7-Epiclusianone, a Benzophenone Extracted from Garcinia brasiliensis (Clusiaceae), Induces Cell Cycle Arrest in G1/S Transition in A549 Cells

Molecules

Marisa Ionta⁴  Guilherme A. Ferreira-Silva⁴  Evandro L. Niero²  짞rson D’Martin Costa³  Adam A. Martens²  Welton Rosa³  Marisi G. Soares³  Gláucia M. Machado-Santelli²  João Henrique G. Lago⁵  Marcelo H. Santos¹ 

[1] Institute of Chemistry, Federal University of Viçosa, 36570-900 Viçosa, Brazil; E-Mail:;Department of Cell and Developmental Biology, Institute of Biomedical Sciences, University of Sao Paulo, 05508-000 São Paulo, Brazil; E-Mails:;Institute of Chemistry, Federal University of Alfenas, 37130-000 Alfenas, Brazil; E-Mails:;Institute of Biomedical Sciences, Federal University of Alfenas, 37130-000 Alfenas, Brazil; E-Mail:;Institute of Environmental, Chemical and Pharmaceutical Sciences, Federal University of Sao Paulo, 09920-000 Diadema, Brazil; E-Mail:

关键词: 7-epiclusianone;    Garcinia brasiliensis;    antiproliferative activity;    lung cancer;    cell cycle arrest;    cell death;   

DOI  :  10.3390/molecules200712804

来源: mdpi

【 摘 要 】

Lung cancer is the leading cause of cancer deaths in the world. Disease stage is the most relevant factor influencing mortality. Unfortunately, most patients are still diagnosed at an advanced stage and their five-year survival rate is only 4%. Thus, it is relevant to identify novel drugs that can improve the treatment options for lung cancer. Natural products have been an important source for the discovery of new compounds with pharmacological potential including antineoplastic agents. We have previously isolated a prenylated benzophenone (7-epiclusianone) from Garcinia brasiliensis (Clusiaceae) that has several biological properties including antiproliferative activity against cancer cell lines. In continuation with our studies, the present work aimed to investigate the mechanisms involved with antiproliferative activity of 7-epiclusianone in A549 cells. Our data showed that 7-epiclusianone reduced the viability of A549 cells in a concentration-dependent manner (IC₅₀ of 16.13 ± 1.12 μM). Cells were arrested in G1/S transition and apoptosis was induced. In addition, we observed morphological changes with cytoskeleton disorganization in consequence of the treatment. Taken together, the results showed that cell cycle arrest in G1/S transition is the main mechanism involved with antiproliferative activity of 7-epiclusianone. Our results are promising and open up the prospect of using this compound in further anticancer in vivo studies.

【 授权许可】

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