scholarly journals Study of Cytotoxic and Photodynamic Activities of Dyads Composed of a Zinc Phthalocyanine Appended to an Organotin

2021 ◽  
Vol 14 (5) ◽  
pp. 413
Author(s):  
Isabelle Toubia ◽  
Christophe Nguyen ◽  
Stéphane Diring ◽  
Marine Pays ◽  
Elodie Mattana ◽  
...  

The combination of photodynamic therapy and chemotherapy is a promising strategy to enhance cancer therapeutic efficacy and reduce drug resistance. In this study two zinc(II) phthalocyanine-tin(IV) conjugates linked by a triethylene glycol chain were synthesized and characterized. In these complexes, the zinc(II) phthalocyanine was used as a potential photosensitizer for PDT and the tin complex was selected as cytostatic moiety. The two dyads composed of zinc(II) phthalocyanine and tin complexes exhibited high cytotoxicity, in absence of light stimulation, against MCF-7 human breast cancer cells with low LC50 values in the range of 0.016–0.453 µM. In addition, these complexes showed superior cytotoxicity than their mixture of equimolar component, accompanied with a higher activity towards cancer cells compared to human healthy fibroblasts. However, under irradiation of the zinc phthalocyanine unit (at 650 nm) no photodynamic activity could be detected, due to the most likely quenching of zinc(II) phthalocyanine singlet excited state by the nearby tin complex according to a photoinduced electron transfer process. This study demonstrates the potential of heterometallic anticancer chemotherapeutics composed of a zinc phthalocyanine and tin complex, and it highlights that the development of such conjugates requires that the sensitizer preserves its photophysical properties and in particular its singlet oxygen sensitization ability in the conjugate in order to combine the PDT activity with the cytotoxicity of the anticancer drug.

Tumor Biology ◽  
2017 ◽  
Vol 39 (10) ◽  
pp. 101042831772727 ◽  
Author(s):  
Eric Chekwube Aniogo ◽  
Blassan Plackal Adimuriyil George ◽  
Heidi Abrahamse

2016 ◽  
Vol 16 (4) ◽  
pp. 4180-4190 ◽  
Author(s):  
Sofia Guzzarlamudi ◽  
Pankaj K Singh ◽  
Vivek K Pawar ◽  
Yuvraj Singh ◽  
Komal Sharma ◽  
...  

Although curcumin (Cur), has been poised to be an anticancer boon for quite some, its progress from bench to bed has been strained due to various pharmaceutical hurdles. Consequently curcumin has been entrapped in methoxy poly ethylene glycol and linoleic acid conjugated polymeric micelles (PMs) to not only tackle the routine issues but to also provide a synergetic effect against MCF-7 breast cancer cells. Optimized PMs of Cur had size 186.53±12.10 nm with polydispersity index 0.143±0.031 and zeta potential −30.1±3.2 mV. Developed formulation (Mpeg-Cla-Cur PMs) was hemocompatible and had high cytotoxicity (IC50 55.80±4.63 μg/mL) against MCF-7 cells in comparison to pure Cur suspension (IC50 75.05±5.75 μg/mL). As postulated cell cycle arrest and apoptosis studies revealed synergetic effect of Mpeg-Cla-Cur PMs with higher cell population in G1 phase in addition to high apoptosis of MCF-7 cells as compared to pure Cur suspension and control group. Pharmacokinetic studies also show PMs enhanced MRT and T1/2 of Cur indicating its longer retention time in body. Mpeg-Cla-Cur PMs might become as an excellent chemotherapeutic alternative candidate for treatment of breast cancer with higher commercial value.


2019 ◽  
Vol 23 (11n12) ◽  
pp. 1486-1494
Author(s):  
Nthabeleng Molupe ◽  
Balaji Babu ◽  
Earl Prinsloo ◽  
Abdessamad Y. A. Kaassis ◽  
Katharina Edkins ◽  
...  

