Vitamin D relatives. Part I. B-thiophene-des-A-cholestanes. Solvolytic reactions of some derivatives of 2,2-disubstituted cyclohexane-1,4-diol and 4-hydroxycyclohexan-1-one

1986 ◽  
Vol 64 (8) ◽  
pp. 1536-1539 ◽  
Author(s):  
Jacek W. Morzycki
Keyword(s):  
Vitamin D ◽  
Thiophene Ring ◽  
Derivatives Of

Some derivatives of des-A-cholestane with a thiophene ring B have been prepared from triketone 2. The reactions of tosylates of C-10 alcohols (7b, 9b, and 8c) leading to A-ring ethers (10 and 11) and olefin 5, respectively, have been studied. The solvolysis of tosylate 4c and the Bamford–Stevens reactions of p-tosylhydrazones 3c and 13b are also discussed.

FOLLOW-UP OF LONG-TERM TREATMENT OF PREDIALYSIS RENAL BONE DISEASE WITH 1-α-HYDROXY-DERIVATIVES OF VITAMIN D

1983 ◽  
pp. 511-516
Author(s):  
J.R. JUTTMANN ◽  
D.H. BIRKENHÄGER-FRENKEL ◽  
T.J. VISSER ◽  
C. VAN KRIMPEN ◽  
J.C. BIRKENHÄGER
Keyword(s):  
Vitamin D ◽  
Bone Disease ◽  
Term Treatment ◽  
Long Term Treatment ◽  
Renal Bone Disease ◽  
Derivatives Of

The biological activity of 26-hydroxy-derivatives of cholecalciferol in vitamin d-deficient rats

FEBS Letters ◽  
1978 ◽  
Vol 96 (1) ◽  
pp. 216-218 ◽  
Author(s):  
J. Redel ◽  
L. Miravet ◽  
Y. Calando ◽  
M. Carre
Keyword(s):  
Vitamin D ◽  
Biological Activity ◽  
Derivatives Of

Design, Synthesis and Evaluation of Side-Chain Hydroxylated Derivatives of Lithocholic Acid as Potent Agonists of the Vitamin D Receptor (VDR)

2021 ◽  
pp. 105202
Author(s):  
Carmen M. González ◽  
Sunil Gaikwad ◽  
Gonzalo Lasanta ◽  
Julian Loureiro ◽  
Niclas Nilsson ◽  
...  
Keyword(s):  
Vitamin D ◽  
Vitamin D Receptor ◽  
Lithocholic Acid ◽  
Side Chain ◽  
Design Synthesis ◽  
Derivatives Of

scholarly journals Comparative studies on the 25-hydroxylations of cholecalciferol and 1α-hydroxycholecalciferol in perfused rat liver

1978 ◽  
Vol 170 (3) ◽  
pp. 495-502 ◽  
Author(s):  
Masafumi Fukushima ◽  
Yasuho Nishii ◽  
Michiko Suzuki ◽  
Tatsuo Suda
Keyword(s):  
Vitamin D ◽  
Rat Liver ◽  
Linear Relation ◽  
Comparative Studies ◽  
Similar Rate ◽  
The Other ◽  
Perfused Rat Liver ◽  
Km Value ◽  
Derivatives Of ◽  
25 Hydroxycholecalciferol

The 25-hydroxylations of [3H]cholecalciferol and 1α-hydroxy[3H]cholecalciferol in perfused rat liver were compared. Results showed that about twice as much 1α(OH)D3 (1α-hydroxycholecalciferol) was incorporated into the liver as cholecalciferol. 25-Hydroxy[3H]cholecalciferol and 1α-25-dihydroxy[3H]cholecalciferol were not incorporated significantly. Livers isolated from vitamin D-deficient rats formed the 25-hydroxy derivatives of cholecalciferol and 1α(OH)D3 respectively linearly with time for at least 120min. The rate of 1α,25(OH)2D3 (1α,25-dihydroxycholecalciferol) production increased exactly 10-fold on successive 10-fold increases in the dose of 1α(OH)D3, suggesting that hepatic 25-hydroxylation of 1α(OH)D3 is not under metabolic control. On the other hand, the rate of conversion of cholecalciferol into 25(OH)D3 (25-hydroxycholecalciferol) did not increase linearly with increase in the amount of cholecalciferol in the perfusate. The 25-hydroxylation of cholecalciferol seemed to proceed at a similar rate to that of 1α(OH)D3 at doses of less than 1nmol, but with doses of more than 2.5nmol, the conversion of cholecalciferol into 25(OH)D3 became much less efficient, though the linear relation between the amounts of substrate and product was maintained. A reciprocal plot of data on the 25-hydroxylation of cholecalciferol gave two Km values of about 5.6nm and 1.0μm, whereas that for the 25-hydroxylation of 1α(OH)D3 gave a single Km value of about 2.0μm. These results suggest that there are two modes of 25-hydroxylation of cholecalciferol in the liver, which seem to be closely related to the mechanism of control of 25(OH)D3 production by the liver.

EFFECTS OF HYDROXYLATED DERIVATIVES OF VITAMIN D3 AND OF AQUEOUS EXTRACTS OF SOLANUM MALACOXYLON ON THE ABSORPTION OF CALCIUM, PHOSPHATE, SODIUM, POTASSIUM AND WATER FROM THE JEJUNUM OF PIGS

1979 ◽  
Vol 82 (3) ◽  
pp. 417-424 ◽  
Author(s):  
J. FOX ◽  
A. D. CARE
Keyword(s):  
Vitamin D ◽  
Calcium Phosphate ◽  
Time Course ◽  
Intestinal Loop ◽  
Delayed Response ◽  
Aqueous Extracts ◽  
Sodium Potassium ◽  
Solanum Malacoxylon ◽  
Derivatives Of ◽  
Sodium And Potassium

The effects of hydroxylated derivatives of vitamin D3 and aqueous extracts of Solanum malacoxylon on the intestinal absorption of calcium, phosphate, sodium, potassium and water have been studied in unstressed vitamin D-replete pigs each of which was surgically prepared beforehand with a Thirty–Vella loop of jejunum. The addition, for six 1 h periods of perfusion, of 1,25-dihydroxycholecalciferol (1,25-(OH)2D3) or 1α-hydroxycholecalciferol at similar concentrations (3·6–3·75 pmol/ml) to the solution used to perfuse the intestinal loop caused a rapid increase in the absorption of calcium but increased the absorption of phosphate only after a delay of at least 12 h. The absorption of both calcium and phosphate reached a maximum on the day following the addition of the vitamin D derivative to the perfusate. The addition of 25-hydroxycholecalciferol (25-(OH)D3) at a concentration of 3·75 pmol/ml was without effect on absorption except for a small increase in the absorption of phosphate on the following day. However, at higher concentrations (> 250 pmol 25-(OH)D3/ml) the absorptions of calcium and phosphate were both increased rapidly. 24,25-Dihydroxycholecalciferol was without effect on absorption at the concentration tested (3·6 pmol/ml). Aqueous extracts (1%) of the leaf of S. malacoxylon showed similar effects on absorption to those of 1,25-(OH)2D3. However, there was one point of difference; the absorption of phosphate was stimulated with a similar time course to that of calcium in contrast to its delayed response to 1,25-(OH)2D3. The absorption rates of water, sodium and potassium were not consistently affected by 1,25-(OH)2D3 or S. malacoxylon. However, the major effects of these derivatives were usually seen on the day following the day of addition to the perfusate. In contrast, 25-(OH)D3 at high concentrations had a marked effect on the absorption of water, sodium and potassium on the day of addition.

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