Antifungal And Acaricidal Activities Of Sanguinarine And Chelerythrine And Their Direviatives

Sanguinarine and chelerythrine belong to the Quaternary benzo[c]phenanthridine alkaloids(QBAs), which exhibit distinct activities, such as cytotoxic, antiviral, and antimicrobial activities. Antifungal experiment and the acaricidal activity analysis were conducted, and the structure-activity relationship (SAR) of sanguinarine and chelerythrine was elaborated .1. A new method was found to separate sanguinarine and chelerythrine from Macleaya microcarpa.,which is high effective and convenient.2. A series of substituted analogues of the two alkaloids have been synthesized, based on the modification of the C=N+ positions. The structures of the compounds were confirmed by 1H NMR, 13C NMR and ESI MS.3. We choosed Curvularia lunata, Valsa mali, Fusarium solani, Fusarium oxysporium, Fusarium oxysporum, Alternaria brassicae, Blast Fungus, Alternario solani,Clanerela cinyulate, Alternaria longipes, Fusarium bulbigenum, as tested phytopathogenic fungi; The antifungal activity was tested by growth rate method. Anfungi virulence test showed that EC50 of 6-methoxydihydrochelerythrine to seven phytopathogenic fungi were 16.22～50.12μg/ml.4. We conducted the acaricidal activity analysis. Psoroptes (P.communis cuniculi), isolated from rabbits, was used to evaluate the acaricidal activity of target molecules. And acaricidal virulence test showed that LC50 and LT50 of 6-methoxydihydrosanguinarine was 0.377 mg/ml, and 6.53 h respectively.5. The SAR results showed sanguinarine, chelerythrine and their derivative of antifungal and acaricidal activity are different, It is concluded that C=N+ ionic double-bond is the active position. The structure difference of sanguinarine and chelerythrine induced different antifungal and acaricidal activities, which shows the 7 and 8 positions of the sanguinarine and chelerythrine mybe is the sensitive position.These results provided some theoretical basis for futher knowing about the modification and structure-acaricidal activity of the sanguinarine and chelerythrine. Pseudoalcoholate of sanguinarine and chelerythrine can be used as antifungal and acaricidal prodrugs.