Study On The Antitumor Activity Constituents From Centipeda Minima

Centipeda minima belongs to the family Compositae and is recorded in the Pharmacopoeia of the People's Republie of China in 2010 edition of subdivision as a common traditional Chinese medicinal. Centipeda minima is used for the treatment of nasal obstruction, nasosinusitis runny nose, cough, anemofrigid headache and so on. Modern pharmacological tests have revealed that Centipeda minima possess remarkable antineoplastic activity.Based on the previous studies, this paper adopts several methods such as silica gel column chromatography, gel permeation chromatography and MCI-GEL CHP20P chromatography to systematically isolate and purify the chemical composition from ethyl acetate extract which are responsible for the antitumor activity in Centipeda. Total ten compounds were isolated and furtherly identified as Quercetin-3-Me-ether, Quercetin, Kaempferol-3-O-α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranoside, Stigmasterol-3-O-β-D-glucopyran-oside,β-sitosterol, Centipedaphenol, Spinasterol, Lupeol, Rutin and Esculetin by NMR, MS, and other spectroscopic techniques. It is noteworthy that Centipedaphenol, Rutin and Esculetin are identified from Centipeda minima for the first time. And Centipedaphenol is a new compound, which is checked in the plant by HPLC.To identify which compounds, including ethyl acetate extract previously isolated by our term, are responsible for antitumor activity, this research applied the method of chemical tracing combing with biological tracing to test the susceptibility of these compounds to HeLa cells using MTT approach. And experimental results indicated that six of them showed significant antitumor activity:Brevilin,11,13-dihydrohelenalin, Lupeol, Arnicolide C, Arnicolide B and Centipedaphenol, with IC50 of 10.1μg·mL-1,15.8μg·mL-1,16.9μg·mL-1,26.5μg·mL-1,60.6μg·mL-1,77.4μg·mL-1, respectively. The other two compounds which showed a certain antitumor activity were Quercetin and Quercetin-3-Me-ether, with IC50 of 114.1μg·mL-1 and 166.9μg·mL-1, respectively. Moreover, Arnicolide C, Arnicolide B and Centipedaphenol were firstly found to have obvious antitumor activity. Our research provided scientific evidence for the explicit description of antitumor activity of Centipeda and laid a firm foundation for the in-depth study on Centipeda minima.