Tea-break with epigallocatechin gallate derivatives – Powerful polyphenols of great potential for medicine

Bakun, Paweł; Mlynarczyk, Dariusz T.; Koczorowski, Tomasz; Cerbin-Koczorowska, Magdalena; Piwowarczyk, Ludwika; Kolasiński, Emil; Stawny, Maciej; Kuźmińska, Joanna; Jelińska, Anna; Goslinski, Tomasz

doi:10.1016/j.ejmech.2023.115820

Cited by 21 publications

(4 citation statements)

References 141 publications

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“…(−)-Epigallocatechin-3- O -gallate (EGCG), a major green tea polyphenol and therapeutically active compound known to elicit health-beneficial activities against diseases, including cancer. − EGCG exhibits its anticancer activity by regulating various signaling pathways associated with cancer progression . However, low bioavailability, poor stability, , and less membrane permeability minimize the use of EGCG as a therapeutic agent. , To overcome these shortcomings, various structural derivatizations of EGCG have been carried out to enhance its biological activities .…”

Section: Introductionmentioning

confidence: 99%

4″-Alkyl EGCG Derivatives Induce Cytoprotective Autophagy Response by Inhibiting EGFR in Glioblastoma Cells

Singh,

Ghosh,

Roy

et al. 2024

ACS Omega

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Epidermal growth factor receptor (EGFR)-targeted therapy has been proven vital in the last two decades for the treatment of multiple cancer types, including nonsmall cell lung cancer, glioblastoma, breast cancer and head and neck squamous cell carcinoma. Unfortunately, the majority of approved EGFR inhibitors fall into the drug resistance category because of continuous mutations and acquired resistance. Recently, autophagy has surfaced as one of the emerging underlying mechanisms behind resistance to EGFR-tyrosine kinase inhibitors (TKIs). Previously, we developed a series of 4″-alkyl EGCG (4″-C n EGCG, n = 6, 8, 10, 12, 14, 16, and 18) derivatives with enhanced anticancer effects and stability. Therefore, the current study hypothesized that 4″-alkyl EGCG might induce cytoprotective autophagy upon EGFR inhibition, and inhibition of autophagy may lead to improved cytotoxicity. In this study, we have observed growth inhibition and caspase-3-dependent apoptosis in 4″-alkyl EGCG derivativetreated glioblastoma cells (U87-MG). We also confirmed that 4″-alkyl EGCG could inhibit EGFR in the cells, as well as mutant L858R/T790M EGFR, through an in vitro kinase assay. Furthermore, we have found that EGFR inhibition with 4″-alkyl EGCG induces cytoprotective autophagic responses, accompanied by the blockage of the AKT/mTOR signaling pathway. In addition, cytotoxicity caused by 4″-C 10 EGCG, 4″-C 12 EGCG, and 4″-C 14 EGCG was significantly increased after the inhibition of autophagy by the pharmacological inhibitor chloroquine. These findings enhance our understanding of the autophagic response toward EGFR inhibitors in glioblastoma cells and suggest a potent combinatorial strategy to increase the therapeutic effectiveness of EGFR-TKIs.

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Section: Introductionmentioning

confidence: 99%

4″-Alkyl EGCG Derivatives Induce Cytoprotective Autophagy Response by Inhibiting EGFR in Glioblastoma Cells

Singh,

Ghosh,

Roy

et al. 2024

ACS Omega

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“…Epigallocatechin-3-gallate (EGCG) is the major catechin in green tea and functions as a potent antioxidant, preventing oxidative damage at the cellular level by neutralizing harmful free radicals [1][2][3]. In addition to this effect, extensive studies have demonstrated several pharmacological properties, such as anti-inflammatory, anti-carcinogenic, and neuroprotective effects [4,5]. Thus, to date, EGCG has also been investigated as a potent therapeutic agent.…”

Section: Introductionmentioning

confidence: 99%

“…The PG-EGCG complex can be prepared upon request at the point of care at any time. Using PG as a carrier for EGCG can offer significant advantages over other EGCG delivery systems [1,4,7]. While carriers such as liposomes, nanoparticles, and hydrogels have shown the potential to encapsulate and release EGCG, they often require complex synthesis processes, may cause immune responses, or exhibit limited biocompatibility.…”

