Plasma concentrations of individual tea catechins after a single oral dose in humans

Amelsvoort, J.M.M. van; Hof, K. H. Van Het; Mathot, J. N. J. J.; Mulder, T.P.J.; Wiersma, A.; Tijburg, Lilian B.M.

doi:10.1080/00498250110079149

Cited by 141 publications

(97 citation statements)

References 12 publications

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“…Doxorubicin-resistant cells MDA-MB-231 (231DXR) and HCC1806 (HCCDXR) were developed using a stepwise selection method. Increasing doses of doxorubicin (TEDEC-Meiji Farma) were performed until their corresponding IC 50 was reached. Briefly, initially cells were treated with a concentration of doxorubicin of 0, 1Â IC 50 .…”

Section: Methodsmentioning

confidence: 99%

Preclinical Evaluation of Fatty Acid Synthase and EGFR Inhibition in Triple-Negative Breast Cancer

Giró-Perafita

Palomeras

Lum

et al. 2016

Clinical Cancer Research

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Purpose: Triple-negative breast cancer (TNBC) lacks an approved targeted therapy. Despite initial good response to chemotherapy, 30% of the patients relapse within 5 years after treatment. EGFR overexpression is a common marker in TNBC, and its expression has been correlated with poor outcome. Inhibition of fatty acid synthase (FASN) activity leads to apoptosis of human carcinoma cells overexpressing FASN. We tested the hypothesis that blocking FASN in combination with anti-EGFR signaling agents would be an effective antitumor strategy in sensitive and chemoresistant TNBC.Experimental Design: Several TNBC cell lines and 29 primary tumors were included to determine whether FASN is a potential target in TNBC. Doxorubicin-resistant TNBC cell lines (231DXR and HCCDXR) have been developed and characterized in our laboratory. Cellular and molecular interactions of anti-FASN compounds (EGCG and C75) with cetuximab were analyzed. In vivo tumor growth inhibition was evaluated after cetuximab, EGCG, or the combination in TNBC orthoxenograft models.Results: TNBC cell lines showed overexpression of FASN enzyme and its inhibition correlated to FASN levels. FASN staining was observed in all of the 29 TNBC tumor samples. In vitro, EGCG and C75 plus cetuximab showed strong synergism in sensitive and chemoresistant cells. In vivo, the combination of EGCG with cetuximab displayed strong antitumor activity against the sensitive and chemoresistant TNBC orthoxenografts, without signs of toxicity.Conclusions: Our results show that the simultaneous blockade of FASN and EGFR is effective in preclinical models of sensitive and chemoresistant TNBC.

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Section: Methodsmentioning

confidence: 99%

Preclinical Evaluation of Fatty Acid Synthase and EGFR Inhibition in Triple-Negative Breast Cancer

Giró-Perafita

Palomeras

Lum

et al. 2016

Clinical Cancer Research

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“…EGCG is found at very low levels, if at all, in urine [207,211,212] and interconversion or de-gallation from EGCG to EGC is very limited [211].…”

Section: Effects On Ttr Toxicity In Vivomentioning

confidence: 99%

Modulators of amyloid protein aggregation and toxicity: EGCG and CLR01

Attar

Rahimi

Bitan

2013

Translational Neuroscience

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Abnormal protein folding and self-assembly causes over 30 cureless human diseases for which no diseasemodifying therapies are available. The common side to all these diseases is formation of aberrant toxic protein oligomers and amyloid fibrils. Both types of assemblies are drug targets, yet each presents major challenges to drug design, discovery, and development. In this review, we focus on two small molecules that inhibit formation of toxic amyloid protein assemblies -the green-tea derivative (-)-epigallocatechin-3-gallate (EGCG), which was identified through a combination of epidemiologic data and a compound library screen, and the molecular tweezer CLR01, whose inhibitory activity was discovered in our group based on rational reasoning, and subsequently confirmed experimentally. Both compounds act in a manner that is not specific to one particular protein and thus are useful against a multitude of amyloidogenic proteins, yet they act via distinct putative mechanisms. CLR01 disrupts protein aggregation through specific binding to lysine residues, whereas the mechanisms underlying the activity of EGCG are only recently beginning to unveil. We discuss current in vitro and, where available, in vivo literature related to EGCG and CLR01's effects on amyloid β-protein, α-synuclein, transthyretin, islet amyloid polypeptide, and calcitonin. We also describe the toxicity, pharmacokinetics, and mechanism of action of each compound.

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“…Studies on bioavailability are often conducted collecting specimens at timed intervals (after ingestion). Various studies have been conducted using normally prepared green tea beverages [14][15][16], ingested green tea extract (total catechins) [14,17,18], or ingestion of specific catechins [19][20][21]. These studies have shown that ECG and EGCG, and metabolites of EC and EGC can be detected and measured in blood plasma.…”

Section: Introductionmentioning

confidence: 99%

An Update on the Health Benefits of Green Tea

Reygaert

2017

Beverages

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Abstract:Green tea, which is produced from the leaves of the Camellia sinensis plant, is one of the most popular beverages worldwide. Over the past 30 years or more, scientists have studied this plant in respect to potential health benefits. Research has shown that the main components of green tea that are associated with health benefits are the catechins. The four main catechins found in green tea are: (−)-epicatechin (EC), (−)-epicatechin-3-gallate (ECG), (−)-epigallocatechin (EGC), and (−)-epigallocatechin-3-gallate (EGCG). Of these four, EGCG is present in the largest quantity, and so has been used in much of the research. Among the health benefits of green tea are: anticarcinogenic, anti-inflammatory, antimicrobial, and antioxidant properties, and benefits in cardiovascular disease and oral health. Research has been carried out using various animal models and cells lines, and is now more and more being carried out in humans. This type of research will help us to better understand the direct benefits of green tea. This review will focus primarily on research conducted using human subjects to investigate the health benefits of green tea.

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Plasma concentrations of individual tea catechins after a single oral dose in humans

Cited by 141 publications

References 12 publications

Preclinical Evaluation of Fatty Acid Synthase and EGFR Inhibition in Triple-Negative Breast Cancer

Preclinical Evaluation of Fatty Acid Synthase and EGFR Inhibition in Triple-Negative Breast Cancer

Modulators of amyloid protein aggregation and toxicity: EGCG and CLR01

An Update on the Health Benefits of Green Tea

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