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Application of isodaphnetin compound in preparation of antidiabetic medicines

An anti-diabetic technology of daphnein, which is applied in the fields of active ingredients of heterocyclic compounds, drug combinations, metabolic diseases, etc., can solve the problems such as the anti-diabetic effect of Phnom Penh daphne, which has not yet been seen, and achieve the protection and repair of islet cells, good resistance Diabetes drug efficacy, the effect of large clinical application value

Inactive Publication Date: 2012-08-08
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The present inventor has carried out a systematic study on the chemical components of Daphne Phnom Penh, and found through screening that the chemical composition Isodaphnein has a good anti-diabetic effect. So far, there has been no report on the anti-diabetic effect of Daphne Phnom Penh.

Method used

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  • Application of isodaphnetin compound in preparation of antidiabetic medicines
  • Application of isodaphnetin compound in preparation of antidiabetic medicines
  • Application of isodaphnetin compound in preparation of antidiabetic medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Preparation of Isorphinoid

[0017] 7.5kg Phnom Penh daphne medicinal material (commercially available) is crushed and extracted by percolation with 150L 75% ethanol, and the extract is concentrated under reduced pressure to obtain 8L extract. Ethyl extraction, collecting the ethyl acetate part, weighing 125g, the ethyl acetate part was subjected to silica gel H (200-300 mesh) column chromatography twice, chloroform: acetone (10:1-1:1), chloroform: methanol (50:1~1:1) gradient elution, SephadexLH-20 column chromatography and reversed-phase silica gel (Merck), isolated and obtained 108 mg of the compound isorphinoid.

[0018] The isoretasin prepared in Example 1 was used in the following experiments.

Embodiment 2

[0020] Effects of Isoretelin on Serum Insulin and Glucagon in Rats

[0021] experimental method

[0022] In this experiment, a high-sugar and high-fat diet combined with low-dose streptozotocin (STZ) was used as a rat model of type 2 diabetes. This model is more in line with the pathogenesis of ordinary type 2 diabetes in humans and is conducive to the discovery of therapeutic drugs for type 2 diabetes. Male SD rats were fed high-sugar and high-fat diet for 1 month to induce insulin resistance, and were given a small dose of streptozotocin (STZ) 25 mg / kg and injected intraperitoneally to establish a type 2 diabetic rat model. Drugs were then injected intraperitoneally, and the blood glucose, serum insulin, glucagon, mental state, body weight, water intake, food intake, and urine of the mice were used as detection indicators (Pharmacological Research. 2005, 52: 313-320).

[0023] Experimental steps:

[0024] 1. Material Isorphinoid is prepared from Example 1

[0025] 1.1 Exp...

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Abstract

The invention provides an application of an isodaphnetin compound in the preparation of antidiabetic medicines. The structural formula of isodaphnetin is shown in the specification. According to the invention, a high-sugar high-fat forage combined with a small dosage of streptozotocin (STZ) is applied to establish type 2 diabetes rat models, and male SD adult rats can be fed with the high-sugar high-fat forage for 1 month to induce insulin resistances and injected with a small dosage of the STZ 25mg each kilogram in an abdominal cavity mode to establish the type 2 diabetes rat models; and said given medicine is injected in the abdominal cavity mode, and blood sugar, serum insulin, glucagon, mental states, body weights, water drinking amounts, appetites and the like of the rates are detection indexes. Experiment results show that after treating with isodaphnetin, the blood sugar values and the serum insulin levels of the type 2 diabetes rat models are obviously decreased (P is less than 0.01), and there are no obvious blood sugar value differences among rats having obvious increased insulin levels (P is greater than 0.05). So, isodaphnetin can be used for preparing the antidiabetic medicines. The medicine is a medicinal composition comprising isodaphnetin as an active compound and a medicinal carrier.

Description

technical field [0001] The present invention relates to medicines. It specifically relates to the application of isoretelin compounds in the preparation of antidiabetic drugs. Background technique [0002] In recent years, the incidence of type 2 diabetes has been increasing year by year, seriously threatening human health. Current research has shown that patients with type 2 diabetes have three major deficits: insulin resistance, β-cell dysfunction, and hepatic glucose overproduction. Oral antihyperglycemic drugs commonly used in clinical practice include: PPARγ agonists, insulin secretion-promoting drugs sulfonylureas, glinides, and biguanides. The above drugs are only effective within a certain range, cannot effectively control the development of diabetes, and have limited tolerance or have adverse reactions of varying degrees, such as: glucose intolerance, hypoglycemia, weight gain, lactic acidosis and edema. [0003] Isorphinoids come from Daphne odora Thunb. [000...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/37A61P3/10C07D493/04
CPCA61K31/37C07D493/04A61P3/10
Inventor 张卫东单磊苏娟李慧梁柳润辉沈云亨徐希科张寿德
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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