Anchor Dependency for Non-Glycerol Based Cationic Lipofectins: Mixed Bag of Regular and Anomalous Transfection Profiles
摘要:
Although detailed structure activity, physicochemical and biophysical investigations in probing the anchor influence in liposomal gene delivery have been reported for glycerol-based transfection lipids, the corresponding investigation for non-glycerol based simple monocationic transfection lipids have not yet been undertaken. Towards this end, herein, we delineate our structure - activity and physicochemical approach in deciphering the anchor dependency in liposomal gene delivery using fifteen new structural analogues (lipids 1 - 15) of recently reported nonglycerol based monocationic transfection lipids. The C-14 analogues in both series 1 (lipids 1 - 6) and series 2 (lipids 7-15) showed maximum efficiency in transfecting COS-1 and CHO cells. However, the C-12 analogue of the ether series (lipid 3) exhibited a seemingly anomalous behavior compared with its transfection efficient C-10 and C-14 analogues (lipids 2 and 4) in being completely inefficient to transfect both COS-1 and CHO cells. The present structure - activity investigation also convincingly demonstrates that enhancement of transfection efficiencies through incorporation of membrane reorganizing unsaturation elements in the hydrophobic anchor of cationic lipids is not universal but cell dependent. The strength of the interaction of lipids 1 - 15 with DNA was assessed by their ability to exclude ethidium bromide bound to the DNA. Cationic lipids with long hydrophobic tails were found, in general, to be efficient in excluding EtBr from DNA. Gel to liquid crystalline transition temperatures of the lipids was measured by fluorescence anisotropy measurement technique. In general (lipid 2 being an exception), transfection efficient lipids were found to have their mid transition temperatures at or below physiological temperatures (37degreesC).
HYDROXYSILANE AND POLYMER CONTAINING SILANE GROUPS
申请人:SIKA TECHNOLOGY AG
公开号:US20160102110A1
公开(公告)日:2016-04-14
Special hydroxysilanes, which can be obtained by reacting β-(3,4-epoxycyclohexyl)alkyltrialkoxysilanes with secondary amines, and adducts of the hydroxysilanes in the form of polymers containing silane groups. The hydroxysilanes can be produced having high purity in a simple process and are very stable in storage after production. The polymers containing silane groups that can be obtained by means of the hydroxysilanes have advantageous properties. The polymers enable moisture-curing compositions, which contain no isocyanate groups and which are suitable as elastic adhesives and sealants.
oligoethylene glycols (M-OEGs)-containing symmetrical secondary amines are highly valuable synthetic intermediates in drug development and materials sciences. Scalable three-step synthesis of M-OEGs secondary amines with flexible M-OEGs and/or alkyl chains is described herein. Through reduction amination of diethanolamine, Williamson ether synthesis, and subsequent deprotection, a series of M-OEGs secondary
Synthesis of Secondary Amines with Long Chains Containing Ether Bonds
作者:Songdong Ding、Haowei Xu、Xiuying Yang、Lianjun Song、Xueyu Wang、Qiuju Li、Lanlan He
DOI:10.1055/s-0040-1719921
日期:2022.7
secondary amines with long chains containing ether bonds were synthesized by a three-step protection–etherification–deprotection process from diethanolamine. The optimum reaction conditions were examined. This method has the advantages of simplicity, low cost, and high yield. Furthermore, some new downstream products (diglycolamides) were prepared from the ether-containing long-chain secondary amines as reactants
Die vorliegende Erfindung betrifft spezielle Hydroxysilane, erhältlich durch die Umsetzung von β-(3,4-Epoxycyclohexyl)alkyltrialkoxysilanen mit sekundären Aminen, sowie Addukte dieser Hydroxysilane, insbesondere in Form von Silangruppen-haltigen Polymeren.
Die Hydroxysilane sind in einem einfachen Prozess in hoher Reinheit herstellbar und sind nach der Herstellung sehr lagerstabil. Die damit zugänglichen Silangruppen-haltigen Polymere weisen vorteilhafte Eigenschaften auf. Sie ermöglichen insbesondere Isocyanatgruppen-freie feuchtigkeitshärtende Zusammensetzungen, welche geeignet sind als elastische Kleb- und Dichtstoffe.