Phenolic compound profiling and antioxidant potential of different types of Schisandra henryi in vitro cultures.

Schisandra henryi is an endemic species of medicinal potential known from traditional Chinese medicine. As part of this study, a complex biotechnological and phytochemical assessment was conducted on S. henryi with a focus on phenolic compounds and antioxidant profiling. The following in vitro cultures were tested: microshoot agar and callus, microshoot agitated, and suspension, along with the microshoot culture in PlantForm bioreactors. Qualitative profiling was performed by ultra-high-performance liquid chromatography with a photodiode array detector coupled with ion-trap mass spectrophotometry with electrospray ionization and then quantitative analysis by high-performance liquid chromatography with a diode array detector using standards. In the extracts, mainly the compounds from procyanidins were identified as well as phenolic acids (neochlorogenic acid, caffeic acid, protocatechuic acid) and catechin. The highest content of phenolic compounds was found for in vitro agar microshoot culture (max. total content 229.87 mg/100 g DW) and agitated culture (max. total content 22.82 mg/100 g DW). The max. TPC measured using the Folin-Ciocalteu assay was equal to 1240.51 mg GAE/100 g DW (agar microshoot culture). The extracts were evaluated for their antioxidant potential by the DPPH, FRAP, and chelate iron ion assays. The highest potential was indicated for agar microshoot culture (90% of inhibition and 59.31 nM/L TEAC, respectively). The research conducted on the polyphenol profiling and antioxidant potential of S. henryi in vitro culture extracts indicates the high therapeutic potential of this species. KEY POINTS: • Different types of S. henryi in vitro cultures were compared for the first time. • The S. henryi in vitro culture strong antioxidant potential was determined for the first time. • The polyphenol profiling of different types of S. henryi in vitro cultures was shown.

Epigallocatechin-3-gallate-induced tolerance to cadmium stress involves increased flavonoid synthesis and nutrient homeostasis in tomato roots.

Cadmium (Cd) is a toxic heavy metal, increasingly accumulating in the environment and its presence in various environmental compartments represents a significant risk to human health via the food chain. Epigallocatechin-3-Gallate (EGCG) is a prominent secondary metabolite, which can safeguard plants from biotic and abiotic stress. However, the role of EGCG in flavonoid synthesis, nutrient acquisition and reactive oxygen species (ROS) metabolism under Cd stress remains unclear. Here, we examined the effects of EGCG and Cd treatment on leaf photochemical efficiency, cell ultrastructure, essential element acquisition, antioxidant system, and secondary metabolism in tomato (Solanum lycopersicum L.). The results showed that O2•-, H2O2, and malondialdehyde levels increased after Cd treatment, but Fv/Fm decreased significantly, suggesting that Cd induced oxidative stress and photoinhibition. However, EGCG mitigated the adverse effects of Cd-induced phytotoxicity in both the roots and leaves. A decrease in ROS accumulation under EGCG + Cd treatment was mainly attributed to the significant enhancement in antioxidant enzyme activity, flavonoid content, and PHENYLALANINE AMMONIA-LYASE expression in roots. Moreover, EGCG reduced Cd content but increased some essential nutrient contents in tomato plants. Transmission electron microscopy-based observations revealed that EGCG treatment safeguards leaf and root cell ultrastructure under Cd stress. This implies that tomato plants subjected to Cd stress experienced advantageous effects upon receiving EGCG treatment. The present work elucidated critical mechanisms by which EGCG induces tolerance to Cd, thereby providing a basis for future investigations into environmentally sustainable agricultural practices in areas contaminated with heavy metals, for utilizing naturally occurring substances found in plants.

(-)-Epicatechin ameliorates type 2 diabetes mellitus by reshaping the gut microbiota and Gut-Liver axis in GK rats.

