Quercetin exerts bidirectional regulation effects on the efficacy of tamoxifen in estrogen receptor‐positive breast cancer therapy: An in vitro study

2020 ◽  
Vol 35 (11) ◽  
pp. 1179-1193
Author(s):  
Zhixiang Xu ◽  
Dimeng Zhao ◽  
Xianyao Zheng ◽  
Bin Huang ◽  
Xueshan Xia ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Cancer Therapy ◽  
In Vitro Study ◽  
Vitro Study ◽  
Breast Cancer Therapy ◽  
Bidirectional Regulation ◽  
Estrogen Receptor Positive ◽  
Positive Breast Cancer

scholarly journals Virtual screening of natural compounds as combinatorial agents from indian medicinal plants against estrogen positive breast cancer

2020 ◽  
Vol 3 (10) ◽  
pp. 266-275
Author(s):  
Shaleen Jain ◽  
Dr. Asmita Das
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Virtual Screening ◽  
Medicinal Plants ◽  
Natural Compounds ◽  
Binding Energies ◽  
Common Amino Acid ◽  
Estrogen Receptor Positive ◽  
Positive Breast Cancer

Facing worldwide challenges associated with multifactorial etiology of breast cancer, designing of combinatorial therapies using natural compounds is currently the emergent way of treating several cancers including breast cancer in a synergistic way, which may mitigate several problems associated with multiple receptor targeting. In this research, Estrogen receptor positive breast cancer was taken as prototype and several key receptors associated with this particular disease were targeted by virtual screening of natural compounds found in Indian originated medicinal plants using Computer aided Drug Designing (CADD) strategies. We found the combination of Carpusin, Paulownin Cornigerine, Nororientaline, Oryzalexin B, Romucosine H and Colchicine as effective against six potential receptors i.e. FGFR2, ESR1, PIK3CA, PIK3CB, PIK3CD and AR in Estrogen receptor positive breast cancer with their binding energies in the range of ∆G ≤ -8.0 Kcal/mol as well as significant number of common amino acid binding residues as compared with binding sites of receptors. Thus this research holds significant implications for the designing of combinatorial therapeutic agents against breast cancer which can be further tested in-vitro and in-vivo to prove their synergistic efficiency.

scholarly journals In vitro study of anti-ER positive breast cancer effect and mechanism of 1,2,3,4-6-pentyl-O-galloyl-beta-d-glucose (PGG)

2019 ◽  
Vol 111 ◽  
pp. 813-820 ◽  
Author(s):  
Qiu Xiang ◽  
Juan Tang ◽  
Qin Luo ◽  
Jinfeng Xue ◽  
Yexing Tao ◽  
...  
Keyword(s):  
Breast Cancer ◽  
In Vitro Study ◽  
Vitro Study ◽  
Er Positive ◽  
Positive Breast Cancer

scholarly journals Synthesis and evaluation of coumate analogues as estrogen receptor inhibitors for breast cancer therapy

2019 ◽  
Vol 10 (3) ◽  
pp. 2218-2224
Author(s):  
Selvaraj Jubie ◽  
Basheer A ◽  
Neetu Yadav ◽  
Ashish Wadhwani ◽  
Mohammed Afzal Azam
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Cancer Therapy ◽  
Schiff Bases ◽  
Cell Biology ◽  
Breast Cancer Therapy ◽  
Human Estrogen Receptor ◽  
Ic50 Values ◽  
Mcf 7 ◽  
Positive Breast Cancer

A sulphatase inhibitor 667 COUMATE is in clinical trials for estrogen-positive breast cancer therapy for postmenopausal women, while there are a number of similar sulphatase inbitors are under development. Schiff's bases are versatile pharmacophores in which the N atom involves in hydrogen bonding with active cell centers interfering in normal cell biology. A library of novel coumate analogues with Schiff bases were designed, and structural based drug design was performed with human estrogen receptor (PDB ID: 2IOG) (Already reported). Based on the in-silico outcomes, seven coumate-schiff bases were synthesized. The compounds were obtained in good yield. The novelty had been ascertained by sci finder software. The synthesized molecules were consistent with their assigned spectra such as IR, Mass and NMR spectral data which confirmed their formation. The cytotoxicity study was performed by MTT assay for all the synthesized compounds. Most of the compounds have good IC50 values (below 100 µg/ml).Two of the synthesized compounds COU-2 and COU-5 have shown good IC50 values such as 19µg/ml and 39µg/ml, respectively. They suppressed the proliferation of estrogen receptor overexpressed MCF-7 cells.

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