Studies On The Constituents And Anti-tumor Activity In Vitro Of Arctium Lappa L.

Fructus arctii is the dried seeds of Arctium lappa L. (Compositae). In theory of traditional Chinese medicine, this medicine can disperse wind-heat from the superficies, smooth the throat and disperse the mass due to retention of evils. Ventilating the lung and facilitating eruption, and remove toxic materials and relieve pyogenic infection of the skin. Many chemical and pharmacologic studies on Fructus arctii have been reported. The chemical constituents of it are lignans, essential oil, fatty acid, sesquiterpene, triterpene, and so on. It was reported that arctigenin and arctiin could be used for anti-virus and anti-tumor . whereas the pharmacological reports of other chemical constituents were insufficient. In this paper, isolation, purification, structural elucidation, in vitro activities of the lignan isolates against tumor cells were investigated.Thirteen compounds were isolated from the ethanol extract of Fructus arctii through repeated silica gel, ODS and Sephadex LH-20 and/or separated by preparative HPLC column chromatographies.From the physico-chemical data, including NMR, MS, UV and IR, the chemical structures of the compounds were determined, as isolappaol C (1), lappaol C (2), lappaol H (3), oleic acid (4), lappaol F (5), arctigenin (6), matairesinol (7), lappaol B (8), (+)-7,8-didehydroarctigenin (9), arctiin.(10) , lappaol E(11), isolappaol A(12), and lappaol A(13).In this study anti-tumor effect was evaluated for the lignans isolated from the seeds of Arctium lappa L. and the cytotoxicity of lappaol B, lappaol A, and isolappaol A to K562 cells was reported for the first time. The results showed that IC₅₀ values of lappaol B, lappaol A, and isolappaol A to K 562 cells were 38.5μg/ml, 53.5μg/ml, 51.1μg/ml, respectively.