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 ...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 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 5a,8a-peroxo-6-alkenyl-diosgenin （7） could suppress the production of HBsAg on transfected HepG2.2.15 cells at low-toxic concentration and the in- hibition 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.展开更多
基金Beijing Key Laboratory for Basic and Development Research on Chinese Medicine,(Beijing,100102)National Science and Technology Major Projects for "Major New Drugs Innovation and Development (No.2009ZX09103-356)the Innovation Team Project Foundation of Beijing University of Chinese Medicine (Lead Compound Discovering and Developing Innovation Team Project Foundation,2011-CXTD-15)
文摘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 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 5a,8a-peroxo-6-alkenyl-diosgenin （7） could suppress the production of HBsAg on transfected HepG2.2.15 cells at low-toxic concentration and the in- hibition 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.
