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Alcohol amine type diterpenoid alkaloid with analgesic effect, preparation method and application

A technology based on diterpene alkaloids and alcohol amines, applied in organic chemistry, drug combinations, non-central analgesics, etc., can solve problems such as shock, cardiac arrest, and strong toxicity, and achieve significant economic benefits and huge clinical applications value effect

Inactive Publication Date: 2022-05-17
YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, Aconitum is highly toxic, and improper use often causes severe side effects such as cardiac arrest and shock.

Method used

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  • Alcohol amine type diterpenoid alkaloid with analgesic effect, preparation method and application
  • Alcohol amine type diterpenoid alkaloid with analgesic effect, preparation method and application
  • Alcohol amine type diterpenoid alkaloid with analgesic effect, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1, the LD of the nyolin of the alcoholamine type diterpene alkaloid 50 Obtain it as follows:

[0023] (1) Animal grouping: Take 72 Kunming mice, half male and half male, and divide them into 6 groups, blank control group, neoline (neoline) 89.2531mg / kg, 137.3125mg / kg, 211.2500mg / kg, 325.0000mg / kg, 500.0000mg / kg group, 12 rats in each group;

[0024] (2) Experimental method: The same volumes of different concentrations and dosage groups were injected intramuscularly once, and the blank control group was given a blank solvent system. The acute toxic reaction and death of animals in each group were observed after administration for 14 consecutive days. Animals that died during the observation period and animals that were sacrificed after the observation period were dissected, and the volume, color, and texture of various tissues and organs were checked with naked eyes for abnormalities. According to the death rate of animals in each group, the Bliss method w...

Embodiment 2

[0026] Example 2, the analgesic effect of the alcohol-amine-type diterpene alkaloid neoline on pain induced by acetic acid in mice was specifically verified by the following process:

[0027] (1) Animal grouping: 60 Kunming mice, half male and half male, were randomly divided into 5 groups, blank control group, aspirin group, neoline low, medium and high dose groups, 12 in each group;

[0028](2) Experimental method: the mice in each group were administered with a volume of 0.1mL / 10g, and the blank control group was intramuscularly injected with a blank solvent system; the mice in the aspirin group were injected intraperitoneally with 600mg / kg body weight of aspirin; The dosage groups were administered by intramuscular injection of 3.0086mg / kg, 5.0143mg / kg, and 10.0287mg / kg respectively. 30 minutes after administration, the mice in each group were intraperitoneally injected with 0.2 mL of 0.6% glacial acetic acid, recorded the number of writhing times of the mice within 20 min...

Embodiment 3

[0030] Example 3, the analgesic effect of the alcohol-amine-type diterpene alkaloid neoline on the pain caused by hot plates in mice was specifically verified by the following process:

[0031] (1) Animal screening: take Kunming female mice, 18-22g, put them on a hot plate at (55±0.5)℃, stimulate the mouse feet to produce pain response (lick the hind feet), and measure the pain of the mice Threshold (time to lick hind paws when pain response occurs), those who added hind paws within 5s and those who did not lick their hind paws or avoided within 30s were discarded, and 60 qualified female mice were screened out.

[0032] (2) Animal grouping: 60 qualified female mice were randomly divided into 5 groups, blank control group, morphine group, neoline low, medium and high dose groups, 12 in each group;

[0033] (3) Experimental method: The pain threshold of mice in each group was measured twice before administration, and the average value was taken as the pain threshold before admi...

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Abstract

The invention discloses an alcohol amine type diterpenoid alkaloid with an analgesic effect, a preparation method and application, the alcohol amine type diterpenoid alkaloid is derived from neoline of aconitum brachypodum which is a cirrhosaidae Aconitum plant, and the molecular weight of the alcohol amine type diterpenoid alkaloid is 437; the Neole has an analgesic effect and is high in safety, the acute toxicity LD50 of mice subjected to intramuscular injection administration is equal to 300.8600 mg / kg, and the 95% confidence interval is 257.5 mg / kg to 351.9000 mg / kg. Researches prove that the toxicity of the nioin of alcohol amine type diterpenoid alkaloid is far less than that of aconitine alkaloid bulleyaconitine in the market, and the nioin has an obvious analgesic effect on mouse pain caused by acetic acid and a hot plate; the compound disclosed by the invention has obvious analgesic effect on acute and chronic pains on a rat formalin pain model, can be used for peripheral and central pains and acute and chronic inflammatory pains, can be used as a novel alkaloid analgesic drug, and has huge clinical application value and obvious potential social benefits and economic benefits.

Description

technical field [0001] The invention belongs to the technical field of traditional Chinese medicine utilization, further belongs to the technical field of separation and extraction of active ingredients of traditional Chinese medicine, and specifically relates to an alcohol-amine type diterpene alkaloid with analgesic effect derived from Artemisia aconitum, which has analgesic effect, Preparation method and application. Background technique [0002] In 1986, the International Society for the Study of Pain defined pain as: an unpleasant sensory and emotional experience associated with tissue damage or potential tissue damage. It is worth noting that most diseases can cause pain, and acute pain may turn into chronic pain as the course of the disease prolongs, so pathological pain is mostly chronic pain. [0003] Chronic pain is a global problem that has reached epidemic proportions. According to statistics from the International Society for Pain Research, one out of every fi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D221/22A61P29/00
CPCC07D221/22A61P29/00
Inventor 马晓霞庄馨瑛苏冬雪彭海燕何芳雁周志宏
Owner YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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