Synthesis and potent cytotoxic activity of diosgenin derivative FZU-0021-194-P2 and its phytosomes against non-small-cell lung cancer cells

  1. Liang Xu,
  2. Dekang Xu,
  3. Ziying Li,
  4. Yu Gao ORCID Logo and
  5. Haijun Chen

Submitting author affiliation: Fuzhou University, Fuzhou, China

Beilstein Arch. 2019, 201961. doi:10.3762/bxiv.2019.61.v1

Published 08 Jul 2019

  • Preprint

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

How to Cite

When a peer-reviewed version of this preprint is available in the Beilstein Journals, this information will be updated in the information box above. If no peer-reviewed version is available, please cite this preprint using the following information:

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

Download Citation
Download RIS (Reference Manager) Download BIB (BIBTEX)

© 2019 Xu et al.; licensee Beilstein-Institut.
This is an Open Access article under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0). Please note that the reuse, redistribution and reproduction in particular requires that the authors and source are credited.
The license is subject to the Beilstein Archives terms and conditions: (https://www.beilstein-archives.org/xiv/terms)

Other Beilstein-Institut Open Science Activities

Logo
Logo
Logo
Symposia