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Pregled bibliografske jedinice broj: 1003915

The photodynamic activities of dimethyl 131-[2- (guanidinyl)ethylamino] chlorin e6 photosensitizers in A549 tumor


Gao, Ying-Hua; Lovreković, Vanda; Kussayeva, Akmaral; Chen, Dan-Ye; Margetić, Davor; Chen, Zhi-Long
The photodynamic activities of dimethyl 131-[2- (guanidinyl)ethylamino] chlorin e6 photosensitizers in A549 tumor // European journal of medicinal chemistry, 177 (2019), 144-152 doi:10.1016/j.ejmech.2019.05.050 (međunarodna recenzija, članak, znanstveni)


Naslov
The photodynamic activities of dimethyl 131-[2- (guanidinyl)ethylamino] chlorin e6 photosensitizers in A549 tumor

Autori
Gao, Ying-Hua ; Lovreković, Vanda ; Kussayeva, Akmaral ; Chen, Dan-Ye ; Margetić, Davor ; Chen, Zhi-Long

Izvornik
European journal of medicinal chemistry (0223-5234) 177 (2019); 144-152

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
Chlorin e6 derivativeGuanidinePhotodynamic therapyPhotosensitizersReactive oxygen speciesTumor

Sažetak
Effective photosensitizers are particularly important factor in clinical photodynamic therapy (PDT). However, there is a scarcity of photosensitizers for simultaneous cancer photo- diagnosis and targeted PDT. Herein, two novel dimethyl 2-(guanidinyl)ethylamino chlorin e6 photosensitizers were synthesized and their efficacy in PDT in A549 tumor was investigated. It was shown that compounds 3 and 4 have a long absorption wavelength in the near infrared region and strong fluorescence emission with slow photo-bleaching rate and markedly strong ability of 1O2 generation. They exhibited lower cytotoxicity and higher photo-cytotoxicity in vitro compared to the known anticancer drug m- THPC in MTT assay in A549 lung cancer cell lines. Compound 4 exhibit better inhibition effect than compound 3 and the IC50 value of compound 4 was 0.197 μM/L under 2 J/cm2 laser irradiation, while compound 3 showed better anti-tumor effects compared to compound 4 in vivo. Intracellular ROS generation was found to be responsible for apoptotic cell death in DCFDA assay. Subcellular localization confirmed the damage site of compounds 3 and 4 in PDT. These findings suggest that the two novel photosensitizers might serve as potential photosensitizers for improved therapeutic efficiency of PDT.

Izvorni jezik
Engleski

Znanstvena područja
Kemija



POVEZANOST RADA


Projekt / tema
HRZZ-IP-2018-01-3298 - Cikloadicijske strategije prema policikličkim gvanidinima (Davor Margetić, )

Ustanove
Institut "Ruđer Bošković", Zagreb

Časopis indeksira:


  • Current Contents Connect (CCC)
  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE


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