Max Planck Institute for Polymer Research, Ackermannweg 10, 55128, Mainz, Germany.
Center for Translational Nanomedicine, Dermatology Clinic, University Medical Center of the Johannes Gutenberg University Mainz, Langenbeckstr. 1, 55131, Mainz, Germany.
Small. 2017 Dec;13(46). doi: 10.1002/smll.201700997. Epub 2017 Oct 12.
Enzyme activity is important for metabolism, cell functions, and treating diseases. However, remote control of enzyme activity in deep tissue remains a challenge. This study demonstrates near-infrared (NIR) light-regulated enzyme activity in living cells based on upconverting nanoparticles (UCNPs) and a photoactivatable Ru complex. The Ru complex is a caged enzyme inhibitor that can be activated by blue light. To prepare a nanocarrier for NIR photoinhibition of enzyme activity, a UCNP and the caged enzyme inhibitors are encapsulated in a hollow mesoporous silica nanoparticle. In such a nanocarrier, the UCNP can harvest NIR light and convert it into blue light, which can activate the caged enzyme inhibitors. This photoactivation process is feasible in deep tissue because of the tissue penetration ability of NIR light. The nanocarrier is compatible to LNCaP, PC3, and SAOS-2 cells, which show high enzyme expression. NIR irradiation induces release of the inhibitors and inhibition of enzyme activity in living cells. NIR light provides high spatiotemporal resolution to regulate enzyme activity in deep tissue.
酶活性对于新陈代谢、细胞功能和疾病治疗都很重要。然而，在深部组织中对酶活性进行远程控制仍然是一个挑战。本研究基于上转换纳米粒子（UCNPs）和光活化的 Ru 配合物，展示了近红外（NIR）光调控活细胞中酶活性的方法。Ru 配合物是一种被笼蔽的酶抑制剂，可以被蓝光激活。为了制备用于 NIR 光抑制酶活性的纳米载体，将 UCNP 和被笼蔽的酶抑制剂封装在中空介孔硅纳米粒子中。在这种纳米载体中，UCNP 可以收集近红外光并将其转化为蓝光，从而激活被笼蔽的酶抑制剂。由于近红外光具有组织穿透能力，这种光激活过程在深部组织中是可行的。该纳米载体与 LNCaP、PC3 和 SAOS-2 细胞兼容，这些细胞表现出高酶表达。近红外辐射诱导抑制剂的释放，并抑制活细胞中的酶活性。近红外光提供了高时空分辨率，可用于调节深部组织中的酶活性。
