| 摘要: | 本計畫以三十種中藥進行抽取，將抽取物進行26S 蛋白質降解酶活性之測試，發現中藥石榴皮及蘇木有明顯的抑制的效果。將石榴皮及蘇木以95 %乙醇進行抽取得到抽取物為PGEtOH 及SCEtOH，此二抽取物分別再以不同的有機溶媒進行分配萃取分別得到PGH、PGM、PGB、PGW、SCH、SCM、SCB 及SCW 八個部分，將此八個萃取質進行26S蛋白質降解酶活性之測試，由實驗研究的結果發現PHM、PGB、PGW、SCM 及SCB 對26S蛋白質降解酶活性有明顯抑制作用。從中藥石榴的皮中分離出7 個化合物及中藥蘇木的根部中分離出14 個化合物，經光譜方法分析及與文獻比對後鑑定其化學結構式。其中發現化合物Brazilein (SCEP-2)有抑制26S蛋白質降解酶活性之作用，化合物Sappanone A、Protosappanin C 及Ursolic acid 對人類皮膚基底細胞癌具有毒性，以及化合物Brazilein、5,6,7,3’,4’-Pentahydroxyisoflavone、Sappanone A、Protosappanin C 及Ursolic acid 對人類頭頸部鄰狀細胞癌具有細胞毒之活性。
We screen 30 kinds of Chinese herbal medicine, Punia granarum and Caesalpinia sappan showed a significant inhibition on 26 S proteasome. Their P. granarum and C. sappan were extracted with 95% ethanol obtained as PGEtOH and SCEtOH, then with different polarity of the solvent extraction layer to give PGH, PHM, PGB, PGW, SCH, SCM, SCB and SCW, successively. We test the different polarity extraction layer of material on the inhibitory of 26S proteasome, the results of the experiment found that PHM, PGB, PGW, SCM and SCB on the inhibitory effect of 26S proteasome. Seven compounds were isolated peel of P. granarum and the roots of C. sappan isolated fourteen compounds. Their structures were determined by spectroscopic methods and comparison with literature. The ability of Brazilein (SCEP-2) to inhibit 26S proteasome was investigated. The compounds, Sappanone A, Protosappanin C, and Ursolic acid shown inhibition human skin basal cell carcinoma and Brazilein, 5,6,7,3’,4’-Pentahydroxyisoflavone, Sappanone A, Protosappanin C, and Ursolic acid inhibition human head and neck squamous cell carcinoma 9 cytotoxic activities. |
