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Chitosan nanobeads loaded with Biginelli hybrids as cell-selective toxicity systems with a homogeneous distribution of the cell cycle in cancer treatment

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2020
Ristovski_RSC-Advances_2020.pdf (857.5Kb)
Authors
Ristovski (Trifunović), Jovana
Žižak, Željko
Marković, Smilja
Janković, Nenad
Ignjatović, Nenad
Article (Published version)
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Abstract
Tetrahydropyrimidines are a class of azaheterocycles, also called Biginelli hybrids (obtained from the Biginelli reaction), that have attracted an enormous interest in the medicinal chemistry community in recent years, due to a broad biological activity, such as anticancer, antiviral, anti-inflammatory, antidiabetic, antituberculosis activities, etc. According to SciFinder®, more than 70 000 different Biginelli-like compounds have been covered in publications. However, although the Biginelli reaction can yield a large number of compounds with a broad range of activities, none of them have been captured in a carrier. In this study, chitosan-based (Ch) nanoparticles (NPs) containing three different molecules (Biginelli hybrids) were developed and tested for the first time as simple and promising vehicles for anticancer Biginelli-based drugs. The key features of NPs, such as size, surface morphology, drug encapsulation efficiency, and in vitro release were systematically investigated. Rat...her weak cell selectivity of pure Biginelli hybrids (A–C) to selected cancer cell lines has improved and this has been accompanied with two-to-four times stronger cytotoxic effect of A–C loaded Ch NPs, with a triple reduction in toxicity to healthy cells (MRC-5). It has been observed that the examined NPs induce apoptosis. The cell cycle analysis has confirmed the influence of A-loaded Ch (A-Ch), B-loaded Ch (B-Ch), and C-loaded Ch (C-Ch) on the cell cycle distribution, which was homogenously affected. This is the difference with regard to the effect of A, B, and C on the cell cycle. It has been established that the increased selectivity and antitumor activity of NPs are related to the presence of the carrier.

Keywords:
drug delivery / bioactivity / chitosan / Biginelli hybrids / toxicity / cancer treatment
Source:
RSC Advances, 2020, 10, 68, 41542-41550
Publisher:
  • Royal Society of Chemistry
Projects:
  • Ministry of Education, Science and Technological Development, Republic of Serbia, Grant no. 451-03-68/2020-14/200175 (Institute of Technical Sciences of SASA, Belgrade) (RS-200175)
  • Ministry of Education, Science and Technological Development, Republic of Serbia, Grant no. 451-03-68/2020-14/200378 (Institute of Information Technology) (RS-200378)
Note:
  • Supplementary material: https://dais.sanu.ac.rs/123456789/9815
Related info:
  • Referenced by
    https://dais.sanu.ac.rs/123456789/9815

