Polycationic amphiphiles

Beta and co-workers created a total of six polycationic amphiphiles (PA) to study the effect of lipid hydrophobicity on the activity of amphiphilic neomycin B conjugates four of the compounds incorporated either palmitic or arachidic dilipid lysine tails and the other two had single fluorinated undecanoic acid tails. They selected 10 bacteria... 

Neomycin is an aminoglycoside antibiotic which acts as a polycationic amphiphile. It is used in topical creams, ointments, lotions, eye preparations and eardrops, and as an antibacterial preservative agent in some vaccines. Neomycin exhibits exceptional activity against Gram-negative bacteria and also has partial activity against Grampositive bacteria [72],... 

Bera and co-workers synthesised six polycationic amphiphiles with the backbone of neomycin B [75]. In their experiment, they converted all six amine groups on neomycin B to guanidine and all six compounds were tested against a panel of... 

Fig. 15 a Synthesis procedures and the structures of ot-CD-OEI star polymers, b Schematic representation of skirt- (left) and jellyfish-type (right) polycationic amphiphilic CDs (paCDs)... 

With a similar star structure, a kind of polycationic amphiphilic cyclodextrins was reported (Fig. 15b) [118]. The structure contains both cationic elements and lipophilic tails, which is similar to the lipid structure. The nanoparticle stability and transfection efficiency can be rationally modulated by judicious tailoring of the molecular topology. Importantly, by using polycationic amphiphilic CDs that present a dendritic arrangement of catioinic elements in the BNL-CL2 and COS-7... 

Fig. 24.23 Schematic representation of the CA4 vector 69 in the optimal upper-rim protonable com arrangement. Schematic representation of the proposed mechanism for pDNA complexation by polycationic amphiphilic macrocycles involving electrostatically- driven templating (a) and bilayer zipping/nanocondensation (b). The TEM micrograph corresponding to the nanocomplexes formulated with compound 69 at N/P 10, is also presented (c). The typical snake-like ultra-thin structure can be appreciated in the insert [72], (Reprinted from Ref. [72])...

Abe, H. Mawatari, Y. Teraoka, H. Fujimoto, K. Inouye, M. Synthesis and molecular recognition of pyrenophanes with polycationic or amphiphilic functionalities artificial plate-shaped cavitant incorporating arenes and nucleotides in water. J. Org. Chem. 2004, 69 (2), 495-504. 

Cyclodextrin polyplexes, which are called CDplexes, were prepared from polycationic thiolated amphiphilic cyclodextrin and DNA for gene delivery (see Figure ll.lC). CDplexes also can be functionalized for cellular targeting, nuclear localization and visualization purposes. ... 

Then in Sect. 2, the interpolyelectrolyte complexes (IPEC) between polycationic polymers and DNA will be addressed as a function of the chemical structure of the polymer (most of the DNA being used is plasmid DNA, consisting of many thousands of base pairs). Water-soluble and amphiphilic polymers will be discussed and then other properties will be taken into consideration such as the polyelectrolyte s nature (strong or weak), the presence of steric stabilizers, etc. Section 3 will deal with complexes of polyamphoteric polymers with DNA. In both parts, the working line is the correlation between physico-chemical properties and efficiency in vitro (transfection potency). 

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