Abstract

Diosgenin (Di), a steroidal sapogenin derived from plants, has been shown to exert anti-cancer 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 (P2P) were prepared to further improve the water solubility of P2. P2P exhibited a particle size of 53.6 ± 0.3 nm with oval shape and a zeta potential of −4.0 ± 0.7 mV. P2P could inhibit the proliferation of lung cancer cells more efficiently than Di phytosomes with 72-h incubation time through the mechanism of inducing cell cycle arrest and apoptosis. The results indicated that P2P could be a promising anticancer formulation for non-small-cell lung cancer.

Keywords: Diosgenin; Non-small-cell lung cancer; Sterol structure; Phytosomes

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Xu, L.; Xu, D.; Li, Z.; Gao, Y.; Chen, H. Beilstein Arch. 2019, 201961. doi:10.3762/bxiv.2019.61.v1

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