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10-丁酰基取代的1,8-二羟基-9-蒽酮(丁蒽酮)对大豆脂氧合酶-1的抑制作用

Inhibition of soybean lipoxygenase-1 by 10-butyryl substituted 1,8-dihydroxy-9-anthrone (butantrone).

作者信息

Laakso S, Römer L, Mustakallio K K

出版信息

Med Biol. 1986;64(1):43-5.

PMID:3088340
Abstract

10-Butyryl substituted 1,8-dihydroxyanthrone (butantrone) inhibited soybean lipoxygenase-1 irreversibly and more efficiently than its parent compound 1,8-dihydroxyanthrone (dithranol, anthralin) (IC50 values 0.090 mM and 1.1 mM, respectively). Intact butantrone rather than its hydrolysis product was the primary effector and the 10-butyryl moiety its site specific probe, probably directing the inhibitor to the proximity of the binding site of the lipid substrate/product.

摘要

10-丁酰基取代的1,8-二羟基蒽醌(丁酮蒽酚)比其母体化合物1,8-二羟基蒽醌(地蒽酚,蒽林)更有效地不可逆抑制大豆脂氧合酶-1(IC50值分别为0.090 mM和1.1 mM)。完整的丁酮蒽酚而非其水解产物是主要效应物,10-丁酰基部分是其位点特异性探针,可能将抑制剂导向脂质底物/产物结合位点附近。

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