The medical use of 7-hydroxy-butylphthalide
A technology of butylphthalide and hydroxyl, which is applied in the field of medicinal chemistry, can solve the problems that the compound has no anti-oxidation, anti-thrombotic and anti-cerebral ischemia effects, and achieve superior anti-platelet aggregation efficacy and high maximum tolerated dose And the toxic dose, the effect of significant antithrombotic effect
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Embodiment 1
[0031] Example 1. Preparation of 7-hydroxy-butylphthalide, 4-hydroxy-butylphthalide and 7-methoxy-butylphthalide
[0032] For the preparation of 7-hydroxy-butylphthalide, 4-hydroxy-butylphthalide and 7-methoxy-butylphthalide, refer to the patent CN201510113631.9, and the Penicillium foxense strain NCC3421 (has been deposited in the collection of common microorganism species in China) Management Center, the preservation number is CGMCC No. 9094) Inoculated in a fermentor equipped with 30L fermentation medium at a temperature of 26 ℃, stirring at 220 rpm, and culturing for 120 h. The obtained culture was centrifuged at 4000 rpm for 20 min, the hyphae were collected, extracted with industrial ethanol, and filtered to obtain the filtrate. The above-mentioned filtrate was diluted with water to an ethanol concentration of 40%, adsorbed on a column with 2L D312 resin, and then eluted with 40%, 55%, and 70% ethanol respectively, and received in parts, combined the parts containing the ta...
Embodiment 2
[0038] Example 2. In vitro anti-platelet aggregation activity
[0039] (1) Experimental method: Evaluation of anti-platelet aggregation activity, with ADP as the inducer, and Born turbidimetric method. Wistar rats (Animal Center of Hebei Medical University, Laboratory Animal Certificate Number: 1304152) orbital blood, anticoagulated with 3.8% sodium citrate (volume ratio of whole blood to anticoagulant 9:1), centrifuged at room temperature ( 500~800 rpm, 10 min), prepare platelet-enriched plasma (PRP), after separating PRP, centrifuge again (3000 rpm, 15 min), prepare platelet-poor plasma (PPP), adjust 0 with PPP. Take PRP (200 μL) and add 5 μL of DMSO solution of equimolar concentration of the target compound, add an equal volume of DMSO to the solvent control group, incubate for 2 min, use 10 μM ADP as an inducer, and measure platelet aggregation reaction according to Born turbidimetric method. The target compound was tested for its anti-platelet aggregation activity in vitro,...
Embodiment 3
[0044] Example 3. In vitro antioxidant capacity
[0045] (1) Experimental materials and methods
[0046] Determination of total reducing power: add 0.5 mL of 0.2 mol / L pH 6.6 phosphate buffer solution and 2.5 mL of potassium ferricyanide with a mass fraction of 1% to 1 mL of samples of different concentrations, and bathe in water at 50 ℃ for 20 min. After rapid cooling in an ice bath, add 2.5 mL of 10% trichloroacetic acid solution, centrifuge at 3000 r / min for 10 min, take the supernatant 1.0 mL, add 1.0 mL distilled water and 0.1% FeCl 3 0. 2mL, mix well, stand at room temperature for 10 minutes, measure the absorbance value at a wavelength of 700 nm, determine the reducing power based on the absorbance value, and calculate the reducing power %.
[0047] Ability to scavenge superoxide anion free radicals: Take different volumes of samples and add 50 mM Tris-HCl buffer with pH 8.2 to prepare solutions of different concentrations. Place the above solution in a constant temperature ...
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