SYNTHESIS OF 25-HYDROXYCHOLECALCIFEROL . A BIOLOGICALLY ACTIVE METABOLITE OF VITAMIN D3
SYNTHESIS OF 25-HYDROXYCHOLECALCIFEROL . A BIOLOGICALLY ACTIVE METABOLITE OF VITAMIN D3
复制标题
DOI：
10.1021/bi00830a031
复制
发表时间：
1969-01-01
期刊：
影响因子：
2.9
通讯作者：
DELUCA, HF
中科院分区：
文献类型：
--
作者：
BLUNT, JW;DELUCA, HF
1968 a，B）。这种代谢物在治疗大鼠佝偻病方面比维生素D3更有效，并且能够比类似量的维生素D3更早地刺激离体大鼠肠囊中的钙转运。此外，大鼠中的骨吸收显示在25-羟基胆钙化醇剂量后比在类似剂量的维生素D3后更早发生（Blunt等人，1968年c）。根据这些实验和前面引用的其他实验（DeLuca，1967），有人提出25-羟基胆钙化醇可能是维生素的代谢活性形式。为了继续研究以证实这一发现，并研究该代谢产物的其他可能用途，有必要合成更大量的25-羟基胆钙化素。因此，用两种方法合成了胆甾-5，7-二烯-3/3，25-二醇，用紫外线照射该二醇，产生了25-羟基胆钙化醇，其在所有方面，包括生物活性，都与以前从猪浆体中分离的物质相同。
1968a, b). This metabolite was shown to be more efficient than vitamin D3 in curing rickets inrats, and was able to stimulate calciumtransport in isolated rat intestinal sacs earlier than a similar amount of vitamin D3. Also, bone resorptionin rats was shown to occur after a dose of 25-hydroxycholecalciferol earlier than after a similar dose of vitamin D3 (Blunt et al., 1968c). As a result of these experiments, and others cited earlier (DeLuca, 1967), the suggestion was made that25-hydroxycholecalciferol was possibly the metabol-ically active form of the vitamin. In order to continue studies to verify thissuggestion, and to investigate other possible uses of the metabolite, it became necessary to synthesize 25-hydroxycholecalciferolin largeramounts. Accordingly, cholesta-5, 7-diene-3/3, 25-diol has been synthesized by two methods, and irradiation of this with ultraviolet light produced 25-hydroxycholecalciferol, identical in all respects, including biological activity, with the material isolated previouslyfrom porcineplasma.