In vitro and in silico evaluation of EGFR targeting activities of curcumin and its derivatives.
Food Funct
; 12(21): 10667-10675, 2021 Nov 01.
Article
en En
| MEDLINE
| ID: mdl-34604873
ABSTRACT
As polyphenols from Curcuma longa, curcumin and its derivatives possess numerous bioactivities. Herein, the epidermal growth factor receptor (EGFR) targeting activities of curcumin and its derivatives, as well as their structure-activity relationship were investigated. All of the tested compounds exhibited significant inhibition activities against EGFR kinase in homogeneous time-resolved fluorescence assay. Then their antiproliferative activities against Caco-2 were confirmed. The expressions of EGFR and phospho-EGFR proteins were regulated by curcumin and its derivatives. The 3,5-dione and methoxyl groups exerted significant influence on their electrostatic interactions with EGFR. Both hydrogen bonds and hydrophobic contacts were crucial for their binding with EGFR. Interestingly, their EGFR targeting activities were structure-dependent. The binding stabilities of curcumin and its derivatives were different from each other due to their structural diversity. This work indicated that curcumin and its derivatives were potential tyrosine kinase inhibitors that target EGFR.
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Curcumina
/
Receptores ErbB
Límite:
Humans
Idioma:
En
Revista:
Food Funct
Año:
2021
Tipo del documento:
Article
País de afiliación:
China