Application of E ring iodine substituted silybin to preparing glycosidase inhibitors

[0023] Example 1: Compound of formula (1) (±)-2-[2,3-dihydro-3-(3-iodo-4-hydroxy-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] UV spectra were measured with a Shimadzu UV-240 UV spectrophotometer; 1H NMR spectroscopy 1 H-NMR was determined by INOVA type superconducting nuclear magnetic resonance spectrometer (VARIAN INOVA-400MHz) (tetramethylsilyl ether TMS as internal standard); electrospray mass spectrometry ESI-MS was determined by BrukerEsquire 3000+ mass spectrometer, and silica gel was used for column chromatography (100-200, 200-300 and 300-400 mesh) and silica gel GF254 (10-40 mesh) for thin layer chromatography are produced by Qingdao Ocean Chemical Factory; all reagents used are of analytical grade; thin layer chromatography (PTLC) ) with the aluminum foil silica gel plate of Merck company; Sephadex LH-20 for column chromatography adopts the pr

[0033] Example 2 : Compound (1)(±)-2-[2,3-dihydro-3-(3-iodo-4-hydroxy-5-methoxyphenyl)-2-hydroxymethyl-1,4-benzene Determination of Inhibitory Activity of Dioxane-6-]-2,3-dihydro-3,5,7-trihydroxy-4H-1-benzopyran-4-one on α-glucosidase

[0034] 2.1 Instruments and Reagents

[0035] 2.1.1 Experimental instrument

[0036] Microplate reader: ELISA plate reader (Bio-Tek Instruments, USA)

[0037] 2.1.2 Reagents

[0038] α-glucosidase, α-D-glucosidase (Sigma, 500U / ml); 4-nitrophenol-α-D-glucopyranoside (PNPG, Merck), reduced glutathione (Shanghai Shenggong) , Acarbose is Baitangping (Bayer Health Care Co., Ltd., Beijing).

[0039] 2.2 Test method

[0040] The inhibitory effect of compounds on α-glucosidase was determined by colorimetric method: phosphate buffer (67 mmol / L, pH 6.8, 170 μL) was added to the sample well, reduced glutathione (1 mg / mL, 5 μl), α-D-glucosidase (diluted to 0.2 U / ml with phosphate buffer, 25 μl), compound (1) was dissolved in dimethyl sulfoxide, d