Structure-activity relationship studies of flavonoids as potent inhibitors of human platelet 12-hLO, reticulocyte 15-hLO-1, and prostate epithelial 15-hLO-2
Structure-activity relationship studies of flavonoids as potent inhibitors of human platelet 12-hLO, reticulocyte 15-hLO-1, and prostate epithelial 15-hLO-2
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DOI：
10.1016/j.bmc.2007.07.036
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发表时间：
2007-12-01
影响因子：
3.5
通讯作者：
Sepulveda-Boza, Silvia
中科院分区：
文献类型：
--
作者：
Vasquez-Martinez, Yesseny;Ohri, Rachana V.;Sepulveda-Boza, Silvia
人脂氧合酶（hLO）同工酶与许多疾病状态有关，并且关于其抑制引起了很多关注。一类抑制剂类黄酮已被证明是有效的脂氧合酶抑制剂，但其研究仅限于自然界中发现的那些化合物，这些化合物具有有限的结构变异性。因此，我们进行了全面的研究，以确定类黄酮的效力和选择性对血小板12-hLO，网织红细胞15-hLO-1，前列腺上皮15-hLO-2的结构要求。我们从这项研究中得出结论，儿茶酚是必不可少的高效力，该黄酮和异黄烷酮倾向于选择对12-hLO，该黄酮倾向于选择对15-hLO-1，但很少有类黄酮的目标15-hLO-2。(C)2007爱思唯尔有限公司保留所有权利。
Human lipoxygenase (hLO) isozymes have been implicated in a number of disease states and have attracted much attention with respect to their inhibition. One class of inhibitors, the flavonoids, have been shown to be potent lipoxygenase inhibitors but their study has been restricted to those compounds found in nature, which have limited structural variability. We have therefore carried out a comprehensive study to determine the structural requirements for flavonoid potency and selectivity against platelet 12-hLO, reticulocyte 15-hLO-1, and prostate epithelial 15-hLO-2. We conclude from this study that catechols are essential for high potency, that isoflavones and isoflavanones tend to select against 12-hLO, that isoflavans tend to select against 15-hLO-1, but few flavonoids target 15-hLO-2. (C) 2007 Elsevier Ltd. All rights reserved.