Studies On The Chemical Constituents And Their Bioactivities Of Three Compositae And One Leguminosae Species

The Ligularia is one of the genus of the tribe Senecioneae in the family Compositae and perennial herbs. More than 100 species are widely distributed in northwestern, southeastern, and northeastern areas of China, of which more than 20 species have been used as traditional Chinese medicinal herbs. Their roots, stems, leaves and flowers possess efficacy of antipyretic, relieving phlegm and relieving cough, invigorating the circulation of blood and soothing pain.The Senecio is one of the genus of the tribe Senecioneae in the family Compositae and perennial herbs. There are about 1500 species in the genus Senecio widely distributed throughout the world, which contains herbs, shrubs, vines and trees. More than 200 species grow in China, mainly distributed in the Shan'xi province, Gansu province, and Qinghai province of China. Their roots, stems, leaves and flowers have long been used for folk medicines in China, and possess efficacy of antipyretic, antitoxin, antihelmintic, antimicrobic, antitreponemal, anti-inflammatory, and antioncotic.The Sophora is one of the genus of the subfamily Faboideae in the family Leguminosae and contains perennial herbs, arbors and shrubs. The species of the genus Sophora are mainly distributed in temperate and semitropical zone, and more than 30 species distributed in China.The chemical constituents and their bioactivities of three Compositae and one Leguminosae species were studied in this thesis. The chemical constituents were isolated by means of silica gel column chromatography (CC), preparative thin layer chromatography (PTLC), and recrystallization etc. The structures of these compounds were elucidated by spectroscopic methods, including IR, UV, CD, EI-MS, FAB-MS, HR-ESI-MS, ¹H-NMR, ¹³C-NMR, DEPT, NOED, ¹H-¹H COSY, HSQC, HMBC, and single-crystal X-ray crystallography. From Ligularia lapathifolia (Franch.) Hand.-Mazz., 26 compounds were isolated, 8 of them are new eremophilane-type sesquiterpene derivatives. From Ligularia odontomanes Hand.-Mazz., 21 compounds were isolated, of which 2 are new including one novel benzofuran derivative and one new olean-type triterpene. From Senecio nemorensis L., 21 compounds were isolated, and 3 eremophilane-type sesquiterpenes are new. From Sophora mollis (Royle) Baker, 10 compounds were isolated.Furthermore the bioactivities of some sesquiterpenes were studied, using MTT method to evaluate their cytotoxic activity against selected cancer cell lines including human stomach carcinoma (MGC-803), human hepatoma (HEP-G2), and murine sarcoma (S-180) cell lines, and using microdilution assay to test their antimicronial activities against Staphylococcus aureus, and Candida albicans. Compound L14 exhibited moderate activity against HEP-G2 cell lines (IC₅₀ = 12.66μM), and compound L16 showed moderate activity against S-180 cell lines (IC₅₀= 19.87μM). All tested compounds did not show significant antimicrobial activities (MIC > 50.0μg/mL).The results would be a supplement for the research on bioactivity of chemical constituents in traditional Chinese medicine, helpful reference for pharmacology, chemotaxonomy and screening new medicines, and may benefit utilizing and developing the natural resources of our country.Finally, the chemical constituents and their activities of the species of the genus Senecio reported in 1993-2007 were reviewed in this thesis.