4 research outputs found
New Biosensor for Determination of Neuropilin-1 with Detection by Surface Plasmon Resonance Imaging
Neuropilin-1 is transmembrane protein with soluble isoforms. It plays a pivotal role in both physiological and pathological processes. NRP-1 is involved in the immune response, formation of neuronal circuits, angiogenesis, survival and migration of cells. The specific SPRI biosensor for the determination of neuropilin-1 was constructed using mouse monoclonal antibody that captures unbound NRP-1 form body fluids. The biosensor exhibits linearity of the analytical signal between 0.01 and 2.5 ng/mL, average precision value 4.7% and recovery between 97% and 104%. The detection limit is 0.011 ng/mL, and the limit of quantification is 0.038 ng/mL. The biosensor was validated by parallel determination of NRP-1 in serum and saliva samples using the ELISA test, with good agreement of the results
General Synthesis of Unsymmetrical 3,3′-(Aza)diindolylmethane Derivatives
Diindolylmethane
(DIM) and its derivatives have recently been in
the focus of interest due to their significant biological activities,
specifically in cancer prevention and therapy. Molecular targets of
DIM have been identified, e.g., the immunostimulatory G protein-coupled
receptor GPR84. However, most of the reported and investigated DIM
derivatives are symmetrical because general methods for obtaining
unsymmetrical DIMs have been lacking. To optimize the interaction
of DIM derivatives with their protein targets, unsymmetrical substitution
is required. In the present study we developed a new, mild and efficient
access to unsymmetrically substituted 3,3′-DIMs by reaction
of (3-indolylmethyl)Âtrimethylammonium iodides with a wide range of
substituted indole derivatives. 7-Azaindole also led to the 3,3′-connected
DIM analogue, while 4- and 5-azaindoles reacted at the <i>N</i>1-nitrogen atom as confirmed by X-ray crystallography. The reactions
were performed in water without the requirement of a catalyst or other
additives. Wide substrate scope, operational simplicity, environmentally
benign workup, and high yields are further advantages of the new method.
The synthetic protocol proved to be suitable for upscaling to yield
gram amounts for pharmacological studies. This procedure will allow
the preparation of a broad range of novel, unsymmetrical DIM derivatives
to exploit their potential as novel drugs