Study On The Stability Of Sulfora Phene And The Construction And Anticancer Activity Of Novel Nano-carriers

Sulforaphene(SFE)is an isothiocyanate compou id that with anticancer ac(?)ivity,prepared from radish seeds.However,i was founded that SFE had a certain degree of instability.SFE will be degraded in the normal temperature or water environment,so there may be a security problem during the actual use.In this paper,the degradation process in different environments,degradation mechanism,the oroperties of degradation products and the stability of SFE were studie<.At the same time,mesopcrous silica nanoparticles(MSNs),as a delivery carrier of SFE and its derivative sulforaphene-glutathione conjugate sodium salt(SFE-GSH-N a)was prepared.It can target cancer cells,make the drugs slow release,to achieve long circulation,improve drug stalbility,in order to achieve be(?)ter anti-cancer effect lay the foundation.1.The stability and degradation mechanism of SFE were studied.The results showed that the degradation products of SFE were different at different temperatures,and two degradation products were produced at above 50 ?.The structure of the two degradation products was identified by LC-MS analysis,elemental analysis and.nuc'ear magnetic resonance aralysis and the purity higher than 95%.One of the degradation products is a cyclic compound 6-[(methylsulfinyl)methyl]-1,3-thiazinar-2-thione,another compound is SFE cimmer.The degradation n echanism of SFE in high temperature aqueous solution was deduced.In o rder to improve the safety of SFE,it should avoid contact with water.SFE can be placed in a vacuum oven containing anhydrous phosphorus pentoxide.The sample can be placed in ampoules,filled with nitrogen to irr prove the stability of SFE.2.The synthesis and drug loading properties of mesc porous silica nanocarbons were studied.The MCM-41 MSNs were prepared by aqueous phase method.The particle size and zeta potential were measured by dynamic light scattering.The morphology was observed by transmission clectron microscopy.The pore size and specifie surface area of the material were characterized by BET.The result s showed that the reaction temperature was 95 ?,TEA was 0.4 wt%,TEOS was 7.5 wt%and reaction time were 1h.MSNs had a size of about 60 nm,were uniform in particle size and had good dispersibility,specifie surface area was 436 m2·g-1,the average pore size was 3 nm.MSNs couId be applied to the subsequent drug loading steps.The drug loading rale and release properties of MSNs as delivery carriers for SFE and SFE-(GSH-Na were studied.The drug loading was about 50%,the encapsulation efficiency was higher than 90,%,the release rate in the acidic environment was high,and there were slow-release effect.3.Cell viability was tested in human fibroblast cell line MRC-5.Anticancer activity was tested in lung cancer cell lines A549,H1299 and gastric cance(?)cel(?)line HGC-27.The results showed that MSNs had a targeted effect on cancer cells and the safety was good,MS Ns were good delivery carrier.In this paper,the stability of SFE and the degradatii-n in aqueous solution at different temperatures were studied.The structure of degradation products and degradation mechanism were ide itified.A new mesoporous silica nanocarrier was synthesized and could be used as delivery carriers for SFE and SFE-GSH-Na.The carrier targeted cancer cells,has a sustained release effect on the drug,througn the surface modification can improve the long cycle time and stability,for the future in vivo anti-c ancei experiments laid the foundation.