DOI: 10.1039/D0RA08085C

ISSN: 2046-2069

WoS: 000591071500027

Scopus: 2-s2.0-85096522402
[ Google Scholar ]
URI
https://pubs.rsc.org/en/content/articlelanding/2020/ra/d0ra08085c
https://dais.sanu.ac.rs/123456789/9814
Collections
  • ITN SANU - Opšta kolekcija / ITS SASA - General collection
Institution
Институт техничких наука САНУ / Institute of Technical Sciences of SASA
TY  - JOUR
AU  - Ristovski (Trifunović), Jovana
AU  - Žižak, Željko
AU  - Marković, Smilja
AU  - Janković, Nenad
AU  - Ignjatović, Nenad
PY  - 2020
UR  - https://pubs.rsc.org/en/content/articlelanding/2020/ra/d0ra08085c
UR  - https://dais.sanu.ac.rs/123456789/9814
AB  - Tetrahydropyrimidines are a class of azaheterocycles, also called Biginelli hybrids (obtained from the Biginelli reaction), that have attracted an enormous interest in the medicinal chemistry community in recent years, due to a broad biological activity, such as anticancer, antiviral, anti-inflammatory, antidiabetic, antituberculosis activities, etc. According to SciFinder®, more than 70 000 different Biginelli-like compounds have been covered in publications. However, although the Biginelli reaction can yield a large number of compounds with a broad range of activities, none of them have been captured in a carrier. In this study, chitosan-based (Ch) nanoparticles (NPs) containing three different molecules (Biginelli hybrids) were developed and tested for the first time as simple and promising vehicles for anticancer Biginelli-based drugs. The key features of NPs, such as size, surface morphology, drug encapsulation efficiency, and in vitro release were systematically investigated. Rather weak cell selectivity of pure Biginelli hybrids (A–C) to selected cancer cell lines has improved and this has been accompanied with two-to-four times stronger cytotoxic effect of A–C loaded Ch NPs, with a triple reduction in toxicity to healthy cells (MRC-5). It has been observed that the examined NPs induce apoptosis. The cell cycle analysis has confirmed the influence of A-loaded Ch (A-Ch), B-loaded Ch (B-Ch), and C-loaded Ch (C-Ch) on the cell cycle distribution, which was homogenously affected. This is the difference with regard to the effect of A, B, and C on the cell cycle. It has been established that the increased selectivity and antitumor activity of NPs are related to the presence of the carrier.
PB  - Royal Society of Chemistry
T2  - RSC Advances
T1  - Chitosan nanobeads loaded with Biginelli hybrids as cell-selective toxicity systems with a homogeneous distribution of the cell cycle in cancer treatment
SP  - 41542
EP  - 41550
VL  - 10
IS  - 68
DO  - 10.1039/D0RA08085C
ER  - 
@article{
author = "Ristovski (Trifunović), Jovana and Žižak, Željko and Marković, Smilja and Janković, Nenad and Ignjatović, Nenad",
year = "2020",
url = "https://pubs.rsc.org/en/content/articlelanding/2020/ra/d0ra08085c, https://dais.sanu.ac.rs/123456789/9814",
abstract = "Tetrahydropyrimidines are a class of azaheterocycles, also called Biginelli hybrids (obtained from the Biginelli reaction), that have attracted an enormous interest in the medicinal chemistry community in recent years, due to a broad biological activity, such as anticancer, antiviral, anti-inflammatory, antidiabetic, antituberculosis activities, etc. According to SciFinder®, more than 70 000 different Biginelli-like compounds have been covered in publications. However, although the Biginelli reaction can yield a large number of compounds with a broad range of activities, none of them have been captured in a carrier. In this study, chitosan-based (Ch) nanoparticles (NPs) containing three different molecules (Biginelli hybrids) were developed and tested for the first time as simple and promising vehicles for anticancer Biginelli-based drugs. The key features of NPs, such as size, surface morphology, drug encapsulation efficiency, and in vitro release were systematically investigated. Rather weak cell selectivity of pure Biginelli hybrids (A–C) to selected cancer cell lines has improved and this has been accompanied with two-to-four times stronger cytotoxic effect of A–C loaded Ch NPs, with a triple reduction in toxicity to healthy cells (MRC-5). It has been observed that the examined NPs induce apoptosis. The cell cycle analysis has confirmed the influence of A-loaded Ch (A-Ch), B-loaded Ch (B-Ch), and C-loaded Ch (C-Ch) on the cell cycle distribution, which was homogenously affected. This is the difference with regard to the effect of A, B, and C on the cell cycle. It has been established that the increased selectivity and antitumor activity of NPs are related to the presence of the carrier.",
publisher = "Royal Society of Chemistry",
journal = "RSC Advances",
title = "Chitosan nanobeads loaded with Biginelli hybrids as cell-selective toxicity systems with a homogeneous distribution of the cell cycle in cancer treatment",
pages = "41542-41550",
volume = "10",
number = "68",
doi = "10.1039/D0RA08085C"
}
Ristovski (Trifunović) J, Žižak Ž, Marković S, Janković N, Ignjatović N. Chitosan nanobeads loaded with Biginelli hybrids as cell-selective toxicity systems with a homogeneous distribution of the cell cycle in cancer treatment. RSC Advances. 2020;10(68):41542-41550
Ristovski (Trifunović), J., Žižak, Ž., Marković, S., Janković, N.,& Ignjatović, N. (2020). Chitosan nanobeads loaded with Biginelli hybrids as cell-selective toxicity systems with a homogeneous distribution of the cell cycle in cancer treatment.
RSC AdvancesRoyal Society of Chemistry., 10(68), 41542-41550. 
https://doi.org/10.1039/D0RA08085C
Ristovski (Trifunović) Jovana, Žižak Željko, Marković Smilja, Janković Nenad, Ignjatović Nenad, "Chitosan nanobeads loaded with Biginelli hybrids as cell-selective toxicity systems with a homogeneous distribution of the cell cycle in cancer treatment" 10, no. 68 (2020):41542-41550,
https://doi.org/10.1039/D0RA08085C .

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