The photodynamic activity of 13-[2'-(2-pyridyl)ethylamine] chlorin e photosensitizer in human esophageal cancer.

Bioorg Med Chem Lett

Department of Pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai 201620, China. Electronic address:

Published: June 2018

A novel 13-pyridine substituted chlorin e derivative (Chlorin A) was synthesized. It has characteristic long wavelength absorption at 664 nm and the emission wavelength at 667 nm. The generation rate of singlet oxygen of this compound is higher than Temoporfin. In vitro, Chlorin A showed higher phototoxicity against the human esophageal cancer cells than Temoporfin while with lower dark-toxicity. Its accumulation effect in mitochondria, lysosomes and endoplasmic reticulum was traced in subcellular localization tests. In flow cytometry obvious apoptosis cells were observed after 2 h irradiation. Significant in vivo photodynamic anti-tumor efficacy was also exhibited on mice bearing esophageal cancer. So Chlorin A could be suggested as a promising anti-tumor drug candidate in photodynamic therapy.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2018.04.025DOI Listing

Publication Analysis

Top Keywords

esophageal cancer
12
human esophageal
8
chlorin
5
photodynamic activity
4
activity 13-[2'-2-pyridylethylamine]
4
13-[2'-2-pyridylethylamine] chlorin
4
chlorin photosensitizer
4
photosensitizer human
4
cancer novel
4
novel 13-pyridine
4

Similar Publications

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!