Carriers for nucleotide 5'-triphosphate. 2. Liquid membrane and liposome transport
摘要:
We describe a series of new cationic carriers for the transport of nucleotide 5'-triphosphates across liquid organic membranes. The tetracationic compound 5, with two diquaternary 1,4-diaza[2.2.2]bicyclooctane (DABCO) units, forms carrier-nucleotide complexes of 1:1 stoichiometry in dichloromethane and strongly accelerates nucleotide transport across this solvent. As a result of a favorable balance of hydrophobicity and hydrophilicity, complexes of 5 do not leak out of the organic phase into the aqueous source or receiving phases. Liposome transport studies demonstrate that caution is strongly advised when extrapolating from liquid membrane studies to the transport across liposomes or cell membranes. The DABCO-based cationic carriers do not mediate specific nucleotide transport across the liposome walls but rather act as detergents to break the liposomal structure.
Lipid complexes for transferring at least a therapeutically active substance, in particular a polynucleotide into a target cell and use in gene therapy
A series of π-extended chelating scaffolds incorporating two hydroxypyridone moieties were synthesized. X-ray crystallographic analysis revealed that a bis(hydroxypyridono)toluene ligand possessed a unique π-extended structure and exhibited efficient phase segregation from the aliphatic chains attached at the heterocyclic nitrogen. The bis-bidentate ligand formed a metal-coordination-induced macrocycle
Novel lipid complexes for transferring at least one therapeutically active substance, in particular a polynucleotide, into a target cell, and use in gene therapy
申请人:——
公开号:US20020025920A1
公开(公告)日:2002-02-28
The present invention relates to a complex comprising at least a lipid and at least a therapeutically active substance for transferring the therapeutically active substance into a target cell. The present invention also relates to a method of transferring a therapeutically active substance into cells.
The present invention relates to the use of a compound of formula (1):
wherein: R1 comprises a carbonyl group and R2 is a hydrocarbyl group; optionally wherein said ring is further substituted; or a pharmaceutically acceptable salt thereof; in the manufacture of a medicament for use in one or more of: modulating the release of intracellular calcium from a store controlled by nicotinic acid adenine dinucleotide phosphate; modulating calcium spikes in mammalian cells; treating diseases in one or more of brain, heart, pancreatic cells (e.g. pancreatic acinar and pancreatic beta cells), immune cells, T-cells, haemopoietic cells including phagocytes; treating diseases in one or more of brain, heart, pancreatic cells (e.g. pancreatic acinar and pancreatic beta cells), immune cells, T-cells, haemopoietic cells including phagocytes by modulating the release of intracellular calcium from a store controlled by nicotinic acid adenine dinucleotide phosphate; treating diseases in one or more of brain, heart, and T-cells by modulating calcium spikes in mammalian cells.
Synthesis and lyotropic phase behavior of novel nonionic surfactants for the crystallization of integral membrane proteins
作者:Jeffrey Walton、Gordon J.T. Tiddy、Simon J. Webb
DOI:10.1016/j.tetlet.2005.11.103
日期:2006.1
A series of new sugar-based nonionic surfactants have been synthesized and their lyotropic liquid crystalline properties characterized. When in contact with water, these surfactants formed a range of lyotropic liquid crystalline phases, including cubic, hexagonal, and lamellar, as well as a separate micellar phase. These are features that have promise for the crystallization of integral membrane proteins. (c) 2005 Elsevier Ltd. All rights reserved.
NOUVEAUX COMPLEXES LIPIDIQUES POUR LE TRANSFERT D'AU MOINS UNE SUBSTANCE THERAPEUTIQUEMENT ACTIVE, NOTAMMENT UN POLYNUCLEOTIDE, DANS UNE CELLULE CIBLE ET UTILISATION EN THERAPIE GENIQUE