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首页> 外文期刊>Life sciences >Effects of artemisinin-tagged holotransferrin on cancer cells.
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Effects of artemisinin-tagged holotransferrin on cancer cells.

机译：青蒿素标记的全运铁蛋白对癌细胞的影响。

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Artemisinin reacts with iron to form free radicals that kill cells. Since cancer cells uptake relatively large amount of iron than normal cells, they are more susceptible to the toxic effect of artemisinin. In previous research, we have shown that artemisinin is more toxic to cancer cells than to normal cells. In the present research, we covalently attached artemisinin to the iron-carrying plasma glycoprotein transferrin. Transferrin is transported into cells via receptor-mediated endocytosis and cancer cells express significantly more transferrin receptors on their cell surface and endocytose more transferrin than normal cells. Thus, we hypothesize that by tagging artemisinin to transferrin, both iron and artemisinin would be transported into cancer cells in one package. Once inside a cell, iron is released and can readily react with artemisinin close by tagged to the transferrin. This would enhance the toxicity and selectivity of artemisinin towards cancer cells. In this paper, we describe a method to synthesize such a compound in which transferrin was conjugated with an analog of artemisinin artelinic acid via the N-glycoside chains on the C-domain. The resulting conjugate ('tagged-compound') was characterized by MALDI-MS, UV/Vis spectroscopy, chemiluminescence, and HPLC. We then tested the compound on a human leukemia cell line (Molt-4) and normal human lymphocytes. We found that holotransferrin-tagged artemisinin, when compared with artemisinin, was very potent and selective in killing cancer cells. Thus, this 'tagged-compound' could potentially be developed into an effective chemotherapeutic agent for cancer treatment.
机译：青蒿素与铁反应形成杀死细胞的自由基。由于癌细胞比正常细胞吸收相对大量的铁，因此它们更容易受到青蒿素的毒性作用。在以前的研究中，我们表明青蒿素对癌细胞的毒性比对正常细胞的毒性更大。在本研究中，我们将青蒿素共价结合到载铁血浆糖蛋白转铁蛋白上。转铁蛋白通过受体介导的内吞作用转运到细胞中，癌细胞在其细胞表面表达的转铁蛋白受体明显多于正常细胞，而内吞的转铁蛋白则多于正常细胞。因此，我们假设通过将青蒿素标记为运铁蛋白，铁和青蒿素都可以在一个包装中转运到癌细胞中。一旦进入细胞，铁就会释放出来，并且可以很容易地与青蒿素发生反应，并通过标记到运铁蛋白上。这将增强青蒿素对癌细胞的毒性和选择性。在本文中，我们描述了一种合成这样的化合物的方法，其中转铁蛋白通过C结构域的N-糖苷链与青蒿素青蒿酸的类似物偶联。通过MALDI-MS，UV / Vis光谱，化学发光和HPLC来表征所得的缀合物（“标记的化合物”）。然后，我们在人白血病细胞系（Molt-4）和正常人淋巴细胞上测试了该化合物。我们发现，与青蒿素相比，带有全运铁蛋白标签的青蒿素在杀死癌细胞方面非常有效且具有选择性。因此，这种“标签化合物”有可能被开发成用于癌症治疗的有效化学治疗剂。

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