The Study On Compounds Of Euphorbia Kansui Based On Toxicity Screening

The dried root of Kansui(Euphorbia kansui T. N. Liou ex T. P. Wang) is a commonly used traditional Chinese medicine(TCM), which was recorded in Shennong-Bencao and has been used as a herbal remedy for edema, ascites, and asthma in China for centuries. Moden pharmacological studies showed that Euphoriba kansui have antitumor, antiviral, antifertility and immunosuppressive effect. However, its clinical application is seriously restricted because of the toxicity and irritation on tissues.In variety of components in Euphoriba kansui, there are about 100 of them have been identified. Summarized all the chenmical data into a database, including 63 diterpenoids, 15 triterpenes, 14 sterols, 3 flavonoids and 2 phenolic derivatives. Some studies found that the diterpenoids are both the bioactive and toxicant fractions. At present, the existing studies mainly focused on traditional quality control, processing technology optimization, pharmacology and toxicology, and there are few reports about the toxicant compositions of Euphoriba kansui.In this study, multidimensional chromatography-mass spectrometry based on advanced pretreatment technology were used to investigate the chemical ingredients and constituents migrating to blood of diterpenoids from Euphoriba kansui. Initially, an efficient accelerated solvent extraction(ASE) was optimized to maximize the extraction yields of diterpenoids from Euphoriba kansui using response surface methodology combining single factor experiments, and 52 diterpenoids was identified from the Euphoriba kansui extracts by HPLC-PDA-ESI-ITMSn. Meanwhile, to research the toxic effect of the ethanol extracts from different polar parts of Euphoriba kansui on the toxicity test in mice. The result was that petroleum ether extract was the most toxic part, and 14 diterpenoids were analyzed by HPLC-PDAESI-ITMSn/TOF-MS. 6 prototype components(Kansuinine G, Kansuinine M, Kansuinine D, 3β,5α,7β,15β-Tetraacetoxy-9α-Nicotinoyloxyjatropha-6(17)-11E-dien-14-one, Kansuinine Eand Kansuinine L) and some metabolities components were analyzed by HPLC-PDA-ESI-ITMSn in rats plasma after intragastric administration of petroleum ether extracts. These data provided the technical and informational foundation for toxic material basic analysis of Euphoriba kansui.In all, with modern techniques of extraction and analysis, an efficient method containing extraction and identification is established, and made a tentative study about the toxic part and the constituents migrating to blood of diterpenoids from Euphoriba kansui. Moreover, the accelerated solvent extraction method is firstly applied in the extract of diterpenoids from Euphoriba kansui. The study is meaningful for clinical application security and new drug development of Euphoriba kansui.