| Illigera henryi W.W.Sm.and Illigera grandiflora W.W.Sm.et J.F.Jeff are important medicinal plants of the genus Illigera(Hernandiaceae).To the best of our knowledge,there is no research on chemical constituents of these two plants that has been reported.To explore the chemical constituents,phytochemical investigations on I.henryi and I.grandiflora were carried out.Afterwards,the tuber of I.henryi was fermented with microorganisms to improve its pharmaceutical effect and obtain more active compounds and biotransformations.Chapter I gives a summarize about the chemical constituents of the genus Illigera.Chapters IIIV describe the chemical constituents and fermentation of I.henryi and I.grandiflora.Thirteen compounds,including aporphine and amide alkaloids,ferulate and steroids were isolated from I.henryi.Illigerones A(1)and B(2)are new secobutanolides bearing long-chain.Compounds 6,7,8,9,11,12,and 13 were isolated from genus illigera for the first time.Illigerones A(1)exhibited moderate cytotoxic activites against five tumour cells,especially for SMMC-7721 cell line.In adiition,the biogenetic pathway for compounds 1 and 2 was proposed.Seven compounds including a new isoquinoline alkaloid,grandifloramine(1),and five known aporphine alkaloids were identified from I.grandiflora.This is the first to report the chemical constituents of I.henryi and I.grandiflora.The results revealed that aporphine alkaloids were the major component in both medicinal plants,and the content of(S)-actinodaphnine is more than half of total chemical constituents.Microbial fermentation is an efficiency method which could improve the efficacy of traditional Chinese medicine.On the basis of the above results,several fungi were used to ferment I.henryi.The acetylcholinesterase(AChE)inhibitory activity of I.henryi was improved after fermented by Clonostachys rogersoniana.A interesting biotransformation was found to be responsible for the improved bioactivity.(S)-actinodaphnine(1)was converted to a new 4-hydroxy-aporphine alkaloid(4R,6aS)-4-hydroxyactinodaphnine(2)which possessed a stronger AChE inhibitory activity with an IC50 value of 17.66±0.66μM.The optimated experiment showed fermentation for 30 days in the ambient tempreture could transform 1 into 2 completely.This paper indicates that C.rogersoniana fermentation might be a potential processing method for I.henryi.This is the first report of I.henryi fermentation with pure strain,which is meaningful for further development of I.henryi.This paper gives a research on the components of I.henryi and I.grandiflora which belong to the genus Illigera(Hernandiaceae),also the fermentation modification on I.henryi by microorganism.These will serve as a theoretical underpinning for the development and utilization of I.henryi and I.grandiflora. |