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Sci Rep ; 10(1): 10534, 2020 06 29.
Artigo em Inglês | MEDLINE | ID: mdl-32601436

RESUMO

The cytotoxic mechanism of the saponin QS-21 and its aglycone quillaic acid (QA) was studied on human gastric cancer cells (SNU1 and KATO III). Both compounds showed in vitro cytotoxic activity with IC50 values: 7.1 µM (QS-21) and 13.6 µM (QA) on SNU1 cells; 7.4 µM (QS-21) and 67 µM (QA) on KATO III cells. QS-21 and QA induce apoptosis on SNU1 and KATO III, as demonstrated by TUNEL, Annexin-V and Caspase Assays. Additionally, we performed in silico docking studies simulating the binding of both triterpenic compounds to key proteins involved in apoptotic pathways. The binding energies (∆Gbin) thus calculated, suggest that the pro-apoptotic protein Bid might be a plausible target involved in the apoptotic effect of both triterpenic compounds. Although QA shows some antiproliferative effects on SNU1 cells cultured in vitro, our results suggest that QS-21 is a more powerful antitumor agent, which merits further investigation regarding their properties as potential therapeutic agents for gastric cancer.


Assuntos
Antineoplásicos/química , Apoptose/efeitos dos fármacos , Ácido Oleanólico/análogos & derivados , Quillaja , Saponinas/química , Neoplasias Gástricas/tratamento farmacológico , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Linhagem Celular Tumoral , Humanos , Simulação de Acoplamento Molecular , Ácido Oleanólico/química , Ácido Oleanólico/farmacologia , Ácido Oleanólico/uso terapêutico , Saponinas/farmacologia , Saponinas/uso terapêutico
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