Yang Min Cheol, Choi Sang Un, Choi Wahn Soo, Kim Sun Yeou, Lee Kang Ro
Natural Products Laboratory, College of Pharmacy, Sungkyunkwan University, Suwon 440-746, Korea.
J Nat Prod. 2008 Apr;71(4):678-83. doi: 10.1021/np800005r. Epub 2008 Mar 4.
Two new guaiane sesquiterpene lactones ( 1 and 2) and seven new amino acid-sesquiterpene lactone conjugates ( 3- 9), together with six known sesquiterpene lactones ( 10- 15), were isolated from the methanol extract of the aerial parts of Saussurea pulchella. Their structures were determined on the basis of spectroscopic and chemical methods to be 8alpha- O-(3'-hydroxy-3'-methylbutyryl)desacylcynaropicrin ( 1), 8alpha- O-(2', 3'-dihydroxyisobutyryl)11beta,13-dihydrodesacylcynaropicrin ( 2), and pulchellamines A, B, C, D, E, F, and G ( 3- 9). The structures of the new amino acid-sesquiterpene lactone conjugates, pulchellamines A, B, C, D, E, F, and G ( 3- 9), were confirmed by synthesis. The isolated compounds were evaluated for cytotoxic activity against four human tumor cell lines. Compounds 11 and 12 exhibited cytotoxicity against skin melanoma (SK-MEL-2) and ovary malignant ascites (SK-OV-3) human tumor cell lines with ED 50 values of 1.53 and 4.07 microM, and 2.49 and 7.42 microM, respectively.
从美丽风毛菊地上部分的甲醇提取物中分离得到两个新的愈创木烷型倍半萜内酯（1和2）和七个新的氨基酸-倍半萜内酯缀合物（3 - 9），以及六个已知的倍半萜内酯（10 - 15）。通过光谱和化学方法确定它们的结构分别为8α - O -（3'-羟基-3'-甲基丁酰基）去酰基刺囊酸（1）、8α - O -（2'，3'-二羟基异丁酰基）11β，13 - 二氢去酰基刺囊酸（2）以及美丽风毛菊胺A、B、C、D、E、F和G（3 - 9）。新的氨基酸-倍半萜内酯缀合物，即美丽风毛菊胺A、B、C、D、E、F和G（3 - 9）的结构通过合成得以确证。对分离得到的化合物针对四种人类肿瘤细胞系进行了细胞毒性活性评估。化合物11和12对皮肤黑色素瘤（SK - MEL - 2）和卵巢恶性腹水（SK - OV - 3）人类肿瘤细胞系表现出细胞毒性，其ED50值分别为1.53和4.07微摩尔/升，以及2.49和7.42微摩尔/升。
