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Application of gamma-mangostin in preparing anti-inflammation and pain-relieving medicament

An anti-inflammatory and analgesic drug technology, applied in the application field of γ-mangostin in the preparation of anti-inflammatory and analgesic drugs, can solve problems such as gastrointestinal tract damage, stem cell damage and necrosis, and abnormal kidney function, and achieve the purpose of inhibiting prostaglandins Synthetic, good analgesic and anti-inflammatory effects, less toxic effect

Inactive Publication Date: 2010-03-03
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Non-steroidal anti-inflammatory drugs can cause many adverse effects, such as gastrointestinal tract damage, abnormal kidney function, stem cell damage and necrosis, etc.
At present, there is no report on the use of γ-mangostin for anti-inflammatory and analgesic drugs

Method used

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  • Application of gamma-mangostin in preparing anti-inflammation and pain-relieving medicament
  • Application of gamma-mangostin in preparing anti-inflammation and pain-relieving medicament
  • Application of gamma-mangostin in preparing anti-inflammation and pain-relieving medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 Separation and preparation of γ-mangostin

[0037] 1. Preparation of total extract of mangosteen husk

[0038] Wash the mangosteen husks, place them in a constant temperature drying box, dry at 60° C. to constant weight, and weigh to obtain 4.37kg; break the dried mangosteen husks into pieces, add 6.4L of 95% by volume ethanol to extract. One week later, the extract was filtered, the filtrate was collected, and concentrated; the concentrate was vacuum-dried for 24 hours to prepare the vacuum-dried mangosteen husk total extract.

[0039] 2. Separation of γ-mangostin

[0040] Column packing, sample loading and elution are all performed by those skilled in the art.

[0041] The mangosteen husk total extract prepared above, get 31g and carry out the following column purification and separation:

[0042] (1) Water-ethyl acetate solution (V 水 : V 乙酸乙酯 =1:1) extracting the total extract of mangosteen husks, collecting the ethyl acetate extraction layer;

[0043...

Embodiment 2

[0055] Example 2 Determination of the analgesic activity of γ-mangostin by hot plate analgesia

[0056] The hot plate analgesia method adopts the routine operation of those skilled in the art to measure the analgesic activity of the α-mangostin (substance A) prepared in Example 1.

[0057] Mice selection conditions: The pain threshold of each mouse was measured before administration, and those with an average value of less than 30s were qualified, and those with jumping phenomenon were discarded.

[0058] According to the above mouse selection conditions, 70 female mice were selected and divided into five groups: lysozyme group, indomethacin group, γ1 group, γ2 group and tramadol group, 10 mice / group, of which the lysozyme group was used as the control group, tramadol group and indomethacin group were all positive control groups.

[0059] Fasting for 12 hours before the experiment, the measurement was started 1 hour after administration, and the measurement was performed ever...

Embodiment 3

[0063] Example 3 Determination of the analgesic and anti-inflammatory activities of γ-mangostin by formalin experiment in mice

[0064] In this example, the analgesic activity of the γ-mangostin prepared in Example 1 was measured by the writhing method using the routine operations of those skilled in the art.

[0065] 70 female mice were divided into 5 groups: lysozyme group, indomethacin group, γ1 group, γ2 group and tramadol group, 10 mice per group. The domethacin group was the positive control group.

[0066] Fasting for 12 hours before the experiment, 1 hour after administration, subcutaneously inject 20 μl of 5% formalin solution into one foot of the mouse, and calculate the time for the mice to lick their feet in the next two phases. The first phase is The continuous foot licking time within 5 min after injection, the second phase is the continuous foot licking time from 25 min to 60 min after the injection, in which each recording time is still 5 min, and the recordin...

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Abstract

The invention discloses application of gamma-mangostin in preparing an anti-inflammation and pain-relieving medicament. The preparation method of the gamma-mangostin comprises the following steps: leaching mangosteen nut shells with 95vol% ethanol to obtain the extract of the mangosteen nut shells, and then carrying out column separation to obtain the gamma-mangostin from the extract. The obtained gamma-mangostin has high purity and better pain-relieving and anti-inflammation effects than those of the extract. Moreover, the research also discovers that the gamma-mangostin has better effect onremoving the hydroxy radical and the oxygen radical and anti-oxidation and nerve protection effects, and can inhibit the synthesis of prostaglandin and interdict the 5-HT2a receptor, thereby performing the anti-inflammation and pain-relieving effects on the centrums and the peripheral regions thereof.

Description

technical field [0001] The invention relates to the fields of natural product chemistry and medicinal chemistry, in particular to the application of active ingredients in mangosteen husks, in particular to the application of γ-mangostin in the preparation of anti-inflammatory and analgesic drugs. Background technique [0002] Pain and inflammatory response are warning signals, indicating that tissue damage has occurred in the body or indicating that it is about to suffer damage, and it is a defensive response of the body's self-protection. If pain and inflammation persist for a long time, it will constitute an unbearable mental torment for the body, seriously affecting study, work, diet and sleep, and ultimately resulting in economic and social problems that cannot be ignored due to the reduced quality of life. [0003] Pain and inflammation are a chain reaction. The two are causal and affect each other, resulting in anti-inflammatory and analgesic drugs. Currently, the main...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P29/00A61P25/04
Inventor 项辉胡雯崔继红
Owner SUN YAT SEN UNIV
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