Department of Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, Universitätsplatz 1, University of Graz, 8010 Graz, Austria.
Molecules. 2014 Jan 20;19(1):1223-37. doi: 10.3390/molecules19011223.
Biphenyl neolignans such as honokiol and magnolol, which are the major active constituents of the Asian medicinal plant Magnolia officinalis, are known to exert a multitude of pharmacological and biological activities. Among these, cytotoxic and tumor growth inhibitory activity against various tumour cell lines are well-documented. To further elucidate the cytotoxic effects of honokiol derivatives, derivatizations were performed using tetrahydrohonokiol as a scaffold. The derivatizations comprised the introduction of functional groups, e.g., nitro and amino groups, as well as alkylation. This way, 18 derivatives, of which 13 were previously undescribed compounds, were evaluated against CCRF-CEM leukemia cells, U251 glioblastoma and HCT-116 colon cancer cells. The results revealed no significant cytotoxic effects in any of the three tested cell lines at a test concentration of 10 µM.
联苯新木脂素如厚朴酚和木兰醇，是亚洲药用植物厚朴的主要活性成分，已知具有多种药理和生物学活性。其中，对各种肿瘤细胞系的细胞毒性和肿瘤生长抑制活性已有充分的文献记载。为了进一步阐明厚朴酚衍生物的细胞毒性作用，使用四氢厚朴酚作为支架进行了衍生化。这些衍生化包括引入功能基团，例如硝基和氨基，以及烷基化。这样，就制备了 18 种衍生物，其中 13 种是以前未描述的化合物，然后对 CCRF-CEM 白血病细胞、U251 神经胶质瘤细胞和 HCT-116 结肠癌细胞进行了评估。结果显示，在测试浓度为 10µM 时，在这三种测试的细胞系中均没有显著的细胞毒性作用。
