关键词: Cancer cell Photocage Reactive oxygen species Rhodamine B

Mesh : Prodrugs / chemistry pharmacology chemical synthesis Humans Antineoplastic Agents / pharmacology chemistry chemical synthesis Rhodamines / chemistry Drug Liberation Fluorescent Dyes / chemistry chemical synthesis Reactive Oxygen Species / metabolism analysis Drug Design Light Cell Line, Tumor

来  源:   DOI:10.1016/j.talanta.2024.126002

Abstract:
Developing probes for simultaneous diagnosis and killing of cancer cells is crucial, yet challenging. This article presents the design and synthesis of a novel Rhodamine B fluorescence probe. The design strategy involves utilizing an anticancer drug (Melphalan) to bind with a fluorescent group (HRhod-OH), forming HRhod-MeL, which is non-fluorescent. However, when exposed to the high levels of reactive oxygen species (ROS) of cancer cells, HRhod-MeL transforms into a red-emitting Photocage (Rhod-MeL), and selectively accumulates in the mitochondria of cancer cells, where, when activated with green light (556 nm), anti-cancer drugs released. The Photocage improve the efficacy of anti-cancer drugs and enables the precise diagnosis and killing of cancer cells. Therefore, the prepared Photocage can detect cancer cells and release anticancer drugs in situ, which provides a new method for the development of prodrugs.
摘要:
开发同时诊断和杀死癌细胞的探针至关重要,但具有挑战性。本文介绍了一种新型罗丹明B荧光探针的设计与合成。设计策略涉及利用抗癌药物(美法仑)与荧光基团(HRhod-OH)结合,形成HRhod-MeL,它是非荧光的。然而,当暴露于癌细胞的高水平活性氧(ROS)时,HRhod-MeL转化为红色发光光子库(Rhod-MeL),并选择性地积累在癌细胞的线粒体中,where,当用绿光(556nm)激活时,抗癌药物发布。Photocage可提高抗癌药物的疗效,并能够精确诊断和杀死癌细胞。因此,所制备的Photocage可以检测癌细胞并原位释放抗癌药物,为开发前药提供了新的方法。
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