As one of the most abundant plant polyphenols in the human diet, (-)-epicatechin (EC) can improve insulin sensitivity and regulate glucose homeostasis. However, the primary mechanisms involved in EC anti-T2DM benefits remain unclear. The present study explored the effects of EC on the gut microbiota and liver transcriptome in type 2 diabetes mellitus (T2DM) Goto-Kakizaki rats for the first time. The findings showed that EC protected glucose homeostasis, alleviated systemic oxidative stress, relieved liver damage, and increased serum insulin. Further investigation showed that EC reshaped gut microbiota structure, including inhibiting the proliferation of lipopolysaccharide (LPS)-producing bacteria and reducing serum LPS. In addition, transcriptome analysis revealed that the insulin signaling pathway may be the core pathway of the EC anti-T2DM effect. Therefore, EC may modulate the gut microbiota and liver insulin signaling pathways by the gut-liver axis to alleviate T2DM. As a diet supplement, EC has promising potential in T2DM prevention and treatment.

Formation of EGCG oxidation self-assembled nanoparticles and their antioxidant activity in vitro and hepatic REDOX regulation activity in vivo.

(-)-Epigallocatechin-3-gallate (EGCG) is a major polyphenol in tea and exerts several health-promoting effects. It easily autoxidizes into complex polymers and becomes deactivated due to the presence of multiple phenolic hydroxyl structures. Nonetheless, the morphology and biological activity of complex EGCG polymers are yet to be clarified. The present study demonstrated that EGCG autoxidation self-assembled nanoparticles (ENPs) exhibit antioxidant activity in vitro and hepatic REDOX homeostasis regulation activity in vivo. Also, the formation of ENPs during the EGCG autoxidation process was based on the intermolecular interaction forces that maintain the stability of the nanoparticles. Similar to EGCG, ENPs are scavengers of reactive oxygen species and hydroxyl radicals in vitro and also regulate hepatic REDOX activity through liver redox enzymes, including thioredoxin reductase (TrxR), thioredoxin (Trx), glutathione reductase (GR), glutaredoxin (Grx), and glutathione S-transferase (GST) in vivo. Moreover, ENPs activate the NRF2 antioxidant-responsive element pathway, exerting a detoxification effect at high doses. Unlike EGCG, ENPs do not cause liver damage at low doses and also maintain liver biosafety at high doses through self-assembly, forming large particles, which is supported by the unchanged levels of liver damage biomarkers, including serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), liver γ-phosphorylated histone 2AX (γ-H2AX), and P53-related genes (Thbs, MDM2, P53, and Bax). Collectively, these findings revealed that ENPs, with adequate biosafety and regulation of hepatic redox activity in vivo, may serve as substitutes with significant potential for antioxidant applications or as food additives to overcome the instability and liver toxicity of EGCG.

[Dynamic Chemistry of Tannins].

Tannins are a group of polyphenols that possess the ability to precipitate proteins, causing an undesirable astringent taste by interacting with salivary peptides. This interaction deactivates the digestive enzymes; therefore, tannins are considered as plant defense substances. The health benefits of tannins and related polyphenols in foods and beverages have been demonstrated by biological and epidemiological studies; however, their metabolism in living plants and the chemical changes observed during processing of foods and medicinal herbs raises some questions. This review summarizes our studies concerning dynamic changes observed in tannins. Ellagitannins present in the young leaves of Camellia japonica and Quercus glauca undergo oxidative degradation as the leaves mature. Similar oxidative degradation is also observed in whiskey when it is kept for aging in oak barrels, and in decaying wood caused by fungi in natural forests. In contrast, ellagitannins have been observed to undergo reduction in the leaves of Carpinus, Castanopsis, and Triadica species as the leaves mature. This phenomenon of reductive metabolism in leaves enabled us to propose a new biosynthetic pathway for the most fundamental ellagitannin acyl groups, which was also supported by biomimetic synthetic studies. Polyphenols undergo dynamic changes during the process of food processing. Catechin in tea leaves undergo oxidation upon mechanical crushing to generate black tea polyphenols. Though detailed production mechanisms of catechin dimers have been elucidated, structures of thearubigins (TRs), which are complex mixtures of oligomers, remain ambiguous. Our recent studies suggested that catechin B-ring quinones couple with catechin A-rings during the process of oligomerization.

