying mechanism(s) remains unknown. This study investigated a change in raloxifene's solubility as the responsible mechanism. Methods: The effects of green tea extract, (–)-epigallocatechin gallate (EGCG), and (–)-epigallocatechin (EGC) on raloxifene's solubility were assessed in fasted state simulated intestinal fluids (FaSSIF) and fed state simulated intestinal fluids (FeSSIF). EGCG and EGC represent green tea's main bioactive constituents, flavan-3-gallate and flavan-3-ol catechins respectively, and the tested concentrations (mM) match the µg/mg of each compound in the extract. Our mouse study (n = 5/time point) evaluated the effect of green tea extract and EGCG on the systemic exposure of raloxifene. Results: EGCG (1 mM) and EGC (1.27 mM) decreased raloxifene's solubility in FaSSIF by 78% and 13%, respectively. Micelle size in FaSSIF increased with increasing EGCG concentrations (> 1000% at 1 mM), whereas EGC (1.27 mM) did not change micelle size. We observed 3.4-fold higher raloxifene solubility in FeSSIF compared to FaSSIF, and neither green tea extract nor EGCG significantly affected raloxifene solubility or micelle size in FeSSIF. The mice study showed that green tea extract significantly decreased raloxifene Cmax by 44%, whereas EGCG had no effect. Green tea extract and EGCG did not affect the AUC0-24 h of raloxifene or the metabolite-to-parent AUC ratio. Conclusions: This study demonstrated flavan-3-gallate catechins may decrease solubility of poorly water-soluble drugs such as raloxifene, particularly in the fasted state. [ABSTRACT FROM AUTHOR]

An antifungal coating of zein nanofibers with jackfruit leaf extract was successfully elaborated by electrospinning. The nanofibers were characterized based on thickness, tensile test, water vapor permeability, water solubility, differential scanning calorimetry, thermogravimetric analysis, scanning electron microscopy, and presumptive identification of some compounds in the extract and fibers with extract by HPLC-Masses. The average diameter of the pure nanofibers was 305 nm and for the nanofibers with extract was 731 nm. An encapsulation efficiency of 72% was obtained. FTIR results demonstrated that the jackfruit leaf extract was successfully encapsulated in the zein fibers and did not show strong chemical interactions with the extract. The TGA analysis showed that the zein fibers offered thermoprotection to the compounds in the extract. Inhibition of mycelial growth and spore germination of jackfruit leaf extract against Cladosporium tenuissimum and Aspergillus sydowii in vitro showed good results which were attributed to the antimicrobial activity of some phenolic compounds in the extract such as caffeic acid, kaempferol 3–O– rutinoside, and catechin. The preventive and curative treatments evaluated with the application of the nanofibers showed a decrease in the severity and incidence in the infected Averrhoa carambola L. fruits. The results indicate the encapsulation of the jackfruit leaf extract, as well as the thermoprotection and release of antimicrobial compounds from this matrix. [ABSTRACT FROM AUTHOR]

Environmentally benign aqueous biphasic separation (ABS) methods for separation of no-carrier added (NCA) 90Nb and 89Zr from alpha particle irradiated natY target have been developed using nature resourced chemical, catechins, which is the most abundant polyphenol in green tea. 90Nb was preferentially extracted in the catechins-PEG 6000 phase with a separation factor of 1.04 × 103 where the salt phase was NaHSO3. Similarly, 89Zr was also preferentially extracted in the catechins-PEG 6000 phase with a separation factor of 1.92 × 104, where the salt phase was Na2SO4. [ABSTRACT FROM AUTHOR]

Background: Annual production of areca nut in Karnataka state exceeds 1.08 million tonnes, contributing 80% and 49% to Indian and global production, respectively. Areca nut (pericarp of Areca catechu L.) is found to be a rich source of valuable phenolic compounds. Total phenolic content (TPC) and total flavonoid content (TFC) were estimated in 21 unripe areca nut samples collected from the major areca nut growing regions of Karnataka state. Arecoline, a prominent alkaloid present in areca nut was estimated and phenolic profile of one areca nut sample was generated using UHPLC–MS/MS studies. Results: A significant variability was found in TPC, TFC and arecoline content among the samples, belongs to different agroclimatic zones. Flavonoids were found to be the major phenolic compounds present in these unripe areca nut samples. The median values of TPC, TFC and arecoline were found to be 99.609 ± 0.002 mg gallic acid equivalent, 78.86 ± 0.007 mg catechin equivalent and 2.17 ± 0.13 mg/g of the sample on fresh weight basis. A positive correlation was found to exist between TPC and arecoline content in the green unripe areca nuts of 6–7 months' maturity. Through UHPLC–MS/MS studies, 61 prominent compounds have been identified. Conclusion: The TPC and TFC of areca nuts collected from different districts of Karnataka falling in various agroclimatic zones varied significantly. In general, the arecoline content found in all these samples was less than that reported elsewhere, and the variability among the samples was also found to be minimal. A positive correlation was observed between TPC and arecoline. UHPLC–MS/MS studies showed the presence of about 52 unique phenolic compounds. [ABSTRACT FROM AUTHOR]

Summary: This study aimed to evaluate the convective drying of a by‐product obtained by hydrodistillation of Pfaffia glomerata roots (PGB) and investigate the utilisation of the resulting powder in the preparation of cereal bars. Drying at 80 °C for 120 min was the selected condition for PGB due to the higher levels of phenolic acids (gallic, coumaric and ferulic) catechin and higher antioxidant activity than drying at 60 °C for 180 min, and, better technological properties and higher β‐ecdysone content than drying at 100 °C for 100 min. There was an increase in fibre content (110%), antioxidant compounds (97%) and compressive strength (377%) and a decrease in lipid content (31%) when the PGB content of cereal bars was increased from 0% to 9%. Colour parameters, purchase intention and most sensory parameters were similar among cereal bar formulations, indicating that PGB is a promising ingredient for the nutritional enrichment of cereal bars. [ABSTRACT FROM AUTHOR]

