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APS8 delays tumor growth in mice by inducing apoptosis of lung adenocarcinoma cells expressing high number of α7 nicotinic receptors
ID
Berne, Sabina
(
Avtor
),
ID
Čemažar, Maja
(
Avtor
),
ID
Frangež, Robert
(
Avtor
),
ID
Juntes, Polona
(
Avtor
),
ID
Kranjc Brezar, Simona
(
Avtor
),
ID
Grandič, Marjana
(
Avtor
),
ID
Savarin, Monika
(
Avtor
),
ID
Turk, Tom
(
Avtor
)
PDF - Predstavitvena datoteka,
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MD5: 82D9A7BF7CE28A6F22ED41CB6A446070
URL - Izvorni URL, za dostop obiščite
https://www.mdpi.com/1660-3397/16/10/367
Galerija slik
Izvleček
The alkylpyridinium polymer APS8, a potent antagonist of α7 nicotinic acetylcholine receptors (nAChRs), selectively induces apoptosis in non-small cell lung cancer cells but not in normal lung fibroblasts. To explore the potential therapeutic value of APS8 for at least certain types of lung cancer, we determined its systemic and organ-specific toxicity in mice, evaluated its antitumor activity against adenocarcinoma xenograft models, and examined the in-vitro mechanisms of APS8 in terms of apoptosis, cytotoxicity, and viability. We also measured Ca$^{2+}$ influx into cells, and evaluated the effects of APS8 on Ca$^{2+}$ uptake while siRNA silencing of the gene for α7 nAChRs, CHRNA7. APS8 was not toxic to mice up to 5 mg/kg i.v., and no significant histological changes were observed in mice that survived APS8 treatment. Repetitive intratumoral injections of APS8 (4 mg/kg) significantly delayed growth of A549 cell tumors, and generally prevented regrowth of tumors, but were less effective in reducing growth of HT29 cell tumors. APS8 impaired the viability of A549 cells in a dose-dependent manner and induced apoptosis at micro molar concentrations. Nano molar APS8 caused minor cytotoxic effects, while cell lysis occurred at APS8 >3 µM. Furthermore, Ca$^{2+}$ uptake was significantly reduced in APS8-treated A549 cells. Observed differences in response to APS8 can be attributed to the number of α7 nAChRs expressed in these cells, with those with more AChRs (i.e., A549 cells) being more sensitive to nAChR antagonists like APS8. We conclude that α7 nAChR antagonists like APS8 have potential to be used as therapeutics for tumors expressing large numbers of α7 nAChRs.
Jezik:
Angleški jezik
Ključne besede:
lung cancer
,
antitumor activity
,
A549
,
HT29
,
CHRNA7
,
alkylpiridinium
,
SCID mice
,
toxicity
,
apoptosis
,
lung neoplasms
,
therapy
,
nicotinic receptors
Vrsta gradiva:
Članek v reviji
Tipologija:
1.01 - Izvirni znanstveni članek
Organizacija:
BF - Biotehniška fakulteta
VF - Veterinarska fakulteta
Status publikacije:
Objavljeno
Različica publikacije:
Objavljena publikacija
Leto izida:
2018
Št. strani:
17 str.
Številčenje:
Vol. 16, iss. 10, art. 367
PID:
20.500.12556/RUL-132067
UDK:
577.1
ISSN pri članku:
1660-3397
DOI:
10.3390/md16100367
COBISS.SI-ID:
4683642
Datum objave v RUL:
11.10.2021
Število ogledov:
763
Število prenosov:
165
Metapodatki:
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Objavi na:
Gradivo je del revije
Naslov:
Marine drugs
Skrajšan naslov:
Mar. drugs
Založnik:
MDPI
ISSN:
1660-3397
COBISS.SI-ID:
23578841
Licence
Licenca:
CC BY 4.0, Creative Commons Priznanje avtorstva 4.0 Mednarodna
Povezava:
http://creativecommons.org/licenses/by/4.0/deed.sl
Opis:
To je standardna licenca Creative Commons, ki daje uporabnikom največ možnosti za nadaljnjo uporabo dela, pri čemer morajo navesti avtorja.
Začetek licenciranja:
03.10.2018
Projekti
Financer:
ARRS - Agencija za raziskovalno dejavnost Republike Slovenije
Številka projekta:
J1-4044
Naslov:
Apoptotično delovanje alkilpiridinijevih spojin na celice pljučnega adenokarcinoma
Financer:
ARRS - Agencija za raziskovalno dejavnost Republike Slovenije
Številka projekta:
P3-0003
Naslov:
Razvoj in ovrednotenje novih terapij za zdravljenje malignih tumorjev
Financer:
ARRS - Agencija za raziskovalno dejavnost Republike Slovenije
Številka projekta:
P4-0053
Naslov:
Endokrini, imunski in encimski odzivi pri zdravih in bolnih živalih
Financer:
ARRS - Agencija za raziskovalno dejavnost Republike Slovenije
Številka projekta:
P4-0092
Naslov:
Zdravje živali, okolje in varna hrana
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