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A rhizogenic culture of Drosera capensis L. was obtained. An HPLC method with UV and mass-spectrometric detection was applied to analyze the effect of different drying protocols on the yield of individual polyphenols and 1,4-naphthoquinones from the rhizogenic culture of D. capensis L. The results of this analysis were compared with similar data obtained on the previously established morphogenic culture of D. rotundifolia L. that has been maintained for more than 15 years. In the rhizogenic culture of D. capensis L., six compounds were identified for the first time (myricetin-3-O-β-glucopyranoside, rossoliside, 3,3'-di-O-methylellagic acid 4-O-β-D-glycopyranoside, myricetin, 3,3'-di-O-methylellagic acid, and plumbagin). [ABSTRACT FROM AUTHOR]

The bioactivity and gastrointestinal stability of epicatechin gallate (ECG) may be affected by processing conditions. Results showed that the antioxidant ability and inhibitory activity on xanthine oxidase (XO) of ECG were higher at low pH values. Appropriate microwave and heating treatments improved the antioxidant (the scavenging rate increased from 71.75% to 92.71% and 80.88% under the microwave and heating treatments) and XO inhibitory activity (the inhibitory rate increased from 47.11% to 56.89% and 51.85% at the microwave and heating treatments) of ECG. The treated ECG led to a more compact structure of XO. Moreover, there may be synergistic antioxidant and inhibitory effects between ECG and its degradation products. The bioaccessibility of ECG after simulated digestion was untreated > microwave > heating, and the microwave−treated ECG still had good XO inhibitory activity after digestion. These findings may provide some significant information for the development of functional foods enriched in catechins. [ABSTRACT FROM AUTHOR]

Camellia bee pollen (CBP) is a major kind of bee product which is collected by honeybees from tea tree (Camellia sinensis L.) flowers and agglutinated into pellets via oral secretion. Due to its special healthcare value, the authenticity of its botanical origin is of great interest. This study aimed at distinguishing CBP from other bee pollen, including rose, apricot, lotus, rape, and wuweizi bee pollen, based on a non-targeted metabolomics approach using ultra-high performance liquid chromatography–mass spectrometry. Among the bee pollen groups, 54 differential compounds were identified, including flavonol glycosides and flavone glycosides, catechins, amino acids, and organic acids. A clear separation between CBP and all other samples was observed in the score plots of the principal component analysis, indicating distinctive metabolic profiles of CBP. Notably, L-theanine (864.83–2204.26 mg/kg) and epicatechin gallate (94.08–401.82 mg/kg) were identified exclusively in all CBP and were proposed as marker compounds of CBP. Our study unravels the distinctive metabolic profiles of CBP and provides specific and quantified metabolite indicators for the assessment of authentic CBP. [ABSTRACT FROM AUTHOR]

Recent improvements in 3D printing technology have increased the usage of 3D printed materials in several areas. An exciting and emerging area of applying these next-generation manufacturing strategies is the development of devices for biomedical applications. The main aim of this work was to investigate the effect of tannic acid, gallic acid, and epicatechin gallate on the physicochemical characteristics of acrylonitrile butadiene–styrene (ABS) and Nylon 3D printing materials using the contact angle method. The adhesion of Staphylococcus aureus on untreated and treated materials was evaluated by scanning electron microscopy (SEM) analysis and the images were treated by MATLAB software. The results of the contact angle measurements showed a significant change in the physicochemical properties of both surfaces, indicated an increase in the electron donor character of 3D printing materials following treatment. Thus, the ABS surfaces treated with tannic acid, gallic acid, and epicatechin gallate have become more electron donating. Furthermore, our results proved the ability of S. aureus to adhere on all materials with a percentage of 77.86% for ABS and 91.62% for nylon. The SEM has shown that all actives molecules were sufficient to obtain better inhibition of bacterial adhesion, which tannic acid has shown a total inhibition of S. aureus on ABS. From these results, our treatment presents a high potential for utilization as an active coating to prevent bacterial attachment and the eventual biofilm development in medical field. [ABSTRACT FROM AUTHOR]