In order to obtain the quality information of Taishan black tea and provide data support for the establishment of assessment criteria for quality control of Taishan black tea, in this study, 45 samples of Taishan black tea were collected during the summer to investigate their quality characteristics. The results showed that the Taishan black tea typically exhibited a dark-brown, curly appearance and a uniform texture. The tea soup displayed a bright orange-red color. The tea was mainly described as having a fruity aroma, followed by a caramel flavor, sweet aroma, flowery flavor, and clean aroma, with a strong and enduring fragrance. The taste profile was mostly heavy and mellow or heavy and strong, with fewer samples exhibiting slight bitterness and astringency. The tea leaves were characterized by a reddish-auburn color, a soft texture, and an even appearance. The main biochemical components of the Taishan black tea fell within the following ranges: water extracts (38.65–43.35%), free amino acids (1.41–3.45%), tea polyphenols (9.80–15.05%), catechins (6.11–9.03%), and caffeine (1.65–3.05%). The phenolic acid/amino acid ratio was 2.31–6.65%. Catechins and tea polyphenols emerged as critical indicators influencing taste quality, followed by amino acids, water extracts, and caffeine. The aroma analysis identified common compounds, such as 3-methyl-butanal, 2-methyl-butanal, decanal, 2-methyl-propanal, 1-octen-3-ol, and β-ionone, in most samples. These compounds exhibited relatively high contents and high odor activity values, making them the primary contributors to the tea's aroma. This investigation into the quality of Taishan black tea offers valuable scientific insights, providing a foundation for the standardization of Taishan black tea's quality. [ABSTRACT FROM AUTHOR]

Tea is an important cash crop that is often consumed by chewing pests, resulting in reduced yields and economic losses. It is important to establish a method to quickly identify the degree of damage to tea plants caused by leaf‐eating insects and screen green control compounds. This study was performed through the combination of deep learning and targeted metabolomics, in vitro feeding experiment, enzymic analysis and transient genetic transformation. A small target damage detection model based on YOLOv5 with Transformer Prediction Head (TPH‐YOLOv5) algorithm for the tea canopy level was established. Orthogonal partial least squares (OPLS) was used to analyze the correlation between the degree of damage and the phenolic metabolites. A potential defensive compound, (‐)‐epicatechin‐3‐O‐caffeoate (EC‐CA), was screened. In vitro feeding experiments showed that compared with EC and epicatechin gallate, Ectropis grisescens exhibited more significant antifeeding against EC‐CA. In vitro enzymatic experiments showed that the hydroxycinnamoyl transferase (CsHCTs) recombinant protein has substrate promiscuity and can catalyze the synthesis of EC‐CA. Transient overexpression of CsHCTs in tea leaves effectively reduced the degree of damage to tea leaves. This study provides important reference values and application prospects for the effective monitoring of pests in tea gardens and screening of green chemical control substances. Summary statement: Based on deep learning and targeted metabolomics, a model was established and (‐)‐epicatechin‐3‐O‐caffeoate (EC‐CA) was screened to have the function of defense against chewing pests, and hydroxycinnamoyl transferase (HCT) was identified as a substrate promiscuity that could efficiently catalyze the synthesis of EC‐CA. [ABSTRACT FROM AUTHOR]

This study aimed to reduce the bitterness and astringency properties of autumn green tea using different yellowing and drying treatments. The results showed that as the yellowing temperature increased, the contents of tea polyphenols, gallated catechins, flavonol glycosides, and bitter amino acids decreased, while the content of soluble sugar and flavonols increased. The tea sample (YEL35 °C) subjected to yellowing treatment at 35 °C exhibited weak bitterness and astringency intensities and a relatively low content of flavonol glycosides. As the drying temperature increased, the content of gallated catechins decreased. In addition, the tea sample (DRY75 °C) subjected to drying treatment at 75 °C exhibited weak bitterness and astringency intensities, the highest contents of umami amino acids and Thea, and a relatively low content of gallated catechins. Multivariate statistical analysis revealed that vitexin-2-O-rhamnoside, pferol-3-O-rutinoside, myricetin-3-O-galactoside, and quercetin-3-O-glucoside played an important role in the astringency property of the tea. In addition, Asn, Thr, Pro, and Met were positively correlated with umami. Hence, the quality of autumn green tea was improved under optimal yellowing and drying temperatures of 35 and 75 °C, respectively. [ABSTRACT FROM AUTHOR]

Nanovesicles produced with lipids and polymers are promising devices for drug and bioactive delivery and are of great interest in pharmaceutical applications. These nanovesicles can be engineered for improvement in bioavailability, patient compliance or to provide modified release or enhanced delivery. However, their applicability strongly depends on the safety and low immunogenicity of the components. Despite this, the use of unsaturated lipids in nanovesicles, which degrade following oxidation processes during storage and especially during the proper routes of administration in the human body, may yield toxic degradation products. In this study, we used a biopolymer (chitosan) labeled with flavonoid (catechin) as a component over a lipid bilayer for micro- and nanovesicles and characterized the structure of these vesicles in oxidation media. The purpose of this was to evaluate the in situ effect of the antioxidant in three different vesicular systems of medium, low and high membrane curvature. Liposomes and giant vesicles were produced with the phospholipids DOPC and POPC, and crystalline cubic phase with monoolein/DOPC. Concentrations of chitosan–catechin (CHCa) were included in all the vesicles and they were challenged in oxidant media. The cytotoxicity analysis using the MTT assay (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide) revealed that concentrations of CHCa below 6.67 µM are non-toxic to HeLa cells. The size and zeta potential of the liposomes evidenced the degradation of their structures, which was minimized by CHCa. Similarly, the membrane of the giant vesicle, which rapidly deteriorated in oxidative solution, was protected in the presence of CHCa. The production of a lipid/CHCa composite cubic phase revealed a specific cubic topology in small-angle X-ray scattering, which was preserved in strong oxidative media. This study demonstrates the specific physicochemical characteristics introduced in the vesicular systems related to the antioxidant CHCa biopolymer, representing a platform for the improvement of composite nanovesicle applicability. [ABSTRACT FROM AUTHOR]

