Application of polyhydroxybenzopyrrole derivatives
A technology of polyhydroxybenzopyrone and its derivatives, which is applied in the field of medicine and can solve problems such as unseen factors or anti-blood coagulation
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Embodiment 1
[0044] Example 1: Determination of the inhibitory activity of polyhydroxybenzophenone derivatives to FXa
[0045] The test product was prepared as follows:
[0046] The compound of formula I was prepared with DMSO to 100mmol / Lol / L, and then diluted 4 times. The corresponding final concentrations of the system were 1000μmol / L, 250μmol / L, 62.5μmol / L, and 15.625μmol / L.
[0047] The compound of formula II was prepared with DMSO to 100mmol / Lol / L, and then diluted 10 times. The corresponding final concentrations of the system were 1000μmol / L, 100μmol / L, 10μmol / L, 1μmol / L.
[0048] The compound of formula III is formulated with DMSO to 1mmol / Lol / L, and then diluted 3 times, the corresponding final concentration of the system is 10μmol / L, 3.33μmol / L, 1.11μmol / L, 0.37μmol / L, 0.123μmol / L, 0.041μmol / L.
[0049] Rivaroxaban was prepared with DMSO to 1 μmol / L, and then diluted 3 times, the corresponding final concentrations of the system were 10nmol / L, 3.33nmol / L, 1.11nmol / L, 0.37nmol / L...
Embodiment 2
[0053] Example 2: Determination of the inhibition kinetics of polyhydroxybenzophenone derivatives to FXa
[0054] Prepare different concentrations of the test substance with DMSO, so that the concentrations in the above reaction system are respectively:
[0055] Compound of formula III: 300nM, 150nM;
[0056] Compound of formula II: 160 μmol / L, 80 μmol / L;
[0057] Formula I compound: 160 μmol / L, 80 μmol / L;
[0058] Then prepare different concentrations of FXa fluorescent substrates (4mmol / L, 2mmol / L, 1mmol / L, 0.5mmol / L, 0.25mmol / L, 0.125mmol / L);
[0059] Each concentration of the test product corresponds to 6 groups of FXa substrates. According to the change of fluorescence intensity, V is obtained, and the corresponding substrate concentration S is used by the Lineweaver-Burk method, with 1 / s as the abscissa and 1 / V as the ordinate Make graphs according to the L-B equation. The result is as figure 2 shown.
[0060] The results show that the fitting straight lines of ea...
Embodiment 3
[0061] Embodiment three: the mensuration of activated partial thromboplastin time (APTT)
[0062] The test product was prepared as follows:
[0063] Compounds of formula I to formula III were prepared in DMSO to 10mmol / L, and then diluted with physiological saline, and each compound was obtained as a solution of 1mmol / L and 400μmol / L for use;
[0064] Rivaroxaban was prepared with DMSO to 10mmol / L, and then diluted with normal saline to 10μmol / L for use;
[0065] Heparin sodium was prepared with normal saline to 75U / ml for use.
[0066] Collect rabbit blood quickly and put it in a container with 109mmol / L sodium citrate solution in advance. The ratio of sodium citrate solution to blood volume is 1:9. While collecting, shake gently and mix well. Centrifuge for 15 minutes, and immediately separate the plasma. Then put the test cup with a steel ball in the pre-warming position of the semi-automatic coagulation analyzer, take 50ul of plasma, 50ul of the test product (or saline)...
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