A novel Sn(IV) meso-tetraacenaphthylporphyrin (SnTAcP) has been synthesized and characterized. SnTAcP was complexed with methyl-[Formula: see text]-cyclodextrin (m[Formula: see text]-CD), a nanocarrier that enhances water solubility, and the complexes were evaluated as PDT agents using MCF-7 breast cancer cells. A relatively low singlet oxygen quantum yield value of 0.36 was obtained in DMF, and the lowest energy Q band lies at 608 nm on the edge of the therapeutic window. SnTAcP was found to be non-toxic in the dark and phototoxic towards MCF-7 breast cancer cells with a half-maximal inhibitory concentration (IC[Formula: see text] value of 11 ± 1.1 [Formula: see text]g · mL[Formula: see text] after 30 min of irradiation with a 625 nm Thorlabs LED that provides a dose of 432 J · cm[Formula: see text]. A higher IC[Formula: see text] value of 21 ± 1.1 [Formula: see text]g · mL-1 was obtained for the m[Formula: see text]-CD inclusion complex of SnTAcP.


2020 ◽  
Vol 25 (01) ◽  
pp. 47-55
Author(s):  
Gugu Kubheka ◽  
Balaji Babu ◽  
Earl Prinsloo ◽  
Nagao Kobayashi ◽  
John Mack ◽  
...  

Mono- and disubstituted 2,6-dibromo-dimethylaminophenylbuta-1,3-dienylBODIPY dyes were successfully prepared, and their in vitro photodynamic activities against MCF-7 breast cancer cells were evaluated with a Thorlabs M660L4 660 nm LED (336 J · cm[Formula: see text]. The IC[Formula: see text] value of the monophenylbuta-1,3-dienylBODIPY was ca. 2.1 [Formula: see text]M, while that of the diphenylbuta-1,3-dienylBODIPY was > 50 [Formula: see text]M. Both dyes exhibited minimal dark toxicity. The results demonstrate that monosubstituted 2,6-dibromo-dimethylaminophenylbuta-1,3-dienylBODIPY dyes merit further in-depth study for use as photosensitizer dyes in photodynamic therapy.


Author(s):  
Maria Paulina Romero ◽  
Nicholas R.S. Gobo ◽  
Kleber T. de Oliveira ◽  
Yassuko Iamamoto ◽  
Osvaldo A. Serra ◽  
...  

2021 ◽  
Vol 50 (6) ◽  
pp. 2177-2182
Author(s):  
Balaji Babu ◽  
John Mack ◽  
Tebello Nyokong

The utility of Sn(iv) tetraarylchlorins for use as photosensitizer dyes in photodynamic therapy is assessed.


2017 ◽  
Vol 13 (6) ◽  
pp. 625-633 ◽  
Author(s):  
Mayson H. Alkhatib ◽  
Dalal A. Al-Saedi

Background: The combination of anticancer drugs in nanoparticles has great potential as a promising strategy to maximize drug efficacies. Gemcitabine (GEM), a nucleoside analogue, and atorvastatin (ATV), a cholesterol lowering agent, have shown anticancer effect with some limitations. Objective: The study aimed to evaluate antitumor activity of the combination therapy of GEM and ATV encapsulated in nanodroplets of microemulsion (ME) formulation in MCF-7 breast cancer cells and healthy HFS human foreskin cells. Method: The physical characterization of drug formulas has been studied by the transmission electron microscope (TEM). The cytotoxicity and efficacy of the formulation were examined by 3(4,5-dimethylthiazole-2-yl)-2,5-diphyneltetrazolium bromide (MTT) assay, light microscopy, and ApopNexin apoptosis detection kit. Results: It has been found that the IC50, inhibitory concentration at which 50 percent of the cells inhibited, for the combination of GEM and ATV at 1:2 ratio, respectively, in the ME (GEM/2ATVME) with a droplet diameter of 4.81±0.86 nm, subjected into the MCF-7 cells for 24h, was similar to the combination of GEM and ATV at 1:1 ratio, respectively, in water (GEM/ATV). According to the FITC/PI assay, 5 µM of GEM/2ATV-ME was less toxic on the HFS cells as higher percentages of viable cells (85.15%) were detected when compared to the GEM/ATV that caused reduction in the percentages of the viable cells (66.45%). Conclusion: Formulating GEM with ATV in ME has improved the therapeutic anticancer potential of both drugs while reducing their side effects on the normal cells.


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