scholarly journals Design and synthesis of 5-aminolaevulinic acid/3-hydroxypyridinone conjugates for photodynamic therapy: enhancement of protoporphyrin IX production and photo-toxicity in tumor cells

MedChemComm ◽  
2016 ◽  
Vol 7 (6) ◽  
pp. 1190-1196 ◽  
Author(s):  
Tao Zhou ◽  
Le-Le Shao ◽  
Sinan Battah ◽  
Chun-Feng Zhu ◽  
Robert C. Hider ◽  
...  

A series of ALA-HPO conjugates was prepared. One such conjugate was found to possess high phototoxicity.

2019 ◽  
Vol 20 (5) ◽  
pp. 1229 ◽  
Author(s):  
Marta Mascaraque ◽  
Pablo Delgado-Wicke ◽  
Alejandra Damian ◽  
Silvia Lucena ◽  
Elisa Carrasco ◽  
...  

Photodynamic therapy (PDT) constitutes a cancer treatment modality based on the administration of a photosensitizer, which accumulates in tumor cells. The subsequent irradiation of the tumoral area triggers the formation of reactive oxygen species responsible for cancer cell death. One of the compounds approved in clinical practice is methyl-aminolevulinate (MAL), a protoporphyrin IX (PpIX) precursor intermediate of heme synthesis. We have identified the mitotic catastrophe (MC) process after MAL-PDT in HeLa human carcinoma cells. The fluorescence microscopy revealed that PpIX was located mainly at plasma membrane and lysosomes of HeLa cells, although some fluorescence was also detected at endoplasmic reticulum and Golgi apparatus. Cell blockage at metaphase-anaphase transition was observed 24 h after PDT by phase contrast microscopy and flow cytometry. Mitotic apparatus components evaluation by immunofluorescence and Western blot indicated: multipolar spindles and disorganized chromosomes in the equatorial plate accompanied with dispersion of centromeres and alterations in aurora kinase proteins. The mitotic blockage induced by MAL-PDT resembled that induced by two compounds used in chemotherapy, taxol and nocodazole, both targeting microtubules. The alterations in tumoral cells provided evidence of MC induced by MAL-PDT, resolving mainly by apoptosis, directly or through the formation of multinucleate cells.


2007 ◽  
Vol 86 (1) ◽  
pp. 126-132 ◽  
Author(s):  
S. Grönlund-pakkanen ◽  
T.M. Pakkanen ◽  
M. Talja ◽  
V.-M. Kosma ◽  
M. Ala-opas ◽  
...  

Gut ◽  
1995 ◽  
Vol 36 (1) ◽  
pp. 67-75 ◽  
Author(s):  
J Regula ◽  
A J MacRobert ◽  
A Gorchein ◽  
G A Buonaccorsi ◽  
S M Thorpe ◽  
...  

1996 ◽  
Vol 74 (10) ◽  
pp. 1526-1533 ◽  
Author(s):  
K Svanberg ◽  
DL Liu ◽  
I Wang ◽  
S Andersson-Engels ◽  
U Stenram ◽  
...  

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