A New Synthetic Curcuminoid Displays Antitumor Activities in Metastasized Melanoma.

ABSTRACT:

Aim

The semisynthetic derivatives MePip-SF5 and isogarcinol, which are aligned with the natural products curcumin and garcinol, were tested for their antitumor effects in a preclinical model of pulmonary melanoma metastasis.

Methods and results

MePip-SF5 was almost five times more effective in inhibiting B16F10 melanoma cell proliferation than its original substance of curcumin (IC₅₀ MePip-SF5 2.8 vs. 13.8 µM). Similarly, the melanoma cytotoxicity of isogarcinol was increased by 40% compared to garcinol (IC₅₀ 3.1 vs. 2.1 µM). The in vivo toxicity of both drugs was assessed in healthy C57BL/6 mice challenged with escalating doses. Isogarcinol induced toxicity above a dose of 15 mg/kg, while MePip-SF5 showed no in vivo toxicity up to 60 mg/kg. Both drugs

SUBMITTER: Kaps L 

PROVIDER: S-EPMC10670708 | biostudies-literature | 2023 Nov

REPOSITORIES: biostudies-literature