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雷公藤红素脂质体对前列腺癌细胞的抗癌活性评估。

Evaluation of anticancer activity of celastrol liposomes in prostate cancer cells.

作者信息

Wolfram Joy, Suri Krishna, Huang Yi, Molinaro Roberto, Borsoi Carlotta, Scott Bronwyn, Boom Kathryn, Paolino Donatella, Fresta Massimo, Wang Jianghua, Ferrari Mauro, Celia Christian, Shen Haifa

机构信息

Department of Nanomedicine, Houston Methodist Research Institute , Houston, TX , USA .

出版信息

J Microencapsul. 2014;31(5):501-7. doi: 10.3109/02652048.2013.879932. Epub 2014 Mar 24.

Abstract

CONTEXT

Celastrol, a natural compound derived from the herb Tripterygium wilfordii, is known to have anticancer activity, but is not soluble in water.

OBJECTIVE

Formation of celastrol liposomes, to avoid the use of toxic solubilising agents.

MATERIALS AND METHODS

Two different formulations of PEGylated celastrol liposomes were fabricated. Liposomal characteristics and serum stability were determined using dynamic light scattering. Drug entrapment efficacy and drug release were measured spectrophotometrically. Cellular internalisation and anticancer activity was measured in prostate cancer cells.

RESULTS

Liposomal celastrol displayed efficient serum stability, cellular internalisation and anticancer activity, comparable to that of the free drug reconstituted in dimethyl sulfoxide.

DISCUSSION AND CONCLUSION

Liposomal celastrol can decrease the viability of prostate cancer cells, while eliminating the need for toxic solubilising agents.

摘要

背景

雷公藤红素是一种从草药雷公藤中提取的天然化合物,已知具有抗癌活性,但不溶于水。

目的

制备雷公藤红素脂质体,以避免使用有毒增溶剂。

材料与方法

制备了两种不同配方的聚乙二醇化雷公藤红素脂质体。使用动态光散射测定脂质体特性和血清稳定性。采用分光光度法测定药物包封率和药物释放。在前列腺癌细胞中测定细胞内化和抗癌活性。

结果

脂质体雷公藤红素显示出高效的血清稳定性、细胞内化和抗癌活性,与在二甲基亚砜中重构的游离药物相当。

讨论与结论

脂质体雷公藤红素可降低前列腺癌细胞的活力,同时无需使用有毒增溶剂。

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