The effects of 5-aminolevulinic acid (ALA)-esters on ALA-induced protoporphyrin (PPIX) production and localization on human adenocarcinoma cell lines

Photodynamic therapy (PDT) is a clinically approved, minimally invasive treatment for malignant tumors. Protoporphyrin IX (PpIX), derived from 5-aminolevulinic acid (5-ALA) as the prodrug, is one of the photosensitizers used in PDT. Recently, we reported a significant difference in response to 5-ALA-mediated PDT treatment in two canine primary lung adenocarcinoma cell lines (sensitive to PDT: HDC cells, resistant to PDT: LuBi cells). This study aimed to examine the difference in cytotoxicity of 5-ALA-mediated PDT in these cells. Although intracellular PpIX levels before irradiation were similar between HDC and LuBi cells, the percentage of ROS-positive cells and apoptotic cells in LuBi cells treated with 5-ALA-mediated PDT was significantly lower than that in HDC cells treated with 5-ALA-mediated PDT. A high dosage of the NO donor, DETA NONOate, significantly increased the cytotoxicity of 5-ALA-mediated PDT against LuBi cells. These results suggest that the sensitivity of 5-ALA-mediated PDT might be correlated with NO.

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The Effects of 5-Aminolevulinic Acid Esters on Protoporphyrin IX Production in Human Adenocarcinoma Cell Lines¶

Photochemistry and Photobiology ◽

10.1562/0031-8655(2001)0740721teoaae2.0.co2 ◽

2007 ◽

Vol 74 (5) ◽

pp. 721-725

Author(s):

H. Brunner ◽

F. Hausmann ◽

R. C. Krieg ◽

E. Endlicher ◽

J. Schölmerich ◽

...

Keyword(s):

Cell Lines ◽

Aminolevulinic Acid ◽

Protoporphyrin Ix ◽

Adenocarcinoma Cell ◽

Acid Esters

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Hypericin- and Δ-aminolevulinic acid-induced phototoxicity in squamous and adenocarcinoma cell lines of the esophagus

Gastroenterology ◽

10.1016/s0016-5085(00)82225-8 ◽

2000 ◽

Vol 118 (4) ◽

pp. A39

Author(s):

Andreas Theiss ◽

Michael Hoepfner ◽

Andreas Jansen ◽

Kerstin Maaser ◽

Hanoch Kashtan ◽

...

Keyword(s):

Cell Lines ◽

Aminolevulinic Acid ◽

Adenocarcinoma Cell

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Synthesis, Anti-proliferative Evaluation, and Molecular Docking Studies of 3-(alkylthio)-5,6-diaryl-1,2,4-triazines as Tubulin Polymerization Inhibitors

Letters in Drug Design & Discovery ◽

10.2174/1570180815666180727114216 ◽

2019 ◽

Vol 16 (11) ◽

pp. 1194-1201 ◽

Cited By ~ 3

Author(s):

Farhad Saravani ◽

Ebrahim Saeedian Moghadam ◽

Hafezeh Salehabadi ◽

Seyednasser Ostad ◽

Morteza Pirali Hamedani ◽

...

Keyword(s):

Molecular Modeling ◽

Cytotoxic Activity ◽

Binding Site ◽

Cell Line ◽

Cell Lines ◽

Tubulin Polymerization ◽

Adenocarcinoma Cell Line ◽

Adenocarcinoma Cell ◽

Colchicine Binding Site ◽

Anti Cancer

Background: The role of microtubules in cell division and signaling, intercellular transport, and mitosis has been well known. Hence, they have been targeted for several anti-cancer drugs. Methods: A series of 3-(alkylthio)-5,6-diphenyl-1,2,4-triazines were prepared and evaluated for their cytotoxic activities in vitro against three human cancer cell lines; human colon carcinoma cells HT-29, human breast adenocarcinoma cell line MCF-7, human Caucasian gastric adenocarcinoma cell line AGS as well as fibroblast cell line NIH-3T3 by MTT assay. Docking simulation was performed to insert these compounds into the crystal structure of tubulin at the colchicine binding site to determine a probable binding model. Compound 5d as the most active compound was selected for studying of microtubule disruption. Results: Compound 5d showed potent cytotoxic activity against all cell lines. The molecular modeling study revealed that some derivatives of triazine strongly bind to colchicine binding site. The tubulin polymerization assay kit showed that the cytotoxic activity of 5d may be related to inhibition of tubulin polymerization. Conclusion: The cytotoxicity and molecular modeling study of the synthesized compounds with their inhibition activity in tubulin polymerization demonstrate the potential of triazine derivatives for development of new anti-cancer agents.

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