Semi-Synthesis and In Vitro Anti-Cancer Evaluation of Magnolol Derivatives.
Molecules
; 26(14)2021 Jul 15.
Article
de En
| MEDLINE
| ID: mdl-34299577
ABSTRACT
Magnolol (MAG), a biphenolic neolignan, has various biological activities including antitumor effects. In this study, 15 MAG derivatives were semi-synthesized and evaluated for their in vitro anticancer activities. From these derivatives, compound 6a exhibited the best cytotoxic activity against four human cancer cell lines, with IC50 values ranging from 20.43 to 28.27 µM. Wound-healing and transwell assays showed that compound 6a significantly inhibited the migration and invasion of MDA-MB-231 cells. In addition, Western blotting experiments, performed using various concentrations of 6a, demonstrated that it downregulates the expression of HIF-1α, MMP-2, and MMP-9 in a concentration-dependent manner. Overall, these results suggest that substituting a benzyl group having F atoms substituted at the C2 position on MAG is a viable strategy for the structural optimization of MAG derivatives as anticancer agents.
Mots clés
Texte intégral:
1
Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Dérivés du biphényle
/
Lignanes
/
Antinéoplasiques
Limites:
Female
/
Humans
Langue:
En
Journal:
Molecules
Sujet du journal:
BIOLOGIA
Année:
2021
Type de document:
Article
Pays d'affiliation:
Chine