Purple Sin Anticancer Agents

According to the multiplex antitumor mechanism and considering traditional Chinese medicine principles, ZIQIAN antitumor preparation is a new complex one which has antirumor activity. The formula is composed of Radixa Arnebia seu Lithospermi, Radix Rubiae, Rhizoma zedoariae and Herba Eishoitziae seu Moslae. In the prescription, Radixa Arnebia seu Lithospermi, Radix Rubiae, Rhizoma zedoariae and Herba Eishoitziae seu Moslae are monarchical, ministerical, adjuvant and conductant drugs respectivelyOn the base of the studies of the optimal extraction techniques of each herb in the formula and the preparation's quality standard, the experiment studied the quality standard of ZIQIAN antitumor preparation, the maximum tolerant dosage of mice by gastric perfusion and the formula optimization for tumor model S180. In addition, the experiment also isolated 4 compounds from the diethyl ether part and ethyl acetate part of the ethyl alcohol extracts of Radix Rubiae and did the antitumor experiment in vitro using the ZIQIAN preparation and one compound.Rhizoma zedoariae and Herba Eishoitziae seu Moslae were identified by TLC, with their characteristic mottles obvious. Rhizoma zedoariae was also identified by GC, having the characteristic peak of curcumol and curzernone with the retained time 33min and 40min respectively.The contents of levo-Shikonin and rubimaillin in the ZIQIAN preparation were measured. It was proved that the two kinds of contents had remarkable linear correlation within 20-60 ug/ml and 21 ~105ug/ml -espectively. The mean recovery rate of levo-Shikonin was 100.34%(RSD=0.92%) and that of rubimaillin was 99.8%(RSD=0.85%)o The maximum tolerant dosage of mice by gastric perfusion is 140.58g/kgThe results of the formula optimization througn antitumor experiments of S180 showed that the formula's effection was more significant than others, with the inhibiting tumor rate 40.47%.Crystal compounds I,II,III, IV were isolated rom the diethyl ether part and ethyl acetate part of the ethyl alcohol extracts of Radix Rubiae by silica gel column chromatography. The chemical structures of compo unds I and II were identified as rubimaillin and 2-methyl-l,3,6-trihydroxy-9,10-anthriquinone-3-O-(O-6'-acetyl)-B-Glucoside -(2-1) - a - rhamnosyl respectively.The results of the antitumor experiments in vitro of the ZIQIAN preparation and rubimaillin showed that the preparation's(220ug/ml,herb) inhibiting tumor rate is 47.1% and rubimaillin's(40ug/ml) is 70.8%. The exoeriments determined the quality standard of the ZIQIAN antitumor preparation anc therefore laid a foundation for subsequent clinical experiments...