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Archive > Volume 10 Issue 1 > 2018,10(1):54-58. DOI:10.1016/j.chmed.2017.12.007 Prev Next

Original articles

Synthesis and Biological Evaluation of New Peroxo-bridged Diosgenin Derivatives

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    摘要:


    Abstract:
    Objective: In order to find lead compound with anti-HBV activity from peroxo-bridged diosgenin deriva- tives 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 anti-hepatitis B activity were evaluated via MTS assay and ELISA method, respectively. Results: Six diosgenin derivatives were synthesized, three of which contain peroxo-bridge, and their structures were confirmed by spectroscopy. It showed that 5 α,8 α-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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    Project Supported:
    Beijing Key Laboratory for Basic and Development Research on ChineseMedicine, (Beijing, 100102), National Science and Technology Major Projectsfor "Major New Drugs Innovation and Development (No. 2009ZX09103-356 ), andthe Innovation Team Project Foundation of Beijing University of Chinese Medicine(Lead Compound Discovering and Developing Innovation Team Project Foundation,2011-CXTD-15 ).

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