Cyanidin-3-o-glucoside directly binds to ERα36 and inhibits EGFR-positive triple-negative breast cancer

Wang, Li; Li, Haifeng; Yang, Shi‐Ping; Ma, Wenqiang; Liu, Mei; Guo, Shichao; Zhan, Jun; Zhang, Hongquan; Tsang, Suk Ying; Zhang, Ziding; Wang, Zhaoyi; Li, Xiru; Guo, Yang‐Dong; Li, Xiangdong

doi:10.18632/oncotarget.12025

Cited by 34 publications

(26 citation statements)

References 49 publications

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“…These are compounds known to inhibit the growth and metastatic potential of breast cancer cells. Cy-3-glu directly binds to the LBD of ERα36 and inhibits EGFR/Akt signaling in TNBC cells through EGFR degradation prior to inducing apoptosis [99].…”

Section: Indirect Modulators Of Expressionmentioning

confidence: 99%

“…Finally, it seems that the ERα36/EGFR/HER2 loop plays an important role in tamoxifen resistance as Yin and colleagues showed that inhibition of this loop with a dual tyrosine kinase inhibitor, lapatinib, or ERα36 downregulator Broussoflavonol B restores the sensitivity of MCF-7 cells that were resistant to tamoxifen [88,105]. Furthermore, Icaritin and Cy-3-glu are associated with EGFR-dependent signaling inhibition and apoptosis of MDA-MB-231 triple negative breast cancer cells [97,99]. Therefore, the use of these inhibitors could counteract the positive ERα36/EGFR loop in the progression of triple-negative breast tumors or the ER36/EGFR/HER2 loop in tamoxifen resistance within ERα66-positive breast tumors.…”

Section: Future Prospectsmentioning

confidence: 99%

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The Role of ERα36 in Development and Tumor Malignancy

Thiébaut

Konan

Guerquin

et al. 2020

IJMS

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Estrogen nuclear receptors, represented by the canonical forms ERα66 and ERβ1, are the main mediators of the estrogen-dependent pathophysiology in mammals. However, numerous isoforms have been identified, stimulating unconventional estrogen response pathways leading to complex cellular and tissue responses. The estrogen receptor variant, ERα36, was cloned in 2005 and is mainly described in the literature to be involved in the progression of mammary tumors and in the acquired resistance to anti-estrogen drugs, such as tamoxifen. In this review, we will first specify the place that ERα36 currently occupies within the diversity of nuclear and membrane estrogen receptors. We will then report recent data on the impact of ERα36 expression and/or activity in normal breast and testicular cells, but also in different types of tumors including mammary tumors, highlighting why ERα36 can now be considered as a marker of malignancy. Finally, we will explain how studying the regulation of ERα36 expression could provide new clues to counteract resistance to cancer treatments in hormone-sensitive tumors.

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Section: Indirect Modulators Of Expressionmentioning

confidence: 99%

Section: Future Prospectsmentioning

confidence: 99%

The Role of ERα36 in Development and Tumor Malignancy

Thiébaut

Konan

Guerquin

et al. 2020

IJMS

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“…The free radical-scavenging potential of anthocyanidins and its anti-inflammatory effects have been reported. Cyanidin-3- O -glucoside has been reported to display anti-tumor activity in breast cancer [ 14 ]. In addition to being rich in anthocyanidins, red lettuce is also a good source of different classes of phenolic compounds, primarily hydroxycinnamic acid, usually from caffeic acid derivatives and flavonols [ 10 , 15 ].…”

Section: Introductionmentioning

confidence: 99%

Beneficial Phytochemicals with Anti-Tumor Potential Revealed through Metabolic Profiling of New Red Pigmented Lettuces (Lactuca sativa L.)

