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大头鬼针草(= 大狼把草)中的细胞毒性倍半萜内酯。

Cytotoxic sesquiterpene lactones from Campuloclinium macrocephalum (=Eupatorium macrocephalum).

机构信息

Departamento de Química, Universidade Estadual de Maringá, Av. Colombo 5790, 87020-900, Maringá, PR, Brazil.

Faculdade de Ciências Farmacêuticas, Universidade Estadual de Campinas, R. Candido Portinari 200, Cidade Universitária, 13083871, Campinas, SP, Brazil.

出版信息

Phytochemistry. 2020 Nov;179:112469. doi: 10.1016/j.phytochem.2020.112469. Epub 2020 Aug 14.

Abstract

Three undescribed germacranolide sesquiterpene lactones, named macrocephalides A-C, along with known steroids, triterpenes and flavonoids were isolated from the aerial parts of Campuloclinium macrocephalum. The structures of the undescribed compounds were elucidated with basis on their 1D and 2D-NMR, and HR-ESI-MS data. Their absolute configurations were assigned by comparison of experimental and calculated electronic circular dichroism (ECD) spectra. Additionally, macrocephalides A-C were evaluated for their in vitro cytotoxic activities against nine human cancer cell lines. Macrocephalides A and B exhibited moderate to potent cytotoxic activity, inhibiting 50% of cell growth (GI) at concentrations ranging from 0.576 to 6.37 μM.

摘要

从大冠毛菊的地上部分分离得到三种新的倍半萜内酯,分别命名为大冠毛菊 A-C,以及已知的甾体、三萜和黄酮类化合物。根据 1D 和 2D-NMR 以及 HR-ESI-MS 数据,解析了未知化合物的结构。通过比较实验和计算的电子圆二色谱(ECD)光谱,确定了它们的绝对构型。此外,还评估了大冠毛菊 A-C 对九种人癌细胞系的体外细胞毒性活性。大冠毛菊 A 和 B 表现出中等至较强的细胞毒性活性,在浓度为 0.576 至 6.37 μM 时抑制 50%的细胞生长(GI)。

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