scholarly journals Green Tea Catechins Induce Inhibition of PTP1B Phosphatase in Breast Cancer Cells with Potent Anti-Cancer Properties: In Vitro Assay, Molecular Docking, and Dynamics Studies

Antioxidants ◽  
2020 ◽  
Vol 9 (12) ◽  
pp. 1208
Author(s):  
Alicja Kuban-Jankowska ◽  
Tomasz Kostrzewa ◽  
Claudia Musial ◽  
Giampaolo Barone ◽  
Giosuè Lo-Bosco ◽  
...  

The catechins derived from green tea possess antioxidant activity and may have a potentially anticancer effect. PTP1B is tyrosine phosphatase that is oxidative stress regulated and is involved with prooncogenic pathways leading to the formation of a.o. breast cancer. Here, we present the effect of selected green tea catechins on enzymatic activity of PTP1B phosphatase and viability of MCF-7 breast cancer cells. We showed also the computational analysis of the most effective catechin binding with a PTP1B molecule. We observed that epigallocatechin, epigallocatechin gallate, epicatechin, and epicatechin gallate may decrease enzymatic activity of PTP1B phosphatase and viability of MCF-7 cells. Conclusions: From the tested compounds, epigallocatechin and epigallocatechin gallate were the most effective inhibitors of the MCF-7 cell viability. Moreover, epigallocatechin was also the strongest inhibitor of PTP1B activity. Computational analysis allows us also to conclude that epigallocatechin is able to interact and bind to PTP1B. Our results suggest also the most predicted binding site to epigallocatechin binding to PTP1B.

2021 ◽  
Vol 35 (S1) ◽  
Author(s):  
Arianna Mahadeo ◽  
Leslie Ramirez‐Medrano ◽  
Lissette Delgado‐Cruzata

2019 ◽  
Vol 3 (Supplement_1) ◽  
Author(s):  
Danielly Costa ◽  
Ronimara Santos ◽  
Emmanuele Da Silva Andrade ◽  
Beatriz Louise Themistocles ◽  
Brenda Graziella da Silva ◽  
...  

Abstract Objectives We aimed to obtain a catechin-rich green tea extract (GTE) from Camellia sinensis and to evaluate its antitumor potential on human breast cancer. Green tea (GT) has been extensively studied for its antioxidant property, which is mainly attributed to catechins. These phenolic compounds regulate many cellular targets involved in cancer signaling pathways, including those mediated by p53 tumor suppressor protein. Methods Tea infusion was prepared on a ratio of 1 g:40 mL of boiling distilled water using a combination of temperature and time (70, 75, 80, 85, 90, 95 and 100 ºC/5, 10, 15 min). Infusions were evaluated by polyphenols content (Folin–Ciocalteu's reagent) and antioxidant potential (FRAP). Breast cancer cells (MDA-MB-231 and MCF-7) and non-tumoral cells (MCF-10A), were exposed to different concentrations of GTE (31.5 μg/mL to 1.0 mg/mL) during 24 h-48 h, and cell viability was assessed by Alamar Blue® and Trypan Blue assays. Viability was also acessed in the presence of a p53 protein inibitor, pifithrin-α. Immunocytochemistry and Western blotting analysis were performed to access the expression of p53. Results Our results demonstrated no influence of extraction condition in the total content of polyphenols and antioxidant potential of GT, and a new extract was obtained at 80 ºC/5 min, then freeze dried to be used in cell culture. After exposure for 24 h, GTE already promoted a cytotoxic effect, reducing viability of both breast cancer cell lines (IC50 MDA-MB-231 = 138,8 μg/mL; IC50 MCF-7 = 324,5 μg/mL) without cytotoxic effect on non-tumoral cells (IC50 MCF-10A = 10,097 μg/mL). In addition, GTE promotes an increase of p53 levels on treated MCF-7 cells, which express the wild-type form of the protein. Interestingly, an opposite phenomenon was evidenced in MDA-MB-231 cells, that express the mutated form of p53, in which protein levels seem to be lower in the presence of the extract. Conclusions Our data suggests that GTE has anticarcinogenic potential on breast cancer and it is possible that this capacity might be related with the modulation of p53 tumor suppressor protein. Funding Sources FAPERJ, FUNDAÇÃO DO CÂNCER, CAPES, CNPq.


2006 ◽  
Vol 24 (18_suppl) ◽  
pp. 20097-20097
Author(s):  
T. Cordes ◽  
D. Diesing ◽  
S. Becker ◽  
D. Fischer ◽  
K. Diedrich ◽  
...  

20097 Background: Calcitriol (1,25-dihydroxyvitamin D3) is the most active metabolite of vitamin D. It is known for its antiproliferative and differentiating effects on many cell populations including MCF-7 and other breast cancer cells. 1α-hydroxylase (CYP27B1) one of the key enzymes has been found in breast cancer cells suggesting an autocrine regulation of producing calcitriol. An alternative splicing of the encoding genes for the1α-hydroxylase might play a role in regulating enzyme levels and can explain tissue specific variations of the enzyme activity. Splice variants containing intron 1 may encode for truncated proteins with deletion of protein domains which are essential for its enzymatic activity. Methods: In order to obtain more information on the abundance of 1α-hydroxylase splice variants, we performed a highly specific nested touchdown PCR in MCF-7 cells. The protein products of the full length enzyme and its slice variants were confirmed by Western Blot. Results: The full length sequence of 1α-hydroxylase and two different splice variants including intron 1 were isolated. Conclusion: We hypothesize that the expression of the splice variants can lead to a quantitatively lower expression the mRNA of the full length enzyme. The abundance of less active 1α-hydroxylase protein products can alter the local synthesis of calcitriol in the cells and may explain variations of enzymatic activity in different cells and tissues. No significant financial relationships to disclose.


2020 ◽  
Vol 6 (2) ◽  
Author(s):  
Lisni Noraida Waruwu ◽  
Maria Bintang ◽  
Bambang Pontjo Priosoeryanto

Green tea (Camellia sinensis) is one of traditional plants that have the potential as an anticancer. The sample used in this research commercial green tea extract. The purpose of this study was to test the antiproliferation activity of green tea extract on breast cancer cell MCM-B2 in vitro. Green tea extract fractionated using three solvents, ie water, ethanol 70%, and n-hexane. Extract and fraction of green tea water have value Lethality Concentration 50 (LC50) more than 1000 ppm. The fraction of ethanol 70% and n-hexane had an LC50 value of 883.48 ppm and 600.56 ppm, respectively. The results of the phytochemical screening of green tea extract are flavonoids, tannins, and saponins, while the phytochemical screening results of n-hexane fraction are flavonoids and tannins. Antiproliferation activity was tested on breast cancer cells MCM-B2 and normal cells Vero by trypan blue staining method. The highest MCM-B2 cell inhibitory activity was achieved at a concentration of 13000 ppm green tea extract and 1000 ppm of n-hexane fraction, 59% and 59%, respectively. The extract and n-hexane fraction of green tea are not toxic to normal Vero cells characterized by not inhibiting normal cell proliferation. Keywords: antiproliferative, cancer cell MCM-B2, commercial green tea, cytotoxicity


2014 ◽  
Vol 32 (3) ◽  
pp. 278
Author(s):  
Dongdong SHI ◽  
Yuanyuan KUANG ◽  
Guiming WANG ◽  
Zhangxiao PENG ◽  
Yan WANG ◽  
...  

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