New Trends to Treat Muscular Atrophy: A Systematic Review of Epicatechin.

Epicatechin is a polyphenol compound that promotes skeletal muscle differentiation and counteracts the pathways that participate in the degradation of proteins. Several studies present contradictory results of treatment protocols and therapeutic effects. Therefore, the objective of this systematic review was to investigate the current literature showing the molecular mechanism and clinical protocol of epicatechin in muscle atrophy in humans, animals, and myoblast cell-line. The search was conducted in Embase, PubMed/MEDLINE, Cochrane Library, and Web of Science. The qualitative analysis demonstrated that there is a commonness of epicatechin inhibitory action in myostatin expression and atrogenes MAFbx, FOXO, and MuRF1. Epicatechin showed positive effects on follistatin and on the stimulation of factors related to the myogenic actions (MyoD, Myf5, and myogenin). Furthermore, the literature also showed that epicatechin can interfere with mitochondrias' biosynthesis in muscle fibers, stimulation of the signaling pathways of AKT/mTOR protein production, and amelioration of skeletal musculature performance, particularly when combined with physical exercise. Epicatechin can, for these reasons, exhibit clinical applicability due to the beneficial results under conditions that negatively affect the skeletal musculature. However, there is no protocol standardization or enough clinical evidence to draw more specific conclusions on its therapeutic implementation.

Cocoa flavanols, Nrf2 activation, and oxidative stress in peripheral artery disease: mechanistic findings in muscle based on outcomes from a randomized trial.

The pathophysiology of muscle damage in peripheral artery disease (PAD) includes increased oxidant production and impaired antioxidant defenses. Epicatechin (EPI), a naturally occurring flavanol, has antioxidant properties that may mediate the beneficial effects of natural products such as cocoa. In a phase II randomized trial, a cocoa-flavanol-rich beverage significantly improved walking performance compared with a placebo in people with PAD. In the present work, the molecular mechanisms underlying the therapeutic effect of cocoa flavanols were investigated by analyzing baseline and follow-up muscle biopsies from participants. Increases in nuclear factor erythroid 2-related factor 2 (Nrf2) target antioxidants heme oxygenase-1 (HO-1) and NAD(P)H dehydrogenase [quinone] 1 (NQO1) in the cocoa group were significantly associated with reduced accumulation of central nuclei, a myopathy indicator, in type II muscle fibers (P = 0.017 and P = 0.023, respectively). Protein levels of the mitochondrial respiratory complex III subunit, cytochrome b-c1 complex subunit 2 (UQCRC2), were significantly higher in the cocoa group than in the placebo group (P = 0.032), and increases in UQCRC2 were significantly associated with increased levels of Nrf2 target antioxidants HO-1 and NQO1 (P = 0.001 and P = 0.035, respectively). Exposure of non-PAD human myotubes to ex vivo serum from patients with PAD reduced Nrf2 phosphorylation, an indicator of activation, increased hydrogen peroxide production and oxidative stress, and reduced mitochondrial respiration. Treatment of myotubes with EPI in the presence of serum from patients with PAD increased Nrf2 phosphorylation and protected against PAD serum-induced oxidative stress and mitochondrial dysfunction. Overall, these findings suggest that cocoa flavanols may enhance antioxidant capacity in PAD via Nrf2 activation.NEW & NOTEWORTHY The current study supports the hypothesis that in people with PAD, cocoa flavanols activate Nrf2, thereby increasing antioxidant protein levels, protecting against skeletal muscle damage, and increasing mitochondrial protein abundance. These results suggest that Nrf2 activation may be an important therapeutic target for improving walking performance in people with PAD.

Alleviation effects of epigallocatechin-3-gallate against acute kidney injury following severe burns.

