Institute of Pharmacognosy, Faculty of Pharmacy, University of Szeged, Szeged, Hungary.
Department of Medical Microbiology, Albert Szent-Györgyi Health Center, Albert Szent-Györgyi Medical School, University of Szeged, Szeged, Hungary.
Pharm Biol. 2022 Dec;60(1):1511-1519. doi: 10.1080/13880209.2022.2103574.
L. (Asteraceae) contains sesquiterpene lactones as characteristic secondary metabolites. Many of these compounds exert antiproliferative and cytotoxic effects.
To isolate the sesquiterpene lactones from the aerial part of and to elucidate their cytotoxic, antiproliferative and antibacterial effects.
The compounds were identified by one-dimensional (1D) and 2D NMR, HR-MS spectroscopy from the methanol extract. Isolated compounds were investigated for their cytotoxic and antiproliferative effects on human colonic adenocarcinoma cell lines and human embryonal lung fibroblast cell line using MTT assay. The selectivity of the sesquiterpenes was calculated towards the normal cell line. To check the effect of drug interactions between compounds and doxorubicin, multidrug-resistant Colo 320 cells were used.
A new -psilostachyinolide derivative, 1,10-dihydro-1'-noraltamisin, and seven known compounds were isolated from the methanol extract. Acetoxydihydrodamsin had the most potent cytotoxic effect on sensitive (Colo205) cell line (IC = 7.64 µM), also the strongest antiproliferative effect on Colo205 (IC = 5.14 µM) and Colo320 (IC = 3.67 µM) cell lines. 1'-Noraltamisin (IC = 8.78 µM) and psilostachyin (IC = 5.29 µM) showed significant antiproliferative effects on the multidrug-resistant Colo320 cell line and had moderate selectivity against human embryonal lung fibroblast cell line. Psilostachyin C exhibited cytotoxic effects on Colo205 cells (IC = 26.60 µM). None of the isolated compounds inhibited ABCB1 efflux pump (EP; P-glycoprotein) or the bacterial EPs.
Acetoxydihydrodamsin, 1'-noraltamisin, and psilostachyin showed the most remarkable cytotoxic and antiproliferative activity on tumour cell lines and exerted selectivity towards MRC-5 cell line.
L.（菊科）含有倍半萜内酯作为特征性次生代谢产物。其中许多化合物具有抗增殖和细胞毒性作用。
从地上部分分离倍半萜内酯，并阐明其细胞毒性、抗增殖和抗菌作用。
采用一维（1D）和二维（2D）NMR、高分辨质谱（HR-MS）从甲醇提取物中鉴定化合物。采用 MTT 法测定分离得到的化合物对人结肠腺癌细胞系和人胚肺成纤维细胞系的细胞毒性和抗增殖作用。计算了倍半萜对正常细胞系的选择性。为了检查化合物与阿霉素之间药物相互作用的影响，使用多药耐药 Colo 320 细胞。
从甲醇提取物中分离得到一种新的 -psilostachyinolide 衍生物 1,10-二氢-1'-noraltamisin 和七种已知化合物。乙酰氧基二氢达玛烯具有最强的细胞毒性作用，对敏感（Colo205）细胞系（IC = 7.64μM），对 Colo205（IC = 5.14μM）和 Colo320（IC = 3.67μM）细胞系也具有最强的抗增殖作用。1'-noraltamisin（IC = 8.78μM）和 psilostachyin（IC = 5.29μM）对多药耐药 Colo320 细胞系显示出显著的抗增殖作用，对人胚肺成纤维细胞系具有中等选择性。Psilostachyin C 对 Colo205 细胞表现出细胞毒性作用（IC = 26.60μM）。分离得到的化合物均不能抑制 ABCB1 外排泵（EP；P-糖蛋白）或细菌 EP。
乙酰氧基二氢达玛烯、1'-noraltamisin 和 psilostachyin 对肿瘤细胞系表现出最显著的细胞毒性和抗增殖活性，并对 MRC-5 细胞系表现出选择性。
