Resource Research And Steroids Synthesis Research Of Dioscorea Zingiberensis In Liping,Rongjiang,Dan Zhai And Sandu In Guizhou

Objectives: Dioscorea zingiberensis is rich in steroidal saponins.Saponin extracted from Dioscorea zingiberensis,known as "medicinal gold",is the main raw material of nearly 200 kinds of drugs,such as synthetic steroid hormones.Dioscorea zingiberensis used in the past time mainly originated in excavation of wild plants,and a large number of excavation of without cultivating leaded to resource depletion.At the same time,Guizhou is rich in natural resources and is one of the largest ethnic minority areas,so it is necessary to investigate the resource distribution,growing environment and the ethnic cognize and medicine and food applications.In addition,Dioscorea zingiberensis is rich in diosgenin,a kind of important steroidal hormones and with very similar structure as celastrol,which has remarkable effect in antineoplastic activity,but big toxicity.So it is of great significance to compound Steroids and develop antitumor active new drugs,which is efficient and low toxicity,by taking nontoxic diosgenin as raw material and reference to the construction of celastrol.Methods: Select Liping,Rongjiang,Danzhai,Sandu in the Southeast and South of Guizhou Province for the field site of investigation through the extensive documentation collection and sorting.During the investigation,we will take the local market day as a starting point for the survey,consult the streets herbalist,medicinal herbs paved folks and folk herbal medicine clinic medical researchers and scholars,and visit the local Dong,Shui,Miao people to understand the growing environmentand usage of Dioscorea zingiberensis.In addition,Double dilute pregnenolone acetate can be obtained from steroid saponin in Dioscorea zingiberensis through the method of conventional hydrolysis pregnenolone.Taking Double dilute pregnenolone acetate as raw material and refering to the A ring and B ring structure of celastrol,we will take into the polarity of the hydroxyl and halogen structure,and introduce active functional groups such as double bond the 1st place and 4th place of A ring to get three to seven steroidal four-ring compounds.Finally,we will take these Steroids for antitumor activity test.Results: By comprehensive analysis of the documents and field survey data,we find that Liping,Rongjiang,Sandu and Danzhai have few distribution,and Danzhai,by contrast,has a bit more wild Dioscorea zingiberensis.Dioscorea zingiberensis in medical market,whose amount is very small and comes mainly from cultivation and purchase.In terms of medicinal usage,Dioscorea zingiberensis is mainly used for injuries,boils,and as a tonic.In the aspect of synthetic steroid compounds,we will modify the A ring and B ring of the 3rd hydrolysis product of diosgenin,and through the bromoform reaction,esterification reaction,Oppenauer oxidation,PCC oxidation to get the steroidal compound ramification A2^A8.By using the method of SRB in the antitumor active filter,the synthetic derivatives all have the inhibition of nerve cells?N-04?,lung cancer cell?Lu-04?,and breast cancer cells?Bre-04?.Derivative A7 to the three kinds of cancer cells is stronger(GI₅₀ value are 7.2 x 10^-7mol · L^-1,4.8 x 10^-7mol · L^-1,2.8 x 10^-7mol · L^-1),and derivative A5 also shows a good cytotoxicity to breast cancer?Bre04?(GI₅₀ = 3.8 x 10^-7mol.L^-1).Conclusion: Because of the influence of the natural environment,Dioscorea zingiberensis resource distribution is very little in Liping,Rongjiang,Sandu and Danzhai,the residents there rarely know it.While in medicinal aspects,the residents mainly use Dioscorea zingiberensis for injuries,etc.,which is very scientific through literature analysis method validation,and this medication method is more simple and efficient.Besides,it is used by the residents to make shoe-pads,dispel fishy etc.,which are worthy of our study.Derivatives A5 and A7,two of the seven derivatives of steroidal compound by structure modification of the hydrolysate of diosgenin,show good anti-breast cancer cells?Bre-04?activity,which is stronger than cis-Dichlorodiamineplatinum.Furthermore,the compound A7 also shows good toxicity to nerve cells?N-04?and lung cancer cells?Lu-04?.It lays a good foundation for the future steroidal compounds anticancer drugs.We hope to obtain better antitumor drugs in the next study.