Studies On The Chemical Constituents Of Fissistigma Retusum (Lev.) Rehd

Fissistigma retusum belogs to the Fissistigma genus of Annonaceae family.Which is a common medicinal material of Zhuang nationality,also known as Niu erfeng.Its stems and roots are used to treat diseases such as Rheumatoid Arthritis and poliomyelitis.Alzheimer’s disease（AD）is a neurodegen erative disorder,it affects the quality of life of an increasing number of elderly people all around the world.Two major hypotheses have been proposed regarding the molecular mechanism of pathogenesis:the cholinergic hypothesis and the amyloid cascade hypothesis.In order to explore the basic drug effect and medicinal activity characteristics of the phyllophylla sinensis on Alzheimer’s disease,the chemical constituents of the root of the Fissistigma retusum purified and identified in this paper.Finally,22 compounds were obtained,they are:Fissiretine（1）,Corytuberine（2）,N-methylasimilobine（3）,Romerine（4）,（-）-Anonaine（5）,（-）-Stesakine（6）,Liriodenine（7）,Oxocrebanine（8）,Lysicamine（9）,Annonbraine（10）,（+）-Reticuline（11）,Dehydrodiscretamine（12）,（-）-Spinosine（13）,（-）-Discretamine（14）,（-）-Coreximine（15）,Adenosine（16）,N-cis-feruloyltyramine（17）,N-trans-feruloyltyramine（18）,Myo-inositol（19）,Propanoic acid（20）,β-sitosterol（21）,Daucosterol（22）.Fissiretine（1）are new natural compound.Compounds（2）、（3）、（6）、（10）、（11）、（13）、（15）are isolated from Fissistigma genus for the first time,compounds（4）、（8）、（12）、（14）、（16）、（17）、（19）and（20）are isolated from Fissistigma retusum for the first time.The cholinesterase inhibitory activities of compounds（1）-（18）isolated from Fissistigma retusum were tested.The isolated compounds（1）-（18）mostly inhibited the ACh E and BCh E,compounds（1）、（3）、（4）、（6）、（7）、（8）、（12）and（13）showed good inhibitory activity of acetylcholinesterase.Compounds（4）、（6）and（7）showed better butyrylcholinesterase inhibitory activity,compounds（5）and（14）inhibited the BCh E more than the ACh E.In addition,ABTS free radical scavenging activity test of these compounds.The results showed that compounds（11）and（13）showed outstanding antioxidant activities,the IC₅₀value were 7.06±0.65μM and 9.53±0.98μM.which provided possible research direction and theoretical basis for the treatment of diseases caused by oxidative stress.Finally,The inhibitory activity of Aβ_1-42aggregation of compounds（1）-（18）were tested.The results showed that compounds（3）、（4）、（5）、（6）、（7）、（13）、（15）showed Aβ_1-42 aggregation,compound（7）showed outstanding performance,the IC₅₀ value was 22.92±1.21μM.The above results provide important scientific basis as for the treatment of Alzheimer’s disease.