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Application of lupenone to products for preventing or treating diabetes mellitus

A technology of lupenone and diabetes, which is applied in the application field of lupenone in the preparation of products for preventing or treating diabetes, and can solve problems that do not involve the anti-diabetic effect of lupenone

Active Publication Date: 2012-10-10
GUIYANG COLLEGE OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, in vitro cell studies have shown that lupenone has the ability to inhibit the activity of α-glucosidase, cholinesterase and protein tyrosine phosphatase 1B and has antioxidant effects, but these studies on lupenone were all carried out in vitro. When there is a pathological state of diabetes, lupenone, which is a pentacyclic triterpenoid, may undergo biotransformation in animals, and whether it can exert anti-diabetic effects in vivo is debatable
At the same time, judging whether a product can be used in the clinical treatment of diabetes is based on whether it can improve glucose tolerance in the body, stimulate insulin secretion or reduce the phenomenon of elevated serum insulin caused by insulin resistance, and finally improve the hyperglycemia status of diabetes. The basis and preconditions, but the current research at home and abroad has not involved the anti-diabetic effect of lupenone in vivo

Method used

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  • Application of lupenone to products for preventing or treating diabetes mellitus
  • Application of lupenone to products for preventing or treating diabetes mellitus
  • Application of lupenone to products for preventing or treating diabetes mellitus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Example 1: Preparation of crude lupine ketone: take fresh or dried plantain root, cold soak with water or ethanol, percolate, reflux or ultrasonic extraction for 1 to 6 times, filter, combine the filtrate, and concentrate the filtrate into an extract; The extract is dispersed by adding appropriate amount of water, extracted with petroleum ether for 1 to 8 times until the petroleum ether is colorless, then extracted with ethyl acetate for 1 to 8 times, and ethyl acetate is recovered to obtain ethyl acetate extract; ethyl acetate is used for the extract Mix the sample after dissolving, wet-pack a 200-mesh silica gel column (the ratio of diameter to height is 1:10, and the loading volume is about 30 times), wash with 3-11 times the column volume of petroleum ether, and then use 3-12 times the column volume of petroleum ether Ether: ethyl acetate = 100:1, eluted and recovered to obtain crude lupenone.

Embodiment 2

[0062] Example 2: Preparation of lupine monomer: take fresh or dried plantain root, cold soak with water or ethanol, percolate, reflux or ultrasonically extract 1 to 6 times, filter, combine the filtrate, and concentrate the filtrate into an extract The extract is dispersed by adding appropriate amount of water, extracted with petroleum ether for 1 to 8 times until the petroleum ether is colorless, then extracted with ethyl acetate for 1 to 8 times, and ethyl acetate is recovered to obtain ethyl acetate extract; After the ester is dissolved, mix the sample, wet-pack a 200-mesh silica gel column (the ratio of diameter to height is 1:10, and the sample loading is about 30 times), wash with 3-11 times the column volume of petroleum ether, and then use 3-12 times the column volume Petroleum ether: ethyl acetate = 100:1 elution and recovery to obtain crude lupenone; recrystallization with ethanol to obtain lupenone monomer.

Embodiment 3

[0063] Embodiment 3: Take the crude lupenone obtained in Embodiment 1, add appropriate amount of conventional auxiliary materials, mix evenly, dry, sterilize, put into hard capsules, pack, and make capsules. The preparation is taken 1-3 times a day, 10-20 mg each time, and can be used to treat diabetes.

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Abstract

The invention discloses an application of lupenone to products for preventing or treating diabetes mellitus. Inventors deeply develop the lupenone by adopting the modern medicine efficacy and acute toxicity study technology. Pharmacodynamic experimental study shows that proper medicine can be processed and prepared from the lupenone as major ingredients and is used for preventing and treating the diabetes mellitus, the pharmacological activity is obvious, the performance is stable, safety and reliability are realized, the hyperglycemic effect is obvious, and phenomenon of serum insulin and C peptide rise caused by insulin resistance is also reduced, so the sugar tolerance is improved. In addition, the extraction raw material sources of the lupenone are easy to obtain, the preparation process easily realizes the industrialization, and medicine materials can be driven to be fully developed and utilized, so the lupenone has good application prospects in aspects of diabetes mellitus treatment medicine or health-care products.

Description

[0001] technical field [0002] The invention relates to the application of pentacyclic triterpenoid lupenone in the preparation of products for preventing or treating diabetes. Background technique [0003] Diabetes is a metabolic disease characterized by hyperglycemia caused by defects in insulin secretion and / or its biological effects. Diabetes has become the third serious threat to human health after tumors and cardiovascular and cerebrovascular diseases in the world. chronic disease. [0004] At present, the drugs used clinically to treat diabetes mainly include biguanides, thiazolidinedione, etc., such as metformin, a biguanide, whose main function is to improve insulin sensitivity, increase glucose utilization, inhibit hepatic glucose output, and increase insulin The number and affinity of receptors can reduce the intestinal absorption of glucose and achieve therapeutic effect; as insulin sensitizers, rosiglitazone and pioglitazone can reduce blood sugar by improving...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61P3/10A23L1/29A23L33/00
Inventor 王祥培钱海兵郝俊杰吴红梅靳凤云许士娜
Owner GUIYANG COLLEGE OF TRADITIONAL CHINESE MEDICINE
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