BACKGROUND: Burn patients often face a high risk of acute kidney injury (AKI) after severe burn injuries, meanwhile epigallocatechin-3-gallate (EGCG) has been proven to be effective in alleviating organ injury. METHODS: This study used the classical burn model in rats. Thirty model rats were randomly divided into a Burn group, a Burn + placebo group, a Burn + EGCG (50 mg/kg) group, and ten non-model rats as Sham group. The urinary excretion of the rats was subsequently monitored for a period of 48 h. After 48 h of different treatments, rat serum and kidneys were taken for the further verification. The efficacy of EGCG was assessed in pathological sections, biochemical indexes, and at the molecular level. RESULTS: Pathological sections were compared between the Burn group and Burn + placebo group. The rats in the Burn + EGCG group had less kidney damage. Moreover, the EGCG group maintained significantly elevated urine volumes, biochemical indexes manifested that EGCG could reduce serum creatinine (Cr) and neutrophil gelatinase-associated lipocalin (NGAL) level and inhibit the oxidation-related enzyme malondialdehyde (MDA) level, meanwhile the superoxide dismutase (SOD) level was increased. The molecular level showed that EGCG significantly reduced the mRNA expression levels of the inflammation-related molecules interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α). CONCLUSION: The research indicated that EGCG had an alleviating effect on kidney injury in severely burned rats, and its alleviating effects were related to improving kidney functions, alleviating oxidative stress, and inhibiting the expression of inflammatory factors.

A newly isolated intestinal bacterium involved in the C-ring cleavage of flavan-3-ol monomers and the antioxidant activity of the metabolites.

Flavan-3-ols are an important class of secondary metabolites in many plants. Their bioavailability and bioactivity are largely determined by the metabolism of intestinal microbiota. However, little is known about the intestinal bacteria involved in the metabolism of flavan-3-ols and the activities of the metabolites. C-ring cleavage is the initial and key step in the metabolism of flavan-3-ol monomers. Here, we isolated a strain from porcine cecum content, which is capable of cleaving the heterocyclic C-ring to form 1-(3',4'-dihydroxyphenyl)-3-(2'',4'',6''-trihydroxyphenyl)propan-2-ol from (+)-catechin and (-)-epicatechin, and 1-(3',4',5'-trihydroxyphenyl)-3-(2'',4'',6''-trihydroxyphenyl) propan-2-ol from (-)-epigallocatechin. The strain was identified as Streptococcus pasteurianus (Streptococcus gallolyticus subsp. Pasteurianus, designated as F32-1) based on 16S rDNA similarity and MALDI-TOF-MS identification. The formation of the C-ring cleavage structural unit by the F32-1 strain enhanced the chemical antioxidant ability and altered the cellular antioxidant activity of (+)-catechin, (-)-epicatechin and (-)-epigallocatechin. Overall, in this study we isolated a new intestinal bacterium involved in the C-ring cleavage of flavan-3-ol monomers and elucidated the bioactivity of their metabolites.

The effect of tea catechins on the forensic identification of urine: Urine camouflage to evade drug tests.

BACKGROUND: We encountered a urine sample suspected of being mixed with tea, submitted by a suspect attempting to camouflage illegal drugs. Although urine should turn reddish-pink during a urea test with p-Dimethylaminocinnamaldehyde (DAC), this suspect's sample exhibited a blue coloration when tested with DAC. AIM: Our aim was to examine the influence and mechanism of green tea on various urine identification tests. RESULTS: Our examination revealed that DAC forms a compound with the urea in urine, resulting in a reddish pink coloration with a molecular weight of 217. However, it has been reported that DAC binds to polyphenols such as catechin. In the case of catechin, DAC binds to the C8 position, forming a compound that exhibits the highest absorption at 640 nm and appears blue. we investigated the effect of urine from volunteers who had consumed a large amount of catechin on the urea test with DAC. Additionally, we carried out quantitative analysis of catechin in urine by LC-MS/MS after enzymatic treatment with ß-glucuronidase. The concentration of urinary excreted catechin reached its peak approximately 3 to 4 h after ingestion. During the DAC test, urine samples collected 3 to 4 h after catechin ingestion displayed a bluish pink color, but not the blue color observed in the original suspect sample. CONCLUSION: This study investigated the impact of catechin on urine tests, revealing that a blue color in the DAC test indicates a high likelihood of camouflage by the suspect.

