Aurantiamide acetate, a selective cathepsin inhibitor, produced by Aspergillus penicilloides.
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 microM and 49 microM, respectively. In the adjuvant-arthritic rat model, subcutaneously administered 10 mg/kg body weight of this compound suppressed hind paw swelling.
Isshiki
K
K
Lead Generation Research Laboratory at Toda, Tanabe Seiyaku Co., Ltd., Saitama, Japan.
Asai
Y
Y
Tanaka
S
S
Nishio
M
M
Uchida
T
T
Okuda
T
T
Komatsubara
S
S
Sakurai
N
N
D001230:Aspergillus / Q000378:metabolism*; D002403:Cathepsins / Q000037:antagonists & inhibitors*; D015853:Cysteine Proteinase Inhibitors / Q000494:pharmacology*; D004151:Dipeptides / Q000494:pharmacology*; D013057:Spectrum Analysis
D015853:Cysteine Proteinase Inhibitors; D004151:Dipeptides; C011670:N-benzoylphenylalanylphenylalinol acetate; D002403:Cathepsins