Research On The Chemical Constituents And Microbial Fermentation Of Cyathula Officinalis

This dissertation described the chemical constituents of traditional Chinese medicine Cyathula officinalis and its microbial fermentation.Phytochemical research on Cyathula officinalis from Yunnan Province has enriched the chemical constituents varieties of this medicine,further confirmed the chemical basis for its anti-inflammatory and anti-tumor activities,and provide reference for the development of this medicine.Microbial fermentation is one of the important processing methods for traditional Chinese medicine,which can transform the components,increase the efficacy effectively,enhance the additional value,and improve the "secondary development" and utilization of traditional Chinese medicine.Chapter Ⅰ reviewed the research status of Cyathula officinalis and Achyranthes bidentate,include chemical constituents,pharmacological activities,and clinical application.The difference of two medicines was summarized and emphasized.Chapter Ⅱ focused on the chemical constituents of Cyathula officinalis.Twenty compounds were isolated from the ethyl acetate extraction of the methanol extract of Cyathula officinalis.Their structures were identified as succinic acid(1),scoparone(2),mokko lactone(3),α-spinosterol-3-O-β-D-glucopyranoside(4),daucosterol(5),anthrinone(6),cyasterone(7),isocyasterone(8),28-epi-cyasterone(9),24-hydroxycyasterone(10),sengosterone(11),amarasterone(12),polyporusterone A(13),β-siosterol(14),oleanolic acid(15),oleanolic acid-28-O-?-D-glucopyranoside(16),18-β-H-glycyrrthetinic-30-β-glucopyranose(17),oleanolic acid-3-O-β-D-glucuronidin(18),oleanolic acid-3-O-β-D-glucopyranose(19),oleanolic acid-3-O-β-D-glucopyranosyl methyl-28-O-β-D-glucopyranoside(20).Among them,compounds 3,4,15-18 were isolated from this plant for the first time.Chapter Ⅲ described the microbial fermentation of Cyathula officinalis on the basis of its phytochemical research.Cyathula officinalis was fermented with forty-fourdifferent plant endophytic fungi,and the fermentation results were screened by TLC.Among them,Fusarium solani solid state fermented Cyathula officinalis exhibited significant chemical difference from original plant medicine.Six compounds,eupatoric acid(1),3-oxo-oleanolic acid(2),3-oxo-olean-29-oic acid(3),methyl oleanolate(4),oleanolic acid butyl ester(5),3β,13β-dihydroxy-12,13-dihydro oleanolic acid(6)were isolated from fermented Cyathula officinalis with Fusarium solani.Compound 2 showed weak antibacterial activity against C.albicans with a MIC value of 64 μg/m L.Basing on the structures of the isolated compounds,OH-3 in triterpenoids was supposed to be converted into carbamyl by Fusarium solani fermentation.Therefore,oleanolic acid was transformed by Fusarium solani fermentation.However,compound 2 was not detected in fermentation extraction.The chemical mechanism of Fusarium solani fermentation of Cyathula officinalis to produce compounds 1-6 should be further investigated.This paper focused on the chemical constituents and fermentation of Cyathula officinalis,and could provide reference for the development of this medicine.