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Application of rosmarinic acid as peroxynitrite inhibitor

A technology of rosmarinic acid and inhibitor, applied in the application field of rosmarinic acid as a peroxynitrite inhibitor

Inactive Publication Date: 2009-12-09
BEIJING UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The natural Chinese herbal medicine scavengers currently used to remove peroxynitrite in the body are mainly some compound ingredients (Hye Rhi Choi, Jae Sue Choi, Yong NamHan, et al., Phytother.Res.2002, 16, 364-367), with a single ingredient Rosmarinic acid scavenging peroxynitrite in vivo has not been reported

Method used

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  • Application of rosmarinic acid as peroxynitrite inhibitor
  • Application of rosmarinic acid as peroxynitrite inhibitor
  • Application of rosmarinic acid as peroxynitrite inhibitor

Examples

Experimental program
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Effect test

Embodiment 1

[0125] Embodiment 1: Extraction, separation and purification of rosmarinic acid in rosemary

[0126] Crush the dried stems and leaves of rosemary, weigh 100g of the powder, put it in a conical flask, add 500mL of water, extract in a water bath at 90°C for 45min, extract twice, and combine the extracts. Adjust the pH value to about 2.5 with 18% hydrochloric acid solution. Suction filtration was carried out with a microporous membrane, and then extracted with ethyl acetate. After three extractions, the extracts were combined to remove the ethyl acetate. The rosemary residue was then eluted with 50% ethanol, and after drying, 300 mL of 1% NaHCO was added 3 The aqueous solution was leached three times at 60°C, filtered through a filter membrane, the extracts were combined, concentrated and dried to obtain water-soluble rosmarinic acid. with FeSO 4 Colorimetric method, the absorbance was measured at 572nm, and the yield and concentration of rosmarinic acid were calculated.

Embodiment 2

[0128] Tablets are prepared according to methods known in the art, each containing the following ingredients:

[0129] Rosmarinic Acid 80mg

[0130] Lactose 45mg

[0131] Magnesium Stearate 5mg

[0132] Polyvinylpyrrolidone 10mg

[0133] Microcrystalline Cellulose 20mg

[0134] Total 160mg

Embodiment 3

[0136] Capsules are prepared according to methods known in the art, and each capsule contains the following ingredients:

[0137] Rosmarinic Acid 80mg

[0138] Lactose 45mg

[0139] Corn starch 25mg

[0140] Magnesium Stearate 2mg

[0141] Polyvinylpyrrolidone 8mg

[0142] 160mg total.

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Abstract

The invention provides an application of rosmarinic acid as a peroxynitrite inhibitor. The invention further provides the application of rosmarinic acