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Diaryl heptane dimers, pharmaceutical composition thereof, and preparation method and application of two

A technology of diarylheptane and dimer, applied in the field of medicine, can solve the problem of no compound and the like, and achieve the effects of convenient operation, high yield and simple and easy preparation method

Active Publication Date: 2022-01-14
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] So far, the prior art has no myristyl alcohol C 1 -C 10 (katsumadainols C 1 -C 10 , 1-10) report, also do not have the report of compound 1-10 and pharmaceutical composition thereof as GLP-1 secretagogue and GPa, PTP1B and alpha-glucosidase inhibitor, and in the preparation hypoglycemic medicine or health food reports on applications in

Method used

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  • Diaryl heptane dimers, pharmaceutical composition thereof, and preparation method and application of two
  • Diaryl heptane dimers, pharmaceutical composition thereof, and preparation method and application of two
  • Diaryl heptane dimers, pharmaceutical composition thereof, and preparation method and application of two

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Preparation of Compound 1-10:

[0032] Dried seeds (20kg) of Cardamom grassa, crushed, extracted twice with 90% ethanol under reflux, each time for 2 hours, combined ethanol extracts, recovered ethanol under reduced pressure to obtain extract. The extract was dispersed in water and extracted with ethyl acetate, then concentrated to the ethyl acetate extract. Then the ethyl acetate extract (Fr.A, 1.5kg) was subjected to silica gel column chromatography, and methanol-chloroform (0:100, 2:98, 5:95, 10:90, 20:80 and 100:0, v / v) Eight fractions of Fr.A-1 to Fr.A-8 were obtained by gradient elution of the eluent. Fr.A-7 (50g) was obtained by MCI CHP 20P gel column chromatography (methanol-water, 30:70, 40:60, 50:50, 70:30, 100:0, v / v) to obtain Fr.A -7-1~Fr.A-7-6. Fr.A-7-2 (15g) was purified by silica gel column chromatography (MeOH-CHCl 3 , 10:90 and 20:80) obtained Fr.A-7-2a~Fr.A-7-2e. Fr.A-7-2c (5g) was purified by Sephadex LH-20 (chloroform-methanol, 50:50), silica g...

Embodiment 2

[0154] Compounds promote GLP-1 secretion and GPa, PTP1B, TCPTP and α-glucosidase inhibitory activity.

[0155] 1 Materials and methods

[0156] 1.1 Materials

[0157] STC-1 cells were purchased from ATCC, USA; α-glucosidase and GPa were purchased from Sigma Aldrich (St.Louis, MO, USA); phosphate buffer (≥99%, Meilun Biotech, Dalian); p-nitrobenzene Base-α-D-glucopyranose (≥99%, Yuanye Biotechnology, Shanghai); Acarbose (≥98%, Bayer Pharma, Beijing); PTP1B (protein tyrosine phosphatase) and TCPTP (T- Cell tyrosine phosphatase) was purchased from Sino Biological (Wayne, PA, USA); suramin sodium was purchased from ACROS (New Jersey USA); Hepes was purchased from Beijing Xiasi Biotechnology Co., Ltd. (Beijing); Lun Biotechnology Co., Ltd. (Dalian); α-D-glucose 1-phosphate disodium salt (St.Louis, MO, U.S.A.); ammonium molybdate was purchased from Shanghai Jiuding Chemical Co., Ltd. (Shanghai); malachite green was purchased from China Beijing Balingwei Technology Co., Ltd. (Beij...

preparation Embodiment

[0181] 1. Take any one or any combination of compounds 1-10, dissolve it with a small amount of DMSO, add water for injection as usual, fine filter, potting and sterilize to make an injection.

[0182] 2. Take any one of compounds 1-10 or any combination thereof, dissolve it in a small amount of DMSO, dissolve it in sterile water for injection, stir to dissolve, filter with a sterile suction filter funnel, and then filter aseptically, Packed in ampoules, freeze-dried at low temperature and sealed aseptically to obtain powder injection.

[0183] 3. Take any one of the compounds 1-10 or any combination thereof, and add the excipient at a ratio of 9:1 by weight to the excipient to make a powder.

[0184] 4. Take any one of compounds 1-10 or any combination thereof, add excipients at a weight ratio of 5:1 to excipients, granulate and compress into tablets.

[0185] 5. Take any one of compounds 1-10 or any combination thereof, and make oral liquid according to the conventional ora...

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Abstract

The invention provides ten novel diaryl heptane dimers shown in a structural formula (I), namely katsumadainol C1-C10 1-10, a pharmaceutical composition with the katsumadainol C1-C10 as an active ingredient, and a preparation method and application of the two , and belongs to the technical field of medicines. Thedimers can significantly promote GLP-1 secretion, has GPa, PTP1B and alpha-glucosidase inhibitory activity, can form a pharmaceutical composition with a pharmaceutically acceptable carrier or excipient, and can be used for preparing hypoglycemic drugs or health food.

Description

Technical field: [0001] The invention belongs to the technical field of medicines. Specifically, 10 novel diarylheptane dimers, myristyl alcohol C 1 -C 10 (katsumadainols C 1 -C 10 , 1-10), with compound 1-10 as the pharmaceutical composition of active ingredient, their preparation method, and its application in the preparation of GLP-1 secretagogue medicine, in the preparation of GPa, PTP1B and α-glucosidase The application in inhibitor drugs, and the application in the preparation of hypoglycemic drugs or health food. Background technique: [0002] Type 2 diabetes (Type 2diabetes mellitus, T2DM), as a complex metabolic disease, has become a major global health problem. Due to long-term high blood sugar, type 2 diabetes often leads to serious complications, such as retinopathy, kidney disease, high blood pressure, etc. Currently, there are 7 oral hypoglycemic agents on the market, including biguanides, α-glucosidase inhibitors, insulin secretory agents, insulin sensit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/04C07D309/10A61K31/351A61K31/35A61P3/10A23L33/105
CPCC07D493/04C07D309/10A61P3/10A23L33/105C07B2200/07A23V2002/00A23V2200/328A23V2300/14A23V2300/38Y02A50/30
Inventor 耿长安陈纪军何小凤李天泽张雪梅黄晓燕马云保胡敬
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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