Section: Introductionmentioning

confidence: 99%

Plasma Gel Matrix as a Promising Carrier of Epigallocatechin Gallate for Regenerative Medicine

Ushiki,

Mochizuki,

Osawa

et al. 2024

JFB

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Plasma gel (PG) is a protein matrix prepared from platelet-poor plasma and can be utilized as a drug carrier for controlled release. We previously demonstrated its applicability as a carrier of polyphosphate. Epigallocatechin-3-gallate (EGCG) is the main flavonoid found in green tea and functions as a strong antioxidant. To explore the applicability of PG as an EGCG carrier, we examined the release of EGCG from the PG matrix using an in vitro system. Pooled platelet-poor plasma (PPP) was prepared from four healthy adult male donors, mixed with EGCG, and heated at 75 °C for 10 or 20 min to prepare the PG matrix. The PG–EGCG matrix was incubated in PBS at 37 °C, and the EGCG released into PBS was determined using spectrophotometry. The antioxidant capacity was determined based on the principle of the iodine decolorization reaction. EGCG precipitated and incorporated into the PG matrix during thermal preparation. Trypsin, used to simulate the in vivo degradation of PG, released EGCG from the PG matrix over time. The released EGCG maintained its antioxidant capacity during incubation. These results indicate that thermally prepared PG matrices can be utilized as a promising EGCG carrier in the fields of tissue engineering and regenerative medicine.

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“…According to reports, EGCG and its derivatives have biofunctional properties that can exert an anticancer effect on various types of cancer cells in vivo, such as lung (Chen et al, 2020), colon (Sugihara et al, 2017), liver (Wen et al, 2019), and blood (Della Via et al, 2021), among others. In addition, they have good antioxidant and protective properties in the case of neurodegenerative diseases such as Alzheimer's and Parkinson's (Bakun et al, 2023).…”

Section: Introductionmentioning

confidence: 99%

Extraction of phenolic compounds from lucuma (Pouteria lucuma) seeds with natural deep eutectic solvents: modelling using response surface methodology and artificial neural networks

Puma-Isuiza,

García-Chacón,

Osorio

et al. 2024

Front. Sustain. Food Syst.

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The present study aimed to extract polyphenolic compounds from lucuma (Pouteria lucuma) seeds using natural deep eutectic solvents (NADES) as a green, efficient, and environmentally friendly extraction. This was optimized by using the Response Surface Method (RSM) and comparing its predictive capacity with Artificial Neural Networks (ANN) and Convolutional Neural Networks (CNN). Four NADES were prepared by mixing lactic acid (LA) with each of the following reagents: sodium acetate (SA), urea (U), glucose (G), and ammonium acetate (AA), separately. The yield of total phenolic compounds (TPC) obtained from lucuma seeds with each NADES was measured as an optimization criterion with the Box-Benhken design. The following factors were evaluated: time, temperature, and the lucuma seed flour (LSF): NADES ratio. The response variables were TPC and antioxidant activity. The LA-AA extract was selected because it exhibited the highest TPC value and was analyzed by UHPLC–MS (Ultra-performance Liquid Chromatography-Mass Spectrometry). From the RSM, the optimal extraction parameters were 80 min, 52°C, and LSF: NADES ratio of 8:100 (w/v), obtaining a TPC value of 3601.51 ± 0.51 mg GAE/100 g LFS. UHPLC–MS analysis evidenced the formation of epigallocatechin isomers from epigallocatechin gallate. The predictive ability of ANNs compared to RSM was demonstrated.

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Tea-break with epigallocatechin gallate derivatives – Powerful polyphenols of great potential for medicine

Cited by 21 publications

References 141 publications

4″-Alkyl EGCG Derivatives Induce Cytoprotective Autophagy Response by Inhibiting EGFR in Glioblastoma Cells

4″-Alkyl EGCG Derivatives Induce Cytoprotective Autophagy Response by Inhibiting EGFR in Glioblastoma Cells

Plasma Gel Matrix as a Promising Carrier of Epigallocatechin Gallate for Regenerative Medicine

Extraction of phenolic compounds from lucuma (Pouteria lucuma) seeds with natural deep eutectic solvents: modelling using response surface methodology and artificial neural networks

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