RRC ID 51703
Author Kawano S, Asano M, Adachi Y, Matsui J.
Title Antimitotic and Non-mitotic Effects of Eribulin Mesilate in Soft Tissue Sarcoma.
Journal Anticancer Res
Abstract BACKGROUND:Eribulin mesilate (eribulin), a first-in-class halichondrin B-based microtubule dynamics inhibitor, has been shown to promote vascular remodeling and reversal of epithelial-mesenchymal transition (EMT) apart from its antimitotic activity in breast cancer models.
MATERIALS AND METHODS:Anti-proliferative activity of eribulin was examined in vitro and in vivo in several human soft tissue sarcoma (STS) cell lines. To assess tumor blood perfusion and phenotypic changes, eribulin was investigated in a leiomyosarcoma xenograft and in vitro in liposarcoma and leiomyosarcoma cell lines.
RESULTS:Eribulin showed anti-proliferative activity in vitro against all six cell lines investigated, with 50% inhibitory concentration values of around 1 nmol/l, as well as significant antitumor activity against four xenografts in vivo. In addition, eribulin significantly enhanced tumor blood perfusion in xenografts and induced morphological changes and up-regulation of differentiation marker genes.
CONCLUSION:In pre-clinical models, eribulin showed anti-proliferative activity against a variety of histopathological subtypes of STS. Eribulin might also cause tumor vasculature remodeling to enhance tumor blood perfusion and induce tumor cell differentiation.
Volume 36(4)
Pages 1553-61
Published 2016-4-1
PII 36/4/1553
PMID 27069131
MeSH Animals Antimitotic Agents / pharmacology Antimitotic Agents / therapeutic use* Calcium-Binding Proteins / genetics Cell Differentiation / drug effects Cell Line, Tumor Cell Proliferation / drug effects Furans / pharmacology Furans / therapeutic use* Gene Expression Regulation, Neoplastic / drug effects Humans Ketones / pharmacology Ketones / therapeutic use* Mice, Inbred BALB C Microfilament Proteins / genetics Sarcoma / drug therapy* Sarcoma / genetics Sarcoma / pathology Tumor Burden / drug effects Xenograft Model Antitumor Assays
IF 1.994
Times Cited 26
Human and Animal Cells HS-SY-II(RCB2231)