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Evaluation of anticancer activity of celastrol liposomes in prostate cancer cells

机译:celastrol脂质体在前列腺癌细胞中的抗癌活性评估

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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.
机译:背景:Celastrol是一种源自野生雷公藤的天然化合物,已知具有抗癌活性,但不溶于水。目的:形成天甾醇脂质体,避免使用有毒的增溶剂。材料和方法:制备了两种不同配方的聚乙二醇化的Celastrol脂质体。使用动态光散射测定脂质体特征和血清稳定性。分光光度法测定了药物的包封效率和药物释放。在前列腺癌细胞中测量细胞内在化和抗癌活性。结果:脂质体Celastrol表现出有效的血清稳定性,细胞内在化和抗癌活性,与二甲基亚砜中重构的游离药物相当。讨论与结论:脂质体Celastrol可降低前列腺癌细胞的活力,同时消除对有毒增溶剂的需要。

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