| The root of Rhaponticum uniflorum(L.)DC.,which belongs to the composite family,has been long used against heat-toxin, intoxication, carbuncle and for the treatment of swell.It can inhibit tumor cell proliferation, induce tumor cell apoptosis, directly kill tumor cells, arrest the cell cycle, reverse multi-drug resistance, improve the body function of the immunity,etc.The clinical antitumor efficacy of Rhaponticum uniflorum(L.)DC. is definite, however the material basis is hazy. The model of multiple pharmacodynamics combining with mathematical statistical is used to provide thinking for anti-lung cancer research of Rhaponticum uniflorum(L.)DC.Against lung cancer biological activity oriented, kinds of apparatus and skills such as solid-liquid extraction, macroporous adsorption resin, as well as high performance liquid chromatography (HPLC) are used to seperate and purify the effective fraction concerning lung cancer of Rhaponticum uniflorum(L.)DC..To screen those fraction from Rhaponticum uniflorum(L.)DC., the model of human lung adenocarcinoma cells A549, HI299 and the Lewis transplanted C57 BL/6J mice are established.The results show that the n-butanol extract of Rhaponticum uniflorum(L?)DC has the strongest inhibiting proliferation on A549 and H1299 lung cancer cell,the IC50are 205.43±16.10 μg·mL-1 and 315.87±13.72 μg·mL-1 respectively/The 50% macroporous adsorption resin from Rhaponticum uniflorum(L.)DC. has the strongest inhibiting proliferation on A549 and H1299 lung cancer cells, the IC50 are 163.09±13.22 μg·mL-1 and 287.34±15.04 μg·mL-1.The The results show that the n-butanol extract of Rhaponticum uniflomm(L.)DC. has significantly inhibition on the growth of tumor-burdened Lewis lung tumor in mice, the inhibitory rate of which are 37.43±4.80% and 32.91±7.31% in high and low dose group.UPLC/Q-TOF-MS-MS and HPLC is applied to analysis the active fraction of Rhaponticum uniflorum(L.)DC, the primary components are triterpene represented by oleanolic acid and ursolic acid, sterols represented by β-sitosterol and stigmasterol,phenolic acids represented by caffeic acid and rosmarinic acid.To be domenstrated that the active component of lung cancer are consistent with those chemical components mentioned above,comparing different batches, origin of Rhaponticum uniflorum(L.)DC. by the principal component analysis and cluster analysis.On this basis, according to baseline geometric design combining with uniform design for these components, obtaining 12 groups.The A549 lung cancer cell model is established in this research, the effects of components compatibility on A549 proliferation, apoptosis, invasion and migration are observed, and the regression equation are calculated to get optimal components compatibility and component contribution coefficient;the model of anthropogenic A549 lung cancer cell inoculation of nude mice is established to validate the whole anti-lung cancer effect of optimal compatibility next.The results indicate that the component compatibility 12 is optimizing compatibility,its IC50 of A549 proliferation inhibition is 143.00±28.31μg·mL-1, inducing apoptosis of A549 apoptosis rate is 42.04%, inhibiting number of cells is 87.88±8.36 of A549 lung cancer cells, and A549 wound healing rate is 9.56% due to inhibiting A549 migration. Inhibition of Rhaponticum proportion of 12 inhibited the tumor growth rates is 55.39 ±0.07%.The ratio of 12 for Hebei Rhaponticum group composition, its superiority lies in the unique structure of component ratio, the ratio of active components oleanolic acid, ursolic acid,β-sitosterol, stigmasterol and rosmarinic acid, caffeic acid is 1.00:0.75:0.43:1.03:1.46:0.70.The Rhaponticum uniflorum(L.)DC. play synergistic efficacy of multiple components and multiple effects on the overall lung cancer,which through component of oleanolic acid and ursolic acid as the representative of triterpene,β-sitosterol and stigmasterol as the representative of sterols, caffeic acid and rosmarinic acid as the representative of phenolic acid. |
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