Document Detail


Targeted delivery of a triplex-forming oligonucleotide to hepatic stellate cells.
MedLine Citation:
PMID:  15766277     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Liver fibrosis is characterized by abnormal accumulation of extracellular matrix (ECM), namely, fibrillar collagens in the hepatic stellate cells (HSCs). Earlier, we developed an antigene approach, using a type alpha1(I) collagen gene promoter specific triplex-forming oligonucleotide (TFO) to inhibit collagen gene expression. In this paper, to enhance overall delivery of TFOs to the liver and more specifically to HSCs, we synthesized mannose 6-phosphate-bovine serum albumin (M6P-BSA) by phosphorylating p-nitrophenyl-alpha-d-mannopyranoside, reducing its nitro group, and reacting it with thiophosgene to produce p-isothiocyanatophenyl-6-phospho-alpha-d-mannopyranoside (itcM6P) for conjugation with BSA. (33)P-TFO was conjugated with M6P-BSA via a disulfide bond, and the stability of the (M6P)(20)-BSA-TFO conjugate was determined. Following tail vein injection into rats, (M6P)(20)-BSA-(33)P-TFO rapidly cleared from the circulation and accumulated mainly in the liver. Almost 66% of the injected (M6P)(20)-BSA-(33)P-TFO accumulated in the liver at 30 min postinjection, which was significantly higher than that deposited after injection of (33)P-TFO. A large proportion of the injected (M6P)(20)-BSA-(33)P-TFO was taken up by the HSCs as evidenced by determination of radioactivity in the digested liver cells upon liver perfusion and separation on a Nycodenz gradient. Therefore, this TFO conjugate may be used for the treatment of liver fibrosis.
Authors:
Zhaoyang Ye; Kun Cheng; Ramareddy V Guntaka; Ram I Mahato
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Biochemistry     Volume:  44     ISSN:  0006-2960     ISO Abbreviation:  Biochemistry     Publication Date:  2005 Mar 
Date Detail:
Created Date:  2005-03-15     Completed Date:  2005-05-25     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  0370623     Medline TA:  Biochemistry     Country:  United States    
Other Details:
Languages:  eng     Pagination:  4466-76     Citation Subset:  IM    
Affiliation:
Department of Pharmaceutical, University of Tennessee Health Science Center, Memphis, Tennessee 38163, USA.
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MeSH Terms
Descriptor/Qualifier:
Animals
DNA / administration & dosage*,  chemical synthesis,  metabolism
Disulfides / chemistry
Drug Carriers / administration & dosage,  chemical synthesis,  metabolism
Gene Targeting* / methods
Liver / cytology*,  metabolism*
Male
Mannosephosphates / administration & dosage,  chemical synthesis
Nucleic Acid Conformation* / drug effects
Oligodeoxyribonucleotides / administration & dosage*,  chemical synthesis,  metabolism
Perfusion
Rats
Rats, Sprague-Dawley
Serum Albumin, Bovine / administration & dosage,  chemical synthesis
Succinimides / administration & dosage,  chemical synthesis
Thionucleotides / administration & dosage,  chemical synthesis,  metabolism
Grant Support
ID/Acronym/Agency:
47379//PHS HHS; R01 DK064633/DK/NIDDK NIH HHS
Chemical
Reg. No./Substance:
0/Disulfides; 0/Drug Carriers; 0/Mannosephosphates; 0/Oligodeoxyribonucleotides; 0/Serum Albumin, Bovine; 0/Succinimides; 0/Thionucleotides; 0/triplex DNA; 3672-15-9/mannose-6-phosphate; 68181-17-9/N-succinimidyl 3-(2-pyridyldithio)propionate; 9007-49-2/DNA

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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