Synthesis Of W₃, Active Component Of Wugong Sanqi And Its Anti-tumor Activity

This dissertation is divided into two parts. The first part is the synthesis research of W3, active component of Wugong Sanqi. The second part is about W3's anti-tumor activity.Wugong Sanqi is from rhizome of Anemone flaccida Fr.Schmidt which is efficient at treating rheumatic ache, traumatic injury. We can resolve resources shortage by means of chemosynthesis. In contrast with the way of separating W3 from original plants, chemosynthesis has more advantages such as simpler method, lower cost, shorter time, higher efficiency and suited to commercial process. W3 can be synthesized by five reported compounds in a convergence process. The purity of finally product is up to 90%.A great number of research has confirmed that the Anemone flaccida Fr.Schmidt revealed excellent activity in anti-tumor. This thesis utilized sapoin of Wugong Sanqi, purified saponin of Wugong Sanqi, oleanolic acid to respectively act on cells Hep3B, cells HEL and studied their anti-tumor activity in vitro. In this experiment, drugs were divided into six groups, total saponins of Wugong Sanqi group, W3 group, oleanolic acid group, positive drug control group, DMSO group, blank control group. The inhibition rates of the cell growth of cells Hep3B and cells HEL determined by using MTT assays. After 48 hours, observed morphological changes of these cells and cell cycle distribution and apoptosis rate was analyzed with flow cytometry. Ultrastructural of cells were observed by transmission electron microscope. SPPS15.0 software was used for statistical analysis.Conclusions are obtained as follows:1. In this paper the method of chemosynthesis we have adopted is effective and feasible.2. Inhibition of cells Hep3B with W3 and total saponins of Wugong Sanqi are well-matched in strength. Their inhibitory effect is greater than oleanolic acid. No inhibition of cells HEL with all three.3. Morphological Changes(light and electron microscope):W3 moderate dosage group has the best effect to kill cells Hep3B, the next is the total saponins of Wugong Sanqi, then the third is oleanolic acid.4. The results shows that the action mechanism of W3 is mainly about killing cells Hep3B and inducing cells apoptosis. The total saponins of Wugong Sanqi is mainly about inducing cells apoptosis and the oleanolic acid is mainly about killing cells. W3 has the best anti-tumor activity.