Enzymatic synthesis of I-125/131 labeled 8-hydroxyquinoline glucuronide and in vitro/in vivo evaluation of biological influence


YESILAGAC R., ÜNAK P. , MEDİNE E. İ. , İÇHEDEF Ç. , Ertay T., Muftuler F. Z. B.

APPLIED RADIATION AND ISOTOPES, vol.69, no.2, pp.299-307, 2011 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 69 Issue: 2
  • Publication Date: 2011
  • Doi Number: 10.1016/j.apradiso.2010.10.027
  • Title of Journal : APPLIED RADIATION AND ISOTOPES
  • Page Numbers: pp.299-307

Abstract

8-Hydroxyquinoline (8-OHQ) is a long-known molecule which due to its metal-complexation ability is frequently used for analysis. It is also called oxine. Oxine and derivatives have been investigated to process antitumor and antimicrobial activities. 8-Hydroxyquinolyl-glucuronide (8-OHQ-Glu) was enzymatically synthesized using microsome preparates separated from Hutu-80 cells, labeled with I-125 to perform a radionuclide labeled prodrug and investigated of its biological affinities on Hutu-80 (human duodenum intestinal adenocarcinoma), Caco-2 (human colorectal adenocarcinoma), Detroit 562 (human pharynx adenocarcinoma) cells and ACBRI 519 (primary human small intestine epithelial cells) in this work. UDP-glucuronyl transferase (UDPGT) rich microsome preparates, which are used for glucuronidation in enzymatic synthesis, were extracted from Hutu-80 cells.