- Tris(2-aminoethyl)amine-based α-branched fatty acid amides - Synthesis of lipids and comparative study of transfection efficiency of their lipid formulations This article is dedicated to Professor Gerald Brezesinski on occasion of his 65th birthday.
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The synthesis of a new class of cationic lipids, tris(2-aminoethyl)amine-based α-branched fatty acid amides, is described resulting in a series of lipids with specific variations in the lipophilic as well as the hydrophilic part of the lipids. In-vitro structure/transfection relationships were established by application of complexes of these lipids with plasmid DNA (pDNA) to different cell lines. The α-branched fatty acid amide bearing two tetradecyl chains and two lysine molecules (T14diLys) in mixture with the co-lipid 1,2-di-[(9Z)-octadec-9-enoyl]-sn-glycero-3-phosphoethanolamine (DOPE) (1/2, n/n) exhibits effective pDNA transfer in three different cell lines, namely Hep-G2, A549, and COS-7. The presence of 10% serum during lipoplex incubation of the cells did not affect the transfection efficiency. Based on that, detailed investigations of the complexation of pDNA with the lipid formulation T14diLys/DOPE 1/2 (n/n) were carried out with respect to particle size and charge using dynamic light scattering (DLS), ζ-potential measurements, and transmission electron microscopy (TEM). Additionally, the lipoplex uptake was investigated by confocal laser scanning microscopy (CLSM). Overall, lipoplexes prepared from T14diLys/DOPE 1/2 (n/n) offer large potential as lipid-based polynucleotide carriers and further justify advanced examinations.
- Erdmann, Nicole,W?lk, Christian,Schulze, Ingo,Janich, Christopher,Folz, Manuela,Drescher, Simon,Dittrich, Matthias,Meister, Annette,Vogel, Jürgen,Groth, Thomas,Dobner, Bodo,Langner, Andreas
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p. 349 - 362
(2015/09/28)
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- Development of vizantin, a safe immunostimulant, based on the structure-activity relationship of trehalose-6,6′-dicorynomycolate
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Vizantin, 6,6′-bis-O-(3-nonyldodecanoyl)-α,α′- trehalose, was developed as a safe immunostimulator on the basis of a structure-activity relationship (SAR) study with trehalose 6,6′- dicorynomycolate (TDCM). It was possible to synthesize vizantin on a large scale more easily than in the case of TDCM, and the compound exhibited more potent prophylactic effect on experimental lung metastasis of B16-F0 melanoma cells. Because vizantin stimulated human macrophages, it is a promising candidate for clinical application.
- Yamamoto, Hirofumi,Oda, Masataka,Nakano, Mayo,Watanabe, Naoyuki,Yabiku, Kenta,Shibutani, Masahiro,Inoue, Masahisa,Imagawa, Hiroshi,Nagahama, Masahiro,Himeno, Seiichiro,Setsu, Kojun,Sakurai, Jun,Nishizawa, Mugio
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supporting information
p. 381 - 385
(2013/02/23)
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- TREHALOSE COMPOUND, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL PRODUCT CONTAINING THE COMPOUND
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It is an object of the present invention to provide a trehalose compound having high immunopotentiating activity and low toxicity. The trehalose compound is represented by formula (1). (In the formula, X and X' each represents a phenyl, a naphtyl, R1-CHR1- (wherein R1 and R2 each represents a C7-C21 alkyl group or the like) or the like; and n and n' each independently represents an integer of 0-3). The compound exhibits a high activating effect on macrophages and neutrophils.
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Page/Page column 55
(2011/08/08)
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- TREHALOSE COMPOUND, PROCESS FOR PRODUCTION OF THE COMPOUND, AND IMMUNO-STIMULATIVE AGENT COMPRISING THE COMPOUND
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An object of the present invention is to provide a novel trehalose compound that exhibits excellent immunostimulating activity and that can be supplied in a large quantity in an industrial scale, and a method for producing the trehalose compound, wherein
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Page/Page column 15
(2009/12/07)
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- Sialic acid-containing glycolipid derivatives
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Sialic acid- containing glycolipid derivatives represented by the following general formula, their production method, and the particulate carriers that contain as a constituent the sialic acid-containing glycolipid derivative(s). STR1 wherein represents t
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