Use Of Epigallocatechin-3-gallate Research Articles

The Potential of Epigallocatechin Gallate in Targeting Cancer Stem Cells: A Comprehensive Review.

The dreadful scenario of cancer prevails due to the presence of cancer stem cells (CSCs), which contribute to tumor growth, metastasis, invasion, resistance to chemo- and radiotherapy, and recurrence. CSCs are a small subpopulation of cells within the tumor that are characterized by self-renewal capability and have the potential to manifest heterogeneous lineages of cancer cells that constitute the tumor. The major bioactive green tea polyphenol (-)-epigallocatechin gallate (EGCG) has been fruitful in downgrading cancer stemness signaling and CSC biomarkers in cancer progression. EGCG has been evidenced to maneuver extrinsic and intrinsic apoptotic pathways in order to decrease the viability of CSCs. Cancer stemness is intricately related to epithelial-mesenchymal transition (EMT), metastasis and therapy resistance, and EGCG has been evidenced to regress all these CSC-related effects. By inhibiting CSC characteristics EGCG has also been evidenced to sensitize the tumor cells to radiotherapy and chemotherapy. However, the use of EGCG in in vitro and in vivo cancer models raises concern about its bioavailability, stability and efficacy against spheroids raised from parental cells. Therefore, novel nano formulations of EGCG and adjuvant therapy of EGCG with other phytochemicals or drugs or small molecules may have a better prospect in targeting CSCs. However, extensive clinical research is still awaited to elucidate a full proof impact of EGCG in cancer therapy.

Epigallocatechin-3-gallate Synergistically Enhanced Arecoline-Induced Cytotoxicity by Redirecting Cycle Arrest to Apoptosis.

Carcinogens, such as arecoline, play a crucial role in cancer progression and continuous gene mutations by generating reactive oxygen species (ROS). Antioxidants can reduce ROS levels and potentially prevent cancer progression but may paradoxically enhance the survival of cancer cells. This study investigated whether epigallocatechin-3-gallate (EGCG), an antioxidant from green tea, could resolve this paradox. Prostate cancer cells (PC-3 cell line) were cultured and treated with arecoline combined with NAC (N-acetylcysteine) or EGCG; the combined effects on intracellular ROS levels and cell viability were examined using the MTT and DCFDA assays, respectively. In addition, apoptosis, cell cycle, and protein expression were investigated using flow cytometry and western blot analysis. Our results showed that EGCG, similar to NAC (N-acetylcysteine), reduced the intracellular ROS levels, which were elevated by arecoline. Moreover, EGCG not only caused cell cycle arrest but also facilitated cell apoptosis in arecoline-treated cells in a synergistic manner. These were evidenced by elevated levels of cyclin B1 and p27, and increased fragmentation of procaspase-3, PARP, and DNA. Our findings highlight the potential use of EGCG for cancer prevention and therapy.

Epigallocatechin Gallate Modulates Microglia Phenotype to Suppress Pro-inflammatory Signalling Cues and Inhibit Phagocytosis

Microglia are crucial players in the pathogenesis of late-onset Alzheimer’s disease (AD), with evidence for both deleterious and beneficial effects. Identifying interventions to modulate microglial responsiveness, promote amyloid β (Aβ) clearance, disrupt plaque formation, or dampen excessive inflammation has therapeutic potential. Bioavailable flavonoids, such as the flavan 3-ols, are of interest due to their antioxidant, metal chelating, signalling, and anti-inflammatory potential. Primary microglia were treated with a series of structurally related flavanol 3-ols to assess effects on phagocytosis, cytokine release, and transcriptional responses by RNA sequencing. Data indicated that the extent of hydroxylation and the presence of the galloyl moiety were strong determinants of flavan 3-ol activity. Epigallocatechin gallate (EGCG) was the most effective flavan-3-ol tested and strongly inhibited phagocytosis of Aβ independent of any metal chelating properties, suggesting a more direct modulation of microglia responsiveness. EGCG was broadly anti-inflammatory, reducing cytokine release and downregulating transcription, particularly of components of the microglia extracellular matrix such as MMP3 and SerpinB2. Collectively, this brings new insight into the actions of flavonoids on microglial responsiveness with potential implications for the therapeutic use of EGCG and structurally related flavanol-3-ols in AD.

