Compound-pyrocincholic acid 3beta-O-beta-D-quinovopyranosyl-28-O-beta-D-glucopyranoside (PAQG) for adjusting lipid metabolism and obesity as well as application of compound in pharmacy

A compound and technology for regulating blood lipids, applied in the fields of application, metabolic diseases, medical preparations containing active ingredients, etc.

Inactive Publication Date: 2017-08-01
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

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  • Compound-pyrocincholic acid 3beta-O-beta-D-quinovopyranosyl-28-O-beta-D-glucopyranoside (PAQG) for adjusting lipid metabolism and obesity as well as application of compound in pharmacy
  • Compound-pyrocincholic acid 3beta-O-beta-D-quinovopyranosyl-28-O-beta-D-glucopyranoside (PAQG) for adjusting lipid metabolism and obesity as well as application of compound in pharmacy
  • Compound-pyrocincholic acid 3beta-O-beta-D-quinovopyranosyl-28-O-beta-D-glucopyranoside (PAQG) for adjusting lipid metabolism and obesity as well as application of compound in pharmacy

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Embodiment 1

[0028] The compound PAQG of the present invention has the structural formula shown in the following formula (I), extracted from yellow cotton wood, provided by the Xishuangbanna Tropical Botanical Garden of the Chinese Academy of Sciences. For the preparation method, please refer to the method described in the following documents.

[0029] ZHANG Y,TAN N,HUANG H,et al.Triterpenoid Saponins from Metadinatrichotoma[J].Zeitschrift für Naturforschung B,2007,62(5):745‐748.

[0030]

[0031] 1. PAQG inhibits 3T3-L1 preadipocyte differentiation:

[0032] The 3T3-L1 pre-adipocytes were starved for two days, induced to differentiate for three days with the induction reagent, and then cultured in the maintenance medium for one day, and then replaced with fresh medium for normal culture to differentiate into adipocytes. According to this experimental method, PAQG of different concentrations (0, 2.5 μM, 5 μM, 10 μM, 20 μM) was used during the whole differentiation process, and the control group w...

Embodiment 2

[0049] According to the compound PAQG obtained in Example 1, excipients were added in a ratio of 1:1 or 1:2 by weight of the compound to the excipient, and granulated and compressed.

Embodiment 3

[0051] The compound PAQG was prepared according to Example 1, and was made into capsules according to the conventional capsule preparation method.

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Abstract

The invention provides a new function of a compound-pyrocincholic acid 3beta-O-beta-D-quinovopyranosyl-28-O-beta-D-glucopyranoside (PAQG), extracted from metadina trichotoma, in adjustment and control of lipid metabolism in 3T3-L1 cells, and application of the compound in preparation of medicines, food and health care products which are used for relieving obesity and obesity-related metabolic diseases. The PAQG inhibits the differentiation of the 3T3-L1 preadipocytes by activating adenosine monophosphate-activated protein kinase (AMPK), and down-regulates the expression of differentiation-related transcription factors and proteins (PPAR gamma, C/EBP beta, C/EBP alpha and FABP4) and the release of adiponectin. Furthermore, the PAQG inhibits the fat accumulation in the 3T3-L1 mature adipocytes by inhibiting fatty acid synthesis and promoting lipid oxidation. The PAQG relieves the obesity from both fat cell number and fat content under the premise of safe and effective dosage of administration, thus being used for the preparation of medicines, health care products and functional food which are used for preventing and treating the obesity and the obesity-related metabolic diseases.

Description

[0001] Technical field: [0002] The invention belongs to the technical field of medicines, and specifically relates to an oleanolic acid compound Pyrocincholic Acid 3β-O-β-D-quinovopyranosyl-28-O-β-D-glucopyranoside (PAQG) for regulating lipid metabolism in 3T3-L1 cells New functions and their applications in the preparation of drugs, foods and health products for improving obesity and obesity-related metabolic diseases. [0003] technical background: [0004] Diabetes, as a chronic metabolic disease, its complications seriously endanger human health. Especially, there are more and more researches on type 2 diabetes, which is closely related to human lifestyle. Studies have shown that 50% of obese people have type 2 diabetes, and obesity can increase the prevalence of type 2 diabetes by three times. Therefore, research on obesity and diabetes has attracted more and more attention. [0005] The World Health Organization (WHO) clearly defines obesity as "excessive or abnormal fat acc...

Claims

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Application Information

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IPC IPC(8): A61K31/704A61P3/00A61P3/06A61P3/04A23L33/11
CPCA23V2002/00A61K31/704A23V2200/3262A23V2200/332A23V2250/2136
Inventor 熊文勇张玉梅彭莉胡敬
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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