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Triterpene compound and its preparation method and application

The technology of a triterpenoid compound and composition is applied in the application field of preparing diabetes treatment medicines, which can solve the problems of weak activity and high adverse reactions, and achieve the effects of small molecular weight, good α-glucosidase inhibitory activity, and low dosage.

Active Publication Date: 2019-02-01
JIANGXI SUNWAY CHEM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The present invention aims to overcome the weak activity and high adverse reactions of current α-glucosidase-targeted diabetes treatment drugs, and provide two triterpene compounds with strong α-glucosidase inhibitory activity and their preparation methods and applications

Method used

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  • Triterpene compound and its preparation method and application
  • Triterpene compound and its preparation method and application
  • Triterpene compound and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: the preparation method of compound 1 and 2

[0027] (1) Ganoderma lucidum dried fruiting body (700g) was pulverized, the powder was soaked and extracted four times with isopropanol (3.5 liters each time, 2h each time), the extracts were combined and concentrated under reduced pressure to obtain the extract (20g).

[0028] (2) Pass the obtained extract through the MCI column (4.5×28cm, the filler is MCI gel CHP20P Mitsubishi Chemical Corporation), and carry out gradient elution with methanol / water solution. The steps of the gradient elution are: sequentially use 40% volume fraction , 50%, 60%, 70%, 80%, 90% methanol / water solution, and 100% methanol were eluted for 2 column volumes respectively.

[0029] (3) Collect the 70% methanol / water eluent in step (2), concentrate under reduced pressure, use 200-300 mesh silica gel as column packing, and carry out gradient elution with petroleum ether / ethyl acetate mixed solution, and the gradient elution The steps o...

Embodiment 2

[0041] Embodiment 2: α-glucosidase inhibitory activity test of compound 1, 2

[0042] The two compounds prepared in Example 1 were formulated into solutions with different concentrations according to their solubility, and the α-glucosidase inhibitory activity was tested.

[0043] First, add α-glucosidase 25uL (0.12U / mL) to the enzyme activity assay system of potassium phosphate buffer (pH 6.8), incubate at 37°C for 15min, add pNPG 25uL (5.0mM), react at 37°C for 30min, add 80uL (1.0M) of sodium carbonate was used to stop the reaction and measured at 405nm to obtain the absorbance of the blank group. Then take 100uL of acarbose or screening sample and add it to the enzyme activity assay system. First, incubate the enzyme at 37°C for 15min, then add the substrate pNPG, react at 37°C for 30min, add sodium carbonate to terminate the reaction, and measure the p-nitro group at 405nm. The absorbance of phenol. Calculate the inhibition rate of enzyme activity and calculate the IC 5...

Embodiment 3

[0047] Embodiment 3: capsule preparation

[0048] Take 20g of Compound 1, add 79g of lactose monohydrate, 79g of microcrystalline cellulose and 22g of micropowdered silica gel, mix, granulate, and fill into hard capsules to obtain 1000 capsules.

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PUM

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Abstract

The invention provides a triterpene compound represented by the formula (1) or formula (2). The preparation method comprises the following steps: grinding dry fruiting bodies of lucid ganoderma, extracting the fruiting bodies by isopropanol, concentrating the liquid extract in vacuum to obtain an extract; and subjecting the obtained extract to MCI column chromatography and silica gel column chromatography in sequence to obtain the triterpene compound represented by the formula (1) or formula (2). A pharmaceutical composition made of the triterpene compound and pharmaceutical auxiliary materials can be used to prepare drugs for treating diabetes. The provided triterpene compound has a better activity on inhibiting alpha-glycosidase, compared with acarbose sold on the market. Moreover, the molecular weight of the triterpene compound is small, and thus the dosage is little.

Description

(1) Technical field [0001] The invention belongs to the field of biomedicine, and specifically relates to two new triterpene compounds, a preparation method thereof, and an application in preparation of medicines for treating diabetes. (2) Background technology [0002] Diabetes mellitus is a group of heterogeneous metabolic diseases characterized by chronic hyperglycemia. Insulin secretion defects and / or insulin action defects are caused by polygenetic inheritance and environmental factors. It is characterized by chronic hyperglycemia accompanied by carbohydrate, fat and protein metabolism disorders. It is a chronic wasting disease that seriously endangers human health and patients' quality of life. disease. According to the statistics of the International Diabetes Federation (IDF), there were 151 million diabetic patients in the world in 2000, and 285 million diabetic patients in 2010. It is estimated that there will be nearly 500 million diabetic patients in the world by...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J9/00A61K31/575A61P3/10
CPCC07J9/00
Inventor 马列峰郎黄燕占扎君单伟光
Owner JIANGXI SUNWAY CHEM CO LTD
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