Preparation Of Natural Anthraquinone Antitumor Activity Of Ingredients And Derivatives

Polygonum Cuspidatum Sieb. et Zucc belongs to the genus of Polygonceae,family of Polgohum. Rheum is the radix and rhizome of Rheum palmatum L.,Rheum tanguticum Maxim. ex Balf., Rheum officinale Baill. Semen Cassiaebelongs to the leguminosae, the ripe seeds of Cassia obtusifolia L., C. tora L.. Polygonum Cuspidatum, Rheum and Semen Cassiae were found to shew significant bioactivities in vitro against human, tumor cell lines. The experiment against human tumor and consulting literature indicate that their basis are the compounds of anthraquinone. In order to study many constituents with anticancer and structure activiy and discover natural products with new structures and bioactive activities, we have investigated the Polygonum Cuspidatum, Rheum and Semen Cassiae.MCF-7 bioassay-guided fractionation led to the.isolationof the active constituents. Twelve compounds have been isolated from the ethanolic extracts of Polygonum Cuspidatum, Rheum and Semen Cassiae by repeatedly chromatography on normal. By detailed analysis, of the spectral data (IR, EIMS, ¹H-NMR, ¹³C-NMR, DEPT, COSY, HSQC) and chemical methods, eight were elucidated as following: chrysophanol,physcion, emodin, ambrettolide,β-sitosterol, qleanolic acid, coumarin,2-ethoxy-8-acetyl-1, 4naphthoquinone. CompoundⅧis a new compound and compoundⅣis obtained from this plants of Polygonum Cuspidatum for the first time. 9,10-dihydro-1,6-dihydroxy-3-methyl-9,10-dioxoanthracen-8-yl acetate, 9,10-dihydro-1,8-dihydroxy-3-methyl-9,10-diexoanthraeen-6-yl acetate and ehrysophanol has been synthesized,which is basedon emodin.Some of them were found to show significant bioactivities in vitro against humantumor cell lines. Such as, the quantities of distilling in aether and compoundsⅠ,Ⅱ,Ⅲ,Ⅳ,Ⅷagainst the human tumor cells MCF-7. The result indicate that thesix position of hydroxy in emodin show more activity.We evaluated the activity ofthe compounds of anthraquinone systematically for the first time; The results can bethe reference data for the antieancer of Polygonurn Cuspidatum, Rheum and Semen Cassiae. for the future.These can help people to recognize the constituents of Polygonum Cuspidatum, Rheum and Semen Cassiae and also apply to science research of the new Antineoplastic Constituents.