Synthesis and Biological Activities of 1α,4α,25- and 1α,4β,25-Trihydroxyvitamin D3 and Their Metabolism by Human CYP24A1 and UDP-Glucuronosyltransferase

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概要

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• A previous report has demonstrated the existence of a C4-hydroxylated vitamin D2 metabolite in serum of rats treated with pharmacological doses of vitamin D2. However, the biological significance and metabolic fate of this metabolite have not been described. To explore its potential biological activities, we therefore synthesized 1α,4α,25-trihydroxyvitamin D3 and its diastereoisomer, 1α,4β,25-trihydroxyvitamin D3, using Trost Pd-mediated coupling reaction, and studied their vitamin D receptor (VDR) binding affinity, osteocalcin promoter transactivation activity, and their further metabolism by human CYP24A1 as well as by human liver microsomal fraction based on CYP- and UDP-glucuronosyltransferases (UGTs)-reactions.

著者

• Yasuda Kaori

  Department Of Applied Biology And Chemistry Faculty Of Applied Bioscience Tokyo University Of Agricu

• KITTAKA Atsushi

  Faculty of Pharmaceutical Sciences, Teikyo University

• Sawada Daisuke

  Faculty Of Pharmaceutical Sciences University Of Tokyo

• Chen Tai

  Section Of Endocrinology Diabetes And Nutrition Department Of Medicine Boston University School Of M

• Kittaka Atsushi

  Faculty Of Pharmaceutical Sciences Teikyo University

• Sakaki Toshiyuki

  Department Of Biotechnology Faculty Of Engineering Toyama Prefectural University

• Takenouchi Kazuya

  Teijin Institute for Bio-medical Research, Teijin Pharma Ltd.

• Reddy G.

  Epimer LLC

• Chen Tai

  Section of Endocrinology, Diabetes and Nutrition, School of Medicine, Boston University

• Tsukuda Yuya

  Faculty of Pharmaceutical Sciences, Teikyo University

• Saito Hiroshi

  Teijin Institute for Bio-medical Research, Teijin Pharma Ltd.

• Takagi Ken-ichiro

  Teijin Institute for Bio-medical Research, Teijin Pharma Ltd.

• Sawada Daisuke

  Faculty of Pharmaceutical Sciences, Teikyo University

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