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Use of 15-methano-substituted-andrographolide derivative in preparing anti-inflammatory ntipyretic analgesic medicine

A technology of andrographolide and methylene, which is applied in the fields of anti-inflammatory, antipyretic and analgesic effects, can solve problems such as no related reports, achieve the effect of improving oral efficacy, expanding the range of options, and avoiding side effects

Active Publication Date: 2009-04-29
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The novel α-glucosidase inhibitor 15-methylene substituted andrographolide derivative synthesized with andrographolide (AD) as the lead compound has been reported in the patent CN: 200510107247.4, which is the applicant's previous research results. In the later stage, more in-depth research was carried out on it, and the research showed that this type of compound has significant anti-inflammatory, antipyretic, and analgesic effects. see related reports

Method used

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  • Use of 15-methano-substituted-andrographolide derivative in preparing anti-inflammatory ntipyretic analgesic medicine
  • Use of 15-methano-substituted-andrographolide derivative in preparing anti-inflammatory ntipyretic analgesic medicine
  • Use of 15-methano-substituted-andrographolide derivative in preparing anti-inflammatory ntipyretic analgesic medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Example 1 Pharmacological activity of 15-methylene substituted andrographolide derivatives

[0013] 1. Anti-inflammatory experiment

[0014] 1. Experiment on the effect of p-xylene on mouse ear swelling

[0015] The experimental drugs were drug samples of the present invention, andrographolide provided by Beijing Institute of Medical Engineering Biotechnology, and indomethacin (indomethacin enteric-coated tablets; batch number: 20060502) produced by Shanxi Yunpeng Pharmaceutical Co., Ltd. as a positive control. The drug was prepared by using 0.1% Tween-80 (Tianjin Kemiou Chemical Reagent Development Center, batch number: 20030720) to aid dissolution, and 0.5% sodium carboxymethylcellulose (Shanghai Chemical Reagent Company, batch number: F20020928) for suspension. The experimental animals were clean-grade male Kunming mice (certificate number: 0009255) with a body weight of 20±2 g provided by the Experimental Animal Center of Henan Province. The inflammatory agent xyl...

Embodiment 2

[0046] The acute toxicity of embodiment 2 ADD-3

[0047] Animals: clean-grade Kunming mice, weighing 20±2 g, half male and half male, certificate number: 0009898, provided by the Experimental Animal Center of Henan Province.

[0048] Drugs: 15-methylene substituted andrographolide derivatives of the present invention.

[0049] Experimental method: Take 20 mice weighing 20±2g, half male and half male, and randomly divide them into ADD-3 low-dose group and ADD-3 high-dose group, with 10 mice in each group. After the animals were fasted for 12 hours (drinking water was not restricted), the doses of 2.00 g / kg and 5.00 g / kg of ADD-3 were given by intragastric administration respectively, and the intragastric volume was 0.2 mL / 10 g. Observe and record the poisoning performance of the animals. Weigh once a week. Continuous observation for 14 days. The results are shown in Table 6.

[0050] Experimental results: The mice did not show obvious signs of poisoning and did not die, in...

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Abstract

The invention discloses the application of a 15-methylene replaced andrographolide derivant as shown in general formula 1 in preparing anti-inflammatory, antipyretics and analgetics drugs, pertaining to the pharmaceutical chemistry field. Mice auricular swelling induced by dimethylbenzene, cotton ball granuloma of mice, hyperpyrexia of rats induced by yeast, mouse hot-plate test, writhing test of mice and other models are used for testifying that the 15-methylene replaced andrographolide derivant has anti-inflammatory, antipyretic and analgetic functions. Compared with andrographolide, the 15-methylene replaced andrographolide derivant has better anti-inflammatory, antipyretic and analgetic functions, and the research result of mouse acute toxicity test shows that the toxicity of the 15-methylene replaced andrographolide derivant is very slight. The 15-methylene replaced andrographolide derivant has relatively good application prospect by being applied to the development of anti-inflammatory, antipyretics and analgetics drugs.

Description

technical field [0001] The invention relates to the medicinal use of andrographolide, in particular to the anti-inflammatory, antipyretic and analgesic effects of 15-methylene substituted andrographolide derivatives, and belongs to the field of medicinal chemistry. Background technique [0002] Andrographis paniculata (Burm.f.) Nees is the dry aerial part of the Acanthaceae plant. Its main function is to clear away heat and detoxify, cool blood and reduce swelling. It is often used clinically to treat various infectious diseases, including trauma infection, furuncle, carbuncle, erysipelas, upper respiratory tract infection, acute and chronic tonsillitis, acute and chronic pharyngitis, acute and chronic bronchitis, acute bacillary dysentery, acute gastroenteritis, urinary Road infection, endometritis, pelvic inflammatory disease, otitis media, periodontitis, etc. The main components of Andrographis paniculata include diterpene lactones, sterols, flavonoids, alkaloids, etc. ...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P29/00
Inventor 刘宏民戴桂馥徐海伟陈小让赵进汤臻陈秀英王振基
Owner ZHENGZHOU UNIV
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