In recent years, the research on fluorescent probes has developed rapidly. Coumarin fluorescent probes have also been one of the hot topics in recent years. For the synthesis and application of coumarin fluorescent probes, great progress has been made. Coumarin fluorescent probes have become more and more widely used in biochemistry, environmental protection, and disease prevention, and have broad prospects. This review introduces the three main light emitting mechanisms (PET, ICT, FRET) of fluorescent probes, and enumerates some probes based on this light emitting mechanism. In terms of the synthesis of coumarin fluorescent probes, the existing substituents on the core of coumarin compounds were modified. Based on the positions of the modified substituents, some of the fluorescent probes reported in the past ten years are listed. Most of the fluorescent probes are formed by modifying the 3 and 7 position substituents on the mother nucleus, and the 4 and 8 position substituents are relatively less modified. In terms of probe applications, the detection and application of coumarin fluorescent probes for Cu2+, Hg2+, Mg2+, Zn2+, pH, environmental polarity, and active oxygen and sulfide in the past ten years are mainly introduced.
As Lewis acids, boronic acids can bind with 1,2- or 1,3-diols in aqueous solution reversibly and covalently to form five or six cyclic esters, thus resulting in significant fluorescence changes.
10 April 2023 in Journal of Enzyme Inhibition and Medicinal Chemistry
Flavonoids are ubiquitous compounds in nature and are found in many Chinese herbal medicines. Due to their biological activity, flavonoids show potential for decreasing insulin resistance (IR), thereby delaying the progression of diabetes and accompanying metabolic syndromes. This review focuses on the mechanisms of flavonoids decreasing IR: (1) the interaction between flavonoids and target proteins of the insulin signalling pathway; (2) bioactivities of flavonoids, such as anti-inflammatory, lipid-lowering and antioxidant. Meanwhile, we summarise the structural characteristics, structure activity relationships and biological activity of flavonoids, providing evidence for their potential in the treatment of IR. Here, we also analyse the potential and limitations of their therapeutic use.
Zero-dimensional (0D) black phosphorus quantum dots (BPQDs), the new derivatives of black phosphorus (BP) nanomaterials, have attracted considerable attention since they were first prepared in 2015. Compared to traditional two-dimensional (2D) BP nanosheets, BPQDs exhibit some unique properties and demonstrate great potential for a broad range of applications, especially in the field of biomedicine. Due to the rapid development and substantial research interest in this area, it is urgent to review the current advances, challenges and near-future possibilities of BPQD-related biomedical research, which will benefit the further development of this field. This review is mainly focused on the latest progress of BPQD related applications in the biomedical field, including photothermal therapy (PTT), photodynamic therapy (PDT), drug delivery, biological imaging, etc. The challenges and future prospects are also discussed.
1 January 2019 in Journal of Enzyme Inhibition and Medicinal Chemistry
The work is focused on the design of drugs that prevent and treat Alzheimer’s disease (AD) and its complications. A series of 3–(4-aminophenyl)-coumarin derivatives designed, synthesised, fully characterised and evaluated in vitro/vivo. The biological assay experiments showed that some compounds displayed a clearly selective inhibition for acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Among all compounds, compound 4m exhibited the highest AChE inhibition with an IC50 value of 0.091 ± 0.011 µM and compound 4k exhibited the highest BuChE inhibition with an IC50 value of 0.559 ± 0.017 µM. A zebrafish behaviour analyser (Zebrobox) was used to determine the behavioural effects of the active compound on the movement distance of the aluminium chloride-induced zebrafish. Compound 4m offered a potential drug design concept for the development of therapeutic or preventive agents for AD and its complications.