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Natural activator of soluble guanylate cyclase

A guanylate cyclase, soluble technology, applied in the fields of biochemistry and medicinal chemistry, can solve the problems of inconvenient use, individual differences, and large toxic and side effects

Inactive Publication Date: 2010-03-17
JILIN UNIV
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  • Abstract
  • Description
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Problems solved by technology

However, the individual differences and toxic and side effects of herbal medicines are relatively large, and the effective dose of some herbal medicines is 60% of the toxic dose, which brings great inconvenience to the effective use of this medicinal material.

Method used

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  • Natural activator of soluble guanylate cyclase
  • Natural activator of soluble guanylate cyclase

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0013] (1) Purification, activity determination and purity identification of bovine lung soluble guanylyl cyclase were performed using our established method (Li zhengqiang et al Biochemistry (2005) 44: 939).

[0014] (2) with purified soluble guanylate cyclase and 3 The H-GTP bioassay technology platform screens out the active ingredients in plant medicines with activating effects.

[0015] (3) Separating the components of the screened botanical drugs by category, and then screening to determine the chemical classification of the compound, and use computer-aided optimization technology to determine the structure of YC-1 and BAY chemically synthesized in vitro using combinatorial chemistry methods Comparative analysis and simulation.

[0016] (4) Separation and screening of a single compound.

[0017] (5) The study on the synergistic activation of soluble guanylate cyclase by activators (compounds) and carbon monoxide, Km, Vm determination.

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Abstract

The invention relates to a natural activator of soluble guanylate cyclase, which is characterized in that the soluble guanylate cyclase in a human circulatory system is used as a selected target; <3>Hisotope is used for marking; and natural components capable of activating the soluble guanylate cyclase are selected from plant medicaments for treating cardiovascular-related diseases in Chinese, Indian and European traditional medicine. The natural components capable of activating the soluble guanylate cyclase in the human circulatory system under the condition of vitro experiments are obtainedthrough screening, and structure searches and further activation analyses are carried out on the natural components and metabolic components thereof in the human body. The mother nucleus structure ofa substance capable of activating the soluble guanylate cyclase and the side chain structure information of the mother nucleus are obtained so as to provide the pertinent information for the researchand development of medicaments related to the treatment of cardiovascular diseases relating to the soluble guanylate cyclase-cGMP signal conduction path.

Description

technical field [0001] The invention belongs to the fields of biochemistry and medicinal chemistry, and specifically relates to a 3 The method of H isotope labeling screens natural activators that can activate soluble guanylate cyclase in the circulatory system from plant tissues used in Chinese, Indian and European traditional medicine to treat cardiovascular-related diseases. Background technique [0002] Enzymes have important physiological and biochemical functions in organisms, and the prevention and treatment of many diseases are directly related to the signal transduction involved in enzymes. The signal transduction involving soluble guanylate cyclase (sGC) can regulate platelet aggregation inhibition and vascular smooth muscle relaxation, and play an important role in the prevention and treatment of cardiovascular diseases. [0003] As we all know, cardiovascular and cerebrovascular diseases have become the number one hidden danger to human health. Over the years, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/585A61P7/02A61P9/10A61P9/00
Inventor 李正强程瑛琨吕明张华利张跃斌
Owner JILIN UNIV
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