(-)-Epigallocatechin-3-Gallate Reduces Perfluorodecanoic Acid-Exacerbated Adiposity and Hepatic Lipid Accumulation in High-Fat Diet-Fed Male C57BL/6J Mice.

Perfluorodecanoic acid (PFDA), an enduring and harmful organic pollutant, is widely employed in diverse food-related sectors. Our previous studies have provided evidence that PFDA has the potential to facilitate obesity and hepatic fat accumulation induced by high-fat diet (HFD) intake. Epigallocatechin-3-gallate (EGCG), a polyphenol found in green tea, has been suggested to possess potential preventive effects against metabolic abnormalities and fatty liver. The purpose of this research was to investigate the effects of EGCG on PFDA-exacerbated adiposity and hepatic lipid accumulation in HFD-fed mice. The results showed that EGCG reduced body weight gain; tissue and organ weights; blood glucose, serum insulin, HOMA-IR, leptin, and lipid parameters; serum inflammatory cytokines (IL-1ß, IL-18, IL-6, and TNF-α); and hepatic lipid accumulation in PFDA-exposed mice fed an HFD. Further work showed that EGCG improved liver function and glucose homeostasis in mice fed an HFD and co-exposed to PFDA. The elevated hepatic mRNA levels of SREBP-1 and associated lipogenic genes, NLRP3, and caspase-1 in PFDA-exposed mice fed an HFD were significantly decreased by EGCG. Our work provides evidence for the potential anti-obesity effect of EGCG on co-exposure to HFD and PFDA and may call for further research on the bioactivity of EGCG to attenuate the endocrine disruption effects of long-term exposure to pollutants.

Green Tea-Derived Catechins Suppress the Acid Productions of Streptococcus mutans and Enhance the Efficiency of Fluoride.

Green tea-derived catechins, which can be divided into galloylated (epicatechin gallate: ECG, epigallocatechin gallate: EGCG) and non-galloylated (catechin: C, epicatechin: EC, epigallocatechin: EGC) catechins, are considered to be the main contributors to the caries control potential of green tea. In this study, we intended to compare the antimicrobial effects of these representative green tea-derived catechins and their combined effects with fluoride on the acid production and aggregation of Streptococcus mutans. The effects of different catechins on the growth, aggregation and acid production of S. mutans, and the combined effect of catechins and potassium fluoride (2 mm at pH 7.0, 0.3 mm at pH 5.5) on S. mutans acid production were measured by anaerobic culture, turbidity changes due to aggregation, and pH-stat methods. Molecular docking simulations were also performed to investigate the interactions between catechins and membrane-embedded enzyme II complex (EIIC), a component of the phosphoenolpyruvate-dependent phosphotransferase system (sugar uptake-related enzyme). ECG or EGCG at 1 mg/mL significantly inhibited the growth of S. mutans, induced bacterial aggregation, and decreased glucose-induced acid production (p < 0.05). All catechins were able to bind to EIIC in silico, in the following order of affinity: EGCG, ECG, EGC, EC, and C. Furthermore, they enhanced the inhibitory effects of fluoride at pH 5.5 and significantly inhibited S. mutans acid production by 47.5-86.6% (p < 0.05). These results suggest that both galloylated and non-galloylated catechins exhibit antimicrobial activity, although the former type demonstrates stronger activity, and that the caries control effects of green tea may be due to the combined effects of multiple components, such as catechins and fluoride. The detailed mechanisms underlying these phenomena and the in vivo effect need to be explored further.

A gold-complex initiated functionalization of biologically active polyphenols applied to a 18F-labeled chemical probe.

