N-acylated

摘要： Nucleic acids-based therapies have recently developed as next-generation agents for treating and preventing viral infection, cancer, and genetic disorders, but their use is still limited due to its relatively poor delivery into targeted cells. We designed and synthesized new amphiphilic amino acid derivatives (cysteine-based) of low molecular weight, formed by the same pentapeptide (AG2: WWCOO) N-acylated, with different hydrophobic chains containing from 12 to 18 carbons, named AG2-Cn (N), which dimerize by oxidation in the presence of pLenti-CMV-GFP Puro plasmid (P) in the respective gemini. We determined transfection efficiency, critical micelle concentration, particle size, ζ-potential and cytotoxicity for the derivatives obtained. We found that all the synthesized compounds were active for DNA delivery and had greater ability to transfect CHO-K1 cells. In particular, AG2-C18 is a promising carrier for gene delivery because it showed no cytotoxicity and its activity was greater than or equal to the commercial actives currently used.

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摘要： ［1］Martin Schecher,The Fucik spectrum,Indiana University Mathematics Journal,1994,43(4):1139-1157.［2］Dancer,E.N.,Remarks on jumping nonlinearities,in Topics in Nonlinear Analysis (eds.Escher,Simonett),Basel:Birkhauser,1999,101-116.［3］Dancer,E.N.,Du Yihong,Existence of changing sign solutions for semilinear problems with jumping nonlinearities at zero,Proceedings of the Royal Society of Edinburgh,1994,124A:1165-1176.［4］Dancer,E.N.,Du Yihong,Multiple solutions of some semilinear elliptic equations via generalized conley index,Journal of Mathematical Analysis and Applications,1995,189:848-871.［5］Li Shujie,Zhang Zhitao,Sign-changing solutions and multiple solutions theorems for semilinear elliptic boundary value problems with jumping nonlinearities,Acta Mathematica Sinica,2000,16(1):113-122.［6］Chang Kung-ching,Li Shujie,Liu Jiaquan,Remarks on multiple solutions for asymptotically linear elliptic boundary value problems.Topological methods for Nonlinear Analysis,Journal of the Juliusz Schauder Center,1994,3:179-187.［7］Alfonso Castro,Jorge Cossio,Multiple solutions for a nonlinear Dirichlet problem,SIAM J.Math.Anal.,1994,25(6):1554-1561.［8］Alfonso Castro,Jorge Cossio,John M.Neuberger,A sign-changing solution for a superlinear Dirichlet problem,Rocky Mountain J.M.,1997,27:1041-1053.［9］Alfonso Castro,Jorge Cossio,John M.Neuberger,A minimax principle,index of the critical point,and existence of sign-changing solutions to Elliptic boundary value problems,E.J.Diff.Eqn.,1998 (2):1-18.［10］Thomas Bartsch,Wang Zhiqiang,On the existence of sign-changing solutions for semilinear Dirichlet problems,Topological Methods in Nonlinear Analysis,Journal of the Juliusz Schauder Center,1996,(7):115-131.［11］Li Shujie,Zhang Zhitao,Multiple solutions theorems for semilinear elliptic boundary value problems with resonance at infinity,Discrete and Continuous Dynamical System,1999,5(3):489-493.［12］Mawhin,J.,Willem,M.,Critical Point Theory and Hamiltonian Systems,New York:Springer-Verlag,1989.［13］Chang Kung-ching,A variant mountain pass lemma,Science in China,Ser.A (in Chinese),1983,(4):306-317.［14］Chang Kung-ching,Infinite Dimentional Morse Theory and Multiple Solutions Problems,Basel:Birkhauser,1993.［15］Whyburn,G.T.,Topological Analysis,Princeton:Princeton University Press,1958.［16］Liu Zhaoli,A topological property of the boundary of bounded open sets in R2,Journal of Shandong University,1994,29(3):299-303.［17］Dancer,E.N.,Du Yihong,On sign-changing solutions of certain semilinear elliptic problems,Appl.Anal.,1995,56:193-206.