Chemico-biological aspects of
            <i>(−)-</i>
            epigallocatechin-
            <i>3</i>
            -gallate (EGCG) to improve its stability, bioavailability and membrane permeability: Current status and future prospects

Sahadevan, Revathy; Singh, Satyam; Binoy, Anupama; Sadhukhan, Sushabhan

doi:10.1080/10408398.2022.2068500

Cited by 48 publications

(41 citation statements)

References 317 publications

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“…The chemopreventive effect of EGCG is dependent on its bioavailability and successful interaction with target tissues; however, EGCG is expected to have low lipophilicity ( Figure 2 ), thus limiting its membrane permeability, especially across the intestinal epithelium [ 90 ]. The lack of a receptor-mediated transport suggests that its membrane permeability depends on passive diffusion [ 91 ].…”

Section: Discussionmentioning

confidence: 99%

“…Significant efforts are being made to increase EGCG bioavailability and improve its low cellular uptake. Promising results have been obtained with the development of formulations for encapsulating EGCG within hydrophobic nanocarriers [ 13 , 16 , 91 , 92 ]. These systems prevent the degradation and metabolization of the transported catechins allowing a higher concentration in the bloodstream [ 92 ].…”

Section: Discussionmentioning

confidence: 99%

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The Potential of Epigallocatechin Gallate (EGCG) in Targeting Autophagy for Cancer Treatment: A Narrative Review

Ferrari

Bettuzzi

Naponelli

2022

IJMS

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Autophagy is an evolutionarily conserved process for the degradation of redundant or damaged cellular material by means of a lysosome-dependent mechanism, contributing to cell homeostasis and survival. Autophagy plays a multifaceted and context-dependent role in cancer initiation, maintenance, and progression; it has a tumor suppressive role in the absence of disease and is upregulated in cancer cells to meet their elevated metabolic demands. Autophagy represents a promising but challenging target in cancer treatment. Green tea is a widely used beverage with healthy effects on several diseases, including cancer. The bioactive compounds of green tea are mainly catechins, and epigallocatechin-gallate (EGCG) is the most abundant and biologically active among them. In this review, evidence of autophagy modulation and anti-cancer effects induced by EGCG treatment in experimental cancer models is presented. Reviewed articles reveal that EGCG promotes cytotoxic autophagy often through the inactivation of PI3K/Akt/mTOR pathway, resulting in apoptosis induction. EGCG pro-oxidant activity has been postulated to be responsible for its anti-cancer effects. In combination therapy with a chemotherapy drug, EGCG inhibits cell growth and the drug-induced pro-survival autophagy. The selected studies rightly claim EGCG as a valuable agent in cancer chemoprevention.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

The Potential of Epigallocatechin Gallate (EGCG) in Targeting Autophagy for Cancer Treatment: A Narrative Review

Ferrari

Bettuzzi

Naponelli

2022

IJMS

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“…85 Antioxidant activity of EGCG prevents cells from ROS-mediated DNA damage, thus protecting the occurrence of cancer. [85][86][87] Several natural or synthetic molecules have showed chemo-preventive properties via regulating the cellular redox level. Thus, we explored the in vitro antioxidant capability of 4 00 -C 14 EGCG and EGCG by using DPPH assay.…”

Section: Chemistrymentioning

confidence: 99%

Structure-based design and synthesis of a novel long-chain 4′′-alkyl ether derivative of EGCG as potent EGFR inhibitor: in vitro and in silico studies

et al. 2022

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“…A prime example is the polyphenol epigallocatechin-3-gallate (EGCG) (Figure 8a), which inhibits the formation of both pathological amyloid [103][104][105][106] and FuBA [40]. Although EGCG has shown promising pre-clinical results against pathological amyloids, the compound has not successfully passed clinical trials, possibly because of low chemical stability in vivo (it is prone to epimerization and auto-oxidation above pH 6 [107]) and limited penetration of the blood-brain barrier [106,108]. While EGCG also can inhibit the formation of bacterial amyloid and reduce biofilm formation [40,109], stability issues have also hampered its clinical use against infections [110][111][112].…”

Section: Using Small Molecules and Polyphenols To Target Fuba And Bio...mentioning

confidence: 99%

Functional Bacterial Amyloids: Understanding Fibrillation, Regulating Biofilm Fibril Formation and Organizing Surface Assemblies

2022

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Functional amyloid is produced by many organisms but is particularly well understood in bacteria, where proteins such as CsgA (E. coli) and FapC (Pseudomonas) are assembled as functional bacterial amyloid (FuBA) on the cell surface in a carefully optimized process. Besides a host of helper proteins, FuBA formation is aided by multiple imperfect repeats which stabilize amyloid and streamline the aggregation mechanism to a fast-track assembly dominated by primary nucleation. These repeats, which are found in variable numbers in Pseudomonas, are most likely the structural core of the fibrils, though we still lack experimental data to determine whether the repeats give rise to β-helix structures via stacked β-hairpins (highly likely for CsgA) or more complicated arrangements (possibly the case for FapC). The response of FuBA fibrillation to denaturants suggests that nucleation and elongation involve equal amounts of folding, but protein chaperones preferentially target nucleation for effective inhibition. Smart peptides can be designed based on these imperfect repeats and modified with various flanking sequences to divert aggregation to less stable structures, leading to a reduction in biofilm formation. Small molecules such as EGCG can also divert FuBA to less organized structures, such as partially-folded oligomeric species, with the same detrimental effect on biofilm. Finally, the strong tendency of FuBA to self-assemble can lead to the formation of very regular two-dimensional amyloid films on structured surfaces such as graphite, which strongly implies future use in biosensors or other nanobiomaterials. In summary, the properties of functional amyloid are a much-needed corrective to the unfortunate association of amyloid with neurodegenerative disease and a testimony to nature’s ability to get the best out of a protein fold.

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Chemico-biological aspects of (−)- epigallocatechin- 3 -gallate (EGCG) to improve its stability, bioavailability and membrane permeability: Current status and future prospects

Cited by 48 publications

References 317 publications

The Potential of Epigallocatechin Gallate (EGCG) in Targeting Autophagy for Cancer Treatment: A Narrative Review

The Potential of Epigallocatechin Gallate (EGCG) in Targeting Autophagy for Cancer Treatment: A Narrative Review

Structure-based design and synthesis of a novel long-chain 4′′-alkyl ether derivative of EGCG as potent EGFR inhibitor: in vitro and in silico studies

Functional Bacterial Amyloids: Understanding Fibrillation, Regulating Biofilm Fibril Formation and Organizing Surface Assemblies

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