Background: Staphylococcus aureus is an opportunistic pathogen and a major cause of nosocomial and community-acquired infections. The alarming rise in Methicillin-resistant S. aureus (MRSA) infection worldwide and the emergence of vancomycin-resistant MRSA strains have created an urgent need to identify new and alternative treatment options. Triple combinations of antimicrobials with different antimicrobial mechanisms may be a good choice to overcome antimicrobial resistance. Methods: In this study, we combine two natural compounds: kuraridin from Sophora flavescens and epicatechin gallate (ECG) from Camellia sinensis (Green tea), which could provide the best synergy with antibiotics against a selected panel of laboratory MRSA with known resistant mechanisms and clinical community-associated (CA) and hospital-associated (HA) MRSA as well. Results: The combined use of ECG and kuraridin was efficacious in inhibiting the growth of a panel of tested MRSA strains. The antibacterial activities of gentamicin, fusidic acid and vancomycin could be further enhanced by the addition of ECG and kuraridin. In time-kill study, when vancomycin (0.5 μg/mL) was combined with ECG (2 μg/mL) and kuraridin (2 μg/mL), a very strong bactericidal growth inhibition against 3 tested strains ATCC25923, MRSA ST30 and ST239 was observed from 2 to 24 h. ECG and kuraridin both possess anti-inflammatory activities in bacterial toxin-stimulated peripheral blood mononuclear cells by suppressing the production of inflammatory cytokines (IL-1β, IL-6 and TNFα) and are non-cytotoxic. In a murine pneumonia model infected with ATCC25923, MRSA ST30 or ST239, the combined use of ECG and kuraridin with vancomycin could significantly reduce bacterial counts. Conclusions: The present findings reveal the potential of ECG and kuraridin combination as a non-toxic herbal and antibiotics combination for MRSA treatment with antibacterial and anti-inflammatory activities. [ABSTRACT FROM AUTHOR]

Abstract Coronavirus disease‐19 (COVID‐19) is the global health emergency caused by SARS‐CoV‐2. Upon infection, antigenic determinants of the virus trigger massive production of proinflammatory/pyroptosis‐associated proteins, resulting in cytokine storm, tissue damage, and multiorgan failure. Therefore, these proinflammatory/pyroptosis‐associated mediators are promising therapeutic targets to combat COVID‐19. Epicatechin gallate (ECG) is a polyphenol found in green tea. It has antioxidative and anti‐inflammatory properties. Hence, in the present study, ECG was selected to explore its binding potential for inflammatory mediators such as interleukins, interferon‐γ (IFNγ), and tumor necrosis factor‐α (TNF‐α), along with their native receptors. In addition, the interacting potential of ECG with pyroptosis‐associated proteins, viz. caspases and BAX has also been investigated. Molecular docking analysis has revealed that ECG interacts with interleukins, IFNγ, TNF‐α, cytokine receptors, caspase‐1/4/11, and BAX with significant binding affinity. Several amino acid residues of these mediators were blocked by ECG through stable hydrogen bonds and hydrophobic contacts. ECG interacted with caspase‐11, BAX, and TNF‐R1 with better binding affinities. Therefore, the present in silico study indicates that ECG could be a potential drug to subvert cytokine storm and pyroptosis during COVID‐19.

PM2.5 (particulate matter with aerodynamic diameter ≤ 2.5 μm) is a well-known cytotoxic pollutant that capable to induce severe intracellular oxidative stress while the underlying mechanisms remain unclear. Herein, 4 types of PM2.5 derived from solid fuel burning were selected as stimuli in A549 cells exposure model to evaluate their effects on oxidative stress and inflammatory responses. Although resulting in different responses in cell viability, all PM2.5 exhibited over 50 % higher oxidative stress than control group, expression as intracellular reactive oxygen species, malondialdehyde and superoxide dismutase levels. The Pearson’s correlation results indicated that cations (e.g., Ca2+), heavy metals (e.g., Cr and Pb), nPAHs (nitro-polycyclic aromatic hydrocarbons, e.g., 6-nitrochrysene) and oPAHs (oxygenated PAHs, e.g., 9-fluorenone) were the main functioning toxics (r > 0.6). A key finding was the dual-directional regulation function of ECG (epicatechin gallate), that is, it could either increase the low A549 cell viabilities in coal combustion PM2.5 group or reduce them in charcoal PM2.5 group (P

Camellia bee pollen (CBP) is a major kind of bee product which is collected by honeybees from tea tree (Camellia sinensis L.) flowers and agglutinated into pellets via oral secretion. Due to its special healthcare value, the authenticity of its botanical origin is of great interest. This study aimed at distinguishing CBP from other bee pollen, including rose, apricot, lotus, rape, and wuweizi bee pollen, based on a non-targeted metabolomics approach using ultra-high performance liquid chromatography–mass spectrometry. Among the bee pollen groups, 54 differential compounds were identified, including flavonol glycosides and flavone glycosides, catechins, amino acids, and organic acids. A clear separation between CBP and all other samples was observed in the score plots of the principal component analysis, indicating distinctive metabolic profiles of CBP. Notably, L-theanine (864.83–2204.26 mg/kg) and epicatechin gallate (94.08–401.82 mg/kg) were identified exclusively in all CBP and were proposed as marker compounds of CBP. Our study unravels the distinctive metabolic profiles of CBP and provides specific and quantified metabolite indicators for the assessment of authentic CBP.

