کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1359385 | 981401 | 2014 | 4 صفحه PDF | دانلود رایگان |

Dihydroartemisinin (DHA), a semi-synthetic derivative of the herb artemisinin, has shown commendable bioactivity. In this paper, a novel dihydroartemisinin-organogermanium (DHA-Ge) compound was synthesized, characterized and its potential anti-tumor activity was evaluated by various methods. MTT results demonstrated that DHA-Ge could effectively inhibit the proliferation of HepG2 cells and showed their dose-dependent properties. The IC50 value of inhibition effect on HepG2 cells of DHA-Ge was 10.23 μg/ml which was lower than 39.44 μg/ml of DHA. Flow cytometric results suggested that DHA-Ge could induce apoptosis of HepG2 cells and the apoptosis rate was 20.26% after 24 h treatment with 56.8 μg/ml DHA-Ge concentration. Atomic force microscopy images showed that HepG2 cells were collapsed and the cell nucleus were fragmented after 24 h treatment. All these results together showed that the DHA-Ge possessed desirable synergetic enhanced anti-tumor effects and could be developed as a suitable tumor therapeutic agent.
Combining DHA with Ge-132, we synthesized a novel organogermanium compound that possessed better antitumor activity than both DHA and Ge-132. The MTT assay was used to observe the inhibitory effects of DHA-Ge on tumor cells and flow cytometry was employed to assay apoptosis of tumor cells after treatment with DHA-Ge. Atomic force microscopy was carried out to investigate morphology of cells treated with the synthesized complex. These results suggested that the synthesized compound showed excellent antitumor activity and it may be developed to be a promising anti-tumor reagent.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 22, 15 November 2014, Pages 5294–5297