PubMed · 14195147
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H TIMMEL, H F GERLACH. 1964. [ON STAINING THIN ESTER SECTIONS].. https://pubmed.ncbi.nlm.nih.gov/14195147/
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Commonly used dyes including Evans Blue and Trypan Blue were examined for their inhibitory activities against protein tyrosine phosphatases (PTPases), all of them showed inhibition of PTPases with different potencies. Of the 13 dyes tested, four exhibited IC(50) value of less than 10 microM, Evans Blue lowest IC(50) of 1.3 microM against PTP1B. Care must be taken in the use of dyes for clinical or biochemical experiments to avoid unwanted side effects. Some of the low molecular weight dyes might be useful as lead compounds for the development of potent and selective PTPase inhibitors.
The present work focused on the design of an assembled drug delivery system (DDS) to provide multifunctions, such as drug protection, self-regulated oscillatory release, and targeted uni-directional delivery by a bilayered self-folding gate and simple surface mucoadhesion. In this device, a pH-sensitive hydrogel together with a poly(hydroxyethyl methacrylate) (HEMA) barrier was used as a gate to control drug release. In addition, poly(HEMA) coated with poly(ethylene oxide)/poly(propylene oxide)/poly(ethylene oxide) (PEO-PPO-PEO) surfactant was utilized to enhance mucoadhesion on the device surface. The release profiles of two model drugs, acid orange 8 (AO8) and bovine serum albumin (BSA) were studied in this assembled system, which compared with the conventional drug-entrapped carriers and enteric-coating systems. Furthermore, targeted uni-directional release was demonstrated in a side-by-side diffusion cell. In conclusion, for such an assembled device, the poly(HEMA) layer not only affects the folding direction but also serves as a barrier to protect the model drugs. The release time can be controlled by the thickness of the bilayered gate and the drug reservoir. Due to the reversible swelling behavior of poly(methyacrylic acid-g-ethylene glycol) (p(MAA-g-EG)) gels, the bilayered gate can sense the environmental pH change and achieve an oscillatory release pattern. Moreover, the local targeting and uni-directional release have been successfully demonstrated in vitro.
The synthesis of dendritic multichromophores based on a rigid polyphenylene scaffold is presented. Different rylene chromophores are incorporated into the core, the branches, and the surface of the dendrimer. In this way, two generations of dendritic dyads consisting of a terrylenediimide core, a stiff polyphenylene scaffold, and a perylenemonoimide periphery were obtained. Furthermore, the first synthetic approach to a dendritic triad is introduced. The outer sphere of this macromolecule is formed by naphthalenemonoimide chromophores, whereas perylenemonoimide groups are located in the dendritic scaffold, and the terrylenediimide chromophore serves as a core molecule. This multichromophore absorbs over the whole range of the visible spectrum and shows well-separated absorption envelopes. In the course of dendrimer synthesis new attempts towards a straightforward functionalization strategy for rylene dyes are also presented.