Investigation Of The Chemical Constituents And Biological Activities Of Stellera Chamaejasme L.and Peganum Harmala L

Stellera chamaejasme L.belongs to genus Stellera of the Thymelaeaceae family.Its roots have been used as a poisonous herb in Chinese traditional medicine for a long time.It has been traditionally used as a functional medicine for waking up,detoxifying,eliminating swelling,removing inflammation,treating ulcers and helping skin regeneration.Furthermore,it also has commonly used for the treatment of oral ulcers,dermatosis and bronchial diseases caused by chronic tuberculosis bacilli.Peganum harmala belongs to the genus Peganum of Tribulaceae family.It is a perennial herb widely distributed in the areas of arid grassland and desert of Northwest China.It has been used as folk medicine with wide range of promosing functions,such as reinforcing tendons and veins,coordinating Yin and yang,and dissolving mucus to treat headache,cold,cough,memory decline and other diseases.In this thesis,we have investigated the chemical constitutents and the anticancer bioactivity of the root of Stellera chamaejasme collected at Lijiang of Yunnan province and the whole of plant of Peganum harmala collected in county of Tongwei,Gansu province.The results are summarized as following:(1)Six known compounds were isolated from the roots of Stellera chamaejasme by vernous spectroscopic techniques and their structures were elucidated based on the detailed spectroscopic analysis,including 1D,2D nuclear magnetic resonance(NMR),infrared spectroscopy,mass spectrometry and so on,along with in comparison with the literatures.They are identified as 7,7'-Oxy-dicumarin(1),chamaejasmenin B(2),methylpluviatolide(3),(+)-Guayarol(4),chamaejasmenin A(5),dibutyl phthalate(6),respectively.Among them,the compound 7,7'-Oxy-dicunarin is the first dicumarin isolated from natural resource.(2)Three alkaloids,Harmine(7),Vasicinone(8),1-(2-aminobenzyl)-3-hydroxylpyrr olidin-2-one(9)were isolated from the whole plant of Peganum harmala.And their stuctures were identified by detailed analysis of NMR data,in combined with compared with the literatures.In addition,the absolute configuration of compound 8 was further confirmed by X-ray single crystal diffraction.(3)In order to increase chemical diversity for biological screening,compounds 4 and 8 were modified by acetylation and benzoylation reactions to get three more derivatives 10-12.And their structures were further confirmed by 1H,13C NMR data.In addition,compounds 1-4,7,8,12 were selected to evaluate the anticancer bioactivity against A2780 tumor cells line throght MTT method.And compounds 2 and 4 exhibited excellent anti-proliferation activity against A2780 tumor cells with IC50 values of 9.71 ?M and 9.46 ?M,respectively.Interestingly,The anticancer activity of compound 12 was significantly increased from 57.14 ?M to 18.71 ?M after modification with p-bromobenzoyl.