| Euphorbia kansui T.N.Liou ex T.P.Wang(Euphorbiaceae)is abundantly distributed in the northwestern China.The dried roots of Euhorbia kansui are known as "Kansui" in Chinese medicine."Kansui" was recorded in Sheng Nung' s Herbal as a low grade drug and has been used as a herbal remedy for edema,ascites,asthma and cancer.Previous research of E.kansui has discovered that it contained plentiful ingenane-type diterpenes and euphane/tirucallane-type triterpenes.Kansui is only for external use when it is raw since it's thrill and toxicity,and must be processed if it is to be taken orally,in order to enture the security of the clinical appliation.The acute toxicity of different processed kansui and its extracts based on the model organism zebrafish,the results demonstrated that the alcohol extract of kansui possessed the highest toxicity.From LC50 of samples,we learn that their toxicity from high to low as follows:the crud Radix kansui,simple stir-baking Radix kansui,Radix kansui infiltrated with vinegar,Radix kansui stir-baked with vinegr.And the results indicate the synergic action of both stir-baking and infiltration with vinegar,which provide a basis for the exploration of detoxication mechanism of vinegar-preparation16 compounds were isolated with silica gel,HPLC,and TLC as the main method.Among them,14 comounds were elucidated on the basis of chemical and spectral methods.Six ingenane-type diterpenes were named as kansuiphorin C(EK-01),3-O-(2'E,4'Z-decadienoyl)-20-O-acetylingenol(EK-02),3-O-(2'E,4'E-decadienoyl)-20-O-acetylingenol(EK-03),3-O-benzoy1-20-deoxyingeno1(EK-04),3-O-(2'E,4'Z-decadienoyl)-20-deoxyingenol(EK-05),3-O-(2,3-dimethylbutanoy1)-13-O-dodecanoyl-20-O-acetylingenol(EK-06);three jatrophane-type diterpenes were named as kansuinin A(EK-07),kansuinin C(EK-08),kansuinin B(EK-09);three triterpenes such as e uphol(EK-10),kansenone(EK-11),Epi-kansenone(EK-12);two others such as isoscopletin(EK-13),palmitic acid(EK-14).Eleven terpenoids of kansui with different structures and configuration were selected to test for their inhibitions on the growth of L-02 and GES-1 human nomal cell lines using MTT method.We found that all ingenane-type diterpenoids and triterpenoids compound exhibited stronger potent cytotoxic activity against of different human normal cell lines.The compound of the ingenane-type diterpenoids with 3-unsaturated aliphatic chain possessed stronger cytotoxic activity,and the cytotoxic activity was decreased if the 3-unsaturated aliphatic chain was replaced by other group.There is a weak effect on the cytotoxic activity with 20-0 group.The compound of the triterpenoids showed stronger cytotoxic activity with the structure of 8-ene-7-one.All compounds of jatrophane diterpenoids showed very weak cytotoxic activity against the two type human normal cell lines.We analyzed the chemical constituents of alcohol extract of kansui and vinegar-preparing kansui by UPLC-QTOF analysis.19 compouds were identified.Such as Kansuinin B,Kansuinin C,Kansuinin B,Kansuinin A,Kansuinin E,Kansuiphorin C,5-O-(2'E,4,E-decadienoyl)ingenol,20-O-(2'E,4'Z-decadienoyl)ingenol,20-O-(2'E,4'E-decadienoyl)ingen ol,3-O-(2'E,4'E-decadienoyl)ingenol,3-0-(2'E,4'Z-decadienoyl)ingenol,3-O-(2'E,4'Z-de cadienoyl)-5-O-acetylingenol,3-O-(2'E,4'Z-decadienoyI)-20-O-acetylingenol,3-O-(2'E,4'E-decadienoyl)-20-O-acetylingenol,3-O-(2'E,4'Z-decadienoyl)-20-deoxyingenol,3-O-(2'E,4'E-decadienoyl)-20-deoxyingenol,Epi-kansenone,kansenone,20-O-(2,3-dimethylbutano yl)-13-O-dodecanoylingenol,3-O-(2,3-dimethylbutanoyl)-13-O-dodecanoylingenol.There was a significant difference five of them.The quality control method of Kansui was established by UPLC-TQ-PDA,after being processed,the toxicitic compounds content were declined.The results showed that there was a certain correlation between terpenoids contents and reduced toxic attenuation. |
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