Use of rutacaractone as a histone deacetylase inhibitor
A technology for evodiolide and application, which is applied in the directions of medical preparations, applications, and drug combinations containing active ingredients, and can solve problems such as evodiolide that have not yet been seen
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Embodiment 1
[0013] Example 1: Inhibition of Evodicarpalactone on Histone Deacetylases (HDACs)
[0014] The HDACs kit was used to test the inhibitory activity of Evodia lactone on HDACs, and SAHA was used as the positive control drug. Add bovine serum albumin, HDAC fluorescent substrate, HDACs enzymes (HDAC1, HDAC6, HDAC8) and different concentrations (1×10 -10 , 1×10 -9 , 1×10 -8 , 1×10 -7 , 1×10 -6 , 1×10 - 5 mol L -1 ) of the test compound. After reacting the test plate at 37°C for 30min, add HDAC Developer to each well, and continue to place it at 37°C for 15min, use a microplate reader to measure the fluorescence value of each well at the wavelength of 359nm and 440nm, and then compare the values of each drug concentration The fluorescence values at each concentration were linearly regressed to obtain the dose-response equation, and the IC of Evodia lactone and SAHA were calculated accordingly. 50 value. The results are shown in Table 1.
[0015] Table 1 The ICs of test...
Embodiment 2
[0018] Example 2: Antitumor activity of rutaecaractone
[0019] Gastric cancer BGC-3, lung cancer A549 and liver cancer HepG2 cells were selected as the test cell lines, SAHA was used as the positive control drug, and MTT method was used to evaluate the antitumor activity of evodicarpallide.
[0020] The test cell lines in the logarithmic growth phase were suspended in phenol red-free DMEM medium containing 10% fetal bovine serum, and spread into 96-well culture plates. After the cells were completely adhered to the wall, the original culture solution was discarded, and 100 μL of the culture solution containing the test drug was added (the concentration gradient was 1×10 -8 , 1×10 -7 , 1×10 -6 , 1×10 -5 , 1×10 -4 mol L -1 ) after culturing for 3 days, add 30 μL of 5 mg·mL to each well -1 MTT, continue to incubate in the incubator for 4 hours, then add 100 μL dimethyl sulfoxide to each well to dissolve, use a microplate reader to measure the absorbance value of each well ...
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