| Title | Preparation of Sodium Deoxycholate (DOC) Conjugated Heparin Derivatives for Inhibition of Angiogenesis and Cancer Cell Growth. | | Author(s) | Cho KJ, Moon HT, Park GE, Jeon OC, Byun Y, Lee YK | | Institution | Department of Otolaryngology, Head and Neck Surgery, The Catholic University of Korea, College of Medicine Uijeongbu, St. Mary’s Hospital, Kyunggi-Do 480-717, Korea, Mediplex Corporation, Seoul 135-729, Korea, College of Pharmacy, Seoul National University, San 56-1, Sillim-dong, Gwanak-gu, Seoul 151-742, Korea, and Department of Chemical and Biological Engineering, Chungju National University, Chungbuk 380-702, Korea yrbyun@snu.ac.kr, leeyk@cjnu.ac.kr. | | Source | Bioconjug Chem 2008 Jun 28. | | Abstract | We describe new DOC (sodium deoxycholate)-heparin nanoparticles for in vivo tumor targeting and inhibition of angiogenesis based on chemical conjugation and the enhanced permeability and retention (EPR) effect. Heparin has been used as a potent anticoagulant agent for 70 years, and has recently been found to inhibit the activity of growth factors which stimulate the smooth muscle cells around tumor. From the results, DOC and heparin were conjugated by bonding carboxyl groups of heparin with amine groups of aminated sodium deoxycholate. Larger antitumor effects of the DOC-heparin VI (8.5 mol of DOC coupled with 1.0 mol heparin) were achieved in animal studies, compared to heparin alone. We confirmed that the conjugated heparin retained its ability to inhibit binding with angiogenic factor, showing a significant decrease in endothelial tubular formation. These results provide new insights into the nontoxic anticancer drug carrier as well as the design of multifunctional bioconjugates for targeted drug delivery. | | Language | ENG | | Pub Type(s) | JOURNAL ARTICLE
| | PubMed ID | 18588324 |
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