The bioactivity and gastrointestinal stability of epicatechin gallate (ECG) may be affected by processing conditions. Results showed that the antioxidant ability and inhibitory activity on xanthine oxidase (XO) of ECG were higher at low pH values. Appropriate microwave and heating treatments improved the antioxidant (the scavenging rate increased from 71.75% to 92.71% and 80.88% under the microwave and heating treatments) and XO inhibitory activity (the inhibitory rate increased from 47.11% to 56.89% and 51.85% at the microwave and heating treatments) of ECG. The treated ECG led to a more compact structure of XO. Moreover, there may be synergistic antioxidant and inhibitory effects between ECG and its degradation products. The bioaccessibility of ECG after simulated digestion was untreated > microwave > heating, and the microwave−treated ECG still had good XO inhibitory activity after digestion. These findings may provide some significant information for the development of functional foods enriched in catechins.

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Lewis acid mediated self-condensation of epicatechin gallate derivative was examined. We found that Yb(OTf)3 afforded good yield of the dimeric epicatechin gallate derivative. The condensed product was applied to the synthesis of procyanidin B2 3,3′′-digallate. [ABSTRACT FROM AUTHOR]

[Display omitted] • The composite functional inclusion compounds were prepared by ultrasonic-mediated synthesis. • The fiber film was successfully prepared by electrospinning technology. • The fiber film exhibits excellent physical and chemical properties. • The fiber film has excellent antibacterial effect in vivo and in vitro. In this study, Polycaprolactone (PCL)/Yam Polysaccharide (YP) fiber membranes loaded the ultrasound-mediated assembly of 2-Hydroxypropyl-β-cyclodextrin (HP-β-CD)/Epicatechin gallate (ECG) inclusion complexes were prepared by electrospinning technology for food packaging. Morphology, infrared spectroscopy and X-ray diffraction results showed that the inclusion complexes were successfully assembled. With the addition of inclusion complexes, the average diameter of the fibers increased from 2480.96 to 10179.12 nm, the crystallinity decreased, the thermal stability improved, the hydrophilicity enhanced, and the water vapor permeability enhanced. Meanwhile, thermogravimetry and differential scanning calorimetry results showed that the inclusion complexes formed hydrogen bonds between the fibers, which improved the thermal stability, but the mechanical behavior suffered a certain loss. In addition, the fiber membrane could continuously release ECG within 240 h, which showed excellent antibacterial effects both in vitro and in vivo. These results indicated that the fiber film developed based on electrospinning had a broad application prospect in food packaging. [ABSTRACT FROM AUTHOR]

Background: Staphylococcus aureus is an opportunistic pathogen and a major cause of nosocomial and community-acquired infections. The alarming rise in Methicillin-resistant S. aureus (MRSA) infection worldwide and the emergence of vancomycin-resistant MRSA strains have created an urgent need to identify new and alternative treatment options. Triple combinations of antimicrobials with different antimicrobial mechanisms may be a good choice to overcome antimicrobial resistance. Methods: In this study, we combine two natural compounds: kuraridin from Sophora flavescens and epicatechin gallate (ECG) from Camellia sinensis (Green tea), which could provide the best synergy with antibiotics against a selected panel of laboratory MRSA with known resistant mechanisms and clinical community-associated (CA) and hospital-associated (HA) MRSA as well. Results: The combined use of ECG and kuraridin was efficacious in inhibiting the growth of a panel of tested MRSA strains. The antibacterial activities of gentamicin, fusidic acid and vancomycin could be further enhanced by the addition of ECG and kuraridin. In time-kill study, when vancomycin (0.5 μg/mL) was combined with ECG (2 μg/mL) and kuraridin (2 μg/mL), a very strong bactericidal growth inhibition against 3 tested strains ATCC25923, MRSA ST30 and ST239 was observed from 2 to 24 h. ECG and kuraridin both possess anti-inflammatory activities in bacterial toxin-stimulated peripheral blood mononuclear cells by suppressing the production of inflammatory cytokines (IL-1β, IL-6 and TNFα) and are non-cytotoxic. In a murine pneumonia model infected with ATCC25923, MRSA ST30 or ST239, the combined use of ECG and kuraridin with vancomycin could significantly reduce bacterial counts. Conclusions: The present findings reveal the potential of ECG and kuraridin combination as a non-toxic herbal and antibiotics combination for MRSA treatment with antibacterial and anti-inflammatory activities.

