Synthesis of novel vitamin K analogues with modification at ω-terminal position and evaluation of their transcriptional activity via steroid and xenobiotic receptor (SXR)

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  • 側鎖末端部を修飾した新規ビタミンK誘導体の合成と核内受容体SXRを介した転写活性の検討
  • ガワ クサリマッタンブ オ シュウショク シタ シンキ ビタミン K ユウドウタイ ノ ゴウセイ ト カク ナイ ジュヨウタイ SXR オ カイシタ テンシャ カッセイ ノ ケントウ

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Abstract

Menaquinone-4 (vitamin K_2) is a ligand for a nuclear receptor, steroid and xenobiotic receptor (SXR), that induces the gene expressions of CYP3A4. We synthesized vitamin K_2 analogues with hydroxyl or phenyl groups at the ω-terminal of the side chain. The up-regulation of SXR-mediated transcription of the target gene by the analogues was dependent on the length of the side chain and the hydrophobicity of the ω-terminal residues. A new analogue that has phenyl group introduced to menaquinone-3 showed the most potent activity among our synthesized compounds. The analogue was approximately estimated twice as active as menaquinone-4, and almost same as the known SXR ligand rifampicin.

Journal

  • VITAMINS

    VITAMINS 86 (9), 493-498, 2012

    THE VITAMIN SOCIETY OF JAPAN

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