Gardner R M, Reinhardt T A, Horst R L
National Animal Disease Center, U.S. Department of Agriculture, Ames, IA 50010.
J Steroid Biochem. 1988 Feb;29(2):185-9. doi: 10.1016/0022-4731(88)90264-6.
Biological assays were performed to evaluate 10-oxo-19-nor-vitamin D3 (10-oxo-D3) and 5(E) 25-hydroxy-10-oxo-19-nor-vitamin D3 (25-OH-10-oxo-D3) two bacterial products of vitamin D3 (D3) and 25-hydroxyvitamin D3 (25-OHD3) metabolism, respectively. The 5(Z) and 5(E) isomers of 10-oxo-D3 were, respectively, 40- and 80-fold less active than D3 in stimulating Ca+2 absorption from the gut. 25-Hydroxy-10-oxo-D3 did not stimulate Ca+2 absorption. Only 5(Z) 10-oxo-D3 induced mobilization of bone Ca+2. In addition, both 10-oxo-D3 and 25-OH-10-oxo-D3 showed poor affinities for either the plasma D3-binding protein or the thymus 1,25-dihydroxyvitamin D3 [1,25-(OH)2D3] receptor. 10-Keto-D3 exhibited a plasma half-life of only 6 min. This was a much shorter half-life than that exhibited by other vitamin D metabolites and was expected because of the poor affinity 10-oxo-D3 has for the plasma vitamin D binding protein. Bacterial metabolism of D3 deactivates the vitamin, which allows ruminants to tolerate relatively large oral doses of D3.
进行了生物学测定,以评估10-氧代-19-去甲维生素D3(10-氧代-D3)和5(E)-25-羟基-10-氧代-19-去甲维生素D3(25-OH-10-氧代-D3),它们分别是维生素D3(D3)和25-羟基维生素D3(25-OHD3)代谢的两种细菌产物。10-氧代-D3的5(Z)和5(E)异构体在刺激肠道对Ca+2的吸收方面,活性分别比D3低40倍和80倍。25-羟基-10-氧代-D3不刺激Ca+2的吸收。只有5(Z)-10-氧代-D3能诱导骨Ca+2的动员。此外,10-氧代-D3和25-OH-10-氧代-D3对血浆D3结合蛋白或胸腺1,25-二羟基维生素D3[1,25-(OH)2D3]受体的亲和力都很差。10-酮-D3的血浆半衰期仅为6分钟。这比其他维生素D代谢产物的半衰期短得多,由于10-氧代-D3对血浆维生素D结合蛋白的亲和力差,所以预期会有这样的结果。D3的细菌代谢使维生素失活,这使得反刍动物能够耐受相对大剂量的口服D3。