Pterostilbene, a natural metabolite of resveratrol, has been indicated as a potent anticancer molecule. Recently, several pterostilbene derivatives have been reported to exhibit better anticancer activities than that of the parent pterostilbene molecule. In the present study, a series of pterostilbene derivatives were designed and synthesized by the hybridization of pterostilbene, chalcone, and cinnamic acid. The cytotoxic effect of these hybrid molecules was determined using two oral cancer cell lines, HSC-3 and OECM-1. ()-3-(2-(()-4-Hydroxystyryl)-4,6-dimethoxyphenyl)-1-(2-methoxyphenyl)prop-2-en-1-one (), with IC of 16.38 and 18.06 μM against OECM-1 and HSC-3, respectively, was selected for further anticancer mechanism studies. Results indicated that compound effectively inhibited cell proliferation and induced G2/M cell cycle arrest via modulating p21, cyclin B1, and cyclin A2. Compound ultimately induced cell apoptosis by reducing the expression of Bcl-2 and surviving. In addition, cleavage of PARP and caspase-3 were enhanced following the treatment of compound with increased dose. To conclude, a number of pterostilbene derivatives were discovered to possess potent anticancer potentials. Among them, compound was the most active, more active than the parent pterostilbene.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8401670PMC
http://dx.doi.org/10.3390/molecules26164840DOI Listing

Publication Analysis

Top Keywords

pterostilbene derivatives
12
pterostilbene
8
hybridization pterostilbene
8
potent anticancer
8
parent pterostilbene
8
enhancement anticancer
4
anticancer potential
4
potential pterostilbene
4
pterostilbene derivative
4
derivative chalcone
4

Similar Publications

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!