KOR

e-Article

Evaluating the Anti-Melanoma Effects and Toxicity of Cinnamaldehyde Analogues.
Document Type
Article
Source
Molecules. Nov2023, Vol. 28 Issue 21, p7309. 16p.
Subject
*ACUTE toxicity testing
*DRUG bioavailability
*DRUG accessibility
*LEAD compounds
*TOXICITY testing
Language
ISSN
1420-3049
Abstract
Cinnamaldehyde (CA) showed potent activity against melanoma in our previous study, and the structure of unsaturated aldehydes is envisaged to play a role. Nevertheless, its limited drug availability restricts its clinical application. Therefore, a series of CA analogues were synthesized to evaluate their anti-melanoma activities across various melanoma cell lines. These compounds were also tested for their toxicity against the different normal cell lines. The compound with the most potential, CAD-14, exhibited potent activity against the A375, A875 and SK-MEL-1 cells, with IC50 values of 0.58, 0.65, and 0.82 µM, respectively. A preliminary molecular mechanism study of CAD-14 indicated that it could inhibit the p38 pathway to induce apoptosis, and suppress tumor growth by inhibiting the expression of ENO1. Furthermore, an acute toxicity study depicted that CAD-14 has better safety and tolerability than CA in vivo. These findings indicate that CAD-14 might be a lead compound for exploring effective anti-melanoma drugs. [ABSTRACT FROM AUTHOR]