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., BİBER MÜFTÜLER F. Z.

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

  • Publication Type: Article / Article
  • Volume: 69 Issue: 2
  • Publication Date: 2011
  • Doi Number: 10.1016/j.apradiso.2010.10.027
  • Journal Name: APPLIED RADIATION AND ISOTOPES
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.299-307
  • Keywords: 8-Hydroxyquinoline (8-OHQ), 8-Hydroxyquinolyl-glucuronide (8-OHQ-Glu), beta-Glucuronidase, UDP-glucuronyl transferase (UDPGT), glucuronid prodrugs, Iodine 125, Iodine 131, BETA-D-GLUCURONIDE, ASSISTED SYNTHESIS, RADIOIODINATION, BIOSYNTHESIS, OPTIMIZATION, PRODRUGS, CANCER, I-131
  • Dokuz Eylül University Affiliated: Yes

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.