Glutathione transferase Pi (GSTP1) expression is increased in many cancer types and is associated with multidrug resistance and apoptosis inhibition. Inhibitors of GSTP1-1 have the potential to overcome drug resistance and improve chemotherapy efficacy as adjuvant agents. This study investigated the effects of catechin and gossypol on human glutathione transferase Pi (GSTP1-1) activity and their cytotoxic effects on breast cancer cells (MCF-7) individually and in combination with tamoxifen (TAM). Gossypol effectively inhibited the enzyme with an IC50 value of 40 μM, compared to 200 μM for catechin. Gossypol showed stronger inhibition of GSTP1-1 activity (Ki = 63.3 ± 17.5 μM) compared to catechin (Ki = 220 ± 44 μM). Molecular docking analysis revealed their binding conformations to GSTP1-1, with gossypol binding at the subunit interface in an un-competitive manner and catechin showing mixed non-competitive inhibition. Gossypol had severe cytotoxic effects on both MCF-7 cells and normal BJ1 cells, while catechin had a weak cytotoxic effect on MCF-7 cells only. Combination therapy with TAM resulted in cytotoxicity of 27.3% and 35.2% when combined with catechin and gossypol, respectively. Gossypol showed higher toxicity to MCF-7 cells, but its strong effects on normal cells raised concerns about selectivity and potential side effects. [ABSTRACT FROM AUTHOR]

This study delves into the comprehensive evaluation of phytochemicals extracted from Anvillea radiata, with a focus on their potential anti-inflammatory applications. High-performance liquid Chromatography analysis reveals the dominance of catechin in the aqueous extract, alongside other compounds such as syringic acid, 3,4-dihydroxybenzoic acid, and vanillic acid, as well as quercetin-3-β-D-glucoside and rutin in smaller quantities. An in vitro anti-inflammatory assay demonstrates the superior effectiveness of A. radiata aqueous extract at lower concentrations compared to Aspirin, raising possibilities for reduced side effects and enhanced cost-effectiveness. Drug-likeness predictions emphasize the potential of catechin, syringic acid, and vanillic acid for drug development due to their molecular characteristics. Toxicity risk assessment indicates that catechin, quercetin-3-β-D-glucoside, and rutin exhibit low toxicity risks and favorable drug-likeness properties. Molecular docking analysis highlights promising interactions between the identified compounds and crucial anti-inflammatory (COX-2, MPO, IL1β, IL6, and TNFα.) target proteins. Notably, catechin demonstrates a strong binding affinity to these proteins. Molecular dynamics simulations further support catechin's potential, revealing significant deformability in complexes with COX-2 and MPO, indicating high structural flexibility. The variance map shows higher cumulative variances and the elastic network map yields satisfactory outcomes, further reinforcing the potential of A. radiata aqueous extract compounds, with catechin as a standout candidate for anti-inflammatory drug development. [ABSTRACT FROM AUTHOR]

Traditional textile dyeing uses chemical pigments and dyes, which consumes a large amount of water and causes serious environmental pollution. Structural color is an essential means of achieving green dyeing of textiles, and thin-film interference is one of the principles of structural coloring. In the assembly of structural color films, it is necessary to introduce dark materials to suppress light scattering and improve the brightness of the fabric. In this study, the conditions for the generation of nanofilms of catechin (CC) at the gas–liquid interface were successfully investigated. At the same time, environmentally friendly colored silk fabrics were novelly prepared using polycatechin (PCC) structural color films. In addition, it was found that various structural colors were obtained on the surface of silk fabrics by adjusting the time. Meanwhile, the color fastness of the structural colored fabrics was improved by introducing polyvinylpyrrolidone (PVP) to form a strong hydrogen bond between the fabric and catechin. PCC film is uniform and smooth, with a special double-layer structure, and can be attached to the surface of silk fabrics, giving the fabrics special structural colors. Through the thin-film interference formed between the visible light and the PCC film, the silk fabrics obtain bright, controllable, and uniform structural colors. This method is easy to operate and provides a new way of thinking for environmental-protection-oriented coloring of fabrics. [ABSTRACT FROM AUTHOR]

ZrO2 is considered an important semiconductor and a heterogeneous photocatalyst along with its diversified applications in dentistry and ceramics. In the present study, ZrO2 nanostructures were synthesized by hydrothermal treatment accompanied by calcination at different temperatures, viz. 300–800 °C, using zirconyl chloride octahydrate as a precursor, and pure phytochemical- catechin hydrate as a stabilizing agent. Significant variations in the optical properties viz. absorption spectra, and band gap; and structural properties viz. average particle, and crystallite size of ZrO2 nanostructures were observed due to variable calcination temperatures. The diffraction studies showed that crystallinity appeared in samples synthesized at or above 400 °C. The lowest average crystallite sizes of ~8.96 nm and ~14.5 nm were obtained for the ZrO2 synthesized at calcination temperatures of 400 and 500 °C, respectively. The obtained XRD data of ZrO2 nanostructures were further studied by Rietveld refinement using various space groups viz., Fm-3 m for cubic, P121/c1 for monoclinic, and P42/nmc for tetragonal phases. The refinement illustrated the development of the monoclinic phase of ZrO2 in major composition, for the samples synthesized at or above 400 °C, with preferred orientations along (011), (111), and (1̅11). Furthermore, the HRTEM data showed the formation of the spherical particles with average particle sizes of ~ 47 nm and ~26 nm, prepared at 500 and 600 °C, respectively. Theoretical studies were also carried out to get a mechanistic understanding of the procedure followed in the synthesis and stability of the zirconia nanoparticles. The prepared ZrO2 nanostructures were further investigated for their photodegradable capability of tetracycline hydrochloride (TCH) under visible light irradiation. Among all the prepared materials, ZrO2 prepared at 500 °C exhibited a higher photo-degradation efficiency at 180 min under visible light irradiation. [ABSTRACT FROM AUTHOR]

