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

• Sawada Daisuke

  Faculty of Pharmaceutical Sciences, Teikyo University

• Tsukuda Yuya

  Faculty of Pharmaceutical Sciences, Teikyo University

• Yasuda Kaori

  Department of Biotechnology, Faculty of Engineering, Toyama Prefectural University

• Sakaki Toshiyuki

  Department of Biotechnology, Faculty of Engineering, Toyama Prefectural University

• Saito Hiroshi

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

• Takagi Ken-ichiro

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

• Takenouchi Kazuya

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

• Chen Tai C.

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

• Reddy G. Satyanarayana

  Epimer LLC Department of Chemistry, Brown University

• Kittaka Atsushi

  Faculty of Pharmaceutical Sciences, Teikyo University

書誌事項

タイトル別名

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

抄録

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.

収録刊行物

• ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ

  ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 60 (10), 1343-1346, 2012

  公益社団法人 日本薬学会

キーワード

• trihydroxyvitamin D₃
• vitamin D receptor
• metabolism
• human CYP24A1
• human liver microsome
• UDP-glucuronosyltransferase

詳細情報

• CRID: 1390282679155174144
• NII論文ID: 130001852369
• NII書誌ID: AA00602100
• DOI: 10.1248/cpb.c12-00526
• COI: 1:STN:280:DC%2BC3s%2FisFOmsQ%3D%3D
• ISSN: 13475223
• ISSN: 00092363
• NDL書誌ID: 023971779
• PubMed: 23036975
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I023971779
• Web Site: https://www.jstage.jst.go.jp/article/cpb/60/10/60_c12-00526/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2013124423
• 本文言語コード: en
• データソース種別:
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