Synthesis and biological evaluation of new peroxo-bridged diosgenin derivatives / 中草药·英文版
Chinese Herbal Medicines
; (4): 54-58, 2018.
Article
de Zh
| WPRIM
| ID: wpr-842160
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WPRO
ABSTRACT
Objective: In order to find lead compound with anti-HBV activity from peroxo-bridged diosgenin derivatives obtained with Eosin Y as the photosensitizer. Method: Eosin Y was used as the photosensitizer to activate the oxygen in the air to synthesize novel diosgenin derivatives with peroxo-bridge. The structures of synthesized compounds were identified by NMR and HR-MS. Their cytotoxicity and antihepatitis B activity were evaluated via MTS assay and ELISA method, respectively. Results: Six diosgenin derivatives were synthesized, three of which contained peroxo-bridge, and their structures were confirmed by spectroscopy. It showed that 5α,8α-peroxo-6-alkenyl-diosgenin (7) could suppress the production of HBsAg on transfected HepG2.2.15 cells at low-toxic concentration and the inhibition rate on HepG2.2.15 cells was 18.28% at 12.50 µg/mL, better than that of 3TC (7.30% at 12.50 µg/mL) and others. Conclusion: Due to its lower cytotoxicity and potential anti-hepatitis B activity, compound 7 could be developed as the promising candidate of anti-hepatitis B drug. It also indicated that the peroxo-bridged derivatives had potential biological values for developing clinical agents.
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WPRIM
langue:
Zh
Texte intégral:
Chinese Herbal Medicines
Année:
2018
Type:
Article