Research On Nano-Preparations And Anticancer Activity Of Natural Product Sulforaphene

The natural product sulforaphene was extracted from radish seed.The results of previous research showed that sulforaphene had antibacterial and antitumor activities,but the stability was poor and the drug delivery window was narrow.This study mainly investigated the inclusion of corn oil and hydroxypropyl β-cyclodextrin on sulforaphene,and verified the cooperation by simulation and characterization.The animal experiment was used to evaluate the toxicity and efficacy.The main conclusions are as follows:1.The hydroxypropyl β-cyclodextrin is used to encapsulate the sulforaphene.The nano-scale inclusion powders were obtained by adjusting ionic strength,pH,temperature,host-guest ratio and so on.Secondly,through ab initio molecular dynamics simulation,the inclusion model of hydroxypropyl β-cyclodextrin for the inclusion of sulforaphene was obtained.It was theoretically verified that hydroxypropylβ-cyclodextrin could encapsulate sulforaphene.The presence of hydroxypropyl β-cyclodextrin in the presence of sulforaphene is verified by FTIR,DSC,XRD,Raman,BET and other characterization methods.2.On the basis of the optimization,the in vitro anti-tumor experiment of hydroxypropyl β-cyclodextrin inclusion of sulforaphene showed that the IC50 value between the two groups was closer and closer with time,which indicated that hydroxypropyl β-cyclodextrin inclusion of sulforaphene preparation had a certain sustained-release effect.Acute toxicity test in mice showed that LD50 values of hydroxypropylβ-cyclodextrin inclusion of sulforaphene were basically the same as that of sulforaphene.The in vivo anti-tumor model aimed at NCI-N87 gastric cancer cell line,and the nano-sized sulforaphene had a higher anti-tumor rate.3.Corn oil has a certain protective effect on the degradability of sulforaphene.The sustained-release experiment further proved that there is a certain binding effect between corn oil and sulforaphene,which makes it have a slow release effect.Molecular simulation results verify that triglyceride,the main component of corn oil,has encapsulation effect on sulforaphene and can effectively isolate the invasion of water molecules.It is this encapsulation effect that improves the stability of sulforaphene.Acute toxicity experiments showed that corn oil could reduce the toxicity of sulforaphene,increase LD50 value and expand the drug delivery window.