Abstract
Diosgenin (Di), a steroidal sapogenin derived from plants, has been shown to exert anticancer effects in preclinical studies. Using Di as a starting material, various Di derivatives were designed and synthesized, aiming to discover new steroid-based antitumor agents. In this work, we synthesized several Di derivatives and screened FZU-0021-194-P2 (P2), which showed more potent cytotoxic activities against human non-small-cell lung cancer A549 and PC9 cells. Considering that Di has a unique sterol structure similarly to cholesterol, P2 phytosomes (P2Ps) were prepared to further improve the water solubility of P2. The P2Ps exhibited a particle size of 53.6 ± 0.3 nm with oval shape and a zeta potential of −4.0 ± 0.7 mV. P2Ps could inhibit the proliferation of lung cancer cells more efficiently than Di phytosomes after 72 h of incubation time by inducing cell cycle arrest and apoptosis. The results indicated that P2Ps could be a promising anticancer formulation for non-small-cell lung cancer.
Highlights
Natural products are the most accessible source of lead compounds of anticancer drugs [1]
We investigated the cytotoxicity of these Di derivatives in different cancer cell lines and their IC50 values were calculated
P2 was characterized by 1H Nuclear magnetic resonance (NMR) (Supporting Information File 1, Figure S1), 13C NMR (Supporting Information File 1, Figure S2) and High-resolution mass spectra (HRMS)
Summary
Natural products are the most accessible source of lead compounds of anticancer drugs [1]. One of novel 22-oxo-26-selenocyanocholestanic steroids based on Di synthesized by Fernández-Herrera et al exhibited remarkable antiproliferative activity against HeLa cells, which is close to that of the clinical anticancer agent paclitaxel [14]. These successful examples demonstrated that the steroidal structure of Di is promising for the discovery of new anticancer drugs. Di and its derivatives could be substituted for cholesterol to form novel stable liposome-like phytosomes. The liposome-like phytosomes were prepared by substituting Di and its derivative for cholesterol. The anticancer effects of free drugs and their phytosomes were investigated in non-small-cell lung cancer cells
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