(-)-Epigallocatechin gallate (EGCG), a key component of green tea, exerts therapeutic anticancer and antiallergic properties through its binding to the 67 kDa laminin receptor. The functionalization of EGCG is a promising strategy for creating new drug candidates and chemical probes. In our study, we developed a method for effectively modifying the A ring of EGCG through an electrophilic aromatic substitution with amidomethyl 2-alkynylbenzoates initiated with a gold complex. The 2-alkynylbenzoates treated with (Ph3P)AuOTf under neutral conditions yielded N-acylimines. A further electrophilic aromatic substitution resulted in a mixture of EGCG substituted with acylaminomethyl groups at the 6 and 8 positions with a significant amount noted at the 6 position. We then explored the synthesis of 18F-labeled EGCG with a neopentyl labeling group, an effective labeling group for radiohalogens of not only fluorine-18 but also of astatine-211. To achieve this, we prepared precursors that possessed acid-sensitive protecting groups and base-unstable leaving groups using our established method. Substitution of EGCG with a neopentyl labeling group at either the C6 or C8 position did not affect its anticancer efficacy in U266 cells. Finally, we investigated the preparation of 18F-labeled EGCG. The 18F-fluorination of a mixture of 6- and 8-substituted precursors yielded the corresponding 18F-labeled compounds in 4.5% and 3.0% radiochemical yields (RCYs), respectively. Under acidic conditions, the 18F-labeled 8-substituted compound produced 18F-labeled EGCG in 37% RCY, which heralds the potential of our functionalization approach.

An unconventional proanthocyanidin pathway in maize.

Proanthocyanidins (PAs), flavonoid polymers involved in plant defense, are also beneficial to human health and ruminant nutrition. To date, there is little evidence for accumulation of PAs in maize (Zea mays), although maize makes anthocyanins and possesses the key enzyme of the PA pathway, anthocyanidin reductase (ANR). Here, we explore whether there is a functional PA biosynthesis pathway in maize using a combination of analytical chemistry and genetic approaches. The endogenous PA biosynthetic machinery in maize preferentially produces the unusual PA precursor (+)-epicatechin, as well as 4ß-(S-cysteinyl)-catechin, as potential PA starter and extension units. Uncommon procyanidin dimers with (+)-epicatechin as starter unit are also found. Expression of soybean (Glycine max) anthocyanidin reductase 1 (ANR1) in maize seeds increases the levels of 4ß-(S-cysteinyl)-epicatechin and procyanidin dimers mainly using (-)-epicatechin as starter units. Introducing a Sorghum bicolor transcription factor (SbTT2) specifically regulating PA biosynthesis into a maize inbred deficient in anthocyanin biosynthesis activates both anthocyanin and PA biosynthesis pathways, suggesting conservation of the PA regulatory machinery across species. Our data support the divergence of PA biosynthesis across plant species and offer perspectives for future agricultrural applications in maize.

Hormetic effects of EGC and EGCG on CES1 activity and its rescue from oxidative stress in rat liver S9.

Carboxylesterase 1 (CES1) is a hydrolytic enzyme that plays an important role in the activation or deactivation of many therapeutic agents, thus affecting their pharmacokinetic and pharmacodynamic outcomes. Using rat liver S9 as an enzyme source and enalapril as a CES1 substrate, the present study examined effects of a number of flavonoids on the formation of enalaprilat (the active form of enalapril) produced by CES1-mediated hydrolysis. While a majority of flavonoids tested showed inhibition on CES1, an unexpected hormetic effect was observed for epigallocatechin (EGC) and epigallocatechin gallate (EGCG), i.e., stimulatory effect at low concentrations and enzyme inhibition at high concentrations. Further experiments revealed that oxidative stress caused by hydrogen peroxide, arachidonic acid plus iron, and oxidized low density lipoproteins (oxLOL) reduced CES1 activity in rat liver S9 and the loss of CES1 enzyme activity could be rescued largely by EGC or EGCG. In contrast, such effects were minimal in human liver S9, probably due to the presence of a higher ratio of reduced vs oxidized forms of glutathione. The above findings suggest that the polyphenolic nature of EGC or EGCG might be responsible for rescuing CES1 activity under oxidative stress. Because of the importance of CES1 in drug activation or deactivation and rat liver S9 as a versatile in vitro system used for drug metabolism studies and drug safety assessment, caution should be exercised to avoid potential biases for data interpretation and decision making when CES1 activity in rat liver S9 is evaluated with dependency on experimental conditions.

