Epigallocatechin-3-Gallate Therapeutic Potential in Cancer: Mechanism of Action and Clinical Implications

Abstract

Cellular signaling pathways involved in the maintenance of the equilibrium between cell proliferation and apoptosis have emerged as rational targets that can be exploited in the prevention and treatment of cancer. Epigallocatechin-3-gallate (EGCG) is the most abundant phenolic compound found in green tea. It has been shown to regulate multiple crucial cellular signaling pathways, including those mediated by EGFR, JAK-STAT, MAPKs, NF-κB, PI3K-AKT-mTOR, and others. Deregulation of the abovementioned pathways is involved in the pathophysiology of cancer. It has been demonstrated that EGCG may exert anti-proliferative, anti-inflammatory, and apoptosis-inducing effects or induce epigenetic changes. Furthermore, preclinical and clinical studies suggest that EGCG may be used in the treatment of numerous disorders, including cancer. This review aims to summarize the existing knowledge regarding the biological properties of EGCG, especially in the context of cancer treatment and prophylaxis.

Epigallocatechin-3-gallate inhibit the protein arginine methyltransferase 5 and Enhancer of Zeste homolog 2 in breast cancer bothin vitroandin vivo

“…Many studies using cell lines and animal models have demonstrated anticancer activity of EGCG (16)(17)(18)(19)47,48,57). The information from clinical trials suggested a safety of EGCG (200 mg/day) in men for prostate cancer (58) .…”

“…A large number of studies in animals, as well as epidemiologic, case-control studies in humans, reveal that EGCG significantly reduce the incidence of various cancers (44) . Its therapeutic action was observed to inhibit multiple enzymes, including DNA topoisomerase, tyrosinase, arylamine N-acetyltransferase, glycogen phosphorylase, glutathione transferase, inositol-trisphosphate 3-kinase, inositol-polyphosphate multi kinase, nucleoside-diphosphate kinase, and DNA-directed DNA polymerase (17,18,19,44) . It is also reported that it induces epigenetic modifications, angiogenesis, carcinogenesis, metastasis and enhance the efficacy of conventional anticancer drugs also (19) .…”

“…Its therapeutic action was observed to inhibit multiple enzymes, including DNA topoisomerase, tyrosinase, arylamine N-acetyltransferase, glycogen phosphorylase, glutathione transferase, inositol-trisphosphate 3-kinase, inositol-polyphosphate multi kinase, nucleoside-diphosphate kinase, and DNA-directed DNA polymerase (17,18,19,44) . It is also reported that it induces epigenetic modifications, angiogenesis, carcinogenesis, metastasis and enhance the efficacy of conventional anticancer drugs also (19) . In present study we first time report the inhibition of PRMT5 and EZH2 activity by EGCG.…”

“…It also been reported that EGCG inhibit the angiogenesis, induce epigenetic modifications, carcinogenesis, and metastasis in animal models (17,18) . Plenty of reports in animals, as well as case-control and epidemiologic studies in humans, reveal that green tea consumption or oral administration for long-term significantly reduces the incidence of various cancers (19,20) , indicated a vital role of EGCG in the chemoprevention of cancer. The large number reports suggested the excellent anticancer potency of EGCG alone as well as along other compounds or drugs, however the specific binding target for EGCG is not been studied extensively.…”

Revolutionizing Cancer Treatment: Biopolymer‐Based Aerogels as Smart Platforms for Targeted Drug Delivery

“…[105] The mechanism of action of DOX primarily through intercalation into DNA strands, inhibiting topoisomerase II activity. [106,107] This disrupts DNA replication and repair, leading to cell cycle arrest and apoptosis. Additionally, doxorubicin generates reactive oxygen species, causing oxidative stress and further contributing to its cytotoxic effects on cancer cells.…”