Russian Chemical Bulletin, том 69, издание 4, номера страниц: 793-803

Cellular internalization of targeted and non-targeted delivery systems for contrast agents based on polyamidoamine dendrimers

Тип документаJournal Article
Дата публикации2020-04
ИздательSpringer Nature
Название журналаRussian Chemical Bulletin
Квартиль по SCImagoQ3
Квартиль по Web of ScienceQ4
Импакт-фактор 20211.70
ISSN10665285, 15739171
General Chemistry
Краткое описание
New high-molecular-weight contrast agents based on polyamidoamine (PAMAM) dendrimers for targeted imaging of malignant tumors characterized by overexpression of human epidermal growth factor receptor (EGFR) and human alpha-fetoprotein receptor (RECAF) were designed. Conjugates of second (G2) and third (G3) generation polyamidoamine dendrimers with 1,4,7,10-tetraazocyclodecane-1,4,7,10-tetraacetic acid (DOTA) were obtained. The quantitative composition of the conjugates was determined by 1 HNMR spectroscopy. It was shown that four out of the 16 terminal NH 2 groups in G2-DOTA and nine out of the 32 groups in G3-DOTA were modified with DOTA. The morphology, size, and charge of the synthesized macromolecules were characterized by dynamic light scattering and electrophoresis. Gadolinium(III) was loaded into the conjugates and the Gd content was determined by atomic emission spectroscopy. For increasing the selectivity of accumulation in the tumor cells, two recombinant proteins able to bind selectively to EGFR and RECAF, namely, human recombinant epidermal growth factor (rEGF) and human recombinant 3rd domain of alpha-fetoprotein (3dAFPpG), were conjugated with G2 and G3 dendrimers. The conjugates containing vector molecules were mainly accumulated via clathrin-dependent endocytosis, whereas G2-DOTA and G3-DOTA were absorbed via caveolin-dependent endocytosis and macropinocytosis. The dendrimer conjugates with vector molecules were intensely accumulated in A549 cells characterized by high expression of EGFR (Herl) and RECAF, whereas the accumulation of conjugates in the control K562 cells (with low expression of Her1) and in the CD14 − population of human unstimulated mononuclear white blood cells was insignificant. The 3dAFPpG-conjugated dendrimers were partly recycled. All synthesized conjugates had a rather low toxicity in the range of 350–450 µmol L −1 (IC 50 ).
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1. Sokol M. B. и др. Cellular internalization of targeted and non-targeted delivery systems for contrast agents based on polyamidoamine dendrimers // Russian Chemical Bulletin. 2020. Т. 69. № 4. С. 793–803.


DO - 10.1007/s11172-020-2835-2

UR -

TI - Cellular internalization of targeted and non-targeted delivery systems for contrast agents based on polyamidoamine dendrimers

T2 - Russian Chemical Bulletin

AU - Sokol, M. B.

AU - Faustova, M. R.

AU - Nikolskaya, E. D.

AU - Zhunina, O. A.

AU - Fomicheva, M. V.

AU - Petrov, R. V.

AU - Yabbarov, N. G.

PY - 2020

DA - 2020/04

PB - Springer Science and Business Media LLC

SP - 793-803

IS - 4

VL - 69

SN - 1066-5285

SN - 1573-9171

ER -

BibTex |


doi = {10.1007/s11172-020-2835-2},

url = {},

year = 2020,

month = {apr},

publisher = {Springer Science and Business Media {LLC}},

volume = {69},

number = {4},

pages = {793--803},

author = {M. B. Sokol and M. R. Faustova and E. D. Nikolskaya and O. A. Zhunina and M. V. Fomicheva and R. V. Petrov and N. G. Yabbarov},

title = {Cellular internalization of targeted and non-targeted delivery systems for contrast agents based on polyamidoamine dendrimers},

journal = {Russian Chemical Bulletin}


Sokol, M. B., et al. “Cellular Internalization of Targeted and Non-Targeted Delivery Systems for Contrast Agents Based on Polyamidoamine Dendrimers.” Russian Chemical Bulletin, vol. 69, no. 4, Apr. 2020, pp. 793–803. Crossref,