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Solid phase synthesis of novel asymmetric hydrophilic head cholesterol-based cationic lipids with potential DNA delivery.

Abstract：

:Twenty-four asymmetric divalent head group cholesterol-based cationic lipids were designed and synthesized by parallel solid phase chemistry. These asymmetric head groups composed of amino functionality together with trimethylamino, di(2-hydroxyethyl)amino or guanidinyl groups. Spacers between cationic heads and linker were both equal and unequal in length. These lipids were subjected to evaluation for DNA binding affinities by gel retardation assay and were screened for their transfection efficiency on HEK293 cells. Cationic lipids with equal chain length exhibited high transfection efficiency when polar part contained asymmetric polar heads. In contrast, lipids with unequal chain length exhibited high transfection efficiency when polar part contained symmetric heads. According to the optimal formulation, seven lipids exhibited higher transfection efficiency than the commercially available transfection agents, Effectene, DOTAP and DC-Chol, to deliver DNA into PC3 human prostate adenocarcinoma cells. 3beta-[N-(N'-Guanidinyl)-2'-aminoethyl)-N-(2-aminoethyl)carbamoyl] cholesterol (5) bearing amino and guanidinyl polar heads exhibited highest transfection efficiency with minimal toxicity. The morphology of active liposomes was observed by transmission electron microscopy (TEM) and size of liposomes were around 200-700 nm.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Radchatawedchakoon W,Watanapokasin R,Krajarng A,Yingyongnarongkul BE

doi

10.1016/j.bmc.2009.10.057

subject

Has Abstract

pub_date

2010-01-01 00:00:00

pages

330-42

issue

1

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(09)00992-4

journal_volume

18

pub_type

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