BACKGROUND: Type 2 Diabetes Mellitus (T2DM) is among the most frequent chronic diseases in virtually all countries, posing a global health threat. Therefore, Preventive interventions are critical for reducing the enormous burden of diabetes. Flavanols may assist people with metabolic disorders to maintain glucose homeostasis by inhibiting digestive enzymes and glucose transporters. Green Tea (GT) and cocoa have gotten much attention since their flavanols are high. OBJECTIVES: To investigate the effects of polyphenols from GT and cocoa (>4 weeks) on reducing the incidence of complications and improving glycaemic control and insulin sensitivity in adult patients with T2DM through outcomes Fasting Blood Glucose (FBG), Fasting Blood Insulin (FBI), Haemoglobin A1c (HbA1c) and Homeostatic Model Assessment of Insulin Resistance (HOMA-IR). METHODOLOGY: An electronic research programme was applied, using different databases (including Web of Science, PubMed/Medline, Scopus, and Cochrane Reviews) to find studies that have evaluated the impact of polyphenols from GT and cocoa on reducing the incidence of complications and improving glycaemic control and insulin sensitivity in adult patients with T2DM. Articles published between 2005 and 2021 in English were selected. RESULTS: 15 and 7 studies involved 738 participants on GT (348 male/390 female). In contrast, the ones focused on cocoa had 331 participants (83 male/ 248 female) with T2DM aged 18–65 years, and a BMI range of 25–34.9 kg/m2 was identified and included in the present review. 43 and 27% of studies were low-risk bias in cocoa and GT, respectively. The results of the meta-analysis showed no significant difference in FBG levels following GT and cocoa consumption compared to the control group (SMD: –0.08; 95% CI: –0.43 to 0.28; P = 0.68 and SMD: –0.65; 95% CI, –1.40 to 0.10; P = 0.09, respectively). Also, the results showed no significant difference for GT and cocoa intervention (SMD: 0.18; 95% CI: –0.27 to 0.64; P = 0.43 and SMD: –0.80; 95% CI: –1.92 to 0.31; P = 0.16, respectively). In addition, the results of the HbA1c analysis showed no significant reduction after GT and cocoa consumption (SMD: –0.41; 95% CI: –0.85 to 0.03; P = 0.07 and SMD, –0.37; 95% CI, –0.77 to 0.04; P = 0.08, respectively). There was no evidence that GT and cocoa interventions effectively improved HOMA-IR (SMD: 0.02; 95% CI: –0.16 to 0.20; P = 0.80 and SMD, –1.65; 95% CI, –3.77 to 0.46; P = 0.13, respectively CONCLUSION: The evidence shows that the short-term administration of cocoa and GT did not significantly reduce the FBG, FBI, HbA1c, and HOMA-IR levels in adult patients with T2DM. [ABSTRACT FROM AUTHOR]

With the aggravating aging of modern society, the sarcopenia-based aging syndrome poses a serious potential threat to the health of the elderly. Natural dietary supplements show great potential to reduce muscle wasting and enhance muscle performance. Tea has been widely recognized for its health-promoting effects. which contains active ingredients such as tea polyphenols, tea pigments, tea polysaccharides, theanine, caffeine, and vitamins. In different tea production processes, the oxidative condensation and microbial transformation of catechins and other natural substances from tea promotes the production of various tea pigments, including theaflavins (TFs), thearubigins (TRs), and theabrownins (TBs). Tea pigments have shown a positive effect on maintaining muscle health. Nevertheless, the relationship between tea pigments and skeletal muscle function has not been comprehensively elucidated. In addition, the numerous research on the extraction and purification of tea pigments is disordered with the limited recent progress due to the complexity of species and molecular structure. In this review, we sort out the strategies for the separation of tea pigments, and discuss the structures of tea pigments. On this basis, the regulation mechanisms of tea pigments on muscle functional were emphasized. This review highlights the current understanding on the extraction methods, molecular structures and regulation mechanisms of muscle function of tea pigments. Furthermore, main limitations and future perspectives are proposed to provide new insights into broadening theoretical research and industrial applications of tea pigments in the future. The extraction and isolation methods of tea pigments are detailedly introduced. The structural research progress of tea pigments are summarized. The effects of tea pigments in the prevention of muscle diseases are introduced. The mechanism of tea pigments in enhancing skeletal muscle function are proposed. [ABSTRACT FROM AUTHOR]

Environmentally benign aqueous biphasic separation (ABS) techniques have been developed to separate no‐carrier added (NCA) 71,72As from 46 MeV α‐particles irradiated gallium oxide target. Catechins were isolated from green tea leaves as a nature resourced chemical. Efficacy of catechins on aqueous biphasic separation of NCA 71,72As from bulk gallium was studied at best conditions and found that catechin acted as synergistic agent in the ABS system. Bulk gallium was preferentially extracted into the PEG+ catechins phase (wherein 2 M Na‐malonate was used as salt‐rich phase) with a separation factor of 2.06×103 leaving 71,72As in the salt rich phase. At this condition, 90 % 71,72As was retained in the salt rich phase with bulk gallium contamination less than 0.5 %. [ABSTRACT FROM AUTHOR]

The meticulous harvesting process and appropriate post-harvest techniques play pivotal roles in preserving the quality and health benefits of white tea. This careful approach maintains the bioactive compounds such as polyphenols, caffeine, gallic acid, Epigallocationchin (EGC), Epigallocationchin gallate (EGCG), and Epicatechin gallate (ECG), integral to white tea's health benefits. The stability of catechin content in tea plants is greatly influenced by the environment (clone, plant age, leaf age, altitude, temperature, humidity, processing, and pH when storing dry tea). In Indonesia, the raw materials used to produce white tea are mostly pecco from the superior GMB clone Assamica variety which has high polyphenol content (14.83 - 15.43% dry weight). To increase polyphenol levels, the treatment that needs to be considered is the provision of optimum and appropriate fertilizer. The highest catechin content comes from plucking in summer and spring season. Subsequently, controlled post-harvest processes, including controlled withering and drying, safeguard the integrity of active compounds like catechins as antioxidants in white tea, mitigating free radicals and cellular damage. The highest antioxidant showed from 23 hours whithered. The storage time for white tea also has an impact on quality. The content of catechins and amino acids showed a tendency to decrease with storage time. On the other hand, gallic acid increases with the length of storage. The combined effect of these phases, from harvesting through post-harvesting, contributes significantly to white tea's health benefits, encompassing cardioprotective effects, anti-diabetic potential, prevention of anticarcinogenic and antimutagenic activity, neuroprotective properties, and antimicrobial attributes. [ABSTRACT FROM AUTHOR]

