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Novel Near-Infrared Hypocrellin Derivatives for Synergistic Photodynamic and Photothermal Therapy.
Chemistry - An Asian Journal ( IF 3.5 ) Pub Date : 2020-09-10 , DOI: 10.1002/asia.202000911 Ying Ding 1, 2 , Weimin Liu 1, 2 , Jiasheng Wu 1 , Xiuli Zheng 1 , Jiechao Ge 1, 2 , Haohui Ren 1 , Wenjun Zhang 3 , Chun-Sing Lee 3 , Pengfei Wang 1, 2
Chemistry - An Asian Journal ( IF 3.5 ) Pub Date : 2020-09-10 , DOI: 10.1002/asia.202000911 Ying Ding 1, 2 , Weimin Liu 1, 2 , Jiasheng Wu 1 , Xiuli Zheng 1 , Jiechao Ge 1, 2 , Haohui Ren 1 , Wenjun Zhang 3 , Chun-Sing Lee 3 , Pengfei Wang 1, 2
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Hypocrellin B (HB) derived from naturally produced hypocrellins has attracted considerable attention in photodynamic therapy (PDT) because of its excellent photosensitive properties. However, the weak absorption within a “phototherapy window” (600–900 nm) and poor water solubility of HB have limited its clinical application. In this study, two HB derivatives (i. e., HE and HF) were designed and synthesized for the first time by introducing two different substituent groups into the HB structure. The obtained derivatives showed a broad absorption band covering the near‐infrared (NIR) region, NIR emission (peaked at 805 nm), and singlet oxygen quantum yields of 0.27/0.31. HE‐PEG‐NPs were also prepared using 2‐distearoyl‐sn‐glycero‐3‐phosphoethanolamine‐N‐[methoxy(polyethyleneglycol)‐2000] (DSPE‐mPEG2000) to achieve excellent dispersion in water and further explored their practical applications. HE‐PEG‐NPs not only retained their 1O2‐generating ability, but also exhibited a photothermal conversion efficiency of 25.9%. In vitro and in vivo therapeutic results revealed that the synergetic effect of HE‐PEG‐NPs on PDT and photothermal therapy (PTT) could achieve a good performance. Therefore, HE‐PEG‐NPs could be regarded as a promising phototheranostic agent.
中文翻译：
用于协同光动力和光热疗法的新型近红外hypocrellin衍生物。
天然产生的hypercrellins衍生的hypocrellin B（HB）由于其出色的感光性能而在光动力疗法（PDT）中引起了广泛的关注。但是，“光疗窗口”（600-900 nm）内吸收弱，HB的水溶性差，限制了其临床应用。在该研究中，通过将两个不同的取代基引入HB结构中，首次设计和合成了两种HB衍生物（即，HE和HF）。获得的衍生物显示出覆盖近红外（NIR）区域的宽吸收带，NIR发射（在805 nm处达到峰值）和单重态氧量子产率为0.27 / 0.31。HE‐PEG‐NP还使用2-二硬脂酰基-sn-甘油-3-磷酸乙醇胺-N- [甲氧基（聚乙二醇）-2000]（DSPE-mPEG2000）制备了它们，以实现在水中的优异分散性，并进一步探索了它们的实际应用。HE-PEG-NPs不仅保留了其1 O 2生成能力，而且还表现出25.9％的光热转化效率。体外和体内治疗结果表明，HE-PEG-NPs对PDT和光热疗法（PTT）的协同作用可以达到良好的性能。因此，HE‐PEG‐NPs可以被认为是一种有前途的光热敏剂。
更新日期：2020-11-04
中文翻译：
用于协同光动力和光热疗法的新型近红外hypocrellin衍生物。
天然产生的hypercrellins衍生的hypocrellin B（HB）由于其出色的感光性能而在光动力疗法（PDT）中引起了广泛的关注。但是，“光疗窗口”（600-900 nm）内吸收弱，HB的水溶性差，限制了其临床应用。在该研究中，通过将两个不同的取代基引入HB结构中，首次设计和合成了两种HB衍生物（即，HE和HF）。获得的衍生物显示出覆盖近红外（NIR）区域的宽吸收带，NIR发射（在805 nm处达到峰值）和单重态氧量子产率为0.27 / 0.31。HE‐PEG‐NP还使用2-二硬脂酰基-sn-甘油-3-磷酸乙醇胺-N- [甲氧基（聚乙二醇）-2000]（DSPE-mPEG2000）制备了它们，以实现在水中的优异分散性，并进一步探索了它们的实际应用。HE-PEG-NPs不仅保留了其1 O 2生成能力，而且还表现出25.9％的光热转化效率。体外和体内治疗结果表明，HE-PEG-NPs对PDT和光热疗法（PTT）的协同作用可以达到良好的性能。因此，HE‐PEG‐NPs可以被认为是一种有前途的光热敏剂。
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