Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University-Sofia, Sofia, Bulgaria.
Phytomedicine. 2008 Nov;15(11):1010-5. doi: 10.1016/j.phymed.2008.04.008. Epub 2008 Jun 6.
The cytotoxic effects of hyperatomarin - a prenylated phloroglucinol isolated from Hypericum annulatum Moris subsp. annulatum were assessed in a broad spectrum of tumor cell lines originating from leukemias, lymphomas and solid malignancies. The tested compound exerted strong concentration-dependent cytotoxic effects (IC50 values ranging 0.14-15.7 μM), comparable to and even outclassing in some cell lines those of the established anti-cancer drug daunorubicin. Exposure of different human tumor cell lines to hyperatomarin resulted in strong mono- and oligo-nucleosomal fragmentation of genomic DNA, as evidenced by 'Cell death detection' ELISA kit and by DNA-electrophoresis, which unambiguously indicates that the induction of apoptosis is implicated in the cytotoxic mode of action of the tested compound.
从贯叶连翘(Hypericum annulatum Moris subsp. annulatum)中分离得到的一个被羟化的间苯三酚,即偏诺马琳,其在多种肿瘤细胞系(包括白血病、淋巴瘤和实体恶性肿瘤)中的细胞毒性作用已被评估。该化合物具有较强的浓度依赖性细胞毒性作用(IC50 值范围为 0.14-15.7 μM),与已确立的抗癌药物柔红霉素相比,在某些细胞系中甚至具有更强的作用。不同的人类肿瘤细胞系暴露于偏诺马琳后,基因组 DNA 发生强烈的单聚体和寡聚体核小体片段化,这一点可通过“细胞死亡检测”ELISA 试剂盒和 DNA 电泳得到证明,这明确表明凋亡的诱导与所测试化合物的细胞毒性作用模式有关。