Study On The Constitutes From Fritillaria Walujewii And Their Cholinesterase Activity Inhibitory

Fritillaria walujewii Regel is dry bulb of Fritillaria,with relieving cough and phlegm,reducing blood pressure and anti-ulcer function.it is one of the commonly used traditional Chinese medicine.Fritillaria species has a rich source of steroidal alkaloids.The steroidal alkaloids from Fritillaria can be classified into two groups based on the carbon framework: isosteroidal alkaloids and steroidal alkaloids.This topic purifies the chemical constituents of Fritillaria walujewii Regel with modern chromatographic techniques separates,finally got 10 compounds,respectively Walujewine A(1),Walujewine B(2),Walujewine C(3),Walujewine D(4),tortifoline(5),Ebeiedine(6),Peimisine(7),?-sitosterol(8),Glucose(9),Daucosterol(10).The compounds(1)and(7)are attributable to two jervine-type alkaloids and compounds(1)-(4)are the new compounds.Inhibitory activities on AChE and BChE were determined for isosteroidal alkaloids(1)-(5)?(7)and some of the known compounds isolated from F.walujewii using the methods of improved Ellman founding that jervine-type alkaloids are optimal for the inhibition of AChE.The kinetics of inhibition indicated that compounds(1)-(3),and(5)caused a mixed type of inhibition.The molecular docking calculations implied the interactions between the most selective compound(1)and most active compound(5),and the target of interest(AChE),indicated that they both can inhibit AChE by binding at two different loci,the CAS site and the PAS site.The study lay a favorable foundation for the design and development of novel pleiotropic ChE inhibitors,namely,inhibitors of AChE and BChE,inhibitors of CAS and PAS.