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Medicine composition containing myricetrin or/and myricetin and application of medicine composition in preparation of medicine used for treating Parkinson

A composition and a technology for Parkinson's disease are applied in a pharmaceutical composition containing salicylic glycoside or/and aglycone myricetin to prepare medicines for treating Parkinson's disease, can solve problems such as liver damage, achieve good anti-inflammatory, Good antioxidant activity, high safety effect

Inactive Publication Date: 2013-07-24
无锡艾德美特生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, continuous use of commercially available COMT enzyme inhibitors, such as Tolcapone and Entacapone, can easily cause severe liver damage and other toxic side effects (Neurology2004;62:39-46)
However, PD patients need frequent medication, and long-term use of existing drugs can cause severe liver damage

Method used

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  • Medicine composition containing myricetrin or/and myricetin and application of medicine composition in preparation of medicine used for treating Parkinson
  • Medicine composition containing myricetrin or/and myricetin and application of medicine composition in preparation of medicine used for treating Parkinson
  • Medicine composition containing myricetrin or/and myricetin and application of medicine composition in preparation of medicine used for treating Parkinson

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 Determination of Inhibitory Activity of Myricetin and Its Aglycone Myricetin Monomer to Human COMT Enzyme

[0032] Using the L-dopa methylation reaction as a probe reaction, the IC of myricetin and its aglycon myricetin on the inhibition of COMT enzyme was determined by means of the in vitro incubation system of human hepatocytes 50 , the specific experimental procedure is as follows:

[0033] (1) Add 5mM MgCl to 200 microliters of in vitro metabolic reaction system 2 , 2mM dithiothreitol, 150μM substrate L-dopa, human liver cell plasma protein concentration is 1mg / ml, inhibitor final concentration range is 0.05μM-50μM, pre-incubated at 37℃ for 3 minutes;

[0034] (2) Add S-adenosylmethionine (final concentration: 0.2mM) to the reaction system to initiate the reaction; after reacting at 37°C for 30 minutes, add 200 μl of acetonitrile, shake vigorously, and terminate the reaction;

[0035] (3) Using a high-speed refrigerated centrifuge, under the condition of 2...

Embodiment 2

[0037] Example 2 Toxicity Evaluation of Myricetin and Its Aglycone Myricetin

[0038] Select Kunming mice, weighing 178-22g. The mice were divided into random groups, 20 in each group, half male and half male, and the oral acute toxicity test of myricetin and myricetin were carried out in mice respectively. Myricetin or myricetin were suspended in 0.5% CMC-Na, respectively. Select different doses of oral administration (0.1 ~ 2g / kg); and set 0.5% CMC-Na group as a negative control. Experimental results show that myricetin and myricetin oral administration of LD in mice 50 The value is greater than 2.0g / kg, which belongs to the non-toxic level. In addition, in vitro cell experiments confirmed that myricetin and myricetin had no obvious toxicity to primary human liver cells and kidney cells. At the same time, the myricetin and its aglycone myricetin (final concentration: 100 μM) and reduced glutathione (final concentration: 1000 μM) were respectively added to the human liver...

Embodiment 3

[0039] Example 3 Pharmacokinetic study of myricetin and its aglycon myricetin combined with levodopa

[0040] As a COMT enzyme inhibitor, myricetin or / and myricetin has no therapeutic effect on Parkinson's disease when administered alone, and it is meaningful only when combined with levodopa.

[0041] Select 24 Wistar rats, half male and half female, body weight 180-220g, randomly divided into 4 groups: oral levodopa / carbidopa control group, oral myricetin / levodopa / carbidopa group (myricetin The molar ratio of myricetin to levodopa is 5:1), oral administration of myricetin / levodopa / carbidopa group (the molar ratio of myricetin to levodopa is 5:1), oral administration of myricetin-myricetin mixture / levodopa In the ba / carbidopa group (the molar ratio of the sum of the moles of myricetin and myricetin to levodopa is 5:1), 6 animals / group were used to carry out the overall pharmacokinetic study of L-dopa. The oral dose is 2g / kg. About 0.5ml of rat plasma samples were collected b...

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Abstract

The invention relates to a medicine composition of myricetrin or / and myricetin aglycone thereof and levodopa or of levodopa and carbidopa and an application of myricetrin or / and myricetin aglycone thereof as a synergist in preparation of a medicine used for treating Parkinson. In vitro activity determination finds that IC50 of myricetrin and myricetin inhibiting catechol-O-methyltransferase (COMT) can be a micromole-nanomole scale. Rat overall pharmacokinetic study finds that blood concentration of levodopa can be increased after myricetrin and myricetin aglycone thereof and levodopa are used jointly; and myricetrin and myricetin aglycone thereof are high in safety, no obvious toxicity is produced to main visceral organ cells of a human body, and no active intermediate is produced by virtue of metabolism activation and further no damage done to organs such as liver and kidney is initiated, so that the myricetrin and myricetin aglycone thereof have a good application prospect in adjuvant therapy of Parkinson.

Description

technical field [0001] The present invention relates to a pharmaceutical composition and its use, in particular to a pharmaceutical composition containing myricetin or / and aglycon myricetin and its use in the preparation of medicines for treating Parkinson's disease. Background technique [0002] Parkinson's disease (PD) is a chronic central nervous system degenerative disorder caused by insufficient dopamine in the brain, and the incidence rate in the elderly is as high as 1.7% (Neurology.2000;54:S24-7). my country is the country with the largest number of PD patients in the world. With the advent of my country's aging society, the medical, family, and social problems brought about by PD have become more extensive and severe, and the quality of life of patients has been greatly affected. [0003] At present, the most effective treatment for Parkinson's disease (PD) is dopamine replacement therapy, which converts the prodrug levodopa (L-dopa) into dopamine in the patient's b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K31/352A61P25/16A61K31/198
Inventor 杨凌葛广波孙晓宇宁静夏杨柳邹超
Owner 无锡艾德美特生物科技有限公司
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