Studies On Terpenoids And Their Anti-Inflammatory From Callicarpa Bodinieri

Natural products are the main source of innovative drugs,and their high potency and selectivity for specific targets make them irreplaceable in drug research.The Callicarpa genus plants have been widely used in traditional Chinese medicine to treat rheumatism,analgesia,hemoptysis,gastrointestinal bleeding,scrofula and swollen sores,all of which are associated with inflammation,so the discovery of the anti-inflammatory active molecules in them could provide some theoretical basis for the research and development of anti-inflammatory drugs.In this study,the extraction,isolation,structural identification and biological activity of diterpenoids from C.bodinieri were investigated.106 compounds were isolated from the ethanol extract of the aerial parts of the C.bodinieri by means of a variety of separation and purification techniques.Their structures were identified using modern spectroscopic techniques（NMR,MS,UV,IR,ECD,and X-ray single crystal diffraction）including 48 diterpenoids（1-48）,16 triterpenes and steroids（49-64）,24monoterpenoids,sesquiterpenoids and violetone derivatives（65-88）,and 18 other types compounds（89-106）.Diterpenoids were the focus of this thesis,and we isolated 24 clerodane type（1-24）,20 abietane type（25-44）,and four halimane type diterpenoids（45-48）,among them,26 were undescribed new compounds（1-15,25-33,46,and 48）;The anti-inflammatory activities of these diterpenoids were screened by evaluating the inhibition of NO production stimulated by LPS in RAW 264.7 macrophages cells.As a result,abietane type diterpenoids 27 and 32 showed inhibition effects with IC₅₀ values of 36.35±1.12 and 37.21±0.92μM;western blot assays showed that the abietane type diterpenoid 27 reduced the high levels of nitric oxide synthase and p65 induced by LPS compared to the control.In addition,it was reviewed the structures and sources of diterpenoids,triterpenoids,phenylethanoids,and lridoids obtained from Callicarpa in the last decade,as well as the pharmacological activities of Callicarpa spp.in this thesis.