scholarly journals Photophysical Properties of Linked Zinc Phthalocyanine to Acryloyl Chloride:N-vinylpyrrolidone Copolymer

Polymers ◽  
2021 ◽  
Vol 13 (24) ◽  
pp. 4428
Author(s):  
Tamara Potlog ◽  
Ion Lungu ◽  
Pavel Tiuleanu ◽  
Stefan Robu

This paper focuses on the linking of zinc phthalocyanine (ZnPc) to N-vinylpyrrolidone (N-VP): acryloyl chloride (ClAC) copolymer. The synthesis of binary N-VP:ClAC copolymer was performed by the radical polymerization method and then grafted to ZnPc by the Friedel Crafts acylation reaction. We have developed a water-soluble ZnPc:ClAC:N-VP photosensitizer with a narrow absorption band at 970 nm, fluorescence at λem = 825 nm and the decay fluorescence profile with 3-decay relatively longer times of 1.2 µs, 4.6 µs, and 37 µs. The concentration-dependent dark cytotoxicity investigated in normal fibroblasts (NHDF), malignant melanoma (MeWo), adenocarcinoma (HeLa), and hepatocellular carcinoma (HepG2) cell lines incubated to increased concentrations of ZnPc:ClAC:N-VP (up to 40 μM) for 24 h in the dark show low cytotoxicity. Maximum cell viability in HeLa and HepG2 tumor cell lines was observed.

Molecules ◽  
2020 ◽  
Vol 25 (15) ◽  
pp. 3340
Author(s):  
Duy Khuong Mai ◽  
Byungman Kang ◽  
Temmy Pegarro Vales ◽  
Isabel Wen Badon ◽  
Sung Cho ◽  
...  

The synthesis of three water-soluble lactose-modified 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene (BODIPY)-based photosensitizers with tumor-targeting capabilities is reported, including an investigation into their photodynamic therapeutic activity on three distinct cancer cell lines (human hepatoma Huh7, cervical cancer HeLa, and breast cancer MCF-7 cell lines). The halogenated BODIPY dyes exhibited a decreased fluorescence quantum yield compared to their non-halogenated counterpart, and facilitated the efficient generation of singlet oxygen species. The synthesized dyes exhibited low cytotoxicities in the dark and high photodynamic therapeutic capabilities against the treated cancer cell lines following irradiation at 530 nm. Moreover, the incorporation of lactose moieties led to an enhanced cellular uptake of the BODIPY dyes. Collectively, the results presented herein provide promising insights for the development of photodynamic therapeutic agents for cancer treatment.


2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Shahram Hadizadeh ◽  
Nowruz Najafzadeh ◽  
Mohammad Mazani ◽  
Mojtaba Amani ◽  
Hassan Mansouri-Torshizi ◽  
...  

As a part of a drug development program to discover novel therapeutic and more effective palladium (Pd) based anticancer drugs, a series of water-soluble Pd complexes have been synthesized by interaction between [Pd (phen)(H2O)2(NO3)2] and alkylenebisdithiocarbamate(al-bis-dtc) disodium salts. This study was undertaken to examine the possible cytotoxic effect of three novel complexes (0.125–64 µg/mL) on human gastric carcinoma (AGS), esophageal squamous cell carcinoma (Kyse-30), and hepatocellular carcinoma (HepG2) cell lines. The cytotoxicity was examined using cell proliferation and acridine orange/ethidium bromide (AO/EB) assay. In order to examine the effects of new Pd(II) complexes on cell cycle status, we performed cell cycle analysis. The complexes were found to have completely lethal effects on the cell lines, and the half maximal inhibitory concentration (IC50) values obtained for the cell lines were much lower in comparison with cisplatin. We demonstrated that the three new Pd(II) complexes are able to induce G2/M phase arrest in AGS and HepG2; in addition, the Pd(II) complexes caused an S phase arrest in Kyse-30 cell line. Our results indicate that newly synthesized Pd(II) complexes may provide a novel class of chemopreventive compounds for anticancer therapy.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 642
Author(s):  
Federica De Castro ◽  
Erika Stefàno ◽  
Danilo Migoni ◽  
Giorgia N. Iaconisi ◽  
Antonella Muscella ◽  
...  

