Preparation method and application of pseudolarix lactone H

A technology of pinolactone and golden pine, which is applied in the field of medicine, can solve the problems of insulin dependence, limited application, and large toxic and side effects, and achieve the effects of improving crystal uniformity, accelerating production efficiency, and reducing impurity content

Active Publication Date: 2014-09-03
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Western medicine currently treats diabetes oral drugs mainly include: sulfonylureas (such as glimepiride), biguanides (such as metformin), etc., most of them are synthetic drugs, which can promote insulin secretion, reduce the output of liver glycogen or increase Sensitivity to insulin, but it is easy to cause hypoglycemia or lactic acidosis, and cannot fundamentally prevent further necrosis of islet β cells, leading to insulin dependence
With the in-depth research on the basic theory of diabetes, the research on new diabetes drugs with other mechanisms of action has made progress, and many of them have been applied clinically: α-glucosidase inhibitors (such as acarbose), which can inhibit intestinal The α-glucosidase in the upper part blocks the decomposition of carbohydrates and enters the middle and lower parts of the small intestine for further decomposition and absorption, so that blood sugar can be maintained at a stable level and relieve the rise in blood sugar after meals, but this type of drug will cause abdominal discomfort and flatulence Other gastrointestinal adverse reactions
Aldose reductase inhibitors (such as epalrestat) can prevent and delay diabetic complications by inhibiting the polyalcohol metabolism pathway, but these drugs have relatively large toxic and side effects and unsatisfactory curative effects, which greatly limit their use. application
In addition, there are gluconeogenesis inhibitors, insulin sensitizers, etc., and the scope of application is not very wide.

Method used

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  • Preparation method and application of pseudolarix lactone H
  • Preparation method and application of pseudolarix lactone H
  • Preparation method and application of pseudolarix lactone H

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1: the preparation of chrysanthemum lactone H

[0036] After crushing 12 kg of pine seeds, reflux extraction with 50 liters of dichloromethane at 60°C for 12 hours, after standing still, filter the dichloromethane solution and pine seed raw material powder (filtrate), and concentrate the obtained dichloromethane solution Dry to obtain the concentrated extract A for later use, then reflux the filtered pine seed powder with 50 liters of ethyl acetate at 80°C for 12 hours, filter to obtain the ethyl acetate solution, concentrate and dry the ethyl acetate solution to obtain the concentrated extract B standby. The aforementioned concentrated extract A and concentrated extract B were mixed, and dispersed in 45 liters of methanol-water (volume ratio 5:1) mixed solution, extracted and degreased twice with 45 liters of petroleum ether, and the raffinate was concentrated and dried to obtain 45g of pine seed triterpene extract, wherein the content of triterpenoids meas...

Embodiment 2

[0037] Embodiment 2: the preparation of chrysanthemum lactone H

[0038] After crushing 100 kg of pine seeds, reflux extraction with 300 liters of chloroform at 60°C for 12 hours, after standing still, filter the chloroform solution and pine seed raw material powder (filtrate), and concentrate the chloroform solution Dried to obtain concentrated extract A for later use, then reflux extracted the filtered pine seed powder with 300 liters of acetone at 60°C for 12 hours, filtered to obtain an acetone solution, concentrated and dried the acetone solution to obtain concentrated extract B for later use. The aforementioned concentrated extract A and concentrated extract B were mixed, and dispersed in 300 liters of methanol-water (volume ratio 10:1) mixed solution, extracted and degreased twice with 300 liters of petroleum ether, and the raffinate was concentrated and dried to obtain 351g of the triterpene extract of pine seed, the content of triterpenoids is 58.1% as measured by ult...

Embodiment 3

[0039] Example 3: Test of α-glucosidase inhibitory activity of triterpene extract and its component chrysanthemum lactone H in pine seeds

[0040] α-glucosidase was used to catalyze the hydrolysis of p-nitrophenyl-α-D-glucopyranoside, and the activity of α-glucosidase was determined by measuring the amount of p-nitrophenol released. The enzyme inhibitory activity of the extract was calculated based on the content change of p-nitrophenol in the reaction system within a certain period of time. The specific results are shown in Table 1. The results showed that the triterpene extracts of pine seeds had significant inhibitory activity on α-glucosidase in vitro, which was similar to that of acarbose, while the hypoglycemic effect of chrysanthemum lactone H was better than that of acarbose.

[0041] Table 1 Inhibitory activity of pine seed triterpene extract on α-glucosidase

[0042]

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Abstract

The invention discloses an application of pseudolarix lactone H in pseudolarix seeds in preparation of functional foods and medicines for treating diabetes. The pseudolarix lactone H is prepared by the following methods: grinding the pseudolarix seeds, extracting by using a solvent A, extracting the filter residue by using a solvent B, concentrating and drying the extracting solution extracted twice, and merging to obtain a total crude extract; dispersing the total crude extract in an aqueous solution of low alcohols, extracting and degreasing by using petroleum ether, removing the petroleum ether phase, concentrating and drying the raffinate, and thus obtaining a triterpene extract of the pseudolarix seeds; and further taking a mixed solution of halomethane and acetone as a solvent, recrystallizing the triterpene extract, and thus obtaining the pseudolarix lactone H. The preparation method is simple in process, convenient in operation and low in energy consumption and is suitable for extracting and producing the pseudolarix lactone H from the pseudolarix seeds in a large scale.

Description

(1) Technical field [0001] The invention relates to the application of pseudolarolide H (pseudolarolide H), a component in pine seeds, in the preparation of functional food and medicine for treating diabetes, and a preparation method of pseudolarolide H, belonging to the technical field of medicine. (2) Background technology [0002] With the rapid development of the world economy and the aging of the population, diabetes mellitus (Diatetes mellitus) has become an epidemic non-communicable disease that has ravaged the world. It is one of the three major diseases in the world together with cancer and cardiovascular disease. Diabetes mellitus is an endocrine and metabolic disorder mainly manifested by glucose metabolism disorder. It is a group of metabolic diseases characterized by hyperglycemic metabolism due to defects in insulin secretion, or insulin action, or both. Chronic hyperglycemia in diabetes brings about increased oxidative stress, causing long-term damage to mult...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P3/10A61P3/00A23L1/29C07D493/22A23L33/00
Inventor 郭辉张斌钱俊青
Owner ZHEJIANG UNIV OF TECH
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