Studies On The Diterpene Alkaloids From Aconitum Kongboense Lauener And Their Biological Activities

Aconitum kongboense Lauener belongs to the genus Aconitum of Rannculaceae,which has the effect of dispelling wind,dehumidifying and relieving pain.In Tibet,the roots of Aconitum kongboense Lauener are processed with wine to treat injuries and insect bites.In order to search for structurally unique and promisingly bioactive diterpenoid alkaloids,the diterpenoid alkaloids of the roots of Aconitum kongboense Lauener were studied systematically in this thesis.Various methods including solvent extraction,acid extraction and alkali precipitation were used to gain the crude alkaloids.The compounds were isolated and purified from the crude alkaloids by various column chromatography methods（silica gel,reverse phase silica gel and alkaline Al₂O₃）.Their structures were elucidated by extensive spectroscopic methods（HR-ESI-MS,IR,and NMR）.Twenty-seven diterpenoid alkaloids were obtained from the roots of Aconitum kongboense Lauener,including a new aconitine-type C₁₉-diterpenoid alkaloid,named as kongboensenine（1）,together with twenty-six known ones（2-26）.Their structures were determined as acotarine F（2）,acotarine G（3）,14-acetyltalatisamine（4）,talatisamine（5）,indaconitine（6）,yunaconitine（7）,chasmanine（8）,6-epi-foresticine（9）,homochasmanine（10）,8-deacetyl-yunaconitine（11）,chasmaconitine（12）,pseudaconine（13）,franchetine（14）,ezochasmanine（15）,crassicautine（16）,14-O-deacylcrassicausine（17）,genicunin A（18）,falconeridine（19）,sachaconitine（20）,liljestrandisine（21）,8-methyl-14-acetyltalatisamine（22）,kongboendine（23）,14-benzoylchasmanine（24）,ajaconine（25）,piepunin（26）and bulleyanine B（27）.The known compounds included twenty-one aconitine-type C₁₉-diterpenoid alkaloids,two7,17-seco-type C₁₉-diterpenoid alkaloids,one atisine-type C₂₀-diterpenoid alkaloid and two bis-C₂₀-diterpenoid alkaloids.Compounds 2-4,10,15-19,21-22 and 25-27 were isolated from this plant for the first time.The acetylcholinesterase inhibitory activity of the compounds（1-27）was investigated,and the results showed that none of them showed inhibitory activity on acetylcholinesterase.The anti-inflammatory activity against LPS-induced inflammation in RAW264.7 cells of compounds（1-27）was tested,and compound 14 showed weak anti-inflammatory activity with the IC₅₀ value of 45.85±1.95μM.