Studies On The Synthesis,Crystal Structure And Insecticidal Activity Of Matrine Derivatives

Matrine is a kind of biologically active alkaloid,which is mainly separated from the leguminous plants,such as Radix Sophorae,Sophora flavescens and Radix Leguminosae.Many studies have shown that it has insecticidal activity,bacteriostatic and growth regulation.However,because it has the disadvantages of low bioavailability,large dosage and insoluble water,it limits its popularization and application.By introducing heterocyclic and other active groups on 13 key bits of matrine,this article hopes to improve the bioactivity and bioavailability of matrine,and provide candidate compounds for the creation of high efficiency and environmental protection of matrine.This study is mainly divided into the following aspects:(1)In fruit tree alkali for lead compounds,by Michael addition reaction synthesis Mon-Mat,Nmp-Mat,Cyc-Mat,Ind-Mat,M-Cyc-Mat,Cl-Ind-Mat,S-Cyc-Mat,S-M-Mat,S-Pyd-Mat,S-Die-Mat ten kinds of matrine derivatives,separation,purification,in the process of column chromatography separation for the new mobile phase,reduced the time of separation and elution agent,also improved the security of the experiment.As a single crystal culture object,the crystal structure was successfully cultured,and the functional group was preliminarily determined by infrared spectroscopy analysis,and the structure was determined by single crystal diffraction.(2)from somatic Sf9 insect(lawn greed the moth from ovary cells)for the model,for part of bitter and alkaloid derivatives of independent synthetic cell activity screening,toxicology preliminary forecast analysis its insecticidal activity.Results show that the concentration of 2.5,3 tendency for L tree fruit base(Sop),matrine(Mat),instead of Sf9 cell growth has a promoting effect,to 4,4.5 the tendency for L only have slight inhibitory effect on cells.At the same experimental concentration,the inhibition of Sf9 cell growth to Cyc-Mat was up to 68.56%,and Ind-Mat was up to 81.62%.0.6 S-Die-Mat at mmol/L concentration significantly inhibits cell division,and its inhibition rate is 18.50%.At the concentration of1.6mmol/L,72 h was cultured,the number of cells was significantly decreased,and the inhibition rate was up to 86.34%,significantly higher than the cell activity of Sop and Mat before modification.Cyc-Mat,Ind-Mat and S-Die-Mat have significant time and concentration dependence on the inhibition rate of cell growth.(3)To determine the toxic and killing activity of matrine derivatives on twill moths,cabbage moths,beet moths,corn borers,cotton bollworm,cabbage aphids and mulberry root nematodes.By activity test showed that the target derivatives of plutella xylostella,beet armyworm,cotton bollworm,the moth and corn borer poison activity was not significantlyimproved,some correction only increased by 10-20% mortality.At the same time,the adjusted mortality rate of most targets for aphids and mulberry root nematodes can reach more than 80%,and the adjusted mortality rate relative to matrine can increase by 30-40%.It can be preliminarily proved that the newly synthesized target derivatives have higher insecticidal activity to individual small agricultural pests.Moreover,the introduction of sulfur-containing heterocyclic groups by disulfide addition reaction can improve the insecticidal activity of matrine.