TITLE:
Ursolic Acid Derivatives Induced Apoptosis and Reduces the NF-κB in Human Lung Adenocarcinoma Cells
AUTHORS:
Elaine Carlos Scherrer, Ydia Mariele Valadares, Caio Cesar Souza Alves, Gabriella Freitas Ferreira, Marcela Pereira Leão, Jessica Aline Soares, Fernando Sa Silva, Alessandra Paula Carli, Oswaldo Cardoso Jr., Fabiana Simão Machado, Sandra Bertelli Ribeiro Castro
KEYWORDS:
Ursolic Acid, Apoptosis, NF-κB, A549 Cells, Tumoral
JOURNAL NAME:
Journal of Cancer Therapy,
Vol.10 No.10,
October
23,
2019
ABSTRACT: Lung
cancer is the major cause of death in the neoplastic diseases. In spite
of the advances in the chemotherapy, the lung cancer treatments are still complex
and costly, being necessary the seeking
of new drugs. In this context, the ursolic acid (UA) becomes the target of
studies that investigate its antitumor potential and, thus, structural
modifications can enhance its biological activities. Eight UA semisynthetic
derivative compounds (UAD1-8) were synthesized and evaluated their cytotoxic
activity against human alveolar adenocarcinoma cells (A549). UAD1, UAD3, UAD5,
UAD6 and UAD8 were able to reduce the
viability of the A549 cells. Only UAD1 and UAD6 reduced the viability at 24 h,
and only UAD3 didn’t reduce the NF-κB expression.
The compound UAD1 showed the greater apoptosis induction. Moreover, the compound UAD1 showed better results than UA
in all assays. The present study shows, for the first time, the action of these
compounds in the apoptotic effect, in the expression of NF-κB and in the A549 cell line. The ursolic acid derivatives showed
substantial results in the apoptosis, cytotoxicity and NF-κB inhibition of A549 cells, and further studies are necessary for
the development of possible new therapeutic drugs.