Orostachys species have been recognized as medicinal herbs in East Asia. Although O. fimbriata is known as a traditional medicine, its antioxidant properties have not been investigated compared to other Orostachys species. In this study, we characterized the antioxidant compounds and determined the antioxidant activity of O. fimbriata for the first time. As a result, 1 g of O. fimbriata extracts contains 288.5 ± 7.4 mg polyphenols, which contains 159.7 ± 8.3 mg flavonoids. In particular, 21.6%, 6.6%, and 2.6% of the total flavonoids were identified as epicatechin gallate, quercetin, and kaempferol, respectively, by LC-MS system. The DPPH IC50, ABTS IC50, and FRAP value of the extracts was determined to be 27.6 ± 5.5 μg/mL, 125.7 ± 6.0 μg/mL, and 115.0 ± 4.4 mmol/L, respectively. These activities were 30–57% of the positive control, ascorbic acid. In conclusion, it was demonstrated that O. fimbriata has outstanding antioxidant properties. This study highlights the need for further investigations toward in-depth research on the pharmacological functions of O. fimbriata.

In this study, chitosan (CS) was conjugated with epicatechin gallate (ECG) to prepare CS-ECG conjugates with different substitution degrees (5.18 %, 6.36 % and 7.74 %). Then, antioxidant packaging films were fabricated by blending CS and CS-ECG conjugates. The impact of CS-ECG conjugates' substitution degree on the functionality of CS/CS-ECG films was determined. CS-ECG conjugates showed UV absorption at 275 nm, proton signal at 6.85 ppm and infrared absorption at 1533 cm−1, assigning to the conjugated ECG. As compared with CS, CS-ECG conjugates exhibited less crystalline state but higher antioxidant activity. The structural characterization of CS/CS-ECG films showed CS and CS-ECG conjugates formed hydrogen bonds. CS/CS-ECG films displayed 26.35 %–29.23 % water solubility, 85.61°–86.96° water contact angle, 3.11–3.41 × 10−11 g m−1 s−1 Pa−1 water vapor permeability, 0.29–0.34 cm3 mm m−2 day−1 atm−1 oxygen permeability, 31.54–36.20 MPa tensile strength, 50.12 %–56.40 % elongation at break, as well as potent antioxidant activity and oil oxidation inhibitory ability. Notably, the film containing CS-ECG conjugate with 7.74 % substitution degree had the strongest barrier ability, mechanical property, antioxidant activity and oil oxidation inhibitory ability. Results suggested the substitution degree of CS-ECG conjugates was positively correlated with the barrier, mechanical and antioxidant properties of CS/CS-ECG films. • Chitosan (CS) was reacted with epicatechin gallate (ECG) to prepare conjugates. • Antioxidant packaging films were fabricated based on CS and CS-ECG conjugates. • ECG changed the crystallinity, morphology and antioxidant activity of CS. • CS-ECG conjugates improved the barrier, mechanical and antioxidant activity of films. • The substitution degree of conjugates positively affected the functionality of films. [ABSTRACT FROM AUTHOR]

