scholarly journals Symmetrically Substituted Zn and Al Phthalocyanines and Polymers for Photodynamic Therapy Application

2021 ◽  
Vol 9 ◽  
Author(s):  
Keshavananda Prabhu C. P. ◽  
Manjunatha Nemakal ◽  
Muthumuni Managa ◽  
Tebello Nyokong ◽  
Lokesh Koodlur Sannegowda

N4 macrocyclic complexes of Al and Zn phthalocyanines with symmetrical imine and imidazole moiety at the periphery were synthesized. The synthesized ligands, complexes, and polymers were purified and characterized to study the structure of the molecule. These synthesized complexes were used for photodynamic therapy application as the diamagnetic Zn and Al have the ability to produce and stabilize singlet oxygen species. The synthesized N4 molecules of aluminum iminomethoxy phenyl phthalocyanine and aluminum ethyl phenyl benzimidazolephthalocyanine showed better activity against MCF-7 cells. These results suggest that this assay may be used as an early biomarker of clinical response.

2020 ◽  
Vol 996 ◽  
pp. 82-87
Author(s):  
Shu Guo Dong ◽  
Gui Hua Cui ◽  
Qian Duan

A novel end-functionalized glycopolymer poly (3-O-methacryloyl-D-glucofuranose) -b-poly (2-Diethylaminoethyl Methacrylate) (PMAGlc-b-PDEA-ZnTAPc) with zinc (II) teraamaninophthalocyanine was synthesized. First, a pH-responsive copolymer PMAIpG-b-PDEA was synthesized via reversible addition-fragmentation chain transfer (RAFT) polymerization. Then PMAIpG-b-PDEA reacted with ZnTAPc and deprotected to form a water-soluble and pH-responsive photosensitizer. The structure of the PMAGlc-b-PDEA-ZnTAPc was characterized by 1H NMR and GPC. The photophysical properties were evaluated by UV-Vis and fluorescence spectra. The PMAGlc-b-PDEA-ZnTAPc can generate singlet oxygen species with good singlet oxygen quantum yields (Φ△=0.38), which is believed to be the major cytotoxic reactive oxygen species (ROS) for photodynamic therapy. The ZnPc functionalized glycopolymer will be used as a potential photosensitizer in the fields of photodynamic therapy.


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.


2019 ◽  
Author(s):  
Liyi Huang ◽  
Haidan Lin ◽  
Qing Chen ◽  
Lehua Yu ◽  
dingqun bai

Abstract Abstract Background: Breast cancer is one of the most commonly diagnosed cancers in women, with high morbidity and mortality. Tumor metastasis is implicated in most breast cancer deaths; thus, inhibiting metastasis may provide a therapeutic direction for breast cancer. In the present study, pyropheophorbide-α methyl ester-mediated photodynamic therapy (MPPa-PDT) was used to inhibit metastasis in MCF-7 breast cancer cells. Methods: Uptake of MPPa was detected by fluorescence microscopy. Cell viability was evaluated by the Cell Counting Kit-8 (CCK-8). ROS generation was detected by 2',7'-dichlorodihydrofluorescein diacetate (DCFH-DA). The migration of cells was assessed by wound healing assay, and invasion ability was assessed by Matrigel invasion assay. Levels of MMP2 and MMP9 were measured by PCR. Akt, phospho-Akt (Ser473), phospho-NF-κB p65 (Ser536) and NF-κB p65 were measured by western blotting. The F-actin cytoskeleton was observed by immunofluorescence. Lung tissue was visualized by hematoxylin and eosin staining. Results: Following MPPa-PDT, migration and invasion were decreased in the MCF-7 cells. MPPa-PDT downregulated the expression of MMP2 and MMP9, which are responsible for the initiation of metastasis. MPPa-PDT reduced the phosphorylation of Akt and NF-κB. MPPa-PDT also reduced and destroyed the F-actin cytoskeleton in MCF-7 cells. These effects were blocked by the reactive oxygen species scavenger NAC or the Akt activator SC79, while the PI3K inhibitor LY294002 or the Akt inhibitor triciribine enhanced these effects. Moreover, MPPa-PDT inhibited tumor metastasis and destroyed F-actin in vivo. Conclusion: Taken together, these results demonstrate that MPPa-PDT inhibits the metastasis of MCF-7 cells both in vitro and in vivo and may be involved in the Akt/NF-κB-dependent MMP-9 signaling pathway. Thus, MPPa-PDT may be a promising treatment to inhibit metastasis. Key words: photodynamic therapy, reactive oxygen species, breast tumor, migration, invasion


2013 ◽  
Vol 1569 ◽  
pp. 67-72
Author(s):  
Jiun-Chiou Wei ◽  
Yi-Ting Wang ◽  
Jiang-Jen Lin

ABSTRACTThin silicate nanoplatelets, derived from the exfoliation of natural Sodium montmorillonite (Na+-MMT) clays, show an unexpected antimicrobial property. A physical trapping mechanism has been proposed because the clay nanoplatelets can indiscriminately inhibit the growth of a broad spectrum of bacteria, including drug-resistant species such as methicillin-resistance S. aureus (MRSA) and silver ion-resistant E. coli. The ability to generate singlet oxygen species was first observed for the clay platelets that showed a high-aspect-ratio geometric shape and the presence of surface ionic charges. By comparison, the pristine clay with a multilayered structure failed to generate any singlet oxygen species. The ability to emit singlet oxygen species provides direct evidence for the antimicrobial ability of clay through a non-chemical mechanism, which opens the potential for medical use.


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