Starting from the [PtCl(η1-C2H4OMe)(phen)] (phen = 1,10-phenanthroline, 1) platinum(II) precursor, we synthesized and characterized by multinuclear NMR new [Pt(η1-C2H4OMe)(L)(phen)]+ (L = NH3, 2; DMSO, 3) complexes. These organometallic species, potentially able to interact with cell membrane organic cation transporters (OCT), violating some of the classical rules for antitumor activity of cisplatin analogues, were evaluated for their cytotoxicity. Interestingly, despite both complexes 2 and 3 resulting in greater cell uptake than cisplatin in selected tumor cell lines, only 3 showed comparable or higher antitumor activity. General low cytotoxicity of complex 2 in the tested cell lines (SH-SY5Y, SK-OV-3, Hep-G2, Caco-2, HeLa, MCF-7, MG-63, ZL-65) appeared to depend on its stability towards solvolysis in neutral water, as assessed by NMR monitoring. Differently, the [Pt(η1-C2H4OMe)(DMSO)(phen)]+ (3) complex was easily hydrolyzed in neutral water, resulting in a comparable or higher cytotoxicity in cancer cells with respect to cisplatin. Further, both IC50 values and the uptake profiles of the active complex appeared quite different in the used cell lines, suggesting the occurrence of diversified biological effects. Nevertheless, further studies on the metabolism of complex 3 should be performed before planning its possible use in tissue- and tumor-specific drug design.


2019 ◽  
Vol 29 (5) ◽  
pp. 1143-1152 ◽  
Author(s):  
Seda Çetindere ◽  
Elif Okutan ◽  
Süreyya Oğuz Tümay ◽  
Serkan Yeşilot ◽  
Adem Kılıç

2001 ◽  
Vol 350 (3-4) ◽  
pp. 198-205 ◽  
Author(s):  
Sarah Foley ◽  
Susanna Bosi ◽  
Christain Larroque ◽  
Maurizio Prato ◽  
Jean-Marc Janot ◽  
...  

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 216 ◽  
Author(s):  
Ana Santos-Rebelo ◽  
Catarina Garcia ◽  
Carla Eleutério ◽  
Ana Bastos ◽  
Sílvia Castro Coelho ◽  
...  

Pancreatic cancer is the eighth leading cause of cancer death worldwide. For this reason, the development of more effective therapies is a major concern for the scientific community. Accordingly, plants belonging to Plectranthus genus and their isolated compounds, such as Parvifloron D, were found to have cytotoxic and antiproliferative activities. However, Parvifloron D is a very low water-soluble compound. Thus, nanotechnology can be a promising delivery system to enhance drug solubility and targeted delivery. The extraction of Parvifloron D from P. ecklonii was optimized through an acetone ultrasound-assisted method and isolated by Flash-Dry Column Chromatography. Then, its antiproliferative effect was selectivity evaluated against different tumor cell lines (IC50 of 0.15 ± 0.05 μM, 11.9 ± 0.7 μM, 21.6 ± 0.5, 34.3 ± 4.1 μM, 35.1 ± 2.2 μM and 32.1 ± 4.3 μM for BxPC3, PANC-1, Ins1-E, MCF-7, HaCat and Caco-2, respectively). To obtain an optimized stable Parvifloron D pharmaceutical dosage form, albumin nanoparticles were produced through a desolvation method (yield of encapsulation of 91.2%) and characterized in terms of size (165 nm; PI 0.11), zeta potential (−7.88 mV) and morphology. In conclusion, Parvifloron D can be efficiently obtained from P. ecklonii and it has shown selective cytotoxicity to pancreatic cell lines. Parvifloron D nanoencapsulation can be considered as a possible efficient alternative approach in the treatment of pancreatic cancer.


2019 ◽  
Vol 4 (20) ◽  
pp. 6377-6381 ◽  
Author(s):  
Alexey P. Krinochkin ◽  
Dmitry S. Kopchuk ◽  
Grigory A. Kim ◽  
Il'ya N. Ganebnykh ◽  
Igor S. Kovalev ◽  
...  

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