EVIDENCE FOR THE METABOLISM OF 24R-HYDROXY-25-FLUOROVITAMIN-D3 AND 1ALPHA-HYDROXY-25-FLUOROVITAMIN-D3 TO 1ALPHA,24R-DIHYDROXY-25-FLUOROVITAMIN-D3

被引：18

作者：

NAPOLI, JL ^{[1
]}

MELLON, WS ^{[1
]}

SCHNOES, HK ^{[1
]}

DELUCA, HF ^{[1
]}

机构：

[1] UNIV WISCONSIN,COLL AGR & LIFE SCI,DEPT BIOCHEM,MADISON,WI 53706

来源：

ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS | 1979年 / 197卷 / 01期

基金：

美国国家卫生研究院;

关键词：

D O I：

10.1016/0003-9861(79)90236-4

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

High-pressure liquid chromatography capable of resolving all known vitamin D metabolites and a sensitive competitive binding protein assay specific for 1α,25-dihydroxyvitamin D3 were used to assay the blood of rats dosed with ethanol, 1α-hydroxyvitamin D3, 24R-hydroxy-25-fluorovitamin D3, or 1α-hydroxy-25-fluorovitamin D3. Compared to the ethanoldosed animals, the blood of rats dosed with 1α-hydroxyvitamin D3 had increased levels of 1α,25-dihydroxyvitamin D3; but those dosed with the fluorinated vitamins did not. Instead, their blood contained a compound that cochromatographs with 1α,24R-dihydroxyvitamin D3 on high-pressure liquid chromatography and binds to the 1,25-dihydroxyvitamin D3 receptor proteins. 1α,24R-Dihydroxyvitamin D3 binds as well as 1α, 25-dihydroxyvitamin D3 to the chick-intestinal cytosol receptor protein for 1α,25-dihydroxyvitamin D3; whereas 1α,24S-dihydroxyvitamin D3 binds only one-tenth as well as 1α,25-dihydroxyvitamin D3. Thus it appears that in vivo, the fluorinated vitamin D compounds are converted to a compound likely to be 1α,24R-dihydroxy-25-fluorovitamin D3 and that may rival the potency of 1α,25-dihydroxyvitamin D3. © 1979.

引用

页码：193 / 198

页数：6

共 26 条

[1] REGULATION BY CALCIUM OF IN-VIVO SYNTHESIS OF 1,25-DIHYDROXYCHOLECALCIFEROL AND 21,25-DIHYDROXYCHOLECALCIFEROL [J].

BOYLE, IT ;

GRAY, RW ;

DELUCA, HF .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1971, 68 (09) :2131-&

[2] METABOLISM AND MECHANISM OF ACTION OF VITAMIN-D1 [J].

DELUCA, HF ;

SCHNOES, HK .

ANNUAL REVIEW OF BIOCHEMISTRY, 1976, 45 :631-666

[3]

DELUCA HF, 1978, HDB LIPID RES, V2, P69

[4] SENSITIVE, PRECISE, AND CONVENIENT METHOD FOR DETERMINATION OF 1,25-DIHYDROXYVITAMIN-D IN HUMAN-PLASMA [J].

EISMAN, JA ;

HAMSTRA, AJ ;

KREAM, BE ;

DELUCA, HF .

ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 1976, 176 (01) :235-243

[5] INTESTINAL 1,25-DIHYDROXYVITAMIN-D3 BINDING-PROTEIN - SPECIFICITY OF BINDING [J].

EISMAN, JA ;

DELUCA, HF .

STEROIDS, 1977, 30 (02) :245-257

[6] SYNTHETIC DERIVATIVES OF CORTICAL HORMONES [J].

FRIED, J ;

BORMAN, A .

VITAMINS AND HORMONES, 1958, 16 :303-374

[7] METABOLISM OF 1ALPHA-HYDROXYVITAMIN-D3 TO 1ALPHA,25-DIHYDROXYVITAMIN-D3 IN PERFUSED RAT-LIVER [J].

FUKUSHIMA, M ;

SUZUKI, Y ;

TOHIRA, Y ;

MATSUNAGA, I ;

OCHI, K ;

NAGANO, H ;

NISHII, Y ;

SUDA, T .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1975, 66 (02) :632-638

[8]

HEIDELBERGER C, 1958, CANCER RES, V18, P305

[9]

HENRY HL, 1974, J BIOL CHEM, V249, P7584

[10]

HOLICK MF, 1976, J BIOL CHEM, V251, P1020

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