Qin

Zhang

Han

et al. 2018

IJMS

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The present study aimed to compare polyphenols among red lettuce cultivars and identify suitable cultivars for the development and utilization of healthy vegetables. Polyphenols, mineral elements, and antioxidant activity were analyzed in the leaves of six red pigmented lettuce (Lactuca sativa L.) cultivars; thereafter, we assessed the anti-tumor effects of cultivar B-2, which displayed the highest antioxidant activity. Quadrupole–Orbitrap mass spectrometry analysis revealed four classes of polyphenols in these cultivars. The composition and contents of these metabolites varied significantly among cultivars and primarily depended on leaf color. The B-2 cultivar had the highest antioxidant potential than others because it contained the highest levels of polyphenols, especially anthocyanin, flavone, and phenolic acid; furthermore, this cultivar displayed anti-tumor effects against the human lung adenocarcinoma cell line A549, human hepatoma cell line Bel7402, human cancer colorectal adenoma cell line HCT-8, and HT-29 human colon cancer cell line. Hence, the new red-leaf lettuce cultivar B-2 has a distinct metabolite profile, with high potential for development and utilization of natural phytochemical and mineral resources in lettuces and can be used as a nutrient-dense food product.

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“…Cyanidin, a compound found in fruits, is the derivative from flavonoid and flavanone (Fu, Wei, Zhou, Zhang, & Yang, ). Due to its antioxidant property, cyanidin may help prevent a variety of free oxygen radical related diseases, including cancer and cardiovascular diseases (Pantan, Tocharus, Suksamrarn, & Tocharus, ; Wang et al, ). It has been demonstrated that cyanidin‐treated preadipocytes showed abnormal morphology.…”

Section: Introductionmentioning

confidence: 99%

Cyanidin suppresses autophagic activity regulating chondrocyte hypertrophic differentiation

Cao

Huang

Dou

et al. 2017

Journal Cellular Physiology

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Cartilage is a kind of special connective tissue which does not contain neither blood vessels nor lymphatics and nerves. Therefore, the damage in cartilage is difficult to be repaired spontaneously. Constructing tissue engineered cartilage provides a new technique for cartilage repairing. Mesenchymal stem cells (MSCs) possess a unique capability of self-renew and can differentiate into pre-chondrocytes which are frequently applied as seed cells in tissue engineering. However, in regenerated cartilage the chondrocytes derived from MSCs can hardly maintain homeostasis and preferentially present hypertrophic like phenotype. We investigated the effects of cyanidin, a natural organic compound, on chondrogenic and subsequent hypertrophic differentiation of MSCs in order to seek approaches to inhibit chondrocyte hypertrophy. We evaluated the effects of cyanidin on expression of chondrogenic and hypertrophic marker genes through RT-PCR, Western blot, alcian blue staining, and immunocytochemistry. The results showed that both chondrogenic related genes Sox9, Col2a1, and hypertrophic marker genes Runx2, Col10a1 were inhibited by cyanidin. In addition, we found that cyanidin promoted Nrf2 and p62 expression and suppressed LC3B expression during chondrogenic stage of MSCs. Meanwhile phosphorylation of IκBα and autophagosome related protein LC3B were inactivated by cyanidin during chondrocyte hypertrophic stage. Furthermore, rapamycin, an autophagy activator, abrogated the inhibitory effect of cyanidin on chondrogenic, and hypertrophic differentiation of MSCs. In conclusion, one potential mechanism of cyanidin, by which the chondrogenic and hypertrophic differentiation of MSCs were inhibited, was due to decreased autophagy activity. Our results indicated that cyanidin was a potential therapeutic agent for keeping mature chondrocyte functions.

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Cyanidin-3-o-glucoside directly binds to ERα36 and inhibits EGFR-positive triple-negative breast cancer

Cited by 34 publications

References 49 publications

The Role of ERα36 in Development and Tumor Malignancy

The Role of ERα36 in Development and Tumor Malignancy

Beneficial Phytochemicals with Anti-Tumor Potential Revealed through Metabolic Profiling of New Red Pigmented Lettuces (Lactuca sativa L.)

Cyanidin suppresses autophagic activity regulating chondrocyte hypertrophic differentiation

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