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Application of cholinesterase in antagonistic tachykinin medicine

A technology of cholinesterase and tachykinin, which is applied in the application field of medicine to achieve the effects of small side effects, suitable for industrialization, and wide sources

Inactive Publication Date: 2008-06-04
SHENZHEN DINGXIN BIO MEDICINE TECH DEV +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no report in the literature that cholinesterase is used to prepare drugs for the treatment or prevention of diseases mediated by substance P isotachine

Method used

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  • Application of cholinesterase in antagonistic tachykinin medicine
  • Application of cholinesterase in antagonistic tachykinin medicine
  • Application of cholinesterase in antagonistic tachykinin medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] Embodiment 1 hydrolysis SP test

[0071] Butyrylcholinesterase and acetylcholinesterase, which are used in the market as an enzyme inhibition method to detect pesticide residues, were used to hydrolyze substance P respectively. Reaction and detection conditions:

[0072] 1. Cholinesterase used:

[0073] (1) butyrylcholinesterase, specific activity 200U freeze-dried powder 50mg with 5ml iron ion water (F 3+ Content 1mg / L) dissolved, centrifuged at 10,000 rpm for 4 minutes;

[0074] (2) butyrylcholinesterase, specific activity 200U lyophilized powder 50mg dissolved in 5ml double distilled water, centrifuged at 10000 rpm for 4 minutes;

[0075] (3) Acetylcholinesterase, specific activity 300U freeze-dried powder 20mg dissolved in 1ml double distilled water, centrifuged at 10000 rpm for 4 minutes.

[0076] 2. Substrate

[0077] The purity of SP is 98%, and the concentration of the aqueous solution is 0.5ug / ml.

[0078] 3. Response

[0079] Substrate+enzyme 100ul+100u...

Embodiment 2

[0086] Embodiment 2 prepares acetylcholinesterase aqueous solution

[0087] Use acetylcholinesterase freeze-dried powder produced by SIGMA company, add water to dissolve, add stabilizer propylene glycol, antibacterial agent phenol at the same time, according to each milliliter solution contains acetylcholinesterase enzyme activity from 10 to 1000U, divide into several orders of magnitude, according to the way of use, pack them separately Disposable syringes, spray bottles, or other medically acceptable vials, kept refrigerated. The storage period can be up to 1 year, and it can be administered directly or diluted according to the treatment requirements.

[0088] Vitality assay:

[0089] 1. Theoretical basis: According to the Ellman method, thioacetylcholine iodide (BTCI) is hydrolyzed into thiocholine and acetic acid under the action of cholinesterase (AChE), and thiocholine can be combined with dithiop-nitrobenzoic acid (DTNB) reacts to generate a yellow product, which has ...

Embodiment 3

[0092] Embodiment 3 aqueous solution 2

[0093] Aqueous solution 1 is added with 5% propylene glycol and 0.5% laurocaprazine as a penetration enhancer, combined with transdermal absorption methods such as iontophoresis or ultrasonic method, for external use.

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PUM

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Abstract

The invention belongs to the field of bio-pharmaceutical technology, and discloses the pharmaceutical application of cholinesterase, in particular to the application of cholinesterase in the medicines for treating or preventing the diseases and symptoms mediated by tachykinin in mammals including the human body. The diseases and symptoms include pain, inflammation, central nervous system disease, respiratory disease, gastrointestinal dysfunction and disease, allergy, neuropathological disease, diseases relating to immunopotentiation or immune suppression, rheumatism, skin disease and chronic fatigue syndrome. Being applied in medicines, the cholinesterase provides an effective treatment method with small side effect for people with physiological and pathological changes caused by excessive tachykinin like substance P, etc. The cholinesterase of the invention can be acetylcholinesterase, butyrylcholine esterase, the isoenzyme thereof or the ramification thereof, can derive from the cells, tissues, or blood of animals, or can derive from plants and be obtained through gene recombination. The invention has broad source, does not need to be highly purified, and is suitable for industrialization.

Description

technical field [0001] The present invention relates to a medicine for treating or preventing a disease mediated by a tachykinin, in particular to a cholinesterase which first hydrolyzes an amino acid residue at a C-terminal Leu-Met site to prepare a medicine for treating a disease mediated by a tachykinin in the application. Background technique [0002] Tachykinins (TKs) are a group of peptides with the following series of common amidated carboxy-terminals. Tachykinin C-terminus has -Phe-X-Gly-Leu-Met-NH 2 The common structure is a similar pharmacologically active neuropeptide produced in mammals, including humans, with a variety of physiological functions. The name of tachykinins comes from their stimulating effect on smooth muscle tissue. Mammalian tachykinins mainly include Substance P (Substance P, SP), Neurokinin A (Neurokinin A, NKA) and Neurokinin B (Neurokinin B, NKB). Tachykinins are widely distributed in the central nervous system and peripheral nervous system...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/46A61P29/00A61P25/00A61P11/00A61P1/00A61P37/02A61P17/00A61P43/00
CPCA61K38/465A61K38/46C12Y301/01007C12Y301/01008A61P1/00A61P11/00A61P17/00A61P25/00A61P29/00A61P37/00A61P37/02A61P43/00
Inventor 徐汉虹陶国良
Owner SHENZHEN DINGXIN BIO MEDICINE TECH DEV
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