Research Center for Drug Discovery, School of Pharmaceutical Sciences , Sun Yat-sen University , Guangzhou 510006 , People's Republic of China.
Guangdong Provincial Key Laboratory of New Drug Design and Evaluation , Guangzhou 510006 , People's Republic of China.
J Nat Prod. 2019 Feb 22;82(2):349-357. doi: 10.1021/acs.jnatprod.8b00863. Epub 2019 Feb 6.
Twelve new guaianolide-type sesquiterpenoids (1-12) and five known guaianolide derivatives (13-17) were isolated from an aqueous ethanol extract of the aerial parts of Chrysanthemum indicum. Their structures were determined through spectroscopic data analysis. The absolute configurations of the new compounds were assigned by X-ray crystallography and electronic circular dichroism. Compound 5 shows multiple cytotoxic activities against four human naso-pharyngeal carcinoma (NPC) cell lines (CNE1, CNE2, SUNE-1, and HONE-1) and one human intestinal epithelial cell line (HT-29) with IC values of 4.6, 6.0, 3.5, 4.3, and 9.6 μM, respectively. Compound 16 exhibits weak cytotoxicity against four NPC cell lines, CNE1 (IC = 7.3 μM), CNE2 (IC = 7.4 μM), HONE-1 (IC = 7.6 μM), and SUNE-1 (IC = 5.6 μM), but no cytotoxicity against HT-29 (IC > 10 μM).
从菊花地上部分的水乙醇提取物中分离得到了 12 种新的愈创木烷型倍半萜（1-12）和 5 种已知的愈创木烷型衍生物（13-17）。通过光谱数据分析确定了它们的结构。通过 X 射线晶体学和电子圆二色性确定了新化合物的绝对构型。化合物 5 对 4 个人鼻咽癌（NPC）细胞系（CNE1、CNE2、SUNE-1 和 HONE-1）和 1 个人肠上皮细胞系（HT-29）具有多种细胞毒性活性，IC 值分别为 4.6、6.0、3.5、4.3 和 9.6 μM。化合物 16 对 4 个人 NPC 细胞系 CNE1（IC = 7.3 μM）、CNE2（IC = 7.4 μM）、HONE-1（IC = 7.6 μM）和 SUNE-1（IC = 5.6 μM）表现出较弱的细胞毒性，但对 HT-29 没有细胞毒性（IC > 10 μM）。
