Extraction, Isolation And Modification Of Main Anthraquinone In Polygonum Cuspidatum And Studies On Their Biological Activities

Polyonum cuspidatum Sieb.et Zucc is an important wild plant resource and also a traditional Chinese medicinal material. It contained some medicinal worthily ingredients. The main compounds isolated from the dry roots involved Anthraquinone, stilbene, flavonoids, Phenols etc. The natural anthraquinones which were effecitive composition of Chinese traditional medicine exhibited anti-inflammatory, antitumor and antimicrobial activities. In this thesis studies on isolation and modification of the anthraquinones from Polyonum cuspidatum Sieb.et Zucc were shown. A series of new anthraquinones were synthesized and biological activity of natural and synthetic anthraquinones were investigated. The main results are as follows:1.The recent study of pharmacologic action and clinical application in Polyonum cuspidatum Sieb. et Zucc were overview.2.The base stepwise method for extraction and separation of main anthraquinones in Polyonum cuspidatum Sieb.et Zucc was improved. Three natural anthraquinones were isolated and their structures were identified on the analysis of IR, MS, ~1H NMR and standard samples.3.The best procedure for the total Anthraquinones by the ultrasonic radiation extracting method and HPLC analytic method of main anthraquinones in Polyonum cuspidatum Sieb.et Zucc were set up.4. For the first time, amino groups were connected to 8-position of emodin and four anthraquinone derivatives were synthesized; Their structures were determined by IR, MS, ~1H NMR spectra.5. UV-Vis absorption spectra and fluorescence emission spectra of some natural and synthetic anthraquinones intercalated into DNA were investigated. These compounds exhibited hypochromic effects, bathochromic effects and isosbestic points characterized as intercalating with DNA in UV-Vis absorption spectra for titration of DNA, and showed quenching effect in fluorescence emission spectra for titration of DNA.By compared their intrinsic binding constants and quenching constants, theantitumor activity of these anthraquinones were correlated with their intrinsic binding constants and quenching constants.6. human cancer cell lines Caco-2 were cultivated and the best growth curve was set up,The cytotoxicity of isolated and synthetic anthraquinones were tested by method of MTT and SRB. Emodin had a little cytotoxicity activity; Some of 8-position substituted anthraquinone derivatives had a little cytotoxicity than emodin.