Mango aglycone, preparation purification process and uses thereof

A mangiferin aglycone and purification method technology, which is applied in the fields of organic chemistry, pharmaceutical formulations, and medical preparations containing active ingredients, etc., can solve the limitation of development and utilization in the field of biomedicine, there is no research report on hypoglycemia, and the distribution of mangiferin aglycone is small. and other problems to achieve the effects of good reproducibility, improved glucose tolerance, and high yield

Inactive Publication Date: 2009-02-18
NANJING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Mangiferin aglycon is rarely distributed in plants, and is currently only isolated from plants such as Garcinia microphyllum and Hypericum perforatum, and the amount is s

Method used

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  • Mango aglycone, preparation purification process and uses thereof
  • Mango aglycone, preparation purification process and uses thereof
  • Mango aglycone, preparation purification process and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1 Preparation and purification of mangiferin aglycon

[0025] (1) Heating with a reflux device, first add 12 g of phenol into the three-necked bottle, turn on mechanical stirring, and heat to keep the phenol melted, add 2 g of mangiferin with a grinding funnel, stir until suspended, and cool to room temperature. Measure 22.5ml of HI, and add it dropwise to the three-necked bottle with a constant pressure funnel. Heating with an electric heating pack, stirring mechanically, timing from the beginning of reflux, and reflux for 6 hours.

[0026] (2) Add the solution obtained by reflux for 6h into saturated NaHSO dissolved by ultrasonic 3 , magnetically stirred to fully react. A brown solid was obtained by suction filtration, washed with water several times until the filtrate was colorless. The resulting solid was boiled with 200ml of hot water four times each time, and the filtrate was collected after suction filtration each time. The 800ml filtrates obtained fr...

Embodiment 2

[0031] Example 2 Effect of Mangiferin Aglycone on Blood Glucose in Glucose-Induced Hyperglycemic Mice

[0032] 48 C57BL / 6 mice were randomly divided into control groups and three doses of administration groups, 12 in every group, and the administration groups were given 15, 40, 60 mg / kg mangiferin aglycone solution (with 0.5% CMC-Na aqueous solution suspension), the control group was given 0.5% CMC-Na aqueous solution. The drug was administered by intragastric administration once a day for 7 days. After fasting for 6 hours after the last administration, 1 g / kg ip.20% glucose solution was administered according to the weight of the mice. Before intraperitoneal injection of glucose (ie basal), 15, 30, 60 and 120 min after ip. glucose, blood was taken from the tail of the mice to measure the blood glucose level. See the experimental results figure 2 , image 3 .

[0033] figure 2 Show that compared with the control group, 15, 40, 60mg / kg mangiferin aglycone has obvious in...

Embodiment 3

[0035] Example 3 Effects of mangiferin aglycone on glucose-induced insulin secretion in normal mice

[0036] 80 C57BL / 6 mice were randomly divided into control groups and three doses of administration groups, 20 in every group, and the administration groups were given 15, 40, 60 mg / kg mangiferin aglycone solution (with 0.5% CMC-Na aqueous solution suspension), the control group was given 0.5% CMC-Na aqueous solution. The administration was administered by intragastric administration once a day for 7 days, and the food was fasted for 6 hours after the last administration. Each dosage group first gets 10 mice to pick eyeball and take blood, as the basal of this group; Every remaining 10 mice, intraperitoneal injection (ip.) gives 20% glucose solution (1g / kg), picks eyeball after 30min Take blood. After standing still, the serum was collected by centrifugation, and the serum insulin content was determined by ELISA method. See the experimental results Figure 4 .

[0037]The ...

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Abstract

The present invention belongs to the technical field of biological pharmacy, and in particular relates to a preparation and purification method of tetra-hydroxyl xanthone mango aglycone (norathyriol), and an application thereof in hypoglycemic medicine. Based on biological experiments, mango glycoside is used as raw material; under the condition with phenol and hydroiodic acid, carbon-carbon bonds are broken to produce the crude product of mango aglycone; the crude product is separated and purified through silica gel column chromatography so that the mango aglycone is separated; the yield rate reaches 12 percent, the purity is higher than 95 percent, and the reproduction performance is good; the IGTT of C57BL/6 normal mice is effectively improved with the norathyriol; and simultaneously the quantity of insulin secretion induced by glucose in vivo for the C57BL/6 normal mice can be improved with the norathyriol. Therefore, the mango aglycone can be applied for preparation of hypoglycemic medicine.

Description

1. Technical field [0001] The invention belongs to the technical field of biopharmaceuticals, and in particular relates to the preparation, purification and application of mangiferin aglycone in hypoglycemic drugs. 2. Background technology [0002] Mangiferin (norathyriol), full name 1,3,6,7-tetrahydroxy Ketones (1,3,6,7-tetrahydroxyxanthone). Mangiferin aglycon is rarely distributed in plants, and is currently only isolated from plants such as Garcinia cambogia and Hypericum perforatum, and the amount is small and difficult to obtain. This greatly limits its development and utilization in the field of biomedicine. [0003] Modern pharmacological studies have shown that mangiferin has a variety of physiological effects, such as anti-depression, anti-inflammation, anti-hypertension, anti-tumor, anti-oxidation, and inhibition of the growth of Mycobacterium tuberculosis, among which the research on anti-inflammatory effect is more in-depth. Studies have shown that mangiferi...

Claims

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Application Information

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IPC IPC(8): C07D311/86A61K31/352A61P3/10
Inventor 吕冬张昊邱振均吴冬冬孙凌冰阮小明徐琛林鸿坤张艳张辰宇郭彬歆
Owner NANJING UNIV
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