Ralationships Between Structure And Antibacterial And Acaricidal Activity Of Sanguinarine And Chelerythrine

Natural products are important sources of drug development. Alkaloids are important natural products researched most early, most of which possess biologic activity, and have extensive intensive physiological activity to people, animal and agricultural pests. The active field in the natural products research and exploiture is mainly about using the monomer compound which has good activity as the template and study on systemic structure rebuild and modification, and its structure-activity relationship (SAR). Sanguinarine and chelerythrine are chosen as parent compounds to modify. Meanwhile, the SARs with antibacterial and acaricidal activities are preliminary investigated by determinating and evaluating antibacterial and acaricidal activities. The main works are shown as follows:1. Compared antibacterial and acaricidal activities of the different total alkaloids from Macleaya microcarpa dealt with different solvents.2. Separation of sanguinarine and chelerythrine, synthesis of their analogues and determination antibacterial and acaricidal activities of all compounds.Sanguinarine and chelerythrine, benzo[c]phenanthridines alkaloids, mainly present in Macleaya microcarpa. Two alkaloids possess particular structure rare in nature, existing C=N+ ionic double-bond, showed various biological activities and drawn wide attention. In literature, the two alkaloids had antibacterial activity and the total alkaloids from Macleaya microcarpa had acaricidal activity. Here, a series of substituted analogues of the two alkaloids have been synthesized, based on the modification of the C=N+ positions. All compounds have been determinated by NMR data. The antibacterial activity is assayed by drug sensitive slips method in vitro against Staphylococcus aureas, Escherichia coli, AeromonasPunctat fintestinalis, Aeromonas hydrophila, Pasteurella multocida, Vibrio anguillarum, Vibrio harveyi and Aeromonas salmonicida. The acaricidal activity is tested in laboratory using slide-slip method against Penthaleus maJor. Then the SARs of antibacterial and acariciral activities are analysed. The results show not all compound possess the antibacterial activity. The structure difference of sanguinarine and chelerythrine induces different antibacterial activity against sensitive bacteria. Sanguinarine, chelerythrine and their derivative of antibacterial activity are different. It is concluded that C=N+ ionic double-bond is the active position. All compounds not represent the acaricidal activity (morality con.> 1000 mg·L-1).