Research On The Chemical Composition And Activity Of Zhimu

Anemarrhena asphodeloides Bge.belongs to the family Liliaceae widely distributed in China.Its rhizome has been used as a folk medicine for treatment of febrile diseases with high fever and dire thirst,heat in the lung with dry cough,consumptive fever,diabetes due to internal heat and constipation in China.It has been reported that steroidal saponins were the mainly active components of Anemarrhena asphodeloides.In this thesis,51 compounds were isolated with silica gel,ODS,Sephadex LH-20 and preparation HPLC on the basis of analysis of NMR,MS data and measuring of physic-chemical characters.They were 2,4'-dihydroxy-4-methoxybenzophenone(1),2,6,4'-trihydroxy-4-methoxybenzophenone(2),anemarrhena A(3),anemarrhena B(4),trans-hinokiresinol(5),cis-hinokiresinol(6),monomethyl-cis-hinokiresinol(7),broussonin B(8),7-hydroxy-3-(4-methoxybenzyl)-chroman(9),5,7-dihydroxy-3-(4-methoxybenzyl)-chroman-4-one(10),quercetin(11),4'-methoxyl-8-isopentenyl-3-O-a-L-rhamnopyranosyl-7-O-?-D-glucopyranosyl-flavonoid(12),mangiferin(13),7-O-?-D-glucopyranosyl-mangiferin(14),chrysophanol(15),emodin(16),3,4,6,7-tetramethoxy-9,10-dihydrophenanthren-2-ol(17),N-trans-coumaroyltyramine(18),1,1'-dicyclohexylurea(19),(-)-syringaresinol(20),phenethyl-?-L-rhamnopyranosyl-(1-6)-?-D-glucopyranoside(21),coniferin(22),syringin(23),2',3'-dihydroxy propylpentadecanoate(24),tianshic acid(25),?-sitosterol(26),sarsasapogenin(27),markogenin(28),2?,3?-dihydroxy-23,24-dinor-5?-cholano-22,16-lactone(29),3-O-?-D-glucopyranosyl-(1?2)-?-D-galactopyranosyl-23,24-dinor-5?-cholano-22,16-lactone(30),15a-hydroxy-3-O-?-D-glucopyranosyl-(1?2)-?-D-galactopyranosyl-5?-pregn-16(17)-ene-20-one(31),3-O-?-D-glucopyranosyl-(1?2)-?-D-galactopyranosyl-5?-pregn-16(17)-ene-20-one(32),timosaponin AIV(33),timosaponin A?(34),5?-spirostan-25(27)-ene-3-O-?-D-glucopyranosyl-(1?2)-?-D-galactopyranoside(35),(5?,25R)-spirostan-3?,15?-diol-3-O-?-D-glucopyranosyl-(1?2)-?-D-galactopyranoside(36),anemarrhensaponin ?(37),timosaponin G(38),marcogenin-3-O-?-D-glucopyranosyl(1?2)-?-D-galactopyranoside(39),anemarrhenasaponin I(40),anemarrhenasaponin la(41),(25S)-26-O-?-D-glucopyranosyl-5?-furostan-3?,22?,26-triol(42),(25S)-26-O-?-D-glucopyranosyl-5a-furostan-3?,22?,26-triol(43),(25S)-26-O-?-D-glucopyranosyl-5(6)-ene-furostan-3?,22?,26-triol(44),(25S)-26-O-?-D-glucopyranosyl-5?-20(22)-ene-furostan-3?,26-diol(45),anemarnoside B(46),timosaponin J(47),timosaponin B I(48),timosaponin B?(49),timosaponin B?(50),anemarsaponin C(51).Among them,compounds 3,4,29,30,31,36,43 were new compounds.Alzheimer's disease(AD)is a neurodegenerative disease characterized by progressive memory loss and cognitive impairment.In this study,a bioactivity-oriented screening platform based on a modified Ellman's method and HPLC-Q-TOF-MS technique was developed to rapidly screen active agents of Anemarrhena asphodeloides.The 60%ethanol fraction from an ethyl acetate extract exhibited the most potential anti-cholinesterase activity.Fifteen steroid saponins were identified by the mass spectrum,standards and literature reports.Timosaponin A?,a major saponin found in Anemarrhena asphodeloides,exhibits a wide spectrum of bioactivities.It is believed that it may be further developed into a promising new drug.To better understand the pharmacological activities of the component,the investigation of its in vivo and in vitro metabolism was necessary.In this study,the metabolic profile of timosaponin A? was investigated using liquid chromatography-mass spectrometric techniques.Plasma,bile,urine and feces were collected from rats.A total of 19 metabolites were detected and tentatively identified based on the mass spectral fragmentation patterns,elution order or confirmed using available reference standard.Two metabolites were detected after incubating with rat liver microsomal.