Reversal effects of Raloxifene on paclitaxel resistance in 2 MDR breast cancer cells

Xu, Liang; Lei, Jingyu; Jiang, Donghai; Zhou, Lin; Wang, Shu; Fan, Weimin

doi:10.1080/15384047.2015.1095409

Cited by 5 publications

(5 citation statements)

References 71 publications

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“…Necrotic cells were also significantly increased after RLX-EMLs treatment compared to RLX, and blank EMLs groups ( p < 0.05), Figure 4 D,E. In agreement with our data, RLX at a concentration of 10 µM failed to induce this level of apoptosis in MCF-7 and several breast cancer cell lines such as BCap37, Bats-72, and Bads-200 cells [ 52 , 53 ]. This weak apoptotic effect was further confirmed through examining the cleavage of caspase-9 protein.…”

Section: Resultssupporting

confidence: 88%

“…Although RLX significantly arrested G 2 /M ( p < 0.05) when compared to the control cells, it had little effect upon other cell cycle stages, Figure 3 A,C,E. Similarly, It has been shown that RLX (10 µM) did not influence cell cycle distribution in several breast cancer cell lines such as BCap37, Bats-72, and Bads-200 cells [ 52 , 53 ]. RLX at (15 µM) arrested the cell cycle, promoted the accumulation in the G1 phase and decrease of the percentage of cells in the S and G2/M phases [ 54 ].…”

Section: Resultsmentioning

confidence: 83%

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RETRACTED: Lipidic Nano-Sized Emulsomes Potentiates the Cytotoxic and Apoptotic Effects of Raloxifene Hydrochloride in MCF-7 Human Breast Cancer Cells: Factorial Analysis and In Vitro Anti-Tumor Activity Assessment

et al. 2021

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Raloxifene hydrochloride (RLX), an antiosteoporotic agent, has been utilized for guarding against breast cancer and recently, for the disease management owing to its estrogen antagonist activity. Nevertheless, RLX exhibits poor bioavailability that could be attributed to reduced water solubility and first pass metabolism. To overcome these challenges, this study aimed at formulating and optimizing RLX emulsomes (RLX-EMLs) to enhance the drug antitumor activity. A 4131 factorial design was employed for assessing the effect of lipoid: solid lipid ratio and solid lipid type on the emulsomes characteristics. The anticancer potential of the optimized formulation and apoptotic parameters were assessed. Vesicle size, entrapment, and release efficiency were significantly influenced by both variables, while zeta potential was influenced by lipoid: solid lipid at p < 0.05. The optimal formulation exhibited vesicle size of 236 ± 8.6 nm, zeta potential of −18.6 ± 0.7 mV, drug entrapment of 98.9 ± 4.9%, and release efficiency of 42.7 ± 1.8%. MTT assay showed concentration-dependent inhibition of MCF-7 cells viability. In addition, cells treated with RLX-EMLs showed significant arrest at G2/M phase associated with significant increase in apoptotic and necrotic cells. The enhanced cytotoxic and anti-proliferative effect of RLX-EMLs relative to raw drug was authenticated through increased Bax/Bcl-2 ratio, caspase-9 activation and depletion of mitochondrial membrane potential.

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Section: Resultssupporting

confidence: 88%

Section: Resultsmentioning

confidence: 83%

RETRACTED: Lipidic Nano-Sized Emulsomes Potentiates the Cytotoxic and Apoptotic Effects of Raloxifene Hydrochloride in MCF-7 Human Breast Cancer Cells: Factorial Analysis and In Vitro Anti-Tumor Activity Assessment

et al. 2021

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“…RAL could significantly sensitize estrogen receptor multidrug-resistant (MDR) breast tumors to paclitaxel both in vitro and in vivo. A combination of RAL and paclitaxel could significantly enhance paclitaxel-induced cell apoptosis, G2-M arrest, as well as inhibition of cell proliferation in MDR tumors [32]. These observations indicated that RAL might be a vital chemosensitizer drug for breast cancer therapy.…”

