Synthesis and biological evaluation of phosphatidylcholines with cinnamic and 3- methoxycinnamic acids with potent antiproliferative activity
PBN-AR
Instytucja
Wydział Biotechnologii i Nauk o Żywności (Uniwersytet Przyrodniczy we Wrocławiu)
Informacje podstawowe
Główny język publikacji
angielski
Czasopismo
RSC Advances (35pkt w roku publikacji)
ISSN
2046-2069
EISSN
Wydawca
DOI
URL
Rok publikacji
2018
Numer zeszytu
Strony od-do
35744-35752
Numer tomu
8
Identyfikator DOI
Liczba arkuszy
Autorzy
(liczba autorów: 5)
Pozostali autorzy
+ 3
Streszczenia
Język
angielski
Treść
A series of eight novel phosphatidylcholines containing cinnamic or 3-methoxycinnamic acids (3a-b, 5a-b, 9a-b, 10a-b) at sn-1 and/or sn-2 positions were synthesized and tested for their antiproliferative activity in an in vitro model against representative six human cancer cell lines (MV4-11, A549, MCF-7, LoVo, LoVo/DX, HepG2) and a normal cell line BALB/3T3. The structures of the new compounds were confirmed by spectral analysis. Biological evaluation revealed that all the tested conjugates exhibited higher antitumor activity than the corresponding free aromatic acids. Compounds 3b and 9b turned out to be the most active, with IC50 values of 32.1 and 30.5 mM against the LoVo/DX and MV4-11 cell lines, respectively. Studies of the mechanism of the antitumor action were carried out for 1-palmitoyl-2-cinnamoyl-sn-glycero-3- phosphocholine (5a), and it was shown to be active toward almost all the tested types of cancer cells, showing that this compound could effectively arrest the cell cycle in G2/M and decrease the mitochondrial membrane potential of leukemia MV4-11 cells. The obtained results proved that the strategy of the incorporation of cinnamic and 3-methoxycinnamic acids into phospholipids could expand their potential application in industry, as well as could improve their antiproliferative activity and selectivity toward cancer cell lines.
Inne
System-identifier
PX-5bd07072d5de3e134b71c115