Two Types Of Structural Transformation And Activity Of Natural Compounds

This thesis is composed of three parts.Part A described the structure modification and activity screening of derivatives of sapogenin of protopanaxadiol type crude saponin from Panax notoginseng.Part B described the structure modification of genipin derivatives.Part C is a review of the structure modification of PNS and their biological activities.Part A The structure modification and activity screening of dammarane triterpenoid derivatives of protopanaxadiol type crude saponin from Panax notoginsengThis part reported the reactions of Protopanaxadiol Type Crude Saponin from Panax notoginseng.The crude saponin was oxidized directly with Jones reagent and five derivatives were obtained.The derivatives were further reduced,acylated, peroxidized,halogenated and 19 compounds(H1-H19) were obtained in total. Preliminary bioassay of these products were carried out and they did not show inhibition effects against Cdc25A or Urokinase and Ovarian cancer,but some of them had antibacterial activity.Part B Studies on the synthesis of genipin derivativesThis part reported the synthesis of genipin derivatives.The methods were listed below:The reaction between genipin and ethylenediamine produced the monoterpene alkaloid-like.Mannich reaction between formaldehyde and the alkaloid-like afforded another new alkaloid-like(d).Grignard reaction between d and phenyl magnesium bromide,ethyl magnesium iodide and methyl magnesium iodide were carried out and novel alkaloid-like H20,H21 and H22 were obtained. Part C review of the structure modification of PNS and their biological activitiesThis part summarized the structure modification of PNS and biological activities of the derivatives.