Details

Autor(en) / Beteiligte

• Jiang, Rongsong
• Shen, Fukui
• Zhang, Miaomiao
• Mulati, Shulipan
• Wang, Jinfeng
• Tao, Yicun
• Zhang, Weiyi

Titel

Evaluating the Anti-Melanoma Effects and Toxicity of Cinnamaldehyde Analogues

Ist Teil von

• Molecules (Basel, Switzerland), 2023-10, Vol.28 (21), p.7309

Ort / Verlag

Basel: MDPI AG

Erscheinungsjahr

2023

Quelle

EZB Free E-Journals

Beschreibungen/Notizen

• 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.