ABSTRACT
In this study, fourteen celastrol derivatives (1-14) were synthesised by esterification of celastrol at the 29th position. The in vitro anticancer activity of them was determined by the MTT assay. All the synthetic compounds showed significant antiproliferative activity against six cancer cells, with IC50 of the submicron molar level. The most promising compound (2) blocked the cell cycle in the G2 phase and inhibited the expression of VEGF and MMP-9 in gastric cancer cell line MGC-803. In flow cytometry analysis, compound 2 induced cancer cell apoptosis in a dose-dependent manner. In the mouse tumour xenograft model, compound 2 showed significant anti-tumour activity in vivo at the dosage of 2.5 mg/kg and 1 mg/kg, with a higher inhibition rate than 5-FU (10 mg/kg). What's more, the anticancer mechanism involved in the inhibition of VEGF and the toxicity evaluation of compound 2 were also investigated.
Subject(s)
Antineoplastic Agents , Triterpenes , Humans , Animals , Mice , Triterpenes/pharmacology , Vascular Endothelial Growth Factor A , Antineoplastic Agents/pharmacology , Cell Line, Tumor , Cell Proliferation , Apoptosis , Drug Screening Assays, AntitumorABSTRACT
Luminescent Cu@Cu2S nanozymes have been prepared by a one-pot method, displaying high peroxidase-like and oxidase-like activity. Fluorescence images show that these nanozymes adhere to the surface of the bacterial cell and scanning electron microscopy reveals that the nanomaterials cause folding and collapse of the bacterial surface, resulting in bacterial death.
