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。

Medical biology Pub Date : 1986-01-01

S Laakso, L Römer, K K Mustakallio

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引用次数: 0

摘要

10-丁酰基取代的 1,8-二羟基蒽酮（丁蒽酮）对大豆脂氧合酶-1 的抑制作用不可逆，且比其母体化合物 1,8-二羟基蒽酮（二蒽醇、蒽林）更有效（IC50 值分别为 0.090 mM 和 1.1 mM）。完整的丁蒽酮而非其水解产物是主要的效应物，而 10-丁酰基则是位点特异性探针，可能将抑制剂引向脂质底物/产物的结合位点附近。

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

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.

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Medical biology

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