Investigation of the inhibitory combined effect and mechanism of (−)-epigallocatechin gallate and chlorogenic acid on amylase: Evidence of synergistic interaction

Both (−) -epigallocatechin gallate (EGCG) and chlorogenic acid (CHA) have shown inhibitory effects on α-amylase. However, there may be synergistic or antagonistic effects among them. This study utilized the ZIP model to examine the inhibitory impact of EGCG and CHA on amylase and analyze the mechanism of inhibition. The results showed that EGCG and CHA had a significant synergistic effect when the EGCG was between 0.25 and 0.5 mg/mL and the CHA was 2–4 mg/mL. The optimal synergistic ratio was EGCG:CHA = 1:8. The inhibitory kinetics indicate that EGCG, CHA, and the complex exhibit competitive inhibition, mixed inhibition, and mixed inhibition towards α-amylase, respectively. Fluorescence spectroscopy revealed that the combined use of EGCG and CHA exhibited a more significant quenching effect. The findings from synchronous fluorescence and molecular docking analyses further demonstrated that EGCG and CHA exhibited interactions with distinct amino acids and occupied separate binding sites simultaneously. This study aims to provide valuable insights into the blending of tea and coffee, with the hope of generating new ideas for the development of hypoglycemic food products.

Green Tea Derivative (–)-Epigallocatechin-3-Gallate (EGCG) for Prevention of Acute Radiation-Induced Intestinal Injury: A Prospective Phase II Clinical Study in Pelvic Cancer Patients

Radiation-induced intestinal injury (RIII) remains the most common dose-limiting toxicity following radiotherapy (RT) for pelvic malignancies. However, few efficient and safe methods for the prevention of RIII are available in the clinical practice. Our previous study proved that the green tea polyphenol (-)-epigallocatechin-3-gallate (EGCG) efficiently attenuates radiation-induced intestinal injury (RIII) in animal level. Therefore, this prospective phase II clinical study (ChiCTR2100053703) evaluated the efficacy of EGCG in the prevention of RIII. Cervical or endometrial cancer patients who received adjuvant or radical RT in our department were enrolled, 400mg EGCG was taken daily, and RIII was evaluated weekly according to the RTOG criteria. Between February 2022 to January 2023, 37 patients were enrolled (30 were cervical cancer and the other 7 were endometrial cancer), and were followed-up regularly. Among them, the majority patients (75.7%, 28 patients) developed grade 0 or 1 RIII, for which no medical intervention was required. Meanwhile, the occurrence of grade 2 RIII was 24.3% (9 patients), which was significantly lower than that in the historical controls (usually 60% to 80%). Besides that, no patients developed grade 3 or worse RIII. In this phase II clinical trial, compared to historical controls, the prophylactic use of EGCG significantly reduced the incidence and severity of RIII in patients receiving pelvic RT. Therefore, EGCG has the potential to become a novel medical countermeasure for the prevention of RIII for pelvic cancer patients.

Dual regulations on texture and water mobility of shrimp surimi gel with sustained-release epigallocatechin-3-gallate in γ-cyclodextrin metal organic frameworks: Insights into functionality and mechanisms

Epigallocatechin-3-gallate (EGCG) could demonstrate crosslinking effects on myofibrillar proteins, yet its proneness to self-aggregation could bring excessive crosslinking and water loss within gels, hindering its application as an additive during thermal gelation process. Here, encapsulation with the γ-cyclodextrin metal organic framework (γ-CD-MOF) before the use of EGCG was found to play a dual role: alleviating over-crosslinking of proteins and elevating water retention within gels. Results showed that EGCG got a sustainable release throughout the thermal process due to the gradual fracture of O-K coordinate bounds and structural collapse of γ-CD-MOF. Mechanism insights revealed that the use of EGCG loaded γ-CD-MOF (EGCG@γ-CD-MOF) could regulate formation efficiency on disulfide bounds and promote protonation transition of the amino groups in proteins. Moreover, EGCG@γ-CD-MOF brought a higher retention of phenols within gels through preventing oxidative transformation of phenols towards quinones, which were verified to display a higher affinity towards myosin via molecular calculations.

Epigallocatechin Gallate Affects the Structure of Chromatosomes, Nucleosomes and Their Complexes with PARP1.