Background: Acne is a prevalent skin health problem experienced by teenagers and adults. Green tea is one of the plants that can be used to treat acne. Green tea dregs contain catechins, which have antibacterial activity that causes acne. Objective: This study aims to determine the antibacterial activity of green tea dregs extract against Cutibacterium acnes bacteria. Methods: This study used two brewing time variations and three green tea dregs with maceration variations. The obtained extract was then analyzed for its catechin content using the total phenolic test. Section, which has a high phenolic content, was then tested for its activity against Cutibacterium acnes bacteria using the microdilution method to obtain the MIC50 value. The extract with a brewing time of 2 minutes and the ultrasonic-assisted extraction maceration method had the highest MIC50 value of 8.586 mg/mL. The MIC50 value references extract concentrations used in acne spot cream formulations. The cream obtained after the stability test is semisolid, brown, and smells like tea. Spot cream is also homogeneous and meets the pH range in cosmetic preparations of 5.5. However, the viscosity of spot cream decreased significantly after storage to 4546 cPoise from 8106 cPoise. The decrease in the viscosity of the cream was caused by the catechin content in green tea dregs extract, which is acidic, thus reducing the effectiveness of the emulator in the form of triethanolamine, which is alkaline. The decrease in viscosity of the cream also caused the spreadability of the cream to increase and the stickiness of the cream to decrease. [ABSTRACT FROM AUTHOR]

Natural α-glucosidase inhibitors from plant-based foods such as catechins offer an attractive strategy for their potential anti-diabetic effects. In this study, infusions of three different tea types (green, white, and oolong) were investigated for their total phenolic (TPC) and catechins (EGCG, ECG, EGC, and EC) content, and for their α-glucosidase inhibitory activities. We observed that the level of TPC in white tea was significantly higher compared to oolong and green tea, which suggests higher content of EGCG and ECG catechins in fresh young leaves. Our findings showed that the higher content of such catechins in the infusion of white tea well correlated with a strong inhibition of α-glucosidase, and such inhibition was demonstrated to be more effective than the FDA-approved drug acarbose. Then, we computationally explored the molecular requirements for enzyme inhibition, especially for the most active catechins EGCG and ECG, as well as their disposition/stability within the active site. [ABSTRACT FROM AUTHOR]

Diabetes contributes to the rising global death rate. Despite scientific advancements in understanding and managing diabetes, no single therapeutic agent has been identified to effectively treat and prevent its progression. Consequently, the exploration for new antidiabetic therapeutics continues. This study aimed to investigate the antidiabetic bioactive ethyl acetate fraction of F. lutea at the molecular level to understand the molecular interactions and ligand-protein binding. To do this, the fraction underwent column chromatography fractionation to yield five compounds: lupeol, stigmasterol, α-amyrin acetate, epicatechin, and epiafzelechin. These compounds were evaluated in vitro through α-glucosidase inhibition and glucose utilization assays in C2C12 muscle and H-4-11-E liver cells using standard methods. In silico analysis was conducted using molecular docking and ADMET studies. Epicatechin exhibited the most potent α-glucosidase inhibition (IC50 = 5.72 ± 2.7 µg/mL), while epiafzelechin stimulated superior glucose utilization in C2C12 muscle cells (33.35 ± 1.8%) and H-4-11-E liver cells (46.7 ± 1.2%) at a concentration of 250 µg/mL. The binding energies of the isolated compounds for glycogen phosphorylase (1NOI) and α-amylase (1OSE) were stronger (<−8.1) than those of the positive controls. Overall, all tested compounds exhibited characteristics indicative of their potential as antidiabetic agents; however, toxicity profiling predicted epiafzelechin and epicatechin as better alternatives. The ethyl acetate fraction and its compounds, particularly epiafzelechin, showed promise as antidiabetic agents. However, further comprehensive studies are necessary to validate these findings. [ABSTRACT FROM AUTHOR]

Enterobacter sakazakii is a food-borne bacterium that causes diseases as diverse as necrotizing enteritis, meningitis and infantile sepsis. Catechin is a kind of natural polyphenol products existing in tea and other natural plants, which has good antibacterial activity. In this study, laser confocal scanning microscopy and field emission scanning electron microscopy observations showed that the cell membrane of E. sakazakii was damaged after the action of catechin, and the cell surface adhered and pitted with holes. Under 1 MIC concentration, E. sakazakii membrane potential increased by 24.79%, intracellular reactive oxygen species increased by 4.72 times, intracellular ATP decreased by 4.93 times, and intracellular pH decreased by 45.63%. These results indicate that catechin can achieve antibacterial effect by disrupting cell membrane integrity and changing cell membrane permeability. This study lays a theoretical foundation for the application of catechin as a natural antibacterial agent. [ABSTRACT FROM AUTHOR]

