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Title 

Suppression of cancer cachexia by 20S,21-epoxy-resibufogenin-3-acetate─a novel nonpeptide IL-6 receptor antagonist

Authors 

A EnomotoMun Chual RhoA FukamiO HirakuK KomiyamaM Hayashi

Publisher 

Elsevier

Issue Date 

2004

Citation 

Biochemical and Biophysical Research Communications, vol. 323, no. 3, pp. 1096-1102

Keywords 

5′DFURcancer cachexiaepoxy-resibufogeninIL-6receptor antagonist21 epoxyresibufogenin 3 acetatecalcitriolgranulocyte colony stimulating factorinterleukin 3interleukin 6

Abstract 

While screening for novel IL-6 inhibitors, we synthesized 20S,21-epoxy-resibufogenin-3-acetate (ERBA). ERBA dose-dependently suppressed IL-6-induced cell growth with an IC50 value of 5.3 μM and caused a parallel rightward shift of dose-response curves to IL-6. Analysis of data yields a pA2 of 5.83 and a slope of 0.99. ERBA did not affect IL-2-, IL-3-, and GCSF-dependent cell growth, or tumor necrosis factor α-induced growth suppression, nor did ERBA affect osteoclast formation induced by IL-11, leukemia inhibitory factor, and 1α,25-dihydroxyvitamin D3. Receptor assay showed that ERBA dose-dependently suppressed IL-6 binding to IL-6 receptor (IL-6R). Furthermore, no band existing at the position of IL-6R in Western blots of ERBA-treated cells when stimulated with IL-6:ERBA suppresses IL-6 activity by blocking the binding of IL-6 to IL-6R. In an experimental model of colon 26-induced cancer cachexia, ERBA markedly inhibited body weight loss. ERBA is a specific small molecule with IL-6R-antagonist activity.

ISSN 

0006-291X

Link 

http://dx.doi.org/10.1016/j.bbrc.2004.08.196

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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