title: Benzothiazole head group based cationic lipids: synthesis and application for gene delivery.
abstract: A series of benzothiazole based lipids (1-10) containing different derivatives of benzothiazole in the head group region were synthesized to determine the structure-activity relationship for gene delivery. The liposomes formulated were mixed with plasmid DNA encoding green fluorescent protein (α5GFP) or β-galactosidase (pCMV-SPORT-β-gal) and transfected into B16F10 (Human melanoma cancer cells), CHO (Chinese hamster ovary), A-549 (Human lung carcinoma cells) and MCF-7 (Human breast carcinoma cells) types of cell lines. The efficiencies of lipids 9 and 10 in particular, were found to be comparable and even more when compared to that of LipofectAmine-2000. The transfection profiles of the efficient lipids are proved to be maintained even in the presence of serum. Thus, the benzothiazole head group based lipids developed have the potential to be used as transfection reagents in vitro and in vivo.
authors.affiliation: Department of Chemistry, National Institute of Technology, Warangal 506004, Andhra Pradesh, India.
authors.forename: Bhavani
authors.initials: B
authors.lastname: Kedika
authors.affiliation: Department of Chemistry, National Institute of Technology, Warangal 506004, Andhra Pradesh, India. Electronic address: pv_slakshmi@yahoo.com.
authors.forename: Srilakshmi V
authors.initials: SV
authors.lastname: Patri
mesh_terms: D052160:Benzothiazoles / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry; D002412:Cations; D018014:Gene Transfer Techniques; D008081:Liposomes; D009682:Magnetic Resonance Spectroscopy; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: D052160:Benzothiazoles; D002412:Cations; D008081:Liposomes
keywords: Cationic liposome; DNA release; Gene delivery; Lipofection; Lipoplexes; Reducible tocopherol-based cationic amphiphiles