Aurantiamide Acetate, a Selective Cathepsin Inhibitor, Produced by Aspergillus penicilloides

Kengo ISSHIKI; Yasuyuki ASAI; Sumiko TANAKA; Maki NISHIO; Tomofumi UCHIDA; Toru OKUDA; Saburo KOMATSUBARA; Naoki SAKURAI

doi:10.1271/bbb.65.1195

Microbiology & Fermentation Technology

Aurantiamide Acetate, a Selective Cathepsin Inhibitor, Produced by Aspergillus penicilloides

Kengo ISSHIKI, Yasuyuki ASAI, Sumiko TANAKA, Maki NISHIO, Tomofumi UCHIDA, Toru OKUDA, Saburo KOMATSUBARA, Naoki SAKURAI

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Keywords: cathepsin L, aurantiamide, Aspergillus penicilloides, cysteine proteinase inhibitor

JOURNAL FREE ACCESS

2001 Volume 65 Issue 5 Pages 1195-1197

DOI https://doi.org/10.1271/bbb.65.1195

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Abstract

Aurantiamide acetate was isolated from the fermentation broth of Aspergillus penicilloides for the first time. Aurantiamide acetate inhibited cysteine proteinases, in particular, cathepsin L (3.4.22.15) and B (3.4.22.1) with IC₅₀ of 12 μM and 49 μM, respectiveiy. In the adjuvant-arthritic rat model, subcutaneously administered 10 mg/kg body weight of this compound suppressed hind paw swelling.

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