Flavanol-menthane hybrid and pharmaceutical composition thereof, preparation method and application thereof
A technology of flavanol and menthane, which is applied in the field of flavanol-menthane hybrids, and can solve the problems of compounds 1-8 and their pharmaceutical compositions, etc.
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Embodiment 1
[0028] Preparation of compounds 1-8:
[0029] The dried fruit of Caojiao was crushed and extracted three times with 50% ethanol under reflux for 2 hours each time. The ethanol extracts were combined, and the ethanol was recovered under reduced pressure to obtain the extract. The extract was dispersed in water and extracted with ethyl acetate, and then concentrated to the ethyl acetate extraction part. The ethyl acetate extraction fraction (Fr.A) was then subjected to silica gel column chromatography, eluting with methanol-chloroform (0:100, 5:95, 10:90, 20:80 and 40:60, v / v) Fr.A-1~Fr.A-7 were obtained by gradient elution of Fr.A-7. Fraction Fr.A-6 was subjected to MCI CHP 20P gel column chromatography (methanol-water, 40:60, 60:40, 80:20). and 100:0) to obtain four subfractions Fr.A-6-1 to Fr.A-6-4. Fr.A-6-2 was subjected to silica gel column chromatography (MeOH-CHCl) 3 , 2:98) obtained three subfractions Fr.A-6-2-1~Fr.A-6-2-2. Fr.A-6-2-2 (2.2g) was subjected to Sephadex...
Embodiment 2
[0126] PTP1B and α-glucosidase inhibitory activity
[0127] 1 Materials and methods
[0128] 1.1 Materials
[0129] α-Glucosidase (Sigma Aldrich, St.Louis, MO, USA); Phosphate buffer (≥99%, Meilun Bio, Dalian); p-nitrophenyl-α-D-glucopyranose (≥99 %, Yuanye Bio, Shanghai); Acarbose (≥98%, Bayer Pharmaceuticals, Beijing); PTP1B (Protein Tyrosine Phosphatase) was purchased from Sino Biological (Wayne, PA, USA); Suramin sodium was purchased From ACROS (New Jersey USA)
[0130] 1.2 Instruments
[0131] Flex Station 3 benchtop multi-plate reader (Bio-RAD 680, USA); analytical balance (AG135, Metler Toledo, China); incubator (DHP-9082, Shanghai).
[0132] 1.3 Experimental process
[0133] The PTP1B inhibitory activity was performed according to previous studies by the inventors. Briefly, working buffer (WB) was composed of 3-(N-morpholino)propanesulfonic acid (MOPS, 722.02 mg), dithiothreitol (DTT, 30 mg), EDTA (25.7 mg), It was prepared by dissolving bovine serum albumin (BS...
Embodiment 1～8
[0145] In the following formulation examples, conventional reagents are selected and preparations are prepared according to existing conventional methods. This example only reflects that at least one of the compounds 1 to 8 of the present invention can be prepared into different formulations. The operation is not specifically limited:
[0146] 1. After dissolving at least one of the compounds 1 to 8 prepared in Example 1 with DMSO, adding water for injection according to conventional methods, fine filtration, potting and sterilizing to prepare an injection, the concentration of the injection is 0.5 ~5 mg / mL.
[0147] 2. After dissolving at least one of the compounds 1 to 8 prepared in Example 1 with DMSO, dissolve it in sterile water for injection, stir to dissolve it, filter it with a sterile suction filter funnel, and then sterilize it. Filtered, packed in ampoules, freeze-dried at low temperature and aseptically fused to obtain powder injection.
[0148] 3. At least one o...
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