A nanocarbon-enabled hybridization strategy to construct pharmacologically cooperative therapeutics for augmented anticancer efficacy,Chemical Science

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A nanocarbon-enabled hybridization strategy to construct pharmacologically cooperative therapeutics for augmented anticancer efficacy
Chemical Science ( IF 7.6 ) Pub Date : 2024-09-03 , DOI: 10.1039/d4sc05280c
Huan Wang ₁ , Xinchen Liu ₂ , Xiangyu Yan ₃ , Yong Du ₃ , Fang Pu ₁ , Jinsong Ren ₁ , Xiaogang Qu ₁

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The drug design principles are of great value in developing nanomedicines with favorable functionalities. Herein we propose a nanocarbon-enabled hybridization strategy to construct a pharmacologically cooperative nanodrug for improved cancer therapy in the light of pharmacophore hybridization in medicinal chemistry and the synthetic principles of nanocarbons. An antioxidant defense pharmacological inhibitor and a co-nucleation precursor are structurally hybridized into nanodrugs (SCACDs) via forming carbon quantum dots. These SCACDs elicit dual enhanced bioactivities, including superior sonocatalytic activity that arose from the appropriate band structure of the pharmacophoric carbon cores, and more than an order of magnitude higher antioxidant defense inhibitory activity than the pharmacological inhibitor via conveying the bioactive pharmacophores from the molecular level to nanoscale. In vivo, SCACDs possess a long body retention and desirable biodistribution to eliminate melanoma cells at a very low injection dose. The present study provides a viable yet effective strategy for the development of pharmacologically cooperative nanodrugs to achieve remarkably improved therapeutic efficacy.

中文翻译：

纳米碳杂交策略构建药理学协同疗法以增强抗癌功效

药物设计原理对于开发具有良好功能的纳米药物具有重要价值。在此，我们提出了一种纳米碳杂交策略，根据药物化学中的药效团杂交和纳米碳的合成原理，构建药理学协同纳米药物，以改善癌症治疗。抗氧化防御药理学抑制剂和共核前体通过形成碳量子点在结构上杂交成纳米药物（SCACD）。这些 SCACD 具有双重增强的生物活性，包括由药效团碳核的适当能带结构产生的卓越声催化活性，以及通过将生物活性药效团从分子水平传递到药理学抑制剂，抗氧化防御抑制活性比药理学抑制剂高一个数量级以上。纳米级。在体内，SCACD 具有较长的体内滞留性和理想的生物分布，可以以非常低的注射剂量消除黑色素瘤细胞。本研究为开发药理学协同纳米药物以显着提高治疗效果提供了可行且有效的策略。

更新日期：2024-09-03

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