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Ursolic Acid Derivatives Induced Apoptosis and Reduces the NF-κB in Human Lung Adenocarcinoma Cells

Journal of Cancer Therapy 2019年第10期10卷 863-876页

作者： Elaine Carlos Scherrer ydia mariele valadares Caio Cesar Souza Alves Gabriella Freitas Ferreira Marcela Pereira Leao Jessica Aline Soares Fernando Sa Silva Alessandra Paula Carli Oswaldo Cardoso Jr. Fabiana Simao Machado Sandra Bertelli Ribeiro Castro Life Sciences Institute Federal University of Juiz de ForaGovernador ValadaresMGBrazil Faculty of Medicine Federal University of the Valleys of Jequitinhonha and MucuriTeofilo OtoniMGBrazil Department of Biochemistry and Immunology Federal University of Minas GeraisBelo HorizonteMGBrazil

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.

关键词： Ursolic Acid Apoptosis NF-κB A549 Cells Tumoral

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