The aim of our study was to investigate the potential of rutin, catechin, dehydrozingerone, naringenin, and quercetin, both alone and in combination with temozolomide, to inhibit the expression of O6-methylguanine-DNA methyltransferase (MGMT) in glioma cells. MGMT has been shown to be a major cause of temozolomide resistance in glioma. Our study used both in silico and in vitro methods to assess the inhibitory activity of these phytochemicals on MGMT, with the goal of identifying the most effective combination of compounds for reducing temozolomide resistance. After conducting an initial in silico screening of natural compounds against MGMT protein, five phytochemicals were chosen based on their high docking scores and favorable binding energies. From the molecular docking and simulation studies, we found that quercetin showed a good inhibitory effect of MGMT with its high binding affinity. C6 glioma cells showed increased cytotoxicity when treated with the temozolomide and quercetin combination. It was understood from the isobologram and combination index plot that the drug combination showed a synergistic effect at the lowest dose. Quercetin when combined with temozolomide significantly decreased the MGMT levels in C6 cells in comparison with the other drugs as estimated by ELISA. The percentage of apoptotic cells increased significantly in the temozolomide–quercetin group indicating the potency of quercetin in decreasing the resistance of temozolomide as confirmed by acridine orange/ethidium bromide staining. Our experiment hence suggests that temozolomide resistance can be reduced by combining the drug with quercetin which will serve as an effective therapeutic target for glioblastoma treatment. [ABSTRACT FROM AUTHOR]

In the process of adapting to the environment, tea plants (Camellia sinensis) endow tea with unique flavor and health functions, which should be attributed to secondary metabolites, including catechins, L-theanine, caffeine and terpene volatiles. Since the content of these flavor-contributing metabolites are mainly determined by the growth of tea plant, it is very important to understand their alteration and regulation mechanisms. In the present work, we first summarize the distribution, change characteristics of the main flavor-contributing metabolites in different cultivars, organs and under environmental stresses of tea plant. Subsequently, we discuss the regulating mechanisms involved in the biosynthesis of these metabolites based on the existing evidence. Finally, we propose the remarks and perspectives on the future study relating flavor-contributing metabolites. This review would contribute to the acceleration of research on the characteristic secondary metabolites and the breeding programs in tea plants. [ABSTRACT FROM AUTHOR]

Borrasus flabellifer L. is a plant in the Arecaceae (Palmae) family with numerous bioactivities such as diuretic promotion, antioxidant, and antimicrobial effects. In this study, we are interested in the phytochemical compounds present in B. flabellifer L. male flowers. We investigated the effects of plant stage and solvent used for extraction. Initially, both the young and mature male flowers of this plant were extracted using water or ethanol. Several standard compounds, including gallic acid, catechin, caffeic acid, and quercetin, were utilized to screen the phytochemicals in these plant flowers. After analyzing the samples using High-Performance Liquid Chromatography (HPLC) method, only catechin was detected in all extracts, while the others were not detected (did not match the peak spectrum pattern compared with standard). Using a detection wavelength and curve parameters with an R² value of 0.9999, catechin detection via HPLC was performed at 280 nm within the range of 13.12 to 210.00 μg/mL detection. Regarding the stage of the male flower, the young ones extracted with water provided the highest catechin content at 6.65 μg/mg extract, while the others fell within the range of 4.02 to 4.44 μg/mg extract. Therefore, it has been confirmed that catechin can be found in B. flabellifer L., and water should be used as the solvent for extraction for further applications of this plant. [ABSTRACT FROM AUTHOR]

Summary: Total carotenoid results of fresh and processed purslane samples were recorded between 4.21 (fermented) and 107.40 μg/g) (microwave). Total phenol and flavonoid amounts of purslane were reported to be between 25.21 (fermented) and 143.02 mg GAE/100 g (microwave) to 44.14 (fermented) and 810.48 mg/100 g (microwave), respectively. Antioxidant activity results of fresh and purslane plants were reported between 1.18 (fermented) and 1.54 mmol/kg (DPPH) (fresh and boiled) to 1.43 (fermented) and 13.25 mg/g (FRAP) (oven), respectively. Catechin and rutin results of purslane samples were recorded to be between 0.81 (boiled) and 35.33 mg/100 g (microwave) to 0.14 (fermented) and 21.45 mg/100 g (air dried), respectively. The most abundant element in the purslane samples was K, followed in descending order by Ca, Mg, P and S. Calcium (Ca) and magnesium (Mg) results of purslane samples were detected to be between 2460.92 (boiled) and 17153.18 mg/kg (air dried) to 1159.25 (boiled) and 13428.23 mg/kg (air dried), respectively. A decrease in the protein and mineral contents of purslane was observed by fermentation and boiling. In general, flavour, colour and texture values of fermented purslane sample has reached an acceptable value by consumers. [ABSTRACT FROM AUTHOR]

With the aggravating aging of modern society, the sarcopenia-based aging syndrome poses a serious potential threat to the health of the elderly. Natural dietary supplements show great potential to reduce muscle wasting and enhance muscle performance. Tea has been widely recognized for its health-promoting effects. which contains active ingredients such as tea polyphenols, tea pigments, tea polysaccharides, theanine, caffeine, and vitamins. In different tea production processes, the oxidative condensation and microbial transformation of catechins and other natural substances from tea promotes the production of various tea pigments, including theaflavins (TFs), thearubigins (TRs), and theabrownins (TBs). Tea pigments have shown a positive effect on maintaining muscle health. Nevertheless, the relationship between tea pigments and skeletal muscle function has not been comprehensively elucidated. In addition, the numerous research on the extraction and purification of tea pigments is disordered with the limited recent progress due to the complexity of species and molecular structure. In this review, we sort out the strategies for the separation of tea pigments, and discuss the structures of tea pigments. On this basis, the regulation mechanisms of tea pigments on muscle functional were emphasized. This review highlights the current understanding on the extraction methods, molecular structures and regulation mechanisms of muscle function of tea pigments. Furthermore, main limitations and future perspectives are proposed to provide new insights into broadening theoretical research and industrial applications of tea pigments in the future. The extraction and isolation methods of tea pigments are detailedly introduced. The structural research progress of tea pigments are summarized. The effects of tea pigments in the prevention of muscle diseases are introduced. The mechanism of tea pigments in enhancing skeletal muscle function are proposed. [ABSTRACT FROM AUTHOR]