The natural flavonoid epigallocatechin gallate has a wide range of biological activities, including being capable of binding to nucleic acids; however, the mechanisms of the interactions of epigallocatechin gallate with DNA organized in chromatin have not been systematically studied. In this work, the interactions of epigallocatechin gallate with chromatin in cells and with nucleosomes and chromatosomes in vitro were studied using fluorescent microscopy and single-particle Förster resonance energy transfer approaches, respectively. Epigallocatechin gallate effectively penetrates into the nuclei of living cells and binds to DNA there. The interaction of epigallocatechin gallate with nucleosomes in vitro induces a large-scale, reversible uncoiling of nucleosomal DNA that occurs without the dissociation of DNA or core histones at sub- and low-micromolar concentrations of epigallocatechin gallate. Epigallocatechin gallate does not reduce the catalytic activity of poly(ADP-ribose) polymerase 1, but causes the modulation of the structure of the enzyme-nucleosome complex. Epigallocatechin gallate significantly changes the structure of chromatosomes, but does not cause the dissociation of the linker histone. The reorganization of nucleosomes and chromatosomes through the use of epigallocatechin gallate could facilitate access to protein factors involved in DNA repair, replication and transcription to DNA and, thus, might contribute to the modulation of gene expression through the use of epigallocatechin gallate, which was reported earlier.

Investigation of the inhibitory effect and mechanism of EGCG against Streptococcus suis sortase A.

Streptococcus suis (S. suis) seriously harms people and animals, and importantly, causes great economic losses in the pig industry. Similar to most gram-positive pathogenic bacteria, sortase A (SrtA) of S. suis can mediate the anchoring of a variety of virulence factors that contain specific sorting sequences to the surface of the bacterial cell wall envelope and participate in pathogenicity. The purpose of this study is to clarify the molecular mechanism of epigallocatechin-3-gallate (EGCG) inhibiting Streptococcus suis SrtA and provide more evidence for the development of novel anti- Streptococcus suis infections drugs. Through the SrtA substrate cleavage experiment, we found that the main component of green tea, EGCG, can effectively inhibit the enzyme activity of Streptococcus suis SrtA. Further, molecular docking and molecular dynamics simulation were used to clarify the molecular mechanism of its inhibitory effect, demonstrating that EGCG mainly interacts with amino acids at 113 and 115 to exert its inhibitory function. It was previously found that EGCG can inhibit the growth of S. suis and reduce the activity of suilysin and inhibit its expression. Our research reveals a new function of EGCG in S. suis infection. Our research proves that EGCG can effectively inhibit the transpeptidase activity of SrtA. We also clarify the accompanying molecular mechanism, providing more sufficient evidence for the use of EGCG as a potential lead compound against S. suis infection.

Efficacy and safety of epigallocatechin-3-gallate in treatment acute severe dermatitis in patients with cancer receiving radiotherapy: a phase I clinical trial

To evaluate the safety and effectiveness of epigallocatechin-3-gallate (EGCG) solution treating the acute severe dermatitis in patients receiving radiotherapy. This phase I research enrolled patients with thoracic cancer receiving radiotherapy at Shandong Cancer Hospital and Institute in Shandong, China. EGCG solution was sprayed to the radiation field when grade III radiation-induced dermatitis (RID) first appearance. EGCG concentration escalated from 660 to 2574 μmol/L using modified-Fibonacci dose-escalation. RID and related symptoms were followed up every day. Between March 2021 and November 2021, 19 patients were enrolled in this phase I research. The median dose of grade III RID first observation was 44 Gy (30.6–52 Gy). As the EGCG treatment was performed continuously, all these grade III RID reactions were significantly decreased to grade I or grade II RID at three days after use of EGCG (p < 0.001). Significant relief can be observed in burning sensation (p < 0.001), tractive sensation (p < 0.001), tenderness (p < 0.001), erythema (p < 0.001), itching (p < 0.001) and pain (p < 0.001) after 15 days of EGCG treatment. No radiation therapy delay or interruption for all 19 patients. No adverse events were observed and reported associated with EGCG. The highest dose of this Phase I trial (2574 μmol/L) was recommended for continuous Phase II trial for further evaluation. In this phase I clinical research, use of EGCG solution is safe and can significantly relief grade III RID in patients receiving radiotherapy. Thus, EGCG might be a new choice for acute sever RID.Trial Registration: ClinicalTrials.gov Identifier: NCT02580279 (Full date of first registration: 12/2014).

