Screening Of Sesquiterpenoids In The Root Of Tripterygium Wilfordii Hook.F And Studies On The Cytotoxicity Of Compounds

Objective:In this experiment,the biological activity was used as a guide to extract and separate the active ingredients from the dried roots of the natural plant Tripterygium wilfordii Hook.F.The compounds with antitumor activity were selected.Methods:The ethyl acetate extract of Tripterygium wilfordii root（5.0 kg）was separated and purified by positive and reversed-phase column chromatography and semi-preparative high-performance liquid chromatography separation methods.The MS,UV,IR,1-2D-NMR spectral data of the obtained compounds were analyzed and compared with the literature to finally determine their chemical structures.At the same time,the MTT colorimetric method was used to determine the effective inhibitory concentration of five different tumor cells（A549,HOS,MCF-7,MDA-MB-231,MCF-7/TAMR）.Results:By separating and purifying the ethyl acetate extract from the dried roots of Tripterygium wilfordii Hook.F,nine sesquiterpenoids were obtained,including four new compounds（1-4）and five known compounds（5-9）.The chemical structure of the above compound（1-9）were determined by analyzing the nuclear magnetic data,and named as:1α,2α,5α,7α,11-pentaacetoxy-8α-benzoyloxy-β-dihydroagarofuran（1）,1α,2α,5α,7α,11-Pentaacetoxy-8α-furanyl-β-dihydroagarofuran（2）,1β,2α,5α,7β,11-Pentaacetoxy-8α-furanyl-β-dihydroagarofuran（3）,1α,5α,7α,11-Tetraacetoxy-8α-benzoyloxy-β-dihydroagarofuran（4）,（1α,2α,6β,8α,9α）-1,2,6,8,15-pentakis（acetyloxy）-9-（benzoyloxy）dihydro-β-agarofuran（5）,（1α,6β,8β,15α）-tetraacetoxy-9α-benzoyloxy-β-dihydroagarofuran（6）,（1α,6β,8α,15α）-tetraacetoxy-9α-benzoyloxy-β-dihydroagarofuran（7）,（1α,6β,15α）-1,6,15-triacetoxy-9β-（benzoyloxy）dihydro-β-agarofuran（8）,Wilforsinine B（9）.Concousion:In this paper,four new and five known sesquiterpenes were isolated from the roots of Tripterygium wilfordii.The cytotoxic activity data showed that compounds 2-4 and 7-9 had strong cytotoxic activity,and their IC₅₀0 values were respectively.Compound 2:58.25±2.04μM（MDA-MB-231）;Compound 3:13.77±2.39μM（MDA-MB-231）;Compound 4:42.12±3.26μM（A549）;Compound 7:51.01±2.02μM（MDA-MB-231）;Compound 8:48.71±2.31μM（MDA-MB-231）;Compound 9:62.11±3.19μM（A549）.