The aim of our study was to investigate the potential of rutin, catechin, dehydrozingerone, naringenin, and quercetin, both alone and in combination with temozolomide, to inhibit the expression of O6-methylguanine-DNA methyltransferase (MGMT) in glioma cells. MGMT has been shown to be a major cause of temozolomide resistance in glioma. Our study used both in silico and in vitro methods to assess the inhibitory activity of these phytochemicals on MGMT, with the goal of identifying the most effective combination of compounds for reducing temozolomide resistance. After conducting an initial in silico screening of natural compounds against MGMT protein, five phytochemicals were chosen based on their high docking scores and favorable binding energies. From the molecular docking and simulation studies, we found that quercetin showed a good inhibitory effect of MGMT with its high binding affinity. C6 glioma cells showed increased cytotoxicity when treated with the temozolomide and quercetin combination. It was understood from the isobologram and combination index plot that the drug combination showed a synergistic effect at the lowest dose. Quercetin when combined with temozolomide significantly decreased the MGMT levels in C6 cells in comparison with the other drugs as estimated by ELISA. The percentage of apoptotic cells increased significantly in the temozolomide–quercetin group indicating the potency of quercetin in decreasing the resistance of temozolomide as confirmed by acridine orange/ethidium bromide staining. Our experiment hence suggests that temozolomide resistance can be reduced by combining the drug with quercetin which will serve as an effective therapeutic target for glioblastoma treatment. [ABSTRACT FROM AUTHOR]

Objective: This study aimed at the evaluation of anti antiproliferative activity of Lonicera nummularifolia, Lilium ledebourii, Campsis radicans and Parthenocissus quinquefolia extracts. Materials and Methods: The extract was taken from the fresh leaves and bulbs of the plants by maceration method in the dark. After separating the solvent, the remaining dry matter was added to the culture medium containing G292, A431 and KB cancer and HGF-1 normal cells. Cytotoxicity tests, as well as cell cycle and apoptosis tests were performed on cells treated with dry substances and untreated cells. Finally, the most effective extract was separated into fractions by preparative HPLC and the effective fraction was characterized by Triple-Quad LC/MS connected to the UHPLC system. Results: All extracts significantly enhanced cell death rate in the three cancer cell lines more than the HGF-1 line. The Methanolic extract of L. ledebourii bulbs exhibited considerable efficacy on apoptosis induction in the cancer cell lines. It seems that the mode of action for L. ledebourii methanolic extract is mediated through increased BID/MAPK14 expression and decreased MDM2/BCL2/MYC expression, which led to activation of the p53 protein-induced apoptosis. It was also determined that the effective fraction of L. ledebourii methanolic extract consists of substances such as caffeic acid, ferulic acid, coumarin acid, catechin and apigenin. Conclusion: Overall, the findings suggest that L. ledebourii is a promising source of bioactive compounds with anticancer properties. [ABSTRACT FROM AUTHOR]

Coffee became a beverage that was in demand in the world and consequently produced millions of tons of coffee byproducts namely coffee silverskin (CS). Unutilized CS will be waste and cause environmental pollution such as greenhouse gas emissions, landfill waste, and groundwater contamination. This is a research concern at this time, although many studies have been conducted to find newer applications of CS, exploration of its benefits in the health sector is still limited. Therefore, exploring the benefits of CS to prevent or delay aging will be very interesting to develop in functional food industry technology. Therefore, this study aims to report profiling metabolites or phytochemicals, biological activities in terms of antioxidant activity, and potential anti-aging of CS via molecular docking simulation and in vitro modulation of the mTOR/AMPK/SIRT1 pathway. Something new has been obtained from this work, the profile of phytocompounds, and biological activities both in molecular docking simulation and in vitro studies. Some of the compounds observed in Robusta CS extract (rCSE) such as Epicatechin, Kaempferol, and Quercitrin, and Arabica CS extract (aCSE) such as (+)-Catechin dan Naringin have promising potential as inhibitors of iNOS, mTOR, and HIF-1α via molecular docking simulation. Interestingly, the in vitro biological activity assay of antioxidant and anti-aging activity, rCSE showed the same promising potential as the results of a molecular docking simulation. More interestingly, AMPK/SIRT1/mTOR expressions are well modulated by rCSE compared to aCSE significantly (p < 0.05). This makes the rCSE have promising biological activity as a candidate for functional food development and/or treatment agent in combating free radicals that cause the aging process. In vivo studies and human trials are certainly needed to see the further efficacy of the rCSE in the future. [ABSTRACT FROM AUTHOR]

Background: Arbutus unedo L. is a wild tree of Mediterranean regions used as food and in traditional medicine and important for afforestation programs. There is no detailed information available on the variation of A. unedo leaves metabolome across the seasons. The leaves were analyzed by Proton nuclear magnetic resonance (1 H NMR)-based metabolomics, comparing samples harvested across the seasons and in ten different natural habitats of Sardinia (Italy). Results: Multivariate analysis showed the impact of seasonal variation on the metabolome: glucose and quinic acid increased in summer, while in spring sucrose was accumulated. β-Arbutin, the main known active principle of A. unedo, generally reached the highest concentration in autumn. In winter, O-β-methylglucose, γ-aminobutyric acid (GABA), flavonols (quercetin-3-O-α-rhamnoside, myricetin-3-O-α-rhamnoside, kaempferol-3-O-α-rhamnoside), catechin, and gallocatechin increased. Characteristic metabolomic features were found also for samples collected in different locations. For instance, trees growing at the highest altitude and exposed to lower temperatures produced less flavonols and catechins. The only sample collected on trees growing on limestones, dolomites, and dolomitic limestones type of soil showed generally the highest content of arbutin. The highest phenolics content was found during spring, while samples collected on flowering branches in winter were the ones with the highest flavonoid content. The antioxidant activity was also variated, ranging from 1.3 to 10.1 mg of Trolox equivalents (TE)/mL of extract, and it was positively correlated to both total phenolics and flavonoid content. Winter samples showed the lowest antibacterial activity, while summer and autumn ones exhibited the highest activity (IC50 values ranging from 17.3 to 42.3 µg/mL against Staphylococcal species). Conclusion: This work provides 1 H-NMR fingerprinting of A. unedo leaves, elucidating the main metabolites and their variations during seasons. On the basis of arbutin content, autumn could be considered the balsamic period of this taxon. Samples collected in this season were also the most active ones as antibacterial. Moreover, an interesting metabolomic profile enriched in catechins and flavonols was observed in leaves collected in winter on flowering branches which were endowed with high antioxidant potential. [ABSTRACT FROM AUTHOR]

