Bile acid–oligodeoxynucleotide conjugates: synthesis and liver excretion in rats

The synthesis of bile acid–oligodeoxynucleotide conjugates via the 3-OH group of the bile acids is described. When used in vivo in rats, covalent conjugation of an oligodeoxynucleotide via a linker to cholic acid resulted in an increased biliary excretion of bile acid–oligodeoxynucleotide conjugates...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2001-04, Vol.11 (7), p.945-949
Hauptverfasser:	Starke, Dieter, Lischka, Kerstin, Pagels, Peter, Uhlmann, Eugen, Kramer, Werner, Wess, Günter, Petzinger, Ernst
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Bile Acids and Salts - chemistry Bile Acids and Salts - metabolism Bile Acids and Salts - pharmacokinetics Biological and medical sciences Hepatocytes - metabolism In Vitro Techniques Liver - metabolism Male Medical sciences Miscellaneous Oligodeoxyribonucleotides - chemistry Oligodeoxyribonucleotides - metabolism Oligodeoxyribonucleotides - pharmacokinetics Pharmacology. Drug treatments Rats Rats, Wistar
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Zusammenfassung:	The synthesis of bile acid–oligodeoxynucleotide conjugates via the 3-OH group of the bile acids is described. When used in vivo in rats, covalent conjugation of an oligodeoxynucleotide via a linker to cholic acid resulted in an increased biliary excretion of bile acid–oligodeoxynucleotide conjugates compared to unconjugated oligodeoxynucleotides. The synthesis of bile acid–oligodeoxynucleotide conjugates via the 3-OH group of the bile acids is described. When used in vivo in rats, covalent conjugation of an oligodeoxynucleotide via a linker to cholic acid resulted in an increased biliary excretion of bile acid–oligodeoxynucleotide conjugates compared to unconjugated oligodeoxynucleotides.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(01)00048-8