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Application of E ring iodine substituted silybin to preparing glycosidase inhibitors
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A technology of silibinin esters and medicines, which is applied in the field of medicines where E-ring iodine replaces silibinin for the preparation of glycosidase inhibitors, can solve the problems of diabetes without glycosidase inhibition, and achieve a clear industrialization prospect , Conducive to energy saving and emission reduction, the effect of simple and easy preparation method
Inactive Publication Date: 2012-08-22
DALI UNIV
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But it is obvious: the above studies have only focused on the antioxidant and cytoprotective effects of silybin flavonoid lignans
[0007] Although the flavonoid lignan compounds represented by silibinin and dehydrosilibinin have the above-mentioned antioxidant effects, there are no reports on their use in inhibiting glycosidase and treating diabetes
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Embodiment 1
[0023] Example 1: Formula (1) compound (±)-2-[2,3-dihydro-3-(3-iodo-4-hydroxyl-5-methoxyphenyl)-2-hydroxymethyl-1,4-benzene Preparation of dioxane-6-]-2,3-dihydro-3,5,7-trihydroxy-4H-1-benzopyran-4-one
[0024] 1.1 Instruments and reagents:
[0025] The ultraviolet spectrum was measured with a Shimadzu UV-240 ultraviolet spectrophotometer; the hydrogen nuclear magnetic resonance spectrum 1 H-NMR is measured by INOVA type superconducting nuclear magnetic resonance spectrometer (VARIAN INOVA-400MHz) (tetramethylsilyl ether TMS is the internal standard); (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; the reagents used are all 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 of Sweden; Reversed-pha...
Embodiment 2
[0033] Example 2 : Compound (1) (±)-2-[2,3-dihydro-3-(3-iodo-4-hydroxy-5-methoxyphenyl)-2-hydroxymethyl-1,4-benzene Inhibitory activity of dioxane-6-]-2,3-dihydro-3,5,7-trihydroxy-4H-1-chromen-4-one on α-glucosidase
[0034] 2.1 Instruments and reagents
[0035] 2.1.1 Experimental Instruments
[0036] Microplate reader: ELISA plate reader (Bio-Tek Instruments, USA)
[0040] The inhibitory effect of compound on α-glucosidase is determined by colorimetry: add phosphate buffer (67 mmol / liter, pH6.8, 170 microliters), reduced glutathione (1 mg / ml, 5 microliters), α-D-glucosidase (diluted to 0.2U / ml with phosphate buffer, 25 microliters), compound (1) was dissolved in dimethyl sulfoxide, diluted with phosphate buffer...
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Abstract
The invention relates to application of E ring iodine substituted silybin to preparing glycosidase inhibitors and in particular discloses application of E ring iodine substituted silybin ester-type flavonolignans or pharmaceutical salt thereof to preparing drugs for inhibiting alpha-glycosidase and preventing and treating type II diabetes. The flavonolignans has extremely obvious activity for inhibiting alpha-glycosidase and the intensity of activity of the 40mcg / ml flavonolignans for inhibiting alpha-glycosidase reaches 64.1%. The measured half-inhibitory concentration of the flavonolignans shows that the intensity of activity of the flavonolignans for inhibiting alpha-glycosidase is 35 times that of the positive control drug acarbose. The pharmacodynamics result shows that the flavonolignans or pharmaceutical salt thereof can be expected to be applied to preparing glycosidase inhibitors, especially the drugs for preventing and treating type II diabetes.
Description
technical field [0001] The present invention relates to the technical field of medicine, in particular, the present invention relates to a kind of silibinin ester type flavonoid lignan substituted by E-ring iodine or its pharmaceutically acceptable salt for preparing α-glucosidase-inhibiting, preventing and treating type II Diabetes, that is, non-insulin-dependent diabetes drugs, the flavonoid lignans have a very significant inhibitory activity of α-glucosidase, and its inhibitory activity to α-glucosidase at a concentration of 4 micrograms per milliliter has been Reach 64.1%, show by measuring its half maximal inhibitory concentration: the intensity that this flavonoid lignan inhibits α-glucosidase is 35 times that of positive control drug acarbose, therefore this compound or its pharmaceutically acceptable salt, and with The pharmaceutical composition prepared from the pharmaceutical excipients or carriers allowed by the formulation can be expected to be used as a glycosidas...
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