Black and pinto beans (Phaseolus vulgaris L.) unique mexican varieties exhibit antioxidant and anti-inflammatory potential.

Oxidative stress and inflammation play a key role in diverse pathological conditions such as cancer and metabolic disorders. The objective of this study was to determine the antioxidant and anti-inflammatory potentials of crude extract (CE) and phenolic-enriched extract (PHE) obtained from the seed coats (SCs) of black bean (BB) and pinto bean (PB) varieties. Delphinidin-3-O-glucoside (46 mg/g SC), malvidin-3-O-glucoside (29.9 mg/g SC), and petunidin-3-O-glucoside (7.5 mg/g SC) were found in major concentrations in the PHE-BB. Pelargonidin (0.53 mg/g SC) was only identified in the PHE-PB. PHE from both varieties showed antioxidant and radical scavenging capacities, with strong correlations associated with total phenolic content (TPC). Polyphenolics, including catechin, myricetin, kaempferol, quercetin, and isorhamnetin glucosides, were identified in the extracts. In terms of the anti-inflammatory potentials, PHE-PB had an IC50 of 10.5 µg dry extract/mL (µg DE/mL) for cyclooxygenase-2 (COX-2) inhibition. The inhibition values for cyclooxygenase-1 (COX-1) ranged from 118.1 to 162.7 µg DE/mL. Regarding inducible nitric oxide synthase (iNOS) inhibition, PHE-BB had an IC50 of 62.6 µg DE/mL. As determined via in silico analysis, pelargonidin showed binding affinities of -7.8 and -8.5 kcal/mol for COX-1 and iNOS, respectively, and catechin had a value of -8.3 kcal/mol for COX-2. Phenolic-enriched extracts from seed coats of black and pinto beans showed good antioxidant and anti-inflammatory potential that warrants in vitro and in vivo studies.

Tea polyphenol EGCG ameliorates obesity-related complications by regulating lipidomic pathway in leptin receptor knockout rats.

Tea polyphenol epigallocatechin-3-gallate (EGCG) has been widely recognized for antiobesity effects. However, the molecular mechanism of lipidomic pathway related to lipid-lowering effect of EGCG is still not well understood. The aim of this study was to investigate the effects and mechanism of EGCG activated hepatic lipidomic pathways on ameliorating obesity-related complications by using newly developed leptin receptor knockout (Lepr KO) rats. Results showed that EGCG supplementation (100 mg/kg body weight) significantly decreased total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C) and triglyceride (TG) levels both in the serum and liver, and significantly improved glucose intolerance. In addition, EGCG alleviated fatty liver development and restored the normal liver function in Lepr KO rats. Liver lipidomic analysis revealed that EGCG dramatically changes overall composition of lipid classes. Notably, EGCG significantly decreased an array of triglycerides (TGs) and diglycerides (DGs) levels. While EGCG increased 31 glycerophospholipid species and one sphingolipid species levels, such as phosphatidylcholines (PCs), phosphatidylethanolamines (PEs), phosphatidylserines (PSs) and phosphatidylinositols (PIs) levels in the liver of Lepr KO rats. Moreover, 14 diversely regulated lipid species were identified as potential lipid biomarkers. Mechanistic analysis revealed that EGCG significantly activated the SIRT6/AMPK/SREBP1/FAS pathway to decrease DGs and TGs levels and upregulated glycerophospholipids synthesis pathways to increase glycerophospholipid level in the liver of Lepr KO rats. These findings suggested that the regulation of glycerolipids and glycerophospholipid homeostasis might be the key pathways for EGCG in ameliorating obesity-related complications in Lepr KO rats.

An In Vitro Catalysis of Tea Polyphenols by Polyphenol Oxidase.

