Method for preparing quercetin derivative containing benzylpiperazine and gastric mucosal protection effect of quercetin derivative
A technology of benzylpiperazine and quercetin is applied in the field of preparation method of quercetin derivatives containing benzylpiperazine and its protective effect on gastric mucosa, and can solve the limitation of clinical application of quercetin, large intermolecular attraction, low bioavailability
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Embodiment 1
[0021] Example 1: quercetin derivatives containing benzylpiperazine: 8-((4-benzylpiperazine-1-yl)methyl)-2-(3,4-dihydroxyphenyl-3,5 , Preparation of 7-trihydroxy-4H-chroman-4-one (target compound).
[0022]
[0023]
[0024] Add 302 mg of quercetin, 25 mL of absolute ethanol, and 0.08 mL of 37% formaldehyde solution into a 50 mL round-bottomed flask; heat to 58 ± 3 °C, after the reaction solution is clear, add 174 μL of 1-benzylpiperazine; seal, Magnetic stirring was carried out at room temperature for 72 hours, and the progress of the reaction was detected by thin layer chromatography. After the reaction, the precipitated solid was filtered, recrystallized from methanol:chloroform = 1:1, separated and purified to obtain the target compound. The target compound is mixed with sodium carboxymethylcellulose, and the mass ratio of the target substance in the mixture is 1.42%, which can be used as a functional food or medicine for protecting gastric mucosa damage; the target c...
Embodiment 2
[0026] Embodiment 2: Quercetin derivatives containing benzylpiperazine: 8-((4-benzylpiperazine-1-yl)methyl)-2-(3,4-dihydroxyphenyl-3,5 , Preparation of 7-trihydroxy-4H-chroman-4-one (target compound).
[0027] Add 302 mg of quercetin, 25 mL of absolute ethanol, and 0.08 mL of 37% formaldehyde solution into a 50 mL round-bottomed flask; heat to 58 ± 3 °C, after the reaction solution is clear, add 191 μL of 1-benzylpiperazine; seal, The reaction was stirred magnetically at room temperature for 72 hours. After the reaction, the precipitated solid was filtered, and the solid was recrystallized by methanol:chloroform=1:1, and the target compound was separated and purified. The target compound is mixed with carboxymethyl cellulose sodium, and the mass ratio of the target substance in the mixture is 59%, which can be used as a functional food or medicine for protecting gastric mucosa damage; the target compound is dissolved in 1% carboxymethyl cellulose sodium solution , the concen...
Embodiment 3
[0029] Example 3: Study on the protective effect of quercetin derivatives containing benzylpiperazine on gastric mucosal injury
[0030] 1. Experimental materials and methods
[0031] 1.1 Drugs and reagents
[0032] 70% ethanol, CMC (sodium carboxymethylcellulose), etc. are analytical reagents, and ranitidine was purchased from Hongrentang Pharmacy. Synthesized target compound in embodiment 1.
[0033] 1.2 Animals
[0034] SD rats 100-200g, male, purchased from Lukang, animal production license SCXK (Lu) 20130001.
[0035] 1.3 Experimental method
[0036] 1.3.1 Animal grouping and model preparation
[0037] The animals were randomly divided into six groups, 8 rats in each group, at 25°C and 70% humidity.
[0038] The treatment groups and experimental protocol are detailed as follows:
[0039] (1) Reagent control group. 0.5% CMC 1mL was administered orally at 0, 24, 48, and 49 hours, and the rats were killed at 50 hours.
[0040] (2) Ethanol group. 0.5% CMC 1mL wa...
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