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Medicinal application of querecetin dipolymer flavonoids to preparation of glycosidase enzyme inhibitors
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A technology of quercetin and dimer, which is applied in the field of pharmaceutical use of quercetin dimer flavonoids for the preparation of glycosidase inhibitors, and can solve the problem of dimer biological activity and pharmaceutical use that have not been reported, α-glucose Glucosidase inhibitory activity has not been reported and other problems, and achieved the effect of clear industrialization prospect, strong inhibition of α-glucosidase, and simple and easy preparation method
Inactive Publication Date: 2012-08-22
DALI UNIV
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[0006] Quercetin is a kind of flavonol. Previous research results have reported that quercetin has inhibitory activity on aldose reductase. However, there are relatively few literatures on its inhibition of glycosidase and treatment of diabetes, especially its effect on α- The inhibitory activity of glucosidase has not been reported
Hirose et al. found that quercetin can also form a dimer (Chemistry Letters, 1999, 8, 775-776), but there is no report on the biological activity and pharmaceutical use of the dimer
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Embodiment 1
[0019] Example 1 : the preparation of formula (1) compound
[0020] 1.1 Instruments and reagents:
[0021] The ultraviolet spectrum was measured with a Shimadzu UV-240 ultraviolet spectrophotometer; the hydrogen nuclear magnetic resonance spectrum1 H-NMR is measured by INOVA type superconducting nuclear magnetic resonance spectrometer (VARIAN INOVA-400MHz) (tetramethylsilyl ether TMS is the internal standard); electrospray mass spectrometry ESI-MS is measured by Bruker Esquire 3000+ mass spectrometer, column chromatography Silica gel (100-200, 200-300 and 300-400 mesh) and silica gel GF254 (10-40 mesh) for thin-layer chromatography are all produced by Qingdao Ocean Chemical Factory; All reagents used are analytically pure; thin-layer preparative chromatography ( PTLC) uses the aluminum foil silica gel plate of Merck Company; Sephadex LH-20 used for column chromatography adopts the product of Amersham Pharmacia Biotech AB Company in Sweden; Reversed-phase silica gel RP-18 adop...
Embodiment 2
[0025] Example 2 : Compound (1) is tested for the inhibitory activity of α-glucosidase
[0026] 2.1 Instruments and reagents:
[0027] 2.1.1 Experimental Instruments
[0028] Microplate reader: ELISA plate reader (Bio-Tek Instruments, USA)
[0032] The inhibitory effect of compounds on α-glucosidase was determined by colorimetric method. Add phosphate buffer (67 mmol / L, pH6.8, 170 microliters), reduced glutathione (1 mg / ml, 5 microliters), α-D-glucosidase (with phosphate buffer Diluted to 0.2U / ml, 25 microliters), compound (1) was dissolved in dimethyl sulfoxide, diluted with phosphate buffer, 25 microliters per hole, so that the final concentration was 0.04 mg / ml, 0.004 mg / ml, 0.0004 mg / ml, finally add the ...
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Abstract
The invention relates to medicinal application of querecetin dipolymer flavonoids to preparation of glycosidase enzyme inhibitors, in particular to medicinal application of querecetin dipolymer flavonoids or medicinal salts thereof to preparation of medicaments for inhibiting alpha-glucuroide and preventing and curing II type diabetes mellitus. The querecetin dipolymer flavonoids has very obviousactivity of inhibiting the alpha-glucuroide, and when the concentration of the querecetin dipolymer flavonoids is 4 mcg / ml, the alpha-glucuroide inhibiting strength of the querecetin dipolymer flavonoids reaches 75.0%; and the measurement on the half inhibiting concentration of the querecetin dipolymer flavonoids shows that the alpha-glucuroide inhibiting strength of the querecetin dipolymer flavonoids is 88 times of that of acarbose as a positive control medicament. The pharmacodynamics result indicates that the querecetin dipolymer flavonoids or the medicinal salts thereof can be expected to be used for preparing a glycosidase inhibitor medicament, and especially the medicaments for preventing and curing the II type diabetes mellitus.
Description
technical field [0001] The present invention relates to the technical field of medicine, in particular, the present invention relates to a quercetin dimer flavonoid or a pharmaceutically acceptable salt thereof for the preparation of α-glucosidase-inhibiting, prevention and treatment of type II diabetes, that is, non-insulin-dependent diabetes mellitus purposes in medicine, the quercetin dimer flavone has extremely significant inhibitory activity of α-glucosidase, and its inhibitory activity intensity to α-glucosidase has reached 75.0% at a concentration of 4 μg / ml, passed Determination of its half maximal inhibitory concentration shows: the intensity of the quercetin dimer flavone inhibiting α-glucosidase is 88 times that of the positive control drug acarbose, so the compound or its pharmaceutically acceptable salt, and the preparation allow The pharmaceutical composition prepared from the pharmaceutical excipient or carrier can be expected to be used as a glycosidase inhibit...
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