Drug delivery systems play a significant role in drug design.They could perform targeted and controlled release over a period, which is appropriate for poorly water-soluble drugs.The purpose of this study is to develop a drug delivery system, consisting of hydroxyapatite (HAp) polymer and sodium alginate (NaAlg), that covers the magnetic core of iron (III) oxide nanoparticles, in order to increases the loading capacity of iron oxide nanoparticles. In this study, iron (III) oxide nanoparticles were prepared by co-precipitation method and coated with HAp and NaAlg. The nanoparticles were characterized by X-ray diffraction, (FTIR), (SEM), and (TEM). Encapsulation efficiency of catechin hydrate (CH) and drug release rate was examined. The assessment of physicochemical characteristics show the synthesis of spherical particles with nanometer size (9–13 nm) and a high encapsulation efficiency (81.25 ± 2.55%) and drug-loading capacity (20.31 ± 0.64%). Maximum drug release obtain at pH = 5.5 coated. Iron (III) oxide show no significant cytotoxic effects. CH-loaded coated IONPs show a higher toxicity against HT-29 and MCF-7 cancer cells compared to free CH. This in vitro study show that the encapsulation of CH, as a potent herbal drug, into IONPs enhances its bioavailability, suggesting the NPs as an efficient vehicle for targeted drug delivery in cancer treatment. [ABSTRACT FROM AUTHOR]

Background: Rheumatoid arthritis (RA) is associated with increased levels of cytokines, for instance, nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) and interleukin-1 (IL-1), which exhibit potent pro-inflammatory effects and are contributing factors to disease progression. A range of cytokines, cell adhesion molecules, and enzymes that are implicated in the debilitating effects of RA are transcribed by nuclear factor kappa. Objectives: The purpose of this research was to characterize the efficacy of "catechin" as an IkappaB kinase-beta (IKK-β) inhibitor in collagen-induced arthritis (CIA) model in mice, as IKK-β is crucial in the transmission of signal-inducible NF-κβ activation. Methods: Arthritis was brought on in Bagg and Albino, but it is written BALB/c (BALB/c) male mice through subcutaneous immunization with bovine type II collagen on days 0 and 21. Catechin is given orally every day after the onset of the disease. Clinical evaluation of the prevalence and severity of the condition was done throughout the trial, and biochemical testing was done at the end (day 42). Results: In vitro findings of the study demonstrated catechin as a potent inhibitor of IKK-β with Half maximal Inhibitory Concentration (IC50) values of 2.90 μM and 4.358 μM in IKK-β and NF-κβ transactivation activity assay, respectively. Furthermore, catechin (dose range of 10–100 mg/kg, p.o.) was effective in reducing disease incidence and clinical signs in a dose-dependent manner, with an Effective Dose for 50% of the population (ED50) value of 79.579 mg/kg. The findings of this study demonstrate dose-dependent efficacy in terms of both disease severity (clinical scoring) and inflammatory markers (biochemical evaluation of the serum and joints). Conclusions: IKK inhibitors are a prospective target for the creation of new therapeutics for arthritis and other inflammatory diseases because it has been suggested that this enzyme is crucial in the pathophysiology of RA. The finding of this study suggests that "catechin" represents a novel inhibitor of IKK-β with promising anti-inflammatory activity. [ABSTRACT FROM AUTHOR]

Sarcopenia is characterized by a gradual slowing of movement due to loss of muscle mass and quality, decreased power and strength, increased risk of injury from falls, and often weakness. This review will focus on recent research trends in nutritional and pharmacological approaches to controlling sarcopenia. Because nutritional studies in humans are fairly limited, this paper includes many results from nutritional studies in mammals. The combination of resistance training with supplements containing amino acids is the gold standard for preventing sarcopenia. Amino acid (HMB) supplementation alone has no significant effect on muscle strength or muscle mass in sarcopenia, but the combination of HMB and exercise (whole body vibration stimulation) is likely to be effective. Tea catechins, soy isoflavones, and ursolic acid are interesting candidates for reducing sarcopenia, but both more detailed basic research on this treatment and clinical studies in humans are needed. Vitamin D supplementation has been shown not to improve sarcopenia in elderly individuals who are not vitamin D-deficient. Myostatin inhibitory drugs have been tried in many neuromuscular diseases, but increases in muscle mass and strength are less likely to be expected. Validation of myostatin inhibitory antibodies in patients with sarcopenia has been positive, but excessive expectations are not warranted. [ABSTRACT FROM AUTHOR]

The objectives of this study were the selection of the best tea clones with high catechin content among the known tea clones in Rwanda and Kenya, the examination of their antiproliferative effects on the triple-negative breast cancer (TNBC) cell line (4T1), and an evaluation of their combination index with cisplatin. The quantification of catechin contents in 14 different tea clones and 5 different processed teas was performed by high-performance liquid chromatography (HPLC). A comparative study of antiproliferative activities of catechin extracts from purple, TRFK306, and BB35 tea clones on the TNBC cell line (4T1) was undertaken, and their combination index (CI) with cisplatin and the dose reduction index (DRI) were determined. The catechin extract from BB35 had the highest concentration of total catechins (817.81±24.2 mg/g DW). After 72 h, the catechin extracts from TRFK306 showed a high IC50 of 68.68±3.30 µg/mL. The catechin extracts from TRFK306 showed the best synergism with cisplatin (CI=0.59), and they reduced the doses of cisplatin with the highest DRI=3.74493. Catechin extracts from purple tea showed higher antiproliferative activity and synergism with cisplatin against the TNBC cell line. [ABSTRACT FROM AUTHOR]