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Extract of traditional Chinese medicine having alpha-glucosidase inhibitor activity and its application

A technology of glycosidase inhibitors and extracts, which is applied to traditional Chinese medicine extracts with α-glucosidase inhibitor activity and its application fields, and can solve problems such as no involvement of traditional Chinese medicine extracts, no involvement, unclear active ingredients and mechanism of action, etc. question

Active Publication Date: 2007-08-01
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Chinese patent ZL01113191.8 introduces "Chinese medicine extract with α-glucosidase inhibitor activity, its preparation method and use", but this patent does not involve the extraction and preparation of Chinese medicine extract from Guangdong Sangzong (M.atropurpurea Roxb.) , and no cytidine, 2-(1′,2′,3′,4′-tetrahydroxybutyl)-5-(2″,3″,4″-trihydroxybutyl)- Any of the chemical constituents of pyrazine and 1-deoxynojirimycin
Chinese patent ZL200410018677.4 describes "pharmaceutical composition with α-glucosidase inhibitory activity and its use", but this patent does not involve the preparation of traditional Chinese medicine extract from Guangdong mulberry (M.atropurpurea Roxb.), and the extract contains Cytidine, 2-(1′,2′,3′,4′-tetrahydroxybutyl)-5-(2″,3″,4″-trihydroxybutyl)-pyrazine and 1- Any of the chemical constituents of deoxynojirimycin
[0004] Guangdong mulberry (M.atropurpurea Roxb.) is the most widely distributed Morus plant in China and Guangdong. The extract of its leaves can significantly improve the symptoms of hyperglycemia in diabetic mice, and has a good hypoglycemic effect, and it has a significant dosage -Effect relationship, and the effect is better than the hypoglycemic drug glibenclamide, but its active ingredients and mechanism of action are unclear [Zou Yuxiao, Zheng Xiangming, Liao Sentai, etc. Research on the hypoglycemic effect of Sangning tea, Food Science, 2003, (7) :124-127]

Method used

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  • Extract of traditional Chinese medicine having alpha-glucosidase inhibitor activity and its application
  • Extract of traditional Chinese medicine having alpha-glucosidase inhibitor activity and its application
  • Extract of traditional Chinese medicine having alpha-glucosidase inhibitor activity and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment one, the preparation of extract

[0016] Dried 500 g of Guangdong mulberry leaf fine powder, extracted with 4 L of 60% ethanol under reflux for 2 hours, and filtered. Add 3 L of 60% ethanol to the filter residue for reflux extraction for 2 hours, and filter. Combine the extracts, recover until there is no ethanol smell, add an equal volume of ethanol, and centrifuge to remove the precipitate. The supernatant is passed through 732 (H+ type) strong acid ion exchange resin, and eluted with 2L of water and 4L of 0.5N ammonia water respectively. The ammonia water part is concentrated and dried 2g ninhydrin reaction is positive containing more than 10% cytidine, 2-(1', 2', 3', 4'-tetrahydroxybutyl)-5-(2", 3", 4"- Total alkaloid extract of trihydroxybutyl)-pyrazine and 1-deoxynojirimycin.

Embodiment 2

[0017] Embodiment two, the preparation of extract

[0018] Dried 2000g of Guangdong mulberry leaf fine powder, extracted by diafiltration with 20L 50% ethanol, combined the extracts, recovered until there was no ethanol smell, added an equal volume of ethanol, centrifuged to remove the precipitate, and the supernatant was passed through 732 (H+ type) strong acid ion exchange resin , respectively eluted with 3L of water and 6L of 0.5N ammonia water, and the ammonia water part was concentrated and dried to obtain 5 g of positive ninhydrin reaction containing more than 10% of cytidine, 2-(1', 2', 3', 4'-tetra The total alkaloid extract of hydroxybutyl)-5-(2″, 3″, 4″-trihydroxybutyl)-pyrazine and 1-deoxynojirimycin. The total alkaloid extract was passed through HZ-202 strong Basic ion exchange resin, HD-2 weakly acidic cation exchange resin, Dowex1 * 2 (OH-type) ion exchange resin, Sephadex LH-20 column chromatography separation obtains cytidine (96%, 32mg), 2-(1 ', 2', 3', 4'-te...

Embodiment 3

[0019] Embodiment three, the structure of compound

[0020] (1) The structure of cytidine is:

[0021]

[0022] Colorless needle crystal (methanol), C9H13N3O5, ninhydrin is purple. ESI-MS m / z: 266 [M+Na]+, 509 [2M+Na]+. 1H NMR (400MHz, D2O) δ: 7.90 (1H, d, J=7.6Hz, H-6), 6.04 (1H, d, J=7.6Hz, H-5), 5.78 (1H, d, J=3.6 Hz, H-1'), 4.23(1H, t, J=4.8Hz, H-2'), 4.11(1H, t, J=5.6Hz, H-3'), 4.05(1H, m, H- 4'), 3.84 (1H, dd, J=12.8, 2.4Hz, H-5a'), 3.72 (1H, dd, J=12.8, 4.4Hz, H-5b'). 13C NMR (100MHz, D2O) δ: 162.5(C-4), 153.1(C-2), 143.1(C-6), 95.6(C-5), 90.3(C-1'), 84.1(C-4 '), 74.0 (C-2'), 69.2 (C-3'), 60.6 (C-5').

[0023] (2) The structure of 2-(1′, 2′, 3′, 4′-tetrahydroxybutyl)-5-(2″, 3″, 4″-trihydroxybutyl)-pyrazine is:

[0024]

[0025]Colorless needle crystal (methanol), C27H32O14, ninhydrin was purple. ESI-MS m / z: 327 [M+Na]+, 303 [M-H]-. 1H NMR (400MHz, D2O) δ: 8.60 (1H, s, H-3), 8.42 (1H, s, H-6), 5.05 (1H, s, H-1'), 3.94 (1H, m, H -2"), 3.79-3.73(4H, m), 3.60...

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Abstract

The invention discloses anextract of Chinese herbs containing alpha-glycoside enzyme inhibitor, which comprises cytidine, 2-(1',2',3',4'-tetrahydroxylbutyl)-5-(2'',3'',4''-trihydroxybutyl)-pyrazine and 1-deoxynojirimycin. The extract can be obtained from leaves, branches and peels of mulberries. The extract can be used for preparing medicament for treating diabetes.

Description

technical field [0001] The invention relates to a traditional Chinese medicine extract with alpha-glucosidase inhibitor activity, a preparation method and a medical application thereof. Background technique [0002] Diabetes is a common endocrine and metabolic disease caused by genetic and environmental factors. According to the statistics of the World Health Organization (WTO), there are currently more than 150 million diabetic patients in the world, and the current diabetic patients in my country are about 20 million, and it is expected to reach about 40 million by 2025. Diabetes and its chronic complications have become the third major disease that seriously threatens human health after cardiovascular and cerebrovascular diseases and tumors. The treatment of diabetes mainly starts from several aspects such as promoting insulin secretion, improving insulin sensitivity, inhibiting the activity of glycoside hydrolase, and stimulating peroxisome proliferator-activated recept...

Claims

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Application Information

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IPC IPC(8): A61K31/7068A61K36/605A61K9/08A61K9/20A61K9/48A61P3/10A61K31/445A61K31/4965A61K125/00A61K127/00A61K135/00
Inventor 张晓琦叶葳叶文才夏涛
Owner JINAN UNIVERSITY
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