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葫芦脲的细胞和血液相容性评价。

Evaluation of cell and hemocompatibility of Cucurbiturils.

机构信息

Department of Dermatology, Jena University Hospital, Jena, Germany.

Department of Dermatology, Jena University Hospital, Jena, Germany.

出版信息

Eur J Pharm Sci. 2020 Apr 15;146:105271. doi: 10.1016/j.ejps.2020.105271. Epub 2020 Feb 19.

DOI:10.1016/j.ejps.2020.105271
PMID:32084586
Abstract

BACKGROUND

Cucurbiturils (CB) are pumpkin-shaped macrocyclic molecules consisting of methylen-bridged glycoluril units. Because of their complexing characteristics, they can be used as drug containers for medical purposes. For future biomedical and dermal application of CB, the investigation of cell compatibility is essential. Little is known about the influence of CB on eukaryotic cells, especially on dermal keratinocytes. The structurally related cyclodextrins are known to induce cell death by apoptosis in HaCaT keratinocytes as well as hemolysis in erythrocytes.

OBJECTIVE

To examine cytotoxic effects of different CB.

METHODS

Different cytotoxicity tests were performed on HaCaT keratinocytes and erythrocytes incubated with CB[5], CB[6], and CB[7].

RESULTS

CB[5] and CB[6] did not lead to cytotoxic reactions at high concentrations up to 30 mg/mL whereas incubation with CB[7] triggered apoptosis at a concentration of 3.75 mg/mL. None of the investigated CB caused hemolytic effects on erythrocytes.

CONCLUSION

These results confirm the high potential of CB as host-complexes for biomedical and dermal applications.

摘要

背景

葫芦脲(CB)是由亚甲基桥连的甘脲单元组成的南瓜形大环分子。由于其配位特性,它们可用作医疗用途的药物容器。为了将 CB 应用于未来的生物医学和皮肤学,研究细胞相容性至关重要。关于 CB 对真核细胞的影响,特别是对皮肤角质形成细胞的影响,人们知之甚少。结构相关的环糊精已知可诱导 HaCaT 角质形成细胞凋亡和红细胞溶血。

目的

研究不同 CB 的细胞毒性作用。

方法

用 CB[5]、CB[6]和 CB[7]孵育 HaCaT 角质形成细胞和红细胞,进行不同的细胞毒性试验。

结果

CB[5]和 CB[6]在高达 30mg/mL 的高浓度下不会引起细胞毒性反应,而 CB[7]在 3.75mg/mL 的浓度下会引发细胞凋亡。所研究的 CB 均未对红细胞产生溶血作用。

结论

这些结果证实了 CB 作为生物医学和皮肤应用的主体复合物的高潜力。

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