The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Erinacine E as a Kappa Opioid Receptor Agonist and Its New Analogs from a Basidiomycete, Hericium ramosum
TOSHIYUKI SAITO, FUKUMATSU AOKI, HIDEO HIRAI, TAISUKE INAGAKI, YASUE MATSUNAGA, TATSUO SAKAKIBARA, SHINICHI SAKEMI, YUMIKO SUZUKI, SHUZO WATANABE, OSAMU SUGA, TETSUJO SUJAKU, ADAM A. SMOGOWICZ, SUSAN J. TRUESDELL, JOHN W. WONG, ATSUSHI NAGAHISA, YASUHIRO KOJIMA, NAKAO KOJIMA
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1998 Volume 51 Issue 11 Pages 983-990

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Abstract

A κ opioid receptor binding inhibitor was isolated from the fermentation broth of a basidiomycete, Hericium ramosum CL24240 and identified as erinacine E (1). Three analogs of 1 were produced by fermentation in other media and by microbial biotransformation. Of these compounds, 1 was shown to be the most potent binding inhibitor. Preliminary SAR studies of these compounds indicated that all functional groups and side chains were required for the activity. Compound 1 was a highly-selective binding inhibitor for the κ opioid receptor: 0.8 μM (IC50) for κ, > 200 μM for μ, and > 200 μM for δ opioid receptor. Compound 1 suppressed electrically-stimulated twitch responses of rabbit vas deferens with an ED50 of 14 μM. The suppression was recovered by adding a selective κ opioid receptor antagonist nor-binaltorphimine, indicating that 1 is a κ opioid receptor agonist.

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The Journal of Antibiotics, Series A

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