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Gerardo Byk Catherine Dubertret Bertrand Schwartz Marc Frederic Gabrielle Jaslin Ravi Rangara Daniel Scherman 《Letters in Peptide Science》1997,4(4-6):263-267
We have synthesized novel cationiclipids for gene delivery bearing an ester bond betweenthe lipid moiety and the polyamine head. We have foundthat an intramolecular rearrangement occurs duringpurification of one of the products. The rearrangementled to a cyclic lipopolyamine which was active for DNAgene transfer. The formation ofcyclization products depends on the spacer foundbetween the lipid and the polyamine. The introduction ofarginine in the linker position prevents the formation ofcyclic products. Linear as well as cyclicanalogues showed high-efficiency gene transfer whentested in vitro for luciferase gene expressionas compared to dioctadecylamidoglycyl spermineor lipofectamine and also in vivo in the Lewislung carcinoma model. The introduction of arginine in thelinker position promoted increased transfectionactivity, demonstrating that a diversity of linkers,such as short peptides or glycosides, can beintroduced into cationic lipids for targeted gene transfer. 相似文献
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Bessodes M Dubertret C Jaslin G Scherman D 《Bioorganic & medicinal chemistry letters》2000,10(12):1393-1395
Lipidic glycosides with amino alkyl pendent groups were synthesized and evaluated for in vitro DNA transfection activity. The first representative of this new class of cationic lipids showed good gene delivery and low toxicity to HeLa and 3T3 cells. 相似文献
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Byk Gerardo Dubertret Catherine Schwartz Bertrand Frederic Marc Jaslin Gabrielle Rangara Ravi Scherman Daniel 《International journal of peptide research and therapeutics》1997,4(4-6):263-267
Summary We have synthesized novel cationic lipids for gene delivery bearing an ester bond between the lipid moiety and the polyamine
head. We have found that an intramolecular rearrangement occurs during purification of one of the products. The rearrangement
led to a cyclic lipopolyamine which was active for DNA gene transfer. The formation of cyclization products depends on the
spacer found between the lipid and the polyamine. The introduction of arginine in the linker position prevents the formation
of cyclic products. Linear as well as cyclic analogues showed high-efficiency gene transfer when tested in vitro for luciferase
gene expression as compared to dioctadecylamidoglycyl spermine or lipofectamine and also in vivo in the Lewis lung carcinoma
model. The introduction of arginine in the linker position promoted increased transfection activity, demonstrating that a
diversity of linkers, such as short peptides or glycosides, can be introduced into cationic lipids for targeted gene transfer. 相似文献
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