scholarly journals Stable Deuterium Labeling of Histidine-Rich Lysine-Based Dendrimers

Molecules ◽  
2019 ◽  
Vol 24 (13) ◽  
pp. 2481 ◽  
Author(s):  
Nadezhda N. Sheveleva ◽  
Denis A. Markelov ◽  
Mikhail A. Vovk ◽  
Irina I. Tarasenko ◽  
Mariya E. Mikhailova ◽  
...  

Peptide dendrimers, due to their biocompatibility and low toxicity, are highly promising candidates as nanocarriers for drugs and genes. The development of this kind of delivery system requires reliable monitoring of their metabolic and biological pathways. In this respect, hydrogen isotope labeling has tremendous importance, being a safe tool for detection of the labeled nanocarriers. In this work, we have synthesized new histidine-rich lysine-based dendrimers (Lys-2His dendrimer) with two linear histidine (His) residues in every inner segment. The presence of His residues has enabled us to perform controlled deuteration of Lys-2His dendrimers. The high deuteration degree (around 70%) does not practically change after redissolving the samples in H2O and heating them at 40 °C, which indicates the isotopic label stability.

2016 ◽  
Vol 18 (6) ◽  
pp. 1987-1997 ◽  
Author(s):  
Yan Zhang ◽  
Zhijie Yang ◽  
Xinyi Tan ◽  
Xing Tang ◽  
Zaixing Yang

2020 ◽  
Vol 11 (1) ◽  
Author(s):  
Zhaofei Zhang ◽  
Chuntian Qiu ◽  
Yangsen Xu ◽  
Qing Han ◽  
Junwang Tang ◽  
...  

Abstract Precisely controlled deuterium labeling at specific sites of N-alkyl drugs is crucial in drug-development as over 50% of the top-selling drugs contain N-alkyl groups, in which it is very challenging to selectively replace protons with deuterium atoms. With the goal of achieving controllable isotope-labeling in N-alkylated amines, we herein rationally design photocatalytic water-splitting to furnish [H] or [D] and isotope alkanol-oxidation by photoexcited electron-hole pairs on a polymeric semiconductor. The controlled installation of N-CH3, -CDH2, -CD2H, -CD3, and -13CH3 groups into pharmaceutical amines thus has been demonstrated by tuning isotopic water and methanol. More than 50 examples with a wide range of functionalities are presented, demonstrating the universal applicability and mildness of this strategy. Gram-scale production has been realized, paving the way for the practical photosynthesis of pharmaceuticals.


RSC Advances ◽  
2019 ◽  
Vol 9 (4) ◽  
pp. 1982-1989 ◽  
Author(s):  
Chao Zhang ◽  
HongLei Zhang ◽  
MengNan Han ◽  
XueLi Yang ◽  
ChaoHong Pei ◽  
...  

The novel nano-drug cisplatin-DNA tetrahedron-affibody has high specificity, high efficacy, and low toxicity for the treatment of HER2-overexpressing breast cancers.


2016 ◽  
Vol 4 (21) ◽  
pp. 3660-3669 ◽  
Author(s):  
Ling Chen ◽  
Lin Wu ◽  
Fei Liu ◽  
Xueyong Qi ◽  
Yanru Ge ◽  
...  

A smart drug delivery system based on thermo-sensitive molecule was designed. When exposed to near infrared (NIR) light, Fe3O4 nanoparticles transfer the light to heat rapidly, leading to the cleavage of the Azo linker and the release of DOX.


2016 ◽  
Vol 36 (3) ◽  
pp. 227-237 ◽  
Author(s):  
S Arami ◽  
MR Rashidi ◽  
M Mahdavi ◽  
M Fathi ◽  
AA Entezami

The limited effectiveness of the conventional methods for cancer treatment makes the researchers to find novel safe and effective therapeutic strategies. One of these strategies is to use small interfering RNAs (siRNAs). A major challenge here is the siRNA delivery into the cells. The purpose of this study was to design and prepare a biocompatible, biodegradable, and safe nanosized particle for siRNA delivery into human breast cancer MCF-7 and leukemia K562 cells. Chemically synthesized magnetic nanoparticles containing polyethyleneglycol-lactate polymer (PEG-LAC), chitosan, and polyethyleneimine (PEI) were successfully prepared and used as a gene delivery vehicle. The nanoparticles were characterized by Fourier transform infrared spectroscopy and zeta potential. The Fe3O4-PEG-LAC-chitosan-PEI nanoparticle showed efficient and stable survivin siRNA loading in gel retardation assay. The cytotoxicity of the prepared nanoparticle was studied using 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide assay and was compared with that of mitoxantrone (MTX) in combination with the prepared siRNA delivery system to evaluate the possible synergic effect of MTX and survivin siRNA. The nanoparticles with and without noncomplementary siRNA showed low toxicity against both cell lines; however, a twofold decrease was observed in cell survival percent after MTX addition to MCF-7 cells treated with either nanoparticle itself or complexed with noncomplementary siRNA. While survivin siRNA nanoplex caused threefold decrease in the cell survival percent, its combination with MTX did not result in a significant increase in the cytotoxic effect. Therefore, Fe3O4-PEG-LAC-chitosan-PEI nanoparticle should be considered as a potential carrier for enhanced survivin siRNA delivery into MCF-7 and K562 cells.


Sign in / Sign up

Export Citation Format

Share Document