Antitumor and anticancer stem cell activities of eribulin mesylate and antiestrogens in breast cancer cells

Kurebayashi, Junichi; Kanomata, Naoki; Yamashita, Tetsumasa; Shimo, Toshiro; Moriya, Takuya

doi:10.1007/s12282-014-0580-9

Cited by 22 publications

(30 citation statements)

References 28 publications

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“…Our in vitro results in SCLC lines are similar to those found in two recent publications encompassing 22-breast cancer cell lines where 20 lines had eribulin IC 50 concentrations below 5 nM [17,18]. Eribulin has been FDA approved for the treatment of breast cancer patients with metastatic disease who have had at least two treatment regimens with an anthracycline and a taxane.…”

Section: Discussionsupporting

confidence: 86%

Eribulin inhibits the growth of small cell lung cancer cell lines alone and with radiotherapy

2018

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Objectives Small cell lung cancer (SCLC) patients of all stages are treated with etoposide and cisplatin or carboplatin with or without surgery or chest radiotherapy. Initial response rates are ≥70% however the majority of patients relapse and are resistant to additional therapies due to pan-resistance to these salvage therapies. Therefore, new treatments are urgently needed. The non-taxane microtubule inhibitor eribulin has produced responses in heavily pretreated breast cancer patients. We evaluated the efficacy of eribulin alone and in combination with radiation in a panel of SCLC cell lines established from patients prior to or after receiving chemotherapy and or radiation. Material and methods Growth inhibition by eribulin alone, radiation alone and the combination was assessed by MTS assay and clonogenic survival. Eribulin induced cell cycle arrest was evaluated by FACS. Apoptosis was evaluated by using the Caspase-GLO 3/7 luminescent plate assay and by the Vybrant apoptosis assay with analysis by FACS. Results Eribulin mesylate inhibited the growth of all 17-SCLC lines at concentrations of ≤10 nM which is a clinically achievable dose. Growth inhibition was not significantly different between cell lines established prior to or after chemotherapy (p = .5). Concurrent eribulin + radiation induced a greater G2-M arrest, an increase in apoptotic cells and increased growth inhibition over radiation alone. Conclusions Eribulin was highly active alone and in combination with radiation in treatment naïve SCLC lines and lines established from previously treated patients. In vivo pre-clinical studies of eribulin alone and in combination with radiation should be considered in SCLC cell lines.

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Section: Discussionsupporting

confidence: 86%

Eribulin inhibits the growth of small cell lung cancer cell lines alone and with radiotherapy

2018

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“…To evaluate the antitumor effects of combined treatments, a combination index based on the 50% inhibitory concentration (IC 50 ) was calculated according to the following formula: combination index = IC 50 with the combined treatment/IC 50 with the single treatment. A combination index <0.5 was considered evidence of an additive interaction …”

Section: Methodsmentioning

confidence: 99%

“…Flow cytometry was performed with a FACSCalibur flow cytometer (Becton‐Dickinson), and analyzed using CELLQuest Software version 6.0 (Becton‐Dickinson). Cells that express CD44‐high, and CD24‐negative or low were recognized as CSC …”

Section: Methodsmentioning

confidence: 99%

“…These cells were then dispersed, and single‐cell suspensions (5 × 10 3 cells/well) were incubated in MammoCult Basal Medium (STEMCELL Technologies, Vancouver, Canada) supplemented with 10% MammoCult Proliferation Supplements (STEMCELL Technologies, Durham, NC, USA) in non‐adhesive 6‐well plates (Corning Inc., Corning, NY, USA) for 7 days. Mammospheres greater than 60 μm in size were counted with an Olympus phase‐contrast microscope …”

Section: Methodsmentioning

confidence: 99%

“…Estrogen plays critical roles in the development and progression of breast cancer. Recent studies have indicated that estrogen increases not only the cell growth but also the CSC proportion in estrogen receptor (ER)‐positive breast cancer cells . Increased CSC populations may induce the development of metastasis and resistance to endocrine therapy …”

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confidence: 99%

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Anti‐cancer stem cell activity of a hedgehog inhibitor GANT61 in estrogen receptor‐positive breast cancer cells

et al. 2017

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Estradiol (E2) increases not only the cell growth but also the cancer stem cell (CSC) proportion in estrogen receptor (ER)‐positive breast cancer cells. It has been suggested that the non‐canonical hedgehog (Hh) pathway activated by E2 plays an important role in the regulation of CSC proportion in ER‐positive breast cancer cells. We studied anti‐CSC activity of a non‐canonical Hh inhibitor GANT61 in ER‐positive breast cancer cells. Effects of GANT61 on the cell growth, cell cycle progression, apoptosis and CSC proportion were investigated in four ER‐positive breast cancer cell lines. CSC proportion was measured using either the mammosphere assay or CD44/CD24 assay. Expression levels of pivotal molecules in the Hh pathway were measured. Combined effects of GANT61 with antiestrogens on the anti‐cell growth and anti‐CSC activities were investigated. E2 significantly increased the cell growth and CSC proportion in all ER‐positive cell lines. E2 increased the expression levels of glioma‐associated oncogene (GLI) 1 and/or GLI2. GANT61 decreased the cell growth in association with a G1‐S cell cycle retardation and increased apoptosis. GANT61 decreased the E2‐induced CSC proportion measured by the mammosphere assay in all cell lines. Antiestrogens also decreased the E2‐induced cell growth and CSC proportion. Combined treatments of GANT61 with antiestrogens additively enhanced anti‐cell growth and/or anti‐CSC activities in some ER‐positive cell lines. In conclusion, the non‐canonical Hh inhibitor GANT61 inhibited not only the cell growth but also the CSC proportion increased by E2 in ER‐positive breast cancer cells. GANT61 enhanced anti‐cell growth and/or anti‐CSC activities of antiestrogens in ER‐positive cell lines.

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Report on Recently (2017–20) Designed Quinoline‐Based Human Cancer Cell Growth Inhibitors

Dorababu¹

2020

ChemistrySelect

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Quinoline has been a most essential pharmacophore, derivatization of which led to enticing pharmacological properties. Quinoline is responsible for a wide range of biological potencies such as antibacterial, antifungal, anti-leishmanial, antimalarial, antioxidant and anticancer properties. Out of these clinical importances, the anticancer property of heterocycles is of greatest concern as cancer has become a major threat globally. Since some natural products containing quinoline moiety have displayed cancer inhibition potency, quinoline has been given highest priority in the anticancer drug design and development. In addition, quinoline has got eight positions including nitrogen for substitution which may result in some potential anticancer properties. Ever since, this extraordinary potential is being utilized in anticancer drug discovery. In this review, the various trends in drug design of quinoline moiety anticipating finest anticancer properties through cancer cell growth inhibition are collated comprehensively. The review work is classified based on type of quinoline derivatives. Besides this, with the aid of structure-activity relationship discussion, the importance of structural units that contributed to strongest activity towards cancer inhibition is emphasized. The particular activity would help to bring further advanced anticancer agents in the future.

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Antitumor and anticancer stem cell activities of eribulin mesylate and antiestrogens in breast cancer cells

Cited by 22 publications

References 28 publications

Eribulin inhibits the growth of small cell lung cancer cell lines alone and with radiotherapy

Eribulin inhibits the growth of small cell lung cancer cell lines alone and with radiotherapy

Anti‐cancer stem cell activity of a hedgehog inhibitor GANT61 in estrogen receptor‐positive breast cancer cells

Report on Recently (2017–20) Designed Quinoline‐Based Human Cancer Cell Growth Inhibitors

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