Section: IVmentioning

confidence: 82%

“…RAL acts like estrogen to prevent bone loss and improve lipid profiles by decreases total and LDL cholesterol. It can demote the proliferation and progression of estrogen-dependent breast and uterine cancer [32]. RAL could significantly sensitize estrogen receptor multidrug-resistant (MDR) breast tumors to paclitaxel both in vitro and in vivo.…”

Section: IVmentioning

confidence: 99%

In Silico Identification of Apobec3b Small Molecule Inhibitors From DTP-Nci Libraries

Mohamed

Jusril

Adenan³

et al. 2021

Int J App Pharm

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Objective: APOBEC3B (A3B) enzyme causes C-to-T or C-to-G somatic alteration in the cancer genome, leading to the evolution of a broad spectrum of human cancers. The present study aims to identify A3B small molecule inhibitors using a top-down approach via pharmacoinformatic virtual screening. Methods: Virtual screening of 2951 drug-alike molecules with diversified structures from the National Cancer Institute Development Therapeutics Program (DTP-NCI) compounds library was performed using GOLD and AutoDock Vina docking programs against the 3D structure of A3B (PDB ID: 5TD5). Results: Amongst the docked compounds, Nordracorubin, NSC641233 and Raloxifene hydrochloride showed the most potent binding affinities towards A3B on both Autodock/Vina and GOLD. Several significant similarities were observed between A3B and the three hits, including hydrogen bonds and pi-pi stacking. The three compounds also exhibited interaction with the centralized zinc cofactor and amino acid residues that directly contribute the deaminase activity of A3B enzyme. Conclusion: We hypothesize that the findings from this study could significantly shorten the quest for novel molecules against the A3B after confirmation with subsequent in vitro and in vivo studies in the near future.

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“…P-gp is known as multidrug resistance protein 1 (MDR1), which localizes on both, the bronchial and bronchiolar epithelium and the alveolar macrophage plasma membrane, and has been shown to act in a removal of environmental compounds from the lungs [21]. Xu et al evaluated whether raloxifene hydrochloride (RAL) may sensitize MDR to chemotherapy in breast cancer, especially in estrogen receptor-negative (ER-) cases, only to find that RAL could significantly sensitize ER-related MDR breast tumors to paclitaxel [22].…”

mentioning

confidence: 99%

Expression pattern of estrogen receptor β and its correlation with multidrug resistance in non-small cell lung cancer

Huang

Liu

et al. 2019

neo

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The aim of this work was to determine the expression of the ERβ (estrogen receptor β) and multidrug resistance, namely MDR1 (P-glycoprotein, P-gp), in 152 samples of non-small cell lung cancer. The expression pattern of ERβ and MDR1 were assessed by the quantitative reverse-transcriptase polymerase chain reaction (qRT-PCR) and immunohistochemistry. We also analyzed the correlation between ERβ and MDR1 with clinical and pathological data. The co-expression pattern of ERβ and individual MDR1 proteins was assessed by correspondence analysis and chi-squared tests. In the present study, we found that patients with tumor stage I-II showed higher ERβ mRNA expression levels and decreased expression of ERβ protein with increasing tumor grade, which is opposite to MDR1 expression. In addition, an opposite co-expression pattern of ERβ and individual MDR1 proteins was also observed. In conclusion, the results can be used to better understand the expression control of MDR1 and may allow for the establishment of new cancer chemistry strategies that will control P-gp expression in NSCLC.

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Reversal effects of Raloxifene on paclitaxel resistance in 2 MDR breast cancer cells

Cited by 5 publications

References 71 publications

RETRACTED: Lipidic Nano-Sized Emulsomes Potentiates the Cytotoxic and Apoptotic Effects of Raloxifene Hydrochloride in MCF-7 Human Breast Cancer Cells: Factorial Analysis and In Vitro Anti-Tumor Activity Assessment

RETRACTED: Lipidic Nano-Sized Emulsomes Potentiates the Cytotoxic and Apoptotic Effects of Raloxifene Hydrochloride in MCF-7 Human Breast Cancer Cells: Factorial Analysis and In Vitro Anti-Tumor Activity Assessment

In Silico Identification of Apobec3b Small Molecule Inhibitors From DTP-Nci Libraries

Expression pattern of estrogen receptor β and its correlation with multidrug resistance in non-small cell lung cancer

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