N-(tetrahydro-beta-carboline-3-formyl)-N'-amino acid hydrazides, and nanometer structures, activity and application thereof
An amino acid acyl hydrazide and amino acid acyl technology, which can be applied in the fields of blood diseases, extracellular fluid diseases, organic chemistry, etc., and can solve the problems of non-soluble P-selectin
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Embodiment 1
[0021] Example 1 Docking to obtain N-[(1S,3S)-1-methyl-1,2,3,4-tetrahydro-β-carboline-3-formyl]-N'-amino acid acylhydrazine
[0022] Based on the active pocket of the average structure of P-selectin established by the inventor, the inventor constructed a pharmacophore model based on the receptor structure, and confirmed that the structure of the small molecule ligand should conform to figure 2 The five pharmacophore characteristic elements of . Including 1 hydrophobic center (No. 1 grid ball), 2 hydrogen bond acceptors (No. 2 grid ball), and 2 positively charged ion centers (No. 3 grid ball). According to these structural requirements, the compound library with antithrombotic activity was screened to determine that N-[(1S,3S)-1-methyl-1,2,3,4-tetrahydro-β-carboline-3-formyl ]-N'-Amino acid hydrazine is a suitable ligand type. The amino acid acyl group of N-[(1S,3S)-1-methyl-1,2,3,4-tetrahydro-β-carboline-3-formyl]-N'-amino acid hydrazine is L-serine acyl and L-tryptophan a...
experiment example 1
[0024] Experimental example 1 measures the transmission electron micrograph of N-[(1S, 3S)-1-methyl-1,2,3,4-tetrahydro-β-carboline-3-formyl]-N'-amino acid acylhydrazine
[0025] N-[(1S,3S)-1-methyl-1,2,3,4-tetrahydro-β-carboline-3-formyl]-N'-amino acid acylhydrazine (amino acid acyl is L-serine acyl, and amino acid acyl is L-tryptophan acyl) according to 1×10 -6 The concentration of M was prepared as a pure aqueous solution, spread evenly on the copper grid, and the self-assembly properties of the compound were observed under a transmission electron microscope (TEM, JEM-1230, JEOL). Get photos like Figure 5 . The results showed that they could form nanoparticles with a diameter of 20-100 nm in water.
experiment example 2
[0026] Experimental Example 2 Determination of N-[(1S, 3S)-1-methyl-1,2,3,4-tetrahydro-β-carboline-3-formyl]-N'-amino acid acylhydrazine for P-selection Inhibition of
[0027] 1. Draw P-selectin standard curve
[0028] According to the instructions of the P-selectin ELISA kit (USA CUSABIOCO), the P-selectin standard solution was prepared in a 96-well enzyme-labeled plate by the stepwise dilution method. The solution volume in each well was 50 μL, and the final concentration of P-selectin was 600ng / mL, 300ng / mL, 150ng / mL, 75ng / mL, 37.5ng / mL, 18.75ng / mL and 9.37ng / mL. The OD value was measured on a microplate reader. Each concentration was repeated twice, and the average value was calculated. Draw a P-selectin standard curve.
[0029] 2. Preparation of Platelet Samples
[0030] Healthy SD male rats (body weight 180-220g) were anesthetized with urethane, and blood was collected through the carotid artery. The blood was anticoagulated with 3.8% sodium citrate aqueous solutio...
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