Synthesis and potent cytotoxic activity of a novel diosgenin derivative and its phytosomes against lung cancer cells
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 sev...
| Main Authors: | , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Beilstein-Institut
2019-09-01
|
| Series: | Beilstein Journal of Nanotechnology |
| Subjects: | |
| Online Access: | https://doi.org/10.3762/bjnano.10.189 |
| _version_ | 1828836025797967872 |
|---|---|
| author | Liang Xu Dekang Xu Ziying Li Yu Gao Haijun Chen |
| author_facet | Liang Xu Dekang Xu Ziying Li Yu Gao Haijun Chen |
| author_sort | Liang Xu |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-12-12T18:14:27Z |
| format | Article |
| id | doaj.art-0f17352923b048898f1bd1c86bafb14a |
| institution | Directory Open Access Journal |
| issn | 2190-4286 |
| language | English |
| last_indexed | 2024-12-12T18:14:27Z |
| publishDate | 2019-09-01 |
| publisher | Beilstein-Institut |
| record_format | Article |
| series | Beilstein Journal of Nanotechnology |
| spelling | doaj.art-0f17352923b048898f1bd1c86bafb14a2022-12-22T00:16:17ZengBeilstein-InstitutBeilstein Journal of Nanotechnology2190-42862019-09-011011933194210.3762/bjnano.10.1892190-4286-10-189Synthesis and potent cytotoxic activity of a novel diosgenin derivative and its phytosomes against lung cancer cellsLiang Xu0Dekang Xu1Ziying Li2Yu Gao3Haijun Chen4Cancer Metastasis Alert and Prevention Center, College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, ChinaCancer Metastasis Alert and Prevention Center, College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, ChinaCancer Metastasis Alert and Prevention Center, College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, ChinaCancer Metastasis Alert and Prevention Center, College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, ChinaCancer Metastasis Alert and Prevention Center, College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, ChinaDiosgenin (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.https://doi.org/10.3762/bjnano.10.189diosgeninnon-small-cell lung cancerphytosomessterol structure |
| spellingShingle | Liang Xu Dekang Xu Ziying Li Yu Gao Haijun Chen Synthesis and potent cytotoxic activity of a novel diosgenin derivative and its phytosomes against lung cancer cells Beilstein Journal of Nanotechnology diosgenin non-small-cell lung cancer phytosomes sterol structure |
| title | Synthesis and potent cytotoxic activity of a novel diosgenin derivative and its phytosomes against lung cancer cells |
| title_full | Synthesis and potent cytotoxic activity of a novel diosgenin derivative and its phytosomes against lung cancer cells |
| title_fullStr | Synthesis and potent cytotoxic activity of a novel diosgenin derivative and its phytosomes against lung cancer cells |
| title_full_unstemmed | Synthesis and potent cytotoxic activity of a novel diosgenin derivative and its phytosomes against lung cancer cells |
| title_short | Synthesis and potent cytotoxic activity of a novel diosgenin derivative and its phytosomes against lung cancer cells |
| title_sort | synthesis and potent cytotoxic activity of a novel diosgenin derivative and its phytosomes against lung cancer cells |
| topic | diosgenin non-small-cell lung cancer phytosomes sterol structure |
| url | https://doi.org/10.3762/bjnano.10.189 |
| work_keys_str_mv | AT liangxu synthesisandpotentcytotoxicactivityofanoveldiosgeninderivativeanditsphytosomesagainstlungcancercells AT dekangxu synthesisandpotentcytotoxicactivityofanoveldiosgeninderivativeanditsphytosomesagainstlungcancercells AT ziyingli synthesisandpotentcytotoxicactivityofanoveldiosgeninderivativeanditsphytosomesagainstlungcancercells AT yugao synthesisandpotentcytotoxicactivityofanoveldiosgeninderivativeanditsphytosomesagainstlungcancercells AT haijunchen synthesisandpotentcytotoxicactivityofanoveldiosgeninderivativeanditsphytosomesagainstlungcancercells |