RT Journal Article
SR Electronic
T1 Aurelianolides from <em>Aureliana fasciculata</em> var. <em>fasciculata</em> Trigger Apoptosis With Caspase Activation in Human Leukemia Cells
JF Anticancer Research
JO Anticancer Res
FD International Institute of Anticancer Research
SP 1245
OP 1253
DO 10.21873/anticanres.16271
VO 43
IS 3
A1 GUSTAVO WERNECK DE SOUZA E SILVA
A1 ANDRÉ MESQUITA MARQUES
A1 ANA PAULA GREGÓRIO ALVES FONTÃO
A1 SIMONE CRISTINA DE MOURA LIMA
A1 MARIA AUXILIADORA COELHO KAPLAN
A1 MARIA RAQUEL FIGUEIREDO
A1 ANDRÉ LUIZ FRANCO SAMPAIO
YR 2023
UL http://ar.iiarjournals.org/content/43/3/1245.abstract
AB Background/Aim: Aurelianolide A and B were identified and isolated from Aureliana fasciculata var. fasciculata leaves. Withanolides are naturally occurring C-28 steroidal lactone triterpenoids with cytotoxic and anticancer properties, among other relevant pharmacological activities. Herein we have described, for the first time, the cytotoxic effects of aurelianolides on human cancer cells. Materials and Methods: Aurelianolide A and B were tested on human leukemia cell lines: THP-1, MOLT-4, Jurkat, K562 and K562-Lucena 1. Results: For aurelianolide A, MOLT-4 had the lower IC50 (1.17 μM) and for aurelianolide B, Jurkat was the most susceptible cell line (IC50 2.25 μM). On the other hand, the multidrug resistant (MDR) cell line K562-Lucena 1 showed higher IC50 for both aurelianolides. Using 293T, a non-tumor embryonic kidney cell line, we observed an excellent selectivity index for both aurelianolides, from 2.24 (aurelianolide B in K562-Lucena 1) to 45.5 (aurelianolide A in MOLT-4). Aurelianolide A and B activated caspase 3/7 with consequent induction of apoptosis on Jurkat and K562-Lucena 1 cell lines. We have not observed induction of necrosis. Conclusion: Aurelianolides A and B have important cytotoxic effects on human leukemia cell lines by the activation of the caspase pathway.