Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
2000-7-7
pubmed:abstractText
Three novel cationic cholesterol derivatives with different modes of linkage between the cationic headgroup and the cholesteryl backbone have been synthesized and used as mixtures with 1, 2-dioleoyl-L-alpha-glycero-3-phosphatidyl ethanolamine (DOPE) for liposome-mediated gene transfection. A pronounced improvement in gene transfer efficiency was observed when the cationic center was appended to the cholesteryl backbone using an ether linkage as opposed to when the linkages were based on either ester or urethane groups. Amphiphiles with ether links such as cholest-5-en-3beta-oxyethane-N,N,N-trimethyl ammonium bromide (2) and cholest-5-en-3beta-oxyethane-N,N-dimethyl-N-2-hydroxyethyl ammonium bromide (3) showed transfection efficiencies considerably greater than commercially available gene transfer reagents. Notably, the transfection ability of 2 with DOPE in the presence of serum was significantly greater than Lipofectamine((R)) and Lipofectin((R)). Interestingly, 3 did not require the helper lipid DOPE for transfection. This suggests that these newly described cholesterol-based amphiphiles should be very promising in liposome-mediated gene transfection. The advantage that the ether linkage possesses would be important in the design of newer, more efficient cholesterol-based delivery reagents.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
0014-5793
pubmed:author
pubmed:issnType
Print
pubmed:day
19
pubmed:volume
473
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
341-4
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
2000
pubmed:articleTitle
Nature of linkage between the cationic headgroup and cholesteryl skeleton controls gene transfection efficiency.
pubmed:affiliation
Department of Organic Chemistry, Indian Institute of Science, Bangalore, India.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't