• Mesoporous TiO 2 /TSH (TTSH) nanocomposite prepared by wet impregnation method. • The weight percentages of TSH loaded on m-TiO 2 were optimised. • The chemical composition of TSH was predicted as PA and gallic acid. • Epicatechin in TSH produces O 2 .- to promote the efficiency of m-TiO 2. • In TTSH light absorption edge position of m-TiO 2 was moved to the visible region. A novel nanocomposite of tamarind seed husk (TSH) supported mesoporous titanium dioxide (m-TiO 2) nanoparticle (TTSH) was prepared by employing a simple wet-impregnation technique. The chemical composition of the prepared TSH was predicted as gallic acid and proanthocyanidin (PA) derivatives such as epicatechin gallate (ECG) and epigallocatechin gallate (EGCG) using FT-IR and 13C NMR characterization. The XRD and HR-TEM studies clearly revealed the structural and morphological properties of TTSH. The adsorption studies were performed and compared for m-TiO 2 , TSH and TTSH under dark conditions. In comparison to bare m-TiO 2 , TSH with the functional groups C O C, -C O and -OH showed greater adsorption capacity towards the cationic dye methylene blue (MB). TSH (2.588 mgL−1sec−1) showed a higher rate than m-TiO 2 (2.145 mgL−1sec−1) for the degradation of MB under direct solar light. The TTSH nanocomposite contributed enough superoxide anion radicals (O 2 .−), which yields . OH radicals on further series of redox reactions for the degradation of MB. TSH extended the light absorption edge position of m-TiO 2 to the visible region from 400 to 480 nm, hence TTSH functioned as a visible responsive material. This research work brings TSH into the spotlight on a cost-efficient and eco-friendly support material to improve the degradation efficiency of photocatalysts. [Display omitted] [ABSTRACT FROM AUTHOR]

Epicatechin gallate (ECG) is one of the main components of catechins and has multiple bioactivities. In this work, the inhibitory ability and molecular mechanism of ECG on XO were investigated systematically. ECG was determined as a mixed xanthine oxidase (XO) inhibitor with an IC50 value of 19.33 ± 0.45 μM. The promotion of reduced XO and the inhibition of the formation of uric acid by ECG led to a decrease in O2− radical. The stable ECG–XO complex was formed by hydrogen bonds and van der Waals forces, with the binding constant of the magnitude of 104 L mol−1, and ECG influenced the stability of the polypeptide skeleton and resulted in a more compact conformation of XO. Computational simulations further characterized the binding characteristics and revealed that the inhibitory mechanism of ECG on XO was likely that ECG bound to the vicinity of flavin adenine dinucleotide (FAD) and altered the conformation of XO, hindering the entry of substrate and the diffusion of catalytic products. ECG and allopurinol bound to different active sites of XO and exerted a synergistic inhibitory effect through enhancing their binding stability with XO and changing the target amino acid residues of XO. These findings may provide a theoretical basis for the further application of ECG in the fields of food nutrition and functional foods.

Protein glycation can produce the advanced glycation end products (AGEs), which has a potential health risk due to its relevance with diabetic complications. Searching for potent inhibitors to suppress hyperglycemia-induced protein glycation is of great significance. Here, we probed the anti-glycation potential of epicatechin gallate (ECG), an important ingredient of green tea, by spectroscopy and chromatography supplemented by molecular docking. It was found that ECG suppressed the carbonylation and the formation of amyloid cross-β structures of bovine serum albumin (BSA) as well as the generation of AGEs in BSA–fructose model by 65.6%, 73.7% and 87.0%, resepctively. A combination of ECG with epigallocatechin gallate (EGCG) at molar ratios from 0.5:1 to 2:1 exhibited the interactive effects on AGEs formation from moderate antagonism to synergy. Moreover, ECG at 44.2 μg/mL showed a trapping efficiency of 81.6% for the important precursor methylglyoxal (MGO) of AGEs within 24 h, and the formed ECG–mono-MGO and ECG–di-MGO adducts were verified by LC–QqQ–MS analysis. The inhibitory effect of ECG on the protein glycation may be due to its MGO trapping and the specific binding with certain amino acid residues of BSA. These findings may provide the theoretical basis for the development of ECG as an inhibitor of protein glycation. Anti-glycation of epicatechin gallate might be due to its trapping to precursor MGO of AGEs and specific binding with some amino acid residues of protein. Unlabelled Image • Epicatechin gallate (ECG) significantly suppressed protein glycation. • ECG inhibited the carbonylation and cross-linked structures formation of protein. • ECG trapped the precursor MGO of AGEs by forming the ECG–MGO adducts. • Anti-glycation of ECG might be its MGO trapping and binding with certain amino acids. [ABSTRACT FROM AUTHOR]

