阿里山五味子果實活性木酚素成分之研究

Abstract

本論文主要研究臺灣產阿里山五味子(Schisandra arisanensis Hayata)果實部位的丙酮萃取物，進行分離並分析鑑定所含的木酚素成分，實驗結果共分得十七個木酚素化合物。其中包括了四個新的aryltetralone-type lignans，命名為arisantetralones A-D (1-4)，以及七個新的C18-dibenzocyclooctadiene lignans，命名為arisanschinins F-L (5-11)。 以上化合物的結構是利用各種物理數據，包括比旋光度、紅外線、紫外線、CD 光譜、質譜以及配合1D、2D 核磁共振圖譜，並參考相關文獻而建立。化合物1是一柱狀結晶物質，透過X-ray 偵測更能確定其骨架與相對立體結構。 最後，將所分得的十七個化合物進行生物活性檢測。在人類周邊血液單核球(PBMC)免疫調節功能評估試驗中，化合物4 在細胞毒性較小的情況下，對PBMC增生有明顯抑制作用，具有進一步研究的價值。另外，在癌細胞毒殺測試中發現化合物5 對癌細胞株HEp-2、Daoy、MCF-7 和WiDr 具有不錯的細胞毒殺活性，其ED50 值分別為4.12、6.23、4.09 和6.08 μg/ml。

Investigation of an acetone-soluble extract of the fruits of the Taiwanese medicinal plant Schisandra arisanensis Hayata has resulted in the isolation of eleven new oxygenated lignans and six known compounds. Four of the new lignans, arisantetralones A-D (1-4), possess an aryltetralone skeleton, while the other seven new compounds, arisanschinins F-L (5-11), belong to the polyoxygenated C18-dibenzocyclooctadiene lignans. The structural elucidation of these metabolites was determined on the basis of spectroscopic analyses, especially 2D-NMR techniques. And the above-mentioned results were also compared with the published data. The structure of compound 1 was confirmed by X-ray crystallographic analysis. The biological activities of these compounds were also tested and evaluated. The immunomodulatory effect of compound 4 on human peripheral blood mononuclear cells (PBMC) proliferation was better than the others. In addition, compound 5 exhibited cytotoxicity against HEp-2, Daoy, MCF-7, and WiDr tumor cell lines with ED50 values of 4.12, 6.23, 4.09, and 6.08 μg/ml, respectively.