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Title 

Inhibitory effects of bufadienolides on interleukin-6 in MH-60 cells

Authors 

A EnomotoMun Chual RhoK KomiyamaM Hayashi

Publisher 

American Chemical Society

Issue Date 

2004

Citation 

Journal of Natural Products, vol. 67, no. 12, pp. 2070-2072

Keywords 

interleukin 6animal cellcell growthdrug effectinterleukin-6tumor cells, cultured

Abstract 

Derivatives of bufogenin isolated from the skin of the Chinese toad, Bufo bufo gargarizans Cantor ("Ch'an Su"), and several semisynthetic derivatives of 20β,21β-epoxy-resibufogenin (13) have been evaluated for interleukin-6 (IL-6) antagonistic activity due to their growth-inhibitory activities on IL-6-dependent MH-60 cells. Among the naturally derived compounds (1-17), 20S,21-epoxy-resibufogenin formate (1) showed potent inhibitory activity on the IL-6-dependent growth of MH-60 cells. Epoxide groups at both the C-14, C-15 and C-20, C-21 positions are required to exhibit this type of activity. Compounds acetylated at the C-16 position (7 and 9-11) showed a loss of activity. An oxo group at the C-3 position (8, 14, and 15) resulted in cytotoxicity for both cell lines. Stereochemistry is important for selectivity on suppression of IL-6 activity. Among the semisynthetic derivatives (18-25) of 13, compound 19, with an acetyl group introduced at the C-3 position in comparison to 13, demonstrated considerable growth inhibition of IL-6-dependent MH-60 cells.

ISSN 

0163-3864

Link 

http://dx.doi.org/10.1021/np049950e

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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