A novel method was developed to separate the tea polyphenols epigallocatechin gallate (EGCG) and epicatechin gallate (ECG) by two-step chromatography. In the first-step, four different macroporous absorption resins were compared by dynamic desorption, of which only AB-8 resin resulted in enriched fractions for EGCG and ECG. Their purity was 53.69 %, and 65.77 %, with recovery rates of 88.05 %, and 83.46 %, respectively. For the second-step, The recovery rates of 85.36 % and 86.09 % for EGCG and ECG were obtained respectively by a novel stationary phase of ß-CD bonded agar gel. The overall recovery efficiency of the complete procedure was 75.16 % for EGCG and 71.85 % for ECG, respectively, and the purity of the obtained preparations reached 97.63 % for EGCG and 98.09 % for ECG. The chromatographic behavior of ß-cyclodextrin bonded agar gel was studied with elution by acetonitrile, which indicated that both hydrophilic and hydrophobic interactions between the polyphenols and the solid phase occurred. [ABSTRACT FROM AUTHOR]

Interaction of metal, especially iron ions with flavanols is considered as an important feature of these compounds and is believed to contribute to their both antioxidant and prooxidant properties. The aim of this study was to examine how Fe 2+ binding to form a 4:1 (flavanol:Fe 2+ ) mixtures affects the antioxidant properties of flavanols. ABTS ∗ scavenging, protection against fluorescence bleaching induced by AAPH and hypochlorite, protection against lipid peroxidation and protection against hypochlorite-induced hemolysis demonstrated that flavonol-Fe 2+ mixtures retain antioxidant properties, although, in most cases, they are lower with respect to the flavanols alone. No superoxide dismutase-like or catalase-like activity of the mixtures was revealed. [ABSTRACT FROM AUTHOR]

The neurotoxicity of acrylamide (ACR) monomer occurs through different mechanisms such as oxidative stress. Epigallocatechin gallate (EGCG) and epicatechin gallate (ECG) are green tea catechins which are known as powerful antioxidants. In this study, we examined the possible protective effects of ECG and EGCG on ACR neurotoxicity in both in-vitro and in-vivo models. PC12 cells were exposed to different concentrations of ECG and EGCG. After 24 and 48 hours, ACR was added to the cells (IC50 = 4.85 mM) and cell viability was measured through MTT assay after 24 hours. Male Wistar rats were pretreated with ECG, EGCG (10, 20 and 40 mg/kg, i.p) and vitamin E (200 IU/kg i.p.) for 3 days. Afterwards they were treated with ACR (50 mg/kg, i.p.) for 11 days. After the treatment period, gait score examination was performed and molondialdehyde (MDA) and reduced glutathione (GSH) were measured in cerebral cortex. ACR reduced the cell viability in a concentration-dependent manner. Both ECG and EGCG (20 μM) showed inhibitory effects on ACR cytotoxicity. ACR significantly induced gait abnormalities, decreased GSH level and increased lipid peroxidation in cerebral cortex. ECG and EGCG (20 mg/kg) improved all ACR toxic effects. Although the food intake was increased in pretreated groups compared to the ACR-treated group, intensive weight loss was observed due to the green tea’s different weight loss mechanisms. ECG and EGCG inhibited the cytotoxicity of ACR in PC12 cells and increased GSH level and decreased lipid peroxidation in rat cerebral cortex. [ABSTRACT FROM AUTHOR]

Ichthyophthirius multifiliis is a pathogenic parasite of freshwater fish that threatens the sustainability of aquaculture industry globally. Our previous studies have identified Sargentodoxa cuneata ethanol extracts exhibited potent antiparasitic activity against I. multifiliis. However, the active ingredients in S. cuneata remain unknown. In this study, we isolated an active compound from S. cuneata by bioassay-guided fractionation and identified it as epicatechin gallate (ECG) by NMR, FT-IR and HR-MS spectroscopy. In vitro assays revealed that ECG was effective against all the free-living stages of I. multifiliis. ECG could cause 100% mortality of theronts at 0.3 mg/L within 30.6 ± 0.4 min, and terminate reproduction of protomonts and tomonts at concentrations of 2.0 and 10.0 mg/L, respectively. Morphologically, 2.0 mg/L ECG treatment for 2 h induced the loss of plasma membrane integrity and leakage of intracellular contents of the protomont. Moreover, an in vivo parasite‑goldfish infection model was applied to evaluate the efficacy of ECG on prevention and treatment of ichthyophthiriasis. The results showed that 2.0 mg/L ECG treatment for 12 days could cure goldfish ichthyophthiriasis and significantly increase the survival rate of the infected goldfish by 86.7%. Acute toxicity test revealed that ECG was relatively safe to goldfish, with a median lethal concentration (LC 50) value of 63.7 mg/L, which was >30 times higher than effective concentration against I. multifiliis in vivo. Overall, our data indicated that ECG had the potential as a novel antiparasitic agent for the treatment of ichthyophthiriasis in aquaculture. • Epicatechin gallate (ECG) was isolated for the first time from Sargentodoxa cuneata stems by bioassay-guided fractionation. • ECG was effective against all the free-living stages of Ichthyophthirius multifiliis. • ECG treatment could cure goldfish ichthyophthiriasis and significantly increase the survival rate of the goldfish. • ECG had the potential as a novel antiparasitic agent in aquaculture. [ABSTRACT FROM AUTHOR]

