Londowski J M, Revelle L K, Kost S B, Corradino R A, Kumar R
J Steroid Biochem. 1985 Jul;23(1):81-5. doi: 10.1016/0022-4731(85)90264-x.
We synthesized 3 beta-thiovitamin D3 from 7-dehydrocholesterol and tested its biological activity and protein binding properties. The thiovitamin was found to be a weak vitamin D agonist at high doses in vivo. It was poorly bound by both vitamin D-binding protein as well as by the intestinal cytosol receptor for 1,25-dihydroxyvitamin D. It did not increase the synthesis of calcium binding protein in the chick embryonic duodenum and did not block the activity of 1,25-dihydroxyvitamin D3 in this system. We conclude that 3 beta-thiovitamin D3 is a weak vitamin D agonist in vivo with no agonist activity or antagonist activity to 1,25-dihydroxyvitamin D3 in the chick embryonic duodenum.
我们从7-脱氢胆固醇合成了3β-硫代维生素D3，并测试了其生物学活性和蛋白质结合特性。发现该硫代维生素在体内高剂量时是一种弱维生素D激动剂。它与维生素D结合蛋白以及1,25-二羟基维生素D的肠道胞质溶胶受体的结合都很差。它不会增加鸡胚十二指肠中钙结合蛋白的合成，也不会在该系统中阻断1,25-二羟基维生素D3的活性。我们得出结论，3β-硫代维生素D3在体内是一种弱维生素D激动剂，对鸡胚十二指肠中的1,25-二羟基维生素D3没有激动剂活性或拮抗剂活性。
