Cyclopropenone-based Platform for Light-directed Drug Delivery, Photo-medicine, and Bio-imaging

在这个项目的化学结构，动力学和机制B计划的化学部，教授弗拉基米尔Popik化学系在格鲁吉亚（UGA）开发新的光化学反应，具有潜在的应用药物输送和激活。基础化学是基于有机分子进行光诱导解离，其中一氧化碳是产物之一。由于组织的不透明性限制了治疗中可以传递到目标区域的光量，Popik教授探索了通过量子链反应提高光诱导分子释放效率的方法。这是一个过程，其中一个光包（光子）导致多个分子被释放。 这种策略可以允许局部恶性肿瘤的选择性治疗，同时避免常见化疗的常见副作用。该项目为学生提供合成和物理有机化学以及光化学和生物化学的跨学科培训。通过UGA Young Dawgs Program在Popik教授的实验室进行暑期实习的高中生接触到现代科学研究。结晶态环丙烯酮的光脱羰反应的量子效率是溶液的数倍，可以超过400%。Popik教授探索了量子产率放大现象的机制和控制环丙烯酮晶体中能量传播过程的参数。利用量子链式反应，每吸收一个光子就可以产生几个分子的产物。这样的光反应在预期的应用中是特别重要的，其中光传递受到介质的不透明性或散射特性的阻碍。特别设计的环丙烯酮衍生物的纳米晶悬浮液允许量子产率放大的实际应用。晶体的共价表面衍生化和晶体尺寸的控制允许制备稳定的悬浮液或胶体溶液，并提供对纳米晶体的运输和生物分布性质的控制。使用环丙烯酮纳米晶体悬浮液的生物活性底物的光导向递送提供了非常高的光敏性、控制生物分布的能力，并且伴随着一氧化碳的释放，其本身是一种重要的生物活性剂，也是一种有价值的抗-该奖项反映了NSF的法定使命，并通过使用基金会的知识价值和更广泛的影响审查标准。

In this project supported by the Chemical Structure, Dynamics, and Mechanisms-B Program of the Chemistry Division, Professor Vladimir Popik of the Department of Chemistry at the University of Georgia (UGA) develops new photochemical reactions which have potential applications for drug delivery and activation. The fundamental chemistry is based on organic molecules which undergo light-induced dissociation, and where carbon monoxide is one of the products. Since the opacity of tissues limits the amount of light that can be delivered to target areas in therapy, Professor Popik explores methods to boost the efficiency of the photo-induced released of molecules with the body through a quantum chain reaction. This is a process in which one packet (photon) of light causes multiple molecules to be released. This strategy may allow for the selective treatment of localized malignancies, while avoiding common side effects of common chemotherapies. The project provides students with interdisciplinary training at the interface of synthetic and physical organic chemistry, as well as photochemistry and biochemistry. High school students conducting summer internship in Professor Popik's laboratory via the UGA Young Dawgs Program are exposed to modern scientific research.The quantum efficiency of the photodecarbonylation reaction of cyclopropenones in the crystalline state is several times higher than in solution, and could exceed 400%. Professor Popik explores the mechanism of the quantum yield amplification phenomenon and parameters that control the energy propagation process in cyclopropenone crystals. Harnessing the quantum chain reaction allows for the production of several molecules of the product per one photon absorbed. Such photoreactions are especially important in the expected applications, where light delivery is hampered by the opacity or scattering properties of the medium. Nanocrystalline suspensions of specially designed cyclopropenone derivatives permit practical use of the quantum yield amplification. The covalent surface derivatization of the crystals and control of the size of the crystals allows for the preparation of stable suspensions or colloidal solutions and provides control over the transport and bio-distribution properties of nanocrystals. Light-directed delivery of bioactive substrates using cyclopropenone nanocrystalline suspensions offers very high light sensitivity, ability to control bio-distribution, and is accompanied by the release of carbon monoxide, which is an important bio-active agent in itself as well as a valuable adjuvant for anti-cancer antibiotics.This award reflects NSF's statutory mission and has been deemed worthy of support through evaluation using the Foundation's intellectual merit and broader impacts review criteria.