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Adenine-Functionalized Supramolecular Micelles for Selective Cancer Chemotherapy.
Macromolecular Bioscience ( IF 4.4 ) Pub Date : 2020-09-01 , DOI: 10.1002/mabi.202000233
Fasih Bintang Ilhami,Yihalem Abebe Alemayehu,Wen-Lu Fan,Hsieh-Chih Tsai,Chen-Yu Kao,Chih-Chia Cheng

Functional supramolecular micelles containing self‐complementary multiple hydrogen bonding adenine groups (A‐PPG) can spontaneously self‐assemble into stable nanosized micelles in aqueous solution. These micelles can be used to selectively deliver anticancer drugs to cancer cells and effectively promote tumor cell death via apoptosis, without harming normal cells. The drug‐loaded micelles exhibit tunable drug‐loading capacity and rapid pH‐triggered drug release under acidic conditions, as well as a high drug‐entrapment stability in serum‐rich media due to the reversible hydrogen‐bonded adenine–adenine interactions within the micellar interior; these properties are critical to achieving effective chemotherapeutic drug delivery and controlled drug release. In vitro assays show that the drug‐loaded micelles exert significant cytotoxic effects on cancer cells, with minimal effects on normal cells under physiological conditions. Cytotoxicity assays using A‐PPG micelles loaded with different anticancer drugs confirm these effects. Importantly, cellular internalization and flow cytometric analyses demonstrate that the adenine moieties within A‐PPG micelles significantly increase selective endocytic uptake of the supramolecular micelles by cancer cells, which in turn induce apoptotic cell death and substantially enhance the response to chemotherapy. Thus, A‐PPG micelles can improve the safety and efficacy of cancer chemotherapy.

中文翻译:

用于选择性癌症化疗的腺嘌呤功能化超分子胶束。

含有自互补多重氢键腺嘌呤基团(A-PPG)的功能性超分子胶束可以在水溶液中自发自组装成稳定的纳米胶束。这些胶束可用于选择性地向癌细胞递送抗癌药物,并通过凋亡有效促进肿瘤细胞死亡,而不会伤害正常细胞。由于胶束内可逆的氢键腺嘌呤-腺嘌呤相互作用,载药胶束在酸性条件下表现出可调的载药能力和快速的 pH 触发药物释放,以及在富含血清的介质中的高药物包封稳定性内部的; 这些特性对于实现有效的化学治疗药物递送和控制药物释放至关重要。体外试验表明,载药胶束对癌细胞具有显着的细胞毒作用,在生理条件下对正常细胞的影响很小。使用装载不同抗癌药物的 A-PPG 胶束的细胞毒性测定证实了这些作用。重要的是,细胞内化和流式细胞术分析表明,A-PPG 胶束中的腺嘌呤部分显着增加了癌细胞对超分子胶束的选择性内吞作用,进而诱导细胞凋亡并显着增强了对化疗的反应。因此,A-PPG 胶束可以提高癌症化疗的安全性和有效性。重要的是,细胞内化和流式细胞术分析表明,A-PPG 胶束中的腺嘌呤部分显着增加了癌细胞对超分子胶束的选择性内吞作用,进而诱导细胞凋亡并显着增强了对化疗的反应。因此,A-PPG 胶束可以提高癌症化疗的安全性和有效性。重要的是,细胞内化和流式细胞术分析表明,A-PPG 胶束中的腺嘌呤部分显着增加了癌细胞对超分子胶束的选择性内吞作用,进而诱导细胞凋亡并显着增强了对化疗的反应。因此,A-PPG 胶束可以提高癌症化疗的安全性和有效性。
更新日期:2020-09-01
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