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Preparation and application of triterpene drug for inhibiting synthesis and secretion of apoB48 in intestinal tracts

A technology of triterpene compounds and drugs, which can be applied in the direction of drug combinations, organic active ingredients, and medical preparations containing active ingredients, and can solve problems such as limited development

Inactive Publication Date: 2017-03-22
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the development of drugs for regulating intestinal apoB48 is limited, and there is no drug that specifically inhibits the level of apoB48

Method used

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  • Preparation and application of triterpene drug for inhibiting synthesis and secretion of apoB48 in intestinal tracts
  • Preparation and application of triterpene drug for inhibiting synthesis and secretion of apoB48 in intestinal tracts
  • Preparation and application of triterpene drug for inhibiting synthesis and secretion of apoB48 in intestinal tracts

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1 Preparation of Cyclocarya triterpenoids

[0025] 48.5 kg of dried Cyclocarya paliurus leaves were heated and refluxed with 80% ethanol for 3 times, each time for 2 hours, the extracts were combined, concentrated under reduced pressure until there was no alcohol smell, the residue was suspended with water, and then washed with chloroform, ethyl acetate After extraction, the solvent was recovered separately to obtain the chloroform fraction (3.65kg), the ethyl acetate fraction (120g) and the remaining water fraction.

[0026] Take 3kg of the extract from the chloroform part, go through silica gel column chromatography under reduced pressure, and use chloroform-methanol (100:0, 100:5, 5:1, 0:100) gradient elution, and each gradient is combined together to obtain 4 fractions (Fr. 1-4). Fr.2 (400g) was subjected to silica gel column chromatography, eluted with a gradient of chloroform-methanol (100:3→0:100), checked by TLC, and combined to obtain 4 sub-fractions (...

Embodiment 2

[0027] Example 2 Compound structure identification data

[0028] 50 3β, 23-dihydroxy-1, 12-dioxo-oleanolic acid (3β, 23-dihydroxy-1, 12-dioxo-olean-28-oic acid)

[0029] White powder (methanol), mp 287~289℃, (c 0.095MeOH), easily soluble in chloroform, methanol, acetonitrile and other organic solvents, Liebermann-Burchard reaction is positive, vanillin-concentrated sulfuric acid shows blue-purple. IR(KBr)cm -1 : 3441, 2946, 1696, 1050; UVλ max (CH 3 OH): 203nm. HR-TOF-MS m / z: 501.3218[M-H] - (C 30 h 45 o 6 , calcd.501.3216), the molecular formula is C 30 h 46 o 6 , with a molecular weight of 502. The UV spectrum shows a maximum absorption peak at . The IR spectrum shows a strong hydroxyl absorption peak (cm -1 ), C-H bond stretching vibration absorption peak (cm -1 ), carbonyl absorption peak (cm -1 ) and C-O bond stretching vibration absorption peaks (cm -1 ). 1 H NMR (C 5 D. 5 N, 600MHz) and 13 C NMR (C 5 D. 5N, 125MHz) data are shown in Table 1.

[...

Embodiment 3

[0045] Example 3 Cyclocarya triterpenoids regulate the activity of Caco-2 cells secreting apoB48

[0046] 1. Materials

[0047] 1.1 Test article

[0048] The test samples are 22 triterpenoids isolated from Cyclocarya paliurus, numbered 4, 11, 14, 18-23, 30-32, 34-37 and 46-51, and the structural formulas are as described above. Stock solution of the test product: take 1 mg of the triterpene compound, dissolve it in 100 μL of dimethyl sulfoxide (DMSO), and then dilute it 10 times with PBS, store it at 4°C until use.

[0049] 1.2 Drugs and reagents

[0050] Caco-2 cell line was purchased from Nanjing Kaiji Biotechnology Development Co., Ltd. (batch number 20151019).

[0051] Table 4 Experimental reagents and drugs

[0052]

[0053] 2. Experimental method

[0054] 2.1 Establishment of Caco-2 cell model

[0055] (1) Recovery of Caco-2 cells

[0056] Thaw the previously frozen Caco-2 cells in warm water at 37°C, dilute with complete DMEM high-glucose medium containing 10%...

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Abstract

The invention relates to the field of pharmacy, and specifically relates to the preparation and application of a drug. The drug is prepared from triterpene compounds, which are purchased or extracted from cyclocarya paliurus, and is used to inhibit the synthesis and secretion of apoB48 in the intestinal tracts. The invention especially discloses applications of triterpene compounds in the preparation of drugs for preventing hyperlipidemia, cardiovascular and cerebrovascular diseases, and atherosis. The invention further discloses a series of triterpene compounds and the preparation and applications thereof in the preparation of drugs for inhibiting the synthesis and secretion of apoB48 in intestinal tracts.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to the application of a series of triterpene compounds in the preparation of drugs for inhibiting the synthesis and secretion of intestinal apoB48. Especially in the preparation of anti-hyperlipidemia drugs, anti-cardiovascular and cerebrovascular disease drugs, anti-atherosclerosis drugs and the like. Background technique [0002] Hyperlipidemia refers to the state of abnormally elevated serum lipid levels, mainly manifested as high serum levels of total cholesterol, triglycerides, low-density lipoprotein and low high-density lipoprotein, which are considered to induce cardiovascular and cerebrovascular diseases. Such as stroke, coronary heart disease, atherosclerosis, myocardial infarction and other important risk factors. The global annual death rate of cardiovascular and cerebrovascular diseases induced by hyperlipidemia accounts for 30-40% of all disease mortality. [0003] Human bloo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58A61K31/585A61K31/56A61K31/7048A61K31/704A61P3/06A61P9/10
CPCA61K31/58A61K31/56A61K31/585A61K31/704A61K31/7048
Inventor 殷志琦赵苑余操兰洁吴正凤
Owner CHINA PHARM UNIV
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