The food dye FD&C Blue No. 1 (Brilliant Blue FCF [BB FCF]) is structurally similar to the purinergic receptor antagonist Brilliant Blue G (BBG), which is a well-known inhibitor of the ionotropic P2X7 receptor (P2X7R). The P2X7R functionally interacts with the membrane channel protein pannexin 1 (Panx1) in inflammasome signaling. Intriguingly, ligands to the P2X7R, regardless of whether they are acting as agonists or antagonists at the receptor, inhibit Panx1 channels. Thus, because both P2X7R and Panx1 are inhibited by BBG, the diagnostic value of the drug is limited. Here, we show that the food dye BB FCF is a selective inhibitor of Panx1 channels, with an IC50 of 0.27 µM. No significant effect was observed with concentrations as high as 100 µM of BB FCF on P2X7R. Differing by just one hydroxyl group from BB FCF, the food dye FD&C Green No. 3 exhibited similar selective inhibition of Panx1 channels. A reverse selectivity was observed for the P2X7R antagonist, oxidized ATP, which in contrast to other P2X7R antagonists had no significant inhibitory effect on Panx1 channels.Based on its selective action, BB FCF can be added to the repertoire of drugs to study the physiology of Panx1 channels. Furthermore, because Panx1 channels appear to be involved directly or indirectly through P2X7Rs in several disorders, BB FCF and derivatives of this “safe” food dye should be given serious consideration for pharmacological intervention of conditions such as acute Crohn’s disease, stroke, and injuries to the central nervous system.
Three carbazole dicationic salts, namely 3,6-bis(1-methyl-4-vinylpyridinium) carbazole diiodide (BMVC), 9-ethyl-3,6-bis(1-methyl-4-vinylpyridinium) carbazole diiodide (9E-BMVC) and 9-ethyl-3,6-bis(1-hydroxyethyl-4-vinylpyridinium)carbazole diiodide (9E-BHVC), were synthesized successfully. Their photophysical properties were evaluated by absorption, one- and two-photon fluorescence spectra, and their higher fluorescence intensity and larger two-photon excited fluorescence action cross-sections (Φ×δ) in the presence of DNA than those in the absence of DNA give them good DNA two-photon light-switch properties. Furthermore, their ability to image nuclei in living plant cells and turbid tissues by using two-photon excited fluorescence was carefully studied, and the experimental results indicate that these dicationic salts can exclusively label nuclei in intact living plant cells and tissues. In particular, 9E-BHVC exhibits optimized DNA labeling performance. Very importantly, compared to DAPI, 9E-BHVC can be used to carry out deeper observation using the same incident power, or can be used to obtain usable fluorescent images by using a lower incident power.
To systematically explore the influence of the bulky aromatic ring skeleton with a large conjugated pi-system on the structures and properties of their complexes, six CuII, CoII, and NiII complexes with the anthracene-based carboxylic ligand anthracene-9-carboxylic acid (HL1), were synthesized and characterized, sometimes incorporating different auxiliary ligands: [Cu2(L1)4(CH3OH)2](CH3OH) (1), [Cu4(L1)6(L2)4](NO3)2(H2O)2 (2), {[Cu2(L1)4(L3)](CH3OH)0.25}infinity (3), [Co2(L1)4(L4)2(micro-H2O)](CH3OH) (4), {[Co(L1)2(L5)(CH3OH)2]}infinity (5), and {[Ni(L1)2(L5)(CH3OH)2]}infinity (6) (L2 = 2,2'-bipyridine, L3 = 1,4-diazabicyclo[2.2.2]octane, L4 = 1,10-phenanthroline, and L5 = 4,4'-bipyridine). 1 has a dinuclear structure that is further assembled to form a one-dimensional (1D) chain and then a two-dimensional (2D) network by the C-H...O H-bonding and pi...pi stacking interactions jointly. 2 takes a tetranuclear structure due to the existence of the chelating L2 ligand. 3 possesses a 1D chain structure by incorporating the related auxiliary ligand L3, which is further interlinked via interchain pi...pi stacking, resulting in a three-dimensional (3D) network. 4 also has a dinuclear structure and then forms a higher-dimensional supramolecular network through intermolecular pi...pi stacking and/or C-H...pi interactions. 5 and 6 are isostructural complexes, except they involve different metal ions, showing 1D chain structures, which are also assembled into 2D networks from the different crystallographic directions by interchain pi...pi stacking and C-H...pi interactions, respectively. The results reveal that the steric bulk of the anthracene ring in HL1 plays an important role in the formation of 1-6. The magnetic properties of the complexes were investigated, and the very long intermetallic distances result in weak magnetic coupling, with the exception of 1 and 3, which adopt the typical paddle-wheel structure of copper acetate and are thus strongly coupled.
Hepatocellular carcinoma (HCC), which is one of the three major cancers, has attracted growing attention due to its high mortality, health care cost, and circumscribed therapeutic methods. Hence, the development of a fast, accurate, and flexible method to detect α-fetoprotein (AFP), the specific marker of HCC, is significant for diagnosis and treatment of cancer. Here, we constructed a novel SERS biosensing platform combining the target-responsive DNA hydrogel for the sensitive detection of AFP. The linker strand in DNA hydrogel is an aptamer that can specifically recognize AFP and accurately control the release of immunoglobulin G (IgG) encapsulated in hydrogel. In the presence of AFP, the hydrogels were disentangled and the IgG was released. Thereafter, the released IgG was captured by SERS probes and biofunctional magnetic beads through formation of sandwich-like structures, resulting in the signal of Raman tags decreasing in the supernatant after magnetic separation. Due to the ultrahigh sensitivity of the SERS biosensor, the proposed method has a wide detection linear range (50 pg/mL to 0.5 μg/mL) and a detection limit down to 50 pg/mL. Moreover, the sequence of the linker strand in the DNA hydrogel can be specifically encoded into a new aptamer that responds to other cancer markers. This convenient and inexpensive detection method provides a new strategy for the detection of tumor markers.
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