Antitumor Constituents From Paris Polyphalla Smith Var. Yannanensis

RHIZOMA PARIDIS (RP), the dry Rhizome of Paris polyphylla Smith var.yannanensis (Franch.) Hand.-Mazz. and Paris polyphylla Smith var. chinensis(Franch.)Hara,is distributed mainly in Sichuan, Yunnan and guizhou Province, China. In folkmedicine, people always use it to treat cancer disease.In Chinese patent medicines, RP was utilized to cure liver, lung cancer and laryngeal,carcinoma, and as an important constituent in Liulian capsule and Jingfukang drug. Inaddition, it is also a major constituent in Yunnan white drugs, Jideshengsheyaotablets and Gongxuening capsule. Pharmacological experiments indicated its water andethanol extracts, as well as isolated compound (gracillin), have significant anti-tumoractivity. However, the systematical research for bioactive constituents from RP has notbeen carried, especially the bioactivity for pure compounds. Therefore, a systematicresearch for bioactive fractions and constituents is necessary and important.By using column chromatography, including silica gel, flash chromatography, gelpermeation, normal phase and reversed phase preparative HPLC, twenty threecompounds were isolated from P. polyphylla . Compound 1 (falcarindiol) was isolatedfor the fist time.In the in vitro test for anti-tumor activity, EtOAc-and BuOH-ext showed stronganti-tumor effect on Hela and L929 cells. However, The P.E-ext. had no effect at lowconcentrations. Furthermore, the activity of EtOAc-ext. was stronger than those ofBuOH-ext. The inhibition rates of fatty acids were under 10 percent on KB and A2780cells. Some saponins revealed significant anti-tumor activities, and have selectiveactivities for different sell lines. Furthermore, both falcarindiol and saponins showedanti-tumor activities. The number of glycoside and their linked position in thestructure of saponins strongly influenced its anti-tumor activity.In conclusion, there are other types of constituents with anti-tumor active (such aspolyacetylene) in EtOAc-ext. besides saponins from P. polyphylla. We dissolved theanti-tumor fractions and constituents from P. polyphylla, and this paper can berecognized as one of the database for the R&D research of new drug.