Development Of Vinca Alkaloids And The Novel Synthetic Technique Of Anhydrovinblastine

Vinca is an important kind of medical plant belonging to dogbane species. There are more than 100 kinds of alkaloids in vinca plant, including anhydrovinblastine, vinblastine, vincristine and other anti-tumor medicine used in clinic, etc.Vinca dry grass and fresh grass as raw material, by a series of methods: acid dissolving, alkali precipitation and extraction using organic solvent, we gathered and purified vinca alkaloids in our experiments. Adding acid, alkaloids can be transformed salt and improved solubility in the solution, so alkaloids can be in water phase and been extracted from vinca plant; Then adjusting PH to be alkaline, alkaloids can be precipitation in the water phase. Extracting using organic solvent then removing water phase, thus we can removed other mixed substance which dissolved in the water phase. Next adding acid again, alkaloids enter in water phase again. At the moment adding organic solvent to water phase can removed oiled mixed substances, so purified alkaloids remained in the water phase. Adjusting PH of water phase to be alkaline once more, precipitation be cooled and dried in the vacuum until it to be powder. Thus we gained rough vinca alkaloids.There are many kinds of alkaloids in vinca alkaloids. Among these substances, the content of catharanthine and vindoline are bigger, the value respectively are 12.236% and 4.90%. In our experiment, catharanthine and vindoline as materials, Fe3+ as oxidant, we first gained a intermedia, then deoxidize the intermedia using NaBH4, thus we obtained synthesized product. At 0℃,methanol solution, we gained crystal, that is purified anhydrovinblastine. The crystal yield reached 34.29%. And the chemical structure of the crystal is confirmed by UV, IR, MS and 1H-NMR. Compared with the methods in the documents, the new synthetic method is practical and suitable for large scale production. On the same condition of laboratory, product of the new method is more pure, less other product and total yield is highest.Vinca alkaloids as material, by several steps: adding Fe3+, NH3H2O, extraction solution(chloroform: methanol=1:1), NaBH4, we gained a certain substance which is nearly pure and low polarity. The result of MS shows molecular weight is 352. Examination on tumor cell shows the substance have strong anti-tumor activity. The substance have great developing value.