Effect of three A-ring analogs of 1 alpha,25-dihydroxyvitamin D3 on 25-OH-D3-1 alpha-hydroxylase in isolated mitochondria and on 25-hydroxyvitamin D3 metabolism in cultured kidney cells.
Effect of three A-ring analogs of 1 alpha,25-dihydroxyvitamin D3 on 25-OH-D3-1 alpha-hydroxylase in isolated mitochondria and on 25-hydroxyvitamin D3 metabolism in cultured kidney cells.
复制标题
1 α,25-二羟基维生素 D3 的三个 A 环类似物对分离线粒体中 25-OH-D3-1 α-羟化酶和培养肾细胞中 25-羟基维生素 D3 代谢的影响。
DOI：
10.1016/0960-0760(91)90091-i
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发表时间：
1991
期刊：
影响因子：
--
通讯作者：
Okamura,WH
中科院分区：
文献类型：
--
作者：
Henry,HL;Fried,S;Shen,GY;Barrack,SA;Okamura,WH
Three A-ring analogs of 1α,25-dihydroxyvitamin D3(1,25(OH)2D3)—2-nor-1,3-seco-1,25(OH)2D3(2-nor analog), 2-oxa-3-deoxy-25-OH-D3(2-oxa analog), and A-homo-3-deoxy-3,3-dimethyl-2,4-dioxa-25-OH-D3(A-homo analog)—were tested for their ability to inhibit 25-OH-D3-1α-hydroxylase (1α-hydroxylase) in isolated mitochondria and to alter 25-OH-D3metabolism in cultured chick kidney cells. The 2-nor and 2-oxa analogs were relatively potent (Kis of 60 and 30 nM, respectively, compared with 170 nM for 1,25(OH)2D3), whereas the A-homo analog was completely ineffective in inhibiting 1α-hydroxylase activity. In contrast, all three analogs were able to repress 1α-hydroxylase and induce 24-hydroxylase activity in cultured chick kidney cells, suggesting that this process is not one of direct action in the mitochondria, but is more likely to be a receptor-mediated one.