Influence of green tea on alcohol aggravated neurodegeneration of cortex, cerebellum and hippocampus of STZ-induced diabetic rats

The main aim of this study was to evaluate the cytotoxic effects of chronic alcohol consumption on various regions of diabetic brain and preventive role of GTE. Clinical, experimental and histopathological observations indicate chronic, excessive alcohol consumption aggravates the free radical-mediated oxidative and nitrosative stress in several tissues including brain. Treatment with Epigallocatechin gallate (EGCG) significantly reduced the levels of oxidative/nitrosative stress paradigms, increased glutathione (GSH) levels and enhanced the activities of antioxidant enzymes. Histopathology evaluation revealed the possible influence of EGCG in reversing alcohol exacerbated diabetes-induced damage in cortex, cerebellum and hippocampus of brain. Furthermore, these studies have provided evidence to show how EGCG can exactly occupy the position in functional sites of nNOS (neuronal nitric oxide synthase) and induce a conformational change, inhibition of enzymatic activity and prevention of neurodegeneration/necrotic changes of tissue, in comparison with the rosiglitazone and glibenclamide. To summarise, this research has offered useful information on the action of EGCG that would provide potential protection against ethanol exacerbated diabetic brain damageand additional evidence for the use of EGCG as a lead compound for drug discovery.

Mechanism of oxidative damage in Escherichia coli caused by epigallocatechin gallate (EGCG) in the presence of calcium ions

Abstract Tea polyphenols can be developed into new types of disinfectants for drinking water. The antibacterial effect of epigallocatechin gallate (EGCG) on Escherichia coli (E. coli) in the presence of Ca2+ is affected by the Ca2+ concentration. The oxidative damage mechanism and oxidative damage process of EGCG in E. coli under the presence of Ca2+ were deeply analyzed under three aspects: reactive oxygen species (ROS), antioxidant system, and oxidative stress response in E. coli to provide a theoretical basis for the use of EGCG as a disinfectant in drinking water disinfection. EGCG leads to excessive production of superoxide anion in E. coli and the presence of Ca2+ promotes further imbalance of superoxide anion in E. coli; Ca2+ has little effect on EGCG hindering the scavenging of hydroxyl radicals in bacteria; EGCG can hinder the effect of antioxidant enzymes in E. coli, and Ca2+ has a particular regulatory effect on antioxidant enzymes, thus hindering the oxidative damage of EGCG to E. coli; Ca2+ can cause the expression of the oxyR and DPS genes, protect bacterial DNA, and prevent EGCG from damaging bacterial DNA. In the presence of a high concentration of Ca2+, it may activate the cell efflux pump through the soxS gene, resulting in E. coli resistance to EGCG.

Epigallocatechin-3-gallate improves the biocompatibility of bone substitutes in dental pulp stem cells

BackgroundThe Biocompatibility between osteoprogenitor cells and bone substitutes is necessary for cell differentiation and osteogenesis. The aim of this study was to assess the in vitro effect of bovine (Geistlich BioOss®), porcine (OsteoBiol Gen-Os®) and beta-tricalcium phosphate (Cerasorb M®) bone substitutes, and their combination with polyphenol epigallocatechin-3-gallate (EGCG), upon cultured dental pulp stem cells (DPSCs). MethodsThe DPSCs were isolated from third molars extracted from healthy individuals and seeded with 5 mg/ml of Bio-Oss® (BO), Gen-Os® (GO) and Cerasorb® (CE) in combination with EGCG 1 μM. The effects were evaluated based on cell viability / cytotoxicity assay (MTT, cell viability staining test), cell migration, scanning electron microscopy (SEM), and alkaline phosphatase (ALP) activity. ResultsBO and CE produced negative effects upon cell viability and migration, and GO and CE resulted in deficient cell adhesion. On the other hand, all the biomaterials exerted no negative effects upon ALP activity. Interestingly, the addition of EGCG reverted the cytotoxic effect and the loss of migration capacity in the BO and CE groups, and improved cell adhesion in the GO and CE groups. Furthermore, EGCG promoted an overall increased in ALP activity. ConclusionThe addition of EGCG to the tested biomaterials BO, GO and CE reverts their negative impact on DPSCs, and improves their biocompatibility with cultured DPSCs. The use of EGCG, thus, appears to be a promising strategy for restoring and enhancing the osteoconductive properties of BO, GO and CE in bone regeneration treatments.

