利用逆电子需求 Diels-Alder 反应的生物正交胶束纳米反应器用于前药癌症治疗。
Bioorthogonal micellar nanoreactors for prodrug cancer therapy using an inverse-electron-demand Diels-Alder reaction.
机构信息
Department of Chemistry and Materials, Faculty of Textile Science and Technology, Shinshu University, 3-15-1, Tokida, Ueda, Nagano, 386-8567, Japan.
Department of Chemistry and Biochemistry, University of Kitakyushu, 1-1, Hibikino, Kitakyushu, Fukuoka, 808-0135, Japan.
出版信息
Chem Commun (Camb). 2022 Jun 21;58(50):7026-7029. doi: 10.1039/d2cc02121h.
Block copolymer micelles functionalized with tetrazine groups can act as nanoreactors to activate a -cyclooctene-functionalized prodrug for releasing anticancer drugs a bioorthogonal inverse-electron-demand Diels-Alder (IEDDA) reaction. In addition, the IEDDA reaction can be accelerated in the micellar nanoreactor system compared to the free tetrazine system. Moreover, prodrug activation in a mouse tumor model led to the inhibition of tumor growth without significant systemic toxicity. These results demonstrated their potential for applications as bioorthogonal micellar nanoreactors for cancer chemotherapy.
四嗪基团功能化的嵌段共聚物胶束可以作为纳米反应器，激活 -环辛烯功能化的前药，释放抗癌药物，进行生物正交的逆电子需求 Diels-Alder (IEDDA) 反应。此外，与游离四嗪体系相比，该 IEDDA 反应在胶束纳米反应器体系中可以加速。此外，在小鼠肿瘤模型中前药的激活导致肿瘤生长的抑制，而没有明显的全身毒性。这些结果表明它们具有作为用于癌症化疗的生物正交胶束纳米反应器的应用潜力。
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