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Application of mussaenda erythrophylla glucoside U in preparation of antiacetyl-choline medicine

A technology of euphylloside and acetylcholine, which is applied in the direction of drug combination, anti-toxic agent, pharmaceutical formula, etc., and can solve the problems such as no registration of euphylloside U preparation and no anti-acetylcholine effect

Inactive Publication Date: 2015-02-18
GUANGXI INST OF CHINESE MEDICINE & PHARMA SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there is no literature report about the anti-acetylcholine effect of euphylloside U, let alone the registration of euphyroside U preparations as anti-acetylcholine drugs in domestic or foreign drug regulatory agencies, and no information about euphyroside U Report on the medical use of the preparation in the treatment of organophosphorus nerve agent poisoning, acute microcirculation disturbance, gastrointestinal colic, biliary tract or urethral spasm pain

Method used

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  • Application of mussaenda erythrophylla glucoside U in preparation of antiacetyl-choline medicine
  • Application of mussaenda erythrophylla glucoside U in preparation of antiacetyl-choline medicine
  • Application of mussaenda erythrophylla glucoside U in preparation of antiacetyl-choline medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The preparation of embodiment 1 goldenrodine U (hereinafter referred to as saponin U)

[0021] Add 5kg of Jade Leaf Golden Flower coarse powder, add 50L of 60% ethanol and extract under reflux for 3 times, each time for 2 hours, combine the extracts, concentrate in a vacuum until dry to obtain a crude extract, add water to dissolve, then add an equal amount of water-saturated n-butanol to extract more Once, the organic layer was collected and concentrated in vacuo to obtain an extract-like substance. Then, the extract was subjected to macroporous resin column chromatography, followed by eluting with distilled water, 20%, 40%, 60%, and 95% ethanol solution, collecting 60%-95% ethanol eluate, recovering ethanol, and evaporating to dryness. That is, 27g of total saponin crude product was obtained. The crude total saponins were dissolved in methanol, separated by HPLC preparative chromatography, and monitored online by an ultraviolet detector to collect the target componen...

Embodiment 2

[0025] Example 2 Effect test of saponin U on contractility of isolated guinea pig ileum smooth muscle induced by acetylcholine bromide

[0026] Qualified guinea pigs were taken and killed by clubbing. A section of ileum near the cecum was quickly taken and placed in Krebs' solution to separate the longitudinal smooth muscle of the ileum. Immediately add 19.5mL of Krebs' solution to the bath, maintain a constant temperature of 37°C, pass in a mixed gas (5% carbon dioxide, 95% oxygen, the same below), draw electrical signals from the tension sensor to the biological function experiment system, adjust the tension of the silk thread, and make the muscle bundle Load 1 gram, record muscle bundle relaxation and contraction, after 30 minutes of muscle bundle relaxation and contraction stabilization, record a section of muscle contraction force curve, after that, do the following dosing experiment. The same ileal muscle bundle can only be used for one test and will not be used repeated...

Embodiment 3

[0030] Example 3 Effect Test of Saponin U on the Propelling Percentage of Small Intestine Carbon End in M ​​Cholinergic Nervous Excitability Model Mice

[0031] Take 60 fasting mice and randomly divide them into normal group, model group, positive drug (atropine sulfate) group and three administration test groups, 10 in each group. Except for the normal group, the other groups were treated with 10ml.kg -1 Injection volume, intraperitoneal injection concentration is 2.0mg.ml -1 Pilocarpine liquid medicine, dosage 20.0mg.kg -1 . 15 minutes after the injection, the model group was injected with distilled water 10ml.kg into the tail vein -1 ; Positive drug group tail vein injection concentration is 0.025mg.ml -1 Atropine sulfate solution 10ml.kg -1 , dose 2.5mg.kg -1 ; The concentration of tail vein injection in the three administration test groups was 1.0, 0.5, 0.25mg.ml -1 Saponin U liquid 10ml.kg -1 , the doses were 10.0, 5.0, 2.5mg.kg -1 ; The normal group was not adm...

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Abstract

The invention discloses an application of mussaenda erythrophylla glucoside U in preparation of an antiacetyl-choline medicine. An inventor researches influences of mussaenda erythrophylla glucoside U to contractility of ileum smooth muscles of in-vitro guinea pig caused by acetylcholine bromide and the influences to mouse pupil diameter, sialaden secretion quantity and small intestine carbon powder promotion percentage of an M cholinergic neuron excitation model caused by pilocarpine, and the results prove that the of mussaenda erythrophylla glucoside U is the antiacetyl-choline medicine. By performing a mouse acute toxicity test, the half lethal dose of the mussaenda erythrophylla glucoside U for intravenous injection is obtained, and a proper dose of the mussaenda erythrophylla glucoside U for antiacetyl-choline intravenous injection can be obtained by means of calculation based on a mouse in-vivo test dose. Therefore, after a proper dose of the mussaenda erythrophylla glucoside U is taken by a person by intravenous injection or by other methods, a pharmacodynamic effect the same as that of atropine can be played. Thus, the mussaenda erythrophylla glucoside U and a medicine excipient are used for preparing an antiacetyl-choline medicine preparation which can be used for treating clinical patients with organophosphorus nerve agent poisoning, acute microcirculation disturbance, stomach and intestine cramp and biliary tract or urethral canal spasmodic pain.

Description

technical field [0001] The invention belongs to the technical field of anti-acetylcholine drugs, and relates to mussaendoside U (English name: mussaendoside U), especially the application of mussaendoside U in the preparation of anti-acetylcholine drugs. Background technique [0002] Human M cholinergic nerves transmit nerve impulses through the combination of acetylcholine and acetylcholine receptors, and any factors that affect the combination of acetylcholine and acetylcholine receptors will promote or block the transmission of M cholinergic nerve impulses, making the effector organs dysfunctional and pathological. Selecting pseudo- or anti-acetylcholine drugs to regulate the transmission of M cholinergic nerve impulses can partially or completely restore the function of pathological effect organs to normal. Organophosphorus nerve agent poisoning, acute microcirculatory disturbance, gastrointestinal colic, biliary tract or urethral spasm pain and other diseases are all ca...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P39/02A61P9/14A61P1/00A61P1/16A61P13/02
CPCA61K31/7048
Inventor 李嘉曾宪彪张颖姜平川韦宝伟韦桂宁
Owner GUANGXI INST OF CHINESE MEDICINE & PHARMA SCI
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