Fukushima M, Niki R, Ohkawa H, Shimizu T, Matsunaga I, Nakano H, Takagaki Y, Nishii Y, Okano K, Suda T
Endocrinology. 1980 Jul;107(1):328-33. doi: 10.1210/endo-107-1-328.
The comparative effectiveness of vitamin D3 and its derivatives in curing hyperparathyroidism and osteodystrophic bone lesions was examined in a laboratory model of renal osteodystrophy associated with marked secondary hyperparathyroidism in rats. The experimental model was prepared by a single injection of homologous glycopeptide. Plasma levels of 1 alpha,25-dihydroxyvitamin D3 [1 alpha,25(OH)2D3] appeared to decrease in the rats receiving glycopeptide. Various doses of vitamin D3 derivatives [2 or 10 microgram/kg D3, 2 microgram/kg 25-hydroxyvitamin D3 (25OHD3), 0.1 microgram/kg 1 alpha,25(OH)2D3, and 0.1 or 0.2 microgram/kg 1 alpha-hydroxyvitamin D3 (1 alpha OHD3)] were daily administered orally to the nephritic rats for 23 days before sacrifice. 1 alpha,25(OH)2D3 and 1 alpha OHD3 were much more potent than 25OHD3 and D3 in reducing the hyperplasia of parathyroir glands. The potency of 1 alpha OHD3 in curing the histological changes of osteodystrophy appeared to be greater than that of 1 alpha,25(OH)2D3. The same dose level of 1 alpha OHD3 was more effective than 1 alpha,25(OH)2D3 in enhancing plasma 1 alpha,25(OH)2D3 levels.
在大鼠严重继发性甲状旁腺功能亢进相关的肾性骨营养不良实验室模型中,研究了维生素D3及其衍生物在治疗甲状旁腺功能亢进和骨营养不良性骨病变方面的相对疗效。通过单次注射同源糖肽制备实验模型。接受糖肽的大鼠血浆1α,25-二羟维生素D3[1α,25(OH)2D3]水平似乎降低。在处死前23天,每天给患肾病的大鼠口服各种剂量的维生素D3衍生物[2或10微克/千克D3、2微克/千克25-羟维生素D3(25OHD3)、0.1微克/千克1α,25(OH)2D3以及0.1或0.2微克/千克1α-羟维生素D3(1αOHD3)]。1α,25(OH)2D3和1αOHD3在减轻甲状旁腺增生方面比25OHD3和D3有效得多。1αOHD3在治愈骨营养不良组织学变化方面的效力似乎大于1α,25(OH)2D3。相同剂量水平的1αOHD3在提高血浆1α,25(OH)2D3水平方面比1α,25(OH)2D3更有效。