The polyphenol (−)-epicatechin gallate (ECg) inserts into the cytoplasmic membrane (CM) of methicillin-resistant Staphylococcus aureus (MRSA) and reversibly abrogates resistance to β-lactam antibiotics. ECg elicits an increase in MRSA cell size and induces thickened cell walls. As ECg partially delocalizes penicillin-binding protein PBP2 from the septal division site, reduces PBP2 and PBP2a complexation and induces CM remodelling, we examined the impact of ECg membrane intercalation on phospholipid distribution across the CM and determined if ECg affects the equatorial, orthogonal mode of division. The major phospholipids of the staphylococcal CM, lysylphosphatidylglycerol (LPG), phosphatidylglycerol (PG), and cardiolipin (CL), were distributed in highly asymmetric fashion; 95%–97% of LPG was associated with the inner leaflet whereas PG (~90%) and CL (~80%) were found predominantly in the outer leaflet. ECg elicited small, significant changes in LPG distribution. Atomic force microscopy established that ECg-exposed cells divided in similar fashion to control bacteria, with a thickened band of encircling peptidoglycan representing the most recent plane of cell division, less distinct ribs indicative of previous sites of orthogonal division and concentric rings and “knobbles” representing stages of peptidoglycan remodelling during the cell cycle. Preservation of staphylococcal membrane lipid asymmetry and mode of division in sequential orthogonal planes appear key features of ECg-induced stress.

Inhibition of excessive fructose intake in the small intestine could alleviate fructose-induced diseases such as hypertension and non-alcoholic fatty liver disease. We examined the effect of phytochemicals on fructose uptake using human intestinal epithelial-like Caco-2 cells which express the fructose transporter, GLUT5. Among 35 phytochemicals tested, five, including nobiletin and epicatechin gallate (ECg), markedly inhibited fructose uptake. Nobiletin and ECg also inhibited the uptake of glucose but not of L-leucine or Gly-Sar, suggesting an inhibitory effect specific to monosaccharide transporters. Kinetic analysis further suggested that this reduction in fructose uptake was associated with a decrease in the apparent number of cell-surface GLUT5 molecules, and not with a change in the affinity of GLUT5 for fructose. Lastly, nobiletin and ECg suppressed the permeation of fructose across Caco-2 cell monolayers. These findings suggest that nobiletin and ECg are good candidates for preventing diseases caused by excessive fructose intake. [ABSTRACT FROM AUTHOR]

Glioblastoma (GBM) is a deadly brain tumor with a current mean survival of 12-15 months. Despite being a potent anti-cancer agent, the turmeric ingredient curcumin (C) has limited anti-tumor efficacy in vivo due to its low bioavailability. We have reported earlier a strategy involving the use two other polyphenols, epicatechin gallate (E) from green tea and resveratrol (R) from red grapes at a unique, synergistic molar ratio with C (C:E:R: 4:1:12.5, termed TriCurin) to achieve superior potency against HPV+ tumors than C alone at C:E:R (µM): 32:8:100 (termed 32 µM+ TriCurin). We have now prepared liposomal TriCurin (TrLp) and demonstrated that TrLp boosts activated p53 in cultured GL261 mouse GBM cells to trigger apoptosis of GBM and GBM stem cells in vitro. TrLp administration into mice yielded a stable plasma concentration of 210 nM C for 60 min, which, though sub-lethal for cultured GL261 cells, was able to cause repolarization of M2-like tumor (GBM)-associated microglia/macrophages to the tumoricidal M1-like phenotype and intra-GBM recruitment of activated natural killer cells. The intratumor presence of such tumoricidal immune cells was associated with concomitant suppression of tumor-load, and apoptosis of GBM and GBM stem cells. Thus, TrLp is a potential onco-immunotherapeutic agent against GBM tumors. [ABSTRACT FROM AUTHOR]