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Core-Cross-Linking of Polymeric Micelles by Di-para-Substituted S-Aroylthiooximes as Linkers for Controlled H2S Release
ACS Macro Letters ( IF 5.1 ) Pub Date : 2022-04-18 , DOI: 10.1021/acsmacrolett.2c00137 Fan Rong 1 , Tengjiao Wang 1 , Kun Wang 1 , Qian Zhou 1 , Haowei Peng 1 , Peng Li 1
ACS Macro Letters ( IF 5.1 ) Pub Date : 2022-04-18 , DOI: 10.1021/acsmacrolett.2c00137 Fan Rong 1 , Tengjiao Wang 1 , Kun Wang 1 , Qian Zhou 1 , Haowei Peng 1 , Peng Li 1
Affiliation
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As one of the gasotransmitters, the therapeutic effects of hydrogen sulfide (H2S) were reported widespread in recent years. Considering the short physiological half-life and significant dose-dependent effects of H2S, it is vital to achieve controlled H2S delivery for biomedical applications. Polymeric micelles have been explored to regulate H2S delivery. However, the dilution-induced dissociation of micelles in physiological conditions limits their therapeutic effects. The circulation stability of polymeric micelles could be improved through core-cross-linking, but reduced H2S releasing efficiency is usually unavoidable. To solve these problems, we developed di-para-substituted S-aroylthiooximes (p-diSATOs) as linkers, which integrated cross-linking of micelle core and conjugation of H2S donors through one simple reaction. Compared with SATO-bearing non-cross-linked micelle, the core-cross-linked micelle (CCM) prepared through this method exhibited initial rapid H2S release owing to the electron-withdrawing effect of p-diSATOs, and subsequently, a sustained release could last for a long period of time. Considering the characteristic H2S releasing behavior of CCM, it may accelerate wound healing through initial efficient and subsequent prolonged pro-healing effects. As a proof of concept, we explored the therapeutic potential of CCM using a murine burn wound model, which exhibited pro-healing effect on burn wounds.
中文翻译：
双对位取代的 S-芳酰基硫肟作为控制 H2S 释放的连接物对聚合物胶束的核心交联
作为气体递质之一，硫化氢（H 2 S）的治疗作用近年来被广泛报道。考虑到 H 2 S的短生理半衰期和显着的剂量依赖性效应，实现生物医学应用的受控 H 2 S 输送至关重要。聚合物胶束已被探索以调节 H 2 S 的传递。然而，在生理条件下稀释诱导的胶束解离限制了它们的治疗效果。通过核交联可以提高聚合物胶束的循环稳定性，但降低H 2 S 释放效率通常是不可避免的。为了解决这些问题，我们开发了双对位取代S-芳酰基硫肟（p -diSATOs）作为接头，通过一个简单的反应将胶束核心的交联和H 2 S供体的缀合结合起来。与含有SATO的非交联胶束相比，通过该方法制备的核心交联胶束（CCM）由于p - diSATOs的吸电子作用而表现出最初的快速H 2 S释放，随后，释放可能会持续很长时间。考虑到特征 H 2CCM 的 S 释放行为，它可以通过最初的有效和随后延长的促愈合作用加速伤口愈合。作为概念验证，我们使用小鼠烧伤伤口模型探索了 CCM 的治疗潜力，该模型对烧伤伤口表现出促进愈合的作用。
更新日期：2022-04-18
中文翻译：
双对位取代的 S-芳酰基硫肟作为控制 H2S 释放的连接物对聚合物胶束的核心交联
作为气体递质之一，硫化氢（H 2 S）的治疗作用近年来被广泛报道。考虑到 H 2 S的短生理半衰期和显着的剂量依赖性效应，实现生物医学应用的受控 H 2 S 输送至关重要。聚合物胶束已被探索以调节 H 2 S 的传递。然而，在生理条件下稀释诱导的胶束解离限制了它们的治疗效果。通过核交联可以提高聚合物胶束的循环稳定性，但降低H 2 S 释放效率通常是不可避免的。为了解决这些问题，我们开发了双对位取代S-芳酰基硫肟（p -diSATOs）作为接头，通过一个简单的反应将胶束核心的交联和H 2 S供体的缀合结合起来。与含有SATO的非交联胶束相比，通过该方法制备的核心交联胶束（CCM）由于p - diSATOs的吸电子作用而表现出最初的快速H 2 S释放，随后，释放可能会持续很长时间。考虑到特征 H 2CCM 的 S 释放行为，它可以通过最初的有效和随后延长的促愈合作用加速伤口愈合。作为概念验证，我们使用小鼠烧伤伤口模型探索了 CCM 的治疗潜力，该模型对烧伤伤口表现出促进愈合的作用。
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