Studies On The Stilbenes Of Bletilla Striata And Their Cytotoxicities Against A549 Human Lung Cancer Cell Line

The dried fibrous roots of Bletilla striata (Thunb.) Rchb.f., a kind of precious traditional Chinese medicine, for its convergence function, hemostasis, detumescence and promoting granulation, have always been used to treat various kinds of bleeding such as lung injury hemoptysis, nose bleeding and wound bleeding. With the development of Chinese industry and environmental pollution, the lung cancer, pulmonary tuberculosis, bronchitis and other pulmonary diseases are increasing. Bletilla striata is the famous Chinese medicine to cure blood diseases, and the first choice to treat many kinds of lung diseases in TCM clinics. However, the basis of the Bletilla striata and the active substance is not yet very clear, which hinders the development and application in modern clinics. In order to further explore the pharmacodynamic material basis of Bletilla striata, the activity of anti lung cancer A549 cells was oriented, to search the abundant bibenzyls and phenanthrenes which may have potential anti lung cancer activity.By using various kinds of chromatographic techniques and spectroscopic methods such as silica gel, Sephadex LH-20, polyamide, PTLC, semi-preparative HPLC, a total of 55 compounds were isolated and identified, including 39 stilbenes. Among the stilbenes,19 bibenzyls (1*-10*,19-27) and 20 phenanthrenes (11*-16*. 28-41) were included. Besides, a new macrolides (17*), a new man-made chlorine containing steroidal (18*), six C-31 and C-32 cycloartane triterpenoids (42-47), two anthraquinones (48,49), a small molecule peptide (50) and five small molecule aromatics (51-55) were isolated, and totally 18 new compounds (1*-18*). Their names and structures see table 1, figure 1 and figure 2.In this thesis, the antitumor effect of the bibenzyls and phenanthrenes from Bletilla striaia were investigated on the non small cell lung cancer cell line A549 by the method of MTT, and the relationship between the structure and the inhibitory activity against A549 cell proliferation of bibenzyls and phenanthrenes was discussed. The results showed that the compounds 1*-7*,9*,13*,16*,23-27,30,35-41 generally had a significant inhibitory effect on the proliferation of A549 cells, with ICso during 2.35-34.41 ?M. Further structure activity relationship analysis revealed that:(1) The activity of the phenanthrenes were stronger, when more hydroxyl groups were introduced on the benzene rings. (2) The activity of biphenanthrenes were better than phenanthrenes. (3) The activity enhanced when introducing the p-hydroxybenzyl group on the phenanthrene structures. (4) The introduction of hydroxyl group on the simple bibenzyls showed a tendency to increase the activity. (5) The more hydroxyl benzyl group introduced on the bibenzyl parent nucleus, the better of the activity. (6) The greater the degree of polymerization of benzyl, the better of the activity.Besides, this paper reviewed the genus Bletilla about agrostology, the isolated compounds of bibenzyls and phenanthrenes, and the mechanism of anti lung cancer cells of stilbenes (including bibenzyls, phenanthrenes and diphenylethenes), in order to provide a reference for the further study of Bletilla striata.