Tea polyphenol (TPs) oxidation caused by polyphenol oxidase (PPO) in manufacturing is responsible for the sensory characteristics and health function of fermented tea, therefore, this subject is rich in scientific and commercial interests. In this work, an in vitro catalysis of TPs in liquid nitrogen grinding of sun-dried green tea leaves by PPO was developed, and the changes in metabolites were analyzed by metabolomics. A total of 441 metabolites were identified in the catalyzed tea powder and control check samples, which were classified into 11 classes, including flavonoids (125 metabolites), phenolic acids (67 metabolites), and lipids (55 metabolites). The relative levels of 28 metabolites after catalysis were decreased significantly (variable importance in projection (VIP) > 1.0, p < 0.05, and fold change (FC) < 0.5)), while the relative levels of 45 metabolites, including theaflavin, theaflavin-3'-gallate, theaflavin-3-gallate, and theaflavin 3,3'-digallate were increased significantly (VIP > 1.0, p < 0.05, and FC > 2). The increase in theaflavins was associated with the polymerization of catechins catalyzed by PPO. This work provided an in vitro method for the study of the catalysis of enzymes in tea leaves.

EGCG alleviated Mn exposure-caused carp kidney damage via trpm2-NLRP3-TNF-α-JNK pathway: Oxidative stress, inflammation, and tight junction dysfunction.

Manganese (Mn), an essential trace metal element in organisms. However, with extensive use of Mn in industry and agriculture, Mn becomes a heavy metal pollutant in water. (-)-epigallocatechin gallate (EGCG), an tea polyphenols, can alleviate metal toxicity. Kidney is an important detoxifying organ, but toxic mechanism of Mn to kidneys is unclear, which needs further research. Carp is an Asian important economical species for fisheries and a biological model for studying environmental toxicology. Thus, we established excess Mn and EGCG-supplemented carp model to explore molecular mechanism of EGCG alleviating Mn-caused carp kidney damage. In this experiment, we set a control group (the Con group), a Mn treatment group (the Mn group, 90 mg/L Mn), a EGCG supplement group (the EG group, 75 mg/kg EGCG), and a combined group (the Mn + EG group, 90 mg/L Mn and 75 mg/kg EGCG). Transcriptome, qRT-PCR, kit, and morphology method results indicated that excess Mn caused oxidative stress, inflammatory damage, and tight junction dysfunction in carp kidneys. Excess Mn-triggered oxidative stress caused tight junction dysfunction via trpm2-NLRP3-TNF-α-JNK pathway and inflammation. EGCG reversed the harm of Mn to fish through the above mechanism. The findings of this study provided the evidence of EGCG-alleviated Mn poisoning and offered new ideas for reducing heavy metal environmental pollution risk.

The plant specialized metabolite epicatechin- 3-gallate (EC3G) perturbs lipid metabolism and attenuates fat accumulation in pigeonpea pod borer, Helicoverpa armigera.

Control of pod borer Helicoverpa armigera, a notorious polyphagous pest requires paramount attention with focus on environment-friendly management approaches. Overproduction of catechins (epigallocatechin-EGC and epicatechin-3-gallate-EC3G) in the pod borer-resistant pigeonpea wild relative, Cajanus platycarpus during continued herbivory prodded us to assess their underlying molecular effect on H. armigera. Significant reduction in larval and pupal growth parameters was observed when reared on artificial diet incorporated with 100 ppm EC3G vis a vis 100 ppm EGC and EGC + EC3G. Comparative RNAseq analyses of larvae that fed on normal and EC3G-incorporated diet revealed 62 differentially expressed genes dominated by detoxification and lipid metabolism. While lipase and fatty acid-binding protein 2-like were up-regulated, delta9-FADS-like involved in fatty acid synthesis was downregulated, indicating effect of EC3G on fat metabolism. Validation of RNAseq data by qPCR; midgut glutathione-S-transferase and esterase assays depicted increased lipolysis and reduced lipogenesis in EC3G-fed larvae. Additionally, differential accumulation of stearic acid and oleic acid in EC3G-fed and control larvae/adults ascertained perturbation in lipogenesis. Supported by modelling, molecular docking and simulations, we demonstrate the possible involvement of the insect adipokinetic hormone receptor (AKHR) in the EC3G-mediated response. The study demonstrates plant specialized metabolite EC3G as a potential candidate for H. armigera control.