Epigallocatechin-3-gallate Delivered in Nanoparticles Increases Cytotoxicity in Three Breast Carcinoma Cell Lines.

The anticancer activity of epigallocatechin-3-gallate (EGCG), orally administrated, is limited by poor bioavailability, absorption, and unpredictable distribution in human tissues. EGCG charged nanoparticles may represent an opportunity to overcome these limitations. We assayed two different kinds of lipid nanoparticles (LNPs and LNPs functionalized with folic acid) charged with EGCG on three breast carcinoma cell lines (MCF-7, MDA-MB-231, and MCF-7TAM) and the human normal MCF10A mammary epithelial cells. Both LNPs loaded with EGCG, at low concentrations, induced a significant cytotoxicity in the three breast carcinoma cells but not in MCF10A cells. In view of a future application, both LNPs and LNPs-FA were found to be very suitable for in vitro studies and useful to improve EGCG administration in vivo. Since they are produced by inexpensive procedures using bioavailable, biocompatible, and biodegradable molecules, they represent an applicable tool for a more rationale use of EGCG as an anti-cancer agent.

Safety and Efficacy of Dietary Epigallocatechin Gallate Supplementation in Attenuating Hypertension via Its Modulatory Activities on the Intrarenal Renin-Angiotensin System in Spontaneously Hypertensive Rats.

This study aimed to identify the no-observed-adverse-effect level (NOAEL) of dietary epigallocatechin gallate (EGCG) supplementation and its possible antihypertensive and nutrigenomics effects in modulating intrarenal renin-angiotensin system (RAS) gene expression in spontaneously hypertensive rats (SHR). EGCG (50, 250, 500 or 1000 mg/kg b.w. i.g., once daily) was administered to SHR for 28 days. All the SHR survived with no signs of systemic toxicity. Increased alanine aminotransferase (ALT), aspartate aminotransferase (AST) and thiobarbituric acid reactive substances (TBARS) were evident in SHR supplemented with 500 and 1000 mg/kg b.w. but not in those supplemented with lower doses of EGCG. Subsequently, the NOAEL of EGCG was established at 250 mg/kg b.w., and the same protocol was replicated to assess its effects on blood pressure and renal RAS-related genes in SHR. The systolic blood pressure (SBP) of the EGCG group was consistently lower than the control group. The mRNA levels of cortical Agtr2 and Ace2 and medullary Agtr2, Ace and Mas1 were upregulated while medullary Ren was downregulated in EGCG group. Statistical analysis showed that SBP reduction was associated with the changes in medullary Agtr2, Ace, and Ren. Dietary EGCG supplementation exhibits antihypertensive and nutrigenomics effects through activation of intrarenal Ace and Agtr2 and suppression of Ren mediators, while a high dose of EGCG induced liver damage in SHR. In future clinical studies, liver damage biomarkers should be closely monitored to further establish the safety of the long-term use of EGCG.

Metabolomics strategy comprehensively unveils the effect of catechins intervention on the biomarkers of exposure to acrylamide and biomarkers of cardiometabolic risk

Polyphenolic antioxidants have been suggested to control the generation of acrylamide during thermal reactions. However, their role in protecting against the toxicity of acrylamide and the mechanism of action regarding profile alteration of biomarkers and metabolome remains unclear. A total of 65 adults were randomized into tea polyphenols (TP) and control groups and served with potato chips, which corresponded to an intake level of 12.6 μg/kg·bw of acrylamide, followed by capsules containing 200 mg, 100 mg or 50 mg TP, or equivalent placebo. Moreover, nontargeted urinary metabolomics analysis in acrylamide exposed rats was conducted using ultra-high performance liquid chromatography linked with a quadrupole-orbitrap high-resolution mass spectrometry. Our results showed that supplementation with catechins promoted the excretion of N-acetyl-S-(2-carbamoyl-2-hydroxyethyl)-l-cysteine in both humans and rats. We also found that epigallocatechin gallate (EGCG) or epicatechin (EC) intervention attenuated the ratio of hemoglobin adduct of glycidamide to hemoglobin adduct of acrylamide in rat blood. Metabolomics analysis revealed that EGCG/EC intervention regulated the differential expressed metabolites, including l-glutamic acid, 2-oxoglutarate, citric acid, and cysteinylglycine. Kyoto Encyclopedia of Genes and Genomes pathway analysis further showed acrylamide-induced metabolic disorders were improved after EGCG/EC supplementation by glycolipid metabolism (alanine, aspartate and glutamate metabolism, and d-Glutamine and d-glutamate metabolism) and energy metabolism (tricarboxylic acid cycle). Notably, the supplement use of EGCG prevented the cardiometabolic risk after exposure to acrylamide by mediating the phenylalanine and hippuric acid in phenylalanine metabolism. Here we showed the beneficial effect of catechins as major polyphenolic antioxidant ingredients on the toxicity of acrylamide by the changes in biomarkers from metabolic profile analysis based on human and animal studies. These findings shed light into the catechins as natural polyphenolic antioxidants that could be a therapeutic ingredient for preventing acrylamide-induced cardiometabolic toxicity.

Green Tea Polyphenol (-)-Epigallocatechin-3-Gallate (EGCG): A Time for a New Player in the Treatment of Respiratory Diseases?

(-)-Epigallocatechin-3-gallate (EGCG) is a major polyphenol of green tea that possesses a wide variety of actions. EGCG acts as a strong antioxidant which effectively scavenges reactive oxygen species (ROS), inhibits pro-oxidant enzymes including NADPH oxidase, activates antioxidant systems including superoxide dismutase, catalase, or glutathione, and reduces abundant production of nitric oxide metabolites by inducible nitric oxide synthase. ECGC also exerts potent anti-inflammatory, anti-fibrotic, pro-apoptotic, anti-tumorous, and metabolic effects via modulation of a variety of intracellular signaling cascades. Based on this knowledge, the use of EGCG could be of benefit in respiratory diseases with acute or chronic inflammatory, oxidative, and fibrotizing processes in their pathogenesis. This article reviews current information on the biological effects of EGCG in those respiratory diseases or animal models in which EGCG has been administered, i.e., acute respiratory distress syndrome, respiratory infections, COVID-19, bronchial asthma, chronic obstructive pulmonary disease, lung fibrosis, silicosis, lung cancer, pulmonary hypertension, and lung embolism, and critically discusses effectiveness of EGCG administration in these respiratory disorders. For this review, articles in English language from the PubMed database were used.

A mucoadhesive gingival patch with Epigallocatechin-3-gallate green tea (Camellia sinensis) as an alternative adjunct therapy for periodontal disease: A narrative review

Background: Periodontitis is a progressive destructive periodontal disease. The prevalence of periodontal disease in Indonesia reaches 74.1% and mostly occurs in the productive age group. Most of the periodontopathogenic bacteria are gram-negative bacteria and have endotoxin in the form of lipopolysaccharide (LPS), which can penetrate the periodontal tissue and induce an inflammatory response. In inflammatory conditions, osteoclastic activity is higher than osteoblastic activity, which causes bone destruction. This results in an imbalance between osteoclast-induced bone resorption and osteoblast-induced bone formation. The current preferred treatment for periodontitis is scaling root planning (SRP), but this therapy cannot repair the damaged periodontal tissue caused by periodontitis. Purpose: To describe the possibility of using a mucoadhesive gingival patch with Epigallocatechin-3-gallate (EGCG) green tea (Camellia sinensis) as alternative adjunct therapy for periodontal disease. Review: EGCG is the main component of green tea catechins, which have antitumor, antioxidant, anti-inflammatory, anti-fibrotic, and pro-osteogenic effects. However, the weaknesses so far regarding the use of EGCG as an alternative treatment is its low oral bioavailability and the concentration of EGCG absorbed by the body decreasing when accompanied by food. EGCG can be used with a mucoadhesive gingival patch to optimise bioavailability and absorption and increase local concentration and sustained release of EGCG. EGCG encourages bone development and braces mesenchymal stem cells (MSCs) differentiation for osteoblast by enhancing the expression of bone morphogenic protein 2 (BMP2). EGCG also has been proven to increase the expression of RUNX2 and ALP activity that induces osteoblast differentiation and bone mineralisation. Conclusion: A mucoadhesive gingival patch containing EGCG Green Tea (C. sinensis) may potentially induce osteoblastic activity as an adjunct therapy to repair the periodontal tissue damage due to periodontal disease.

Epigallocatechin gallate: Phytochemistry, bioavailability, utilization challenges, and strategies.

Epigallocatechin gallate (EGCG), a green tea catechin, has gained the attention of current study due to its excellent health-promoting effects. It possesses anti-obesity, antimicrobial, anticancer, anti-inflammatory activities, and is under extensive investigation in functional foods for improvement. It is susceptible to lower stability, lesser bioavailability, and lower absorption rate due to various environmental, processing, formulations, and gastrointestinal conditions of the human body. Therefore, it is the foremost concern for the researchers to enhance its bioactivity and make it the most suitable therapeutic compound for its clinical applications. In the current review, factors affecting the bioavailability of EGCG and the possible strategies to overcome these issues are reviewed and discussed. This review summarizes structural modifications and delivery through nanoparticle-based approaches including nano-emulsions, encapsulations, and silica-based nanoparticles for effective use of EGCG in functional foods. Moreover, recent advances to enhance EGCG therapeutic efficacy by specifically targeting its molecules to increase its bioavailability and stability are also described. PRACTICAL APPLICATIONS: The main green tea constituent EGCG possesses several health-promoting effects making EGCG a potential therapeutic compound to cure ailments. However, its low stability and bioavailability render its uses in many disorders. Synthesizing EGCG prodrugs by structural modifications helps against its low bioavailability and stability by overcoming premature degradation and lower absorption rate. This review paper summarizes various strategies that benefit EGCG under different physiological conditions. The esterification, nanoparticle approaches, silica-based EGCG-NPs, and EGCG formulations serve as ideal EGCG modification strategies to deliver superior concentrations with lesser toxicity for its efficient penetration and absorption across cells both in vitro and in vivo. As a result of EGCG modifications, its bioactivities would be highly improved at lower doses. The protected or modified EGCG molecule would have enhanced potential effects and stability that would contribute to the clinical applications and expand its use in various food and cosmetic industries.

Epigallocatechin-3-Gallate Delivery in Lipid-Based Nanoparticles: Potentiality and Perspectives for Future Applications in Cancer Chemoprevention and Therapy.

Chemoprevention is a strategy aimed to not only reduce the risk but also delay the development or recurrence of cancer. An ideal chemopreventive agent is not dangerous and ought not to result in side effects or damage to human health. In this context, epigallocatechin-3-gallate (EGCG) is considered a suitable chemopreventive agent, but its clinical use is limited by many factors, namely, the difference in source, administration, individual metabolism, absorption, and distribution. Genetic and dietary differences greatly cause this variability, which has limited the rational use of EGCG in chemoprevention and, particularly, the definition of a safe and efficient concentration. In the present mini review, the main limitations to a complete understanding of the use of EGCG as a chemopreventive agent will be briefly illustrated. This review also indicates the introduction and trialing of lipid-based nanoparticles (NPs) as a proper strategy to deliver EGCG at a well-defined concentration for better investigation of the chemopreventive activity. Finally, some examples of cancers that might benefit from EGCG treatment in different stages of the disease are proposed.

The potency of PLGA-Encapsulated Epigallocatechin Gallate (EGCG) as adjuvant therapy for chronic kidney disease

Chronic kidney disease (CKD) prevalence keeps increasing worldwide and being particular concern due to its morbidity and mortality. However, current CKD therapy are known to be economically costly and not necessarily provide better outcomes. Epigallocatechin gallate (EGCG) is one of the substances that widely studied as perspective therapeutic agents of CKD due to its anti-inflammatory, antioxidant, and enhancing mitochondrial function ability. However, the use of EGCG is limited to low bioavailability and poor pharmacokinetic profile. Encapsulation of EGCG with PLGA is expected to increase the efficacy of EGCG especially for its use as the kidney protective agent and optimize therapy of CKD. Thus, this study aims to analyze the potency of PLGA-encapsulated EGCG as the adjuvant therapy for CKD. This study was a narrative review summarizes studies related to current adjuvant therapy of CKD. EGCG has beneficial effects in reducing pro-inflammatory cytokines among chronic kidney disease. EGCG also can increase scavenging of free radicals to decrease reactive oxygen species. EGCG is known to enhance mitochondrial function and increase mitochondrial protection to prevent apoptosis in various kidney diseases. Combination of PLGA encapsulation with EGCG has a beneficial effect in improving the delivery, bioavailability, stability, and the pharmacokinetic profile of EGCG. PLGA-encapsulated EGCG also provides a better therapeutic effect on preventing and decreasing progression of kidney damage. Finally, this study concluded that combination of PLGA-encapsulated EGCG has a potency as the adjuvant therapy of CKD.