Study On The Chemical Constituents Of The Aerial Parts Of Uncaria Chinensis. Study On The Cassane-type Diterpenoid Constituents Of Gemugen

The chemical constituents and biological activities of the aerial parts of Cryptolepis buchananii and the roots of Erythrophleum fordii were systematically studied in the thesis.Cryptolepis buchananii Roem.et Schhult.is a plant of the genus Cryotoleois in Asclepiadaceae family,mainly distributed in Guangdong,Guangxi,Yunnan and other provinces in China,as well as India,Myanmar,Sri Lanka,Vietnam and other countries abroad.C.buchananii has the functions of activating collaterals,detumescence and relieving pain,detoxification,and mainly used in the folk and clinical treatment of pain,bruises,cataclasis,carbuncle,cancer,asthma and rheumarthritis.C.buchananii is of the high medical value and curative effect,but little is known about their bioactive substances.Guided by bioactivities,the chemical constituents of the aboveground parts of C.buchananii was systematically studied in the thesis.In the present study,the crude extract of C.buchananii was evaluated for its biological activities on several biological targets that were selected based on the medical usage of this plant and the activities of the constituents from the same family and genus.In the preliminary assays,the CH2Cl2 and the EtOAc extract showed potent cytotoxic effect and anti-inflammatory effect.By using various chromatographic techniques and spectroscopic methods,54 compounds were isolated and identified from these two extracts.These compounds were classified according to their structural features,including 9 cardiac glycosides(1-9),9 C21 steroids(10-18),4 terpenoids compounds(19-22),19 lignans(23-41)and 13 other compounds(42-54).Among them,4 compounds were isolated and identified as new compounds,including two C21 steroids(16*,18*),two megastigmane-type compounds(19*,20*).The isolated compounds were evaluated for their cytotoxic,anti-inflammatory,analgesic,hepatoprotective effects.The results show that the cardiac glycosides 1,2 and 5-8,C21 steroid 17 have strong cytotoxic activity to a variety of tumor cells,IC50 values ranging from 0.004 to 8.101 ?M.C21 steroid 17 showed inhibition activity against NO production with an inhibition rate of 89.27%at a concentration of 10 ?M.C21 steroids 10-12,14-15 and compounds 21,22 exhibited hepatoprotective effect against APAP injured HepG2 cell,compared to the positive control.Erythrophleum fordii Oliver is a plant of the genus of Erythrophleum in Leguminosae family,widely distributed throughout China,Vietnam.As a traditional Chinese medicine,E.fordii has the main action of "invigoration and promoting blood circulation".Previous(?)rich source of sassaine ditemenoid.ester amines and amides.Cassane-type diterpenoids exhibit a wide range of pharmacological activities such as anti-tumor,anti-malarial,anti-inflammatory,immunomodulatory,antimicrobial and anti-viral.In this assay,detailed phytochemical investigation of the roots of E.fordii furnished seven undescribed cassane-type diterpenoids(1*-7*),together with two known diterpenoids(8,9)from the 95%EtOH extractThe antiviral activities of these compounds were evaluated.Among them,compounds 8 and 9 showed antiviral activities against influenza virus and coxsackie virus with IC50 values ranging from 11.11 to 33.33 ?MIn summary,the chemical constituents of the aerial parts of Cryptolepis buchananii and the cassane diterpenes of the roots of Erythrophleum fordii were systematically studied in this paper,which results in the isolation of 63 compounds,thus enriching their structural diversity and novelty.The structural characteristics of the secondary metabolites of these two plants were preliminarily clarified.In addition,several compounds were found to have cytotoxic,hepatoprotective,antiviral and anti-inflammatory effects,which provided a basis for the folk medicine of the target plants and also provided a reference for the research of related diseases.