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Reduction-Triggered Doxorubicin Delivery by Self-Assembled Nanospheres of Lipoylated Caffeine.
ChemMedChem ( IF 3.6 ) Pub Date : 2020-04-02 , DOI: 10.1002/cmdc.202000070 Krishan Kumar 1 , Bharti Rajesh Kumar Shyamlal 1 , Rajbala Verma 2 , Paturu Kondaiah 3 , Sandeep Chaudhary 1
ChemMedChem ( IF 3.6 ) Pub Date : 2020-04-02 , DOI: 10.1002/cmdc.202000070 Krishan Kumar 1 , Bharti Rajesh Kumar Shyamlal 1 , Rajbala Verma 2 , Paturu Kondaiah 3 , Sandeep Chaudhary 1
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This study reports a new amphiphilic bioconjugate (CAFF-LA) derived from the lipoylation of a hydroxyethyl derivative of caffeine. In water, CAFF-LA self-assembles into nanospheres with an average size of 155 nm, as evidenced from dynamic light scattering and electron microscopy studies. The nanospheres are stable in serum and could be disintegrated upon exposure to the reducing environment of dithiothreitol (DTT; 10 mM) and glutathione (GSH; 10 mM). These nanospheres easily encapsulate the chemotherapy medication, doxorubicin (DOX), and demonstrate an efficacious transport into doxorubicin-resistant cervical cancer (HeLa) cells, wherein a marked induction in apoptosis and significantly lower IC50 have been observed when compared to that of free drug. The in vitro assessment of cell viability and hemocompatibility present these nanospheres as potentially safe and efficient intracellular reduction stimulus-responsive drug-delivery vehicles.
中文翻译：
脂质体化咖啡因的自组装纳米球的还原触发阿霉素传递。
这项研究报告了一种新的两亲生物共轭物（CAFF-LA），其衍生自咖啡因的羟乙基衍生物的脂酰化。在水中，CAFF-LA自组装成平均大小为155 nm的纳米球，这通过动态光散射和电子显微镜研究得到了证明。纳米球在血清中是稳定的，并且在暴露于二硫苏糖醇（DTT； 10 mM）和谷胱甘肽（GSH； 10 mM）的还原环境中时可能崩解。这些纳米球易于封装化疗药物阿霉素（DOX），并证明可有效转运至耐阿霉素的宫颈癌（HeLa）细胞，与自由药物相比，已观察到明显的细胞凋亡诱导作用和IC50明显降低。
更新日期：2020-04-02
中文翻译：
脂质体化咖啡因的自组装纳米球的还原触发阿霉素传递。
这项研究报告了一种新的两亲生物共轭物（CAFF-LA），其衍生自咖啡因的羟乙基衍生物的脂酰化。在水中，CAFF-LA自组装成平均大小为155 nm的纳米球，这通过动态光散射和电子显微镜研究得到了证明。纳米球在血清中是稳定的，并且在暴露于二硫苏糖醇（DTT； 10 mM）和谷胱甘肽（GSH； 10 mM）的还原环境中时可能崩解。这些纳米球易于封装化疗药物阿霉素（DOX），并证明可有效转运至耐阿霉素的宫颈癌（HeLa）细胞，与自由药物相比，已观察到明显的细胞凋亡诱导作用和IC50明显降低。
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