Biological evaluation of octahydropyrazin[2,1-a:5,4-a′]diisoquinoline derivatives as potent anticancer agents
PBN-AR
Instytucja
Sieć Badawcza Łukasiewicz - Instytut Farmaceutyczny
Informacje podstawowe
Główny język publikacji
angielski
Czasopismo
TUMOR BIOLOGY (30pkt w roku publikacji)
ISSN
1010-4283
EISSN
1423-0380
Wydawca
SPRINGER
DOI
URL
Rok publikacji
2017
Numer zeszytu
6
Strony od-do
1-13
Numer tomu
39
Identyfikator DOI
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Autorzy
(liczba autorów: 9)
Pozostali autorzy
+ 8
Słowa kluczowe
angielski
diisoquinoline derivatives
apoptosis
caspases
breast cancer cells
Streszczenia
Język
angielski
Treść
In this study, we evaluated the cytotoxic activity and antiproliferative potency of novel octahydropyrazin[2,1-a:5,4-a′] diisoquinoline derivatives (1–7) in MCF-7 and MDA-MB-231 breast cancer cell lines. Annexin V binding assay and disruption of the mitochondrial potential were performed to determine apoptosis. The activity of caspases 3, 8, 9, and 10 was measured after 24 h of incubation with tested compounds to explain detailed molecular mechanism of induction of apoptosis. The results from experiments were compared with effects obtained after incubation in the presence of camptothecin and etoposide. Our study demonstrated that the most active compounds in both analyzed breast cancer cell lines were compounds 3 and 4. We also observed that all compounds induced apoptosis. We demonstrated the higher activity of caspases 3, 8, 9, and 10, which confirmed that induction of apoptosis is associated with external and internal cell death pathway. Our study revealed that the novel compounds in group of diisoquinoline derivatives are promising candidates in anticancer treatment by activation of both extrinsic and intrinsic apoptotic pathways.
Cechy publikacji
oryginalny artykuł naukowy
Inne
System-identifier
PX-59a6f582d5decf2a9c0c39cb
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