Advanced search
Start date
Betweenand
Related content
(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Trans-chalcone increases p53 activity via DNAJB1/HSP40 induction and CRM1 inhibition

Full text
Author(s):
Show less -
Silva, Gabriel [1] ; Marins, Mozart [1, 2] ; Chaichanasak, Nadda [3] ; Yoon, Yongdae [3] ; Fachin, Ana Lucia [1, 2] ; Pinhanelli, Vitor Caressato [1] ; Regasini, Luis Octavio [4] ; dos Santos, Mariana Bastos [4] ; Ayusso, Gabriela Miranda [4] ; Marques, Beatriz de Carvalho [4] ; Wu, Wells W. [5] ; Phue, Je-Nie [5] ; Shen, Rong-Fong [5] ; Baek, Seung Joon [3]
Total Authors: 14
Affiliation:
[1] Univ Ribeirao Preto, Biotechnol Unit, Ribeirao Preto, SP - Brazil
[2] Univ Ribeirao Preto, Med Sch, Ribeirao Preto, SP - Brazil
[3] Seoul Natl Univ, Coll Vet Med & Res Inst Vet Sci, Lab Signal Transduct, Seoul - South Korea
[4] Sao Paulo State Univ UNESP, Dept Chem & Environm Chem, Sao Paulo - Brazil
[5] US FDA, Facil Biotechnol Resources, CBER, Silver Spring, MD - USA
Total Affiliations: 5
Document type: Journal article
Source: PLoS One; v. 13, n. 8 AUG 17 2018.
Web of Science Citations: 3
Abstract

Naturally-occurring chalcones and synthetic chalcone analogues have been demonstrated to have many biological effects, including anti-inflammatory, anti-malarial, anti-fungal, and anti-oxidant/anti-cancerous activities. Compared to other chalcones, trans-chalcone exhibits superior inhibitory activity in cancer cell growth as shown via in vitro assays, and exerts anti-cancerous effects via the activation of the p53 tumor suppressor protein. Thus, characterization of the specific mechanisms, by which trans-chalcone activates p53, can aid development of new chemotherapeutic drugs that can be used individually or synergistically with other drugs. In this report, we found that trans-chalcone modulates many p53 target genes, HSP40 being the most induced gene in the RNA-Seq data using trans-chalcone-treated cells. CRM1 is also inhibited by trans-chalcone, resulting in the accumulation of p53 and other tumor suppressor proteins in the nucleus. Similar effects were seen using trans-chalcone derivatives. Overall, trans-chalcone could provide a strong foundation for the development of chalcone-based anti-cancer drugs. (AU)

FAPESP's process: 14/15307-7 - Molecular analysis of the response of human and canine tumor strain lines to the flavonoid trans-chalcone
Grantee:Mozart de Azevedo Marins
Support Opportunities: Regular Research Grants