Premium
Synthesis and in vitro Inhibition Properties of siRNA Conjugates Carrying Acridine and Quindoline Moieties
Author(s) -
Aviñó Anna,
Ocampo Sandra M.,
Perales José C.,
Eritja Ramon
Publication year - 2012
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.201100321
Subject(s) - acridine , chemistry , hela , conjugate , transfection , acridine derivatives , in vitro , rna , small interfering rna , fluorescence , stereochemistry , oligonucleotide , combinatorial chemistry , biophysics , biochemistry , dna , organic chemistry , biology , gene , mathematical analysis , physics , mathematics , quantum mechanics
The synthesis of RNA molecules carrying acridine or quindoline residues at their 3′‐ and 5′‐termini is reported. These conjugates are fully characterized by MALDI‐TOF mass spectrometry. Modified siRNA duplexes carrying acridine or quindoline moieties were evaluated for inhibition of the tumor necrosis factor. The conjugates showed inhibitory properties similar to those of unmodified RNA duplexes in HeLa cells transfected with oligofectamine. The fluorescent properties of acridine derivatives allow direct observation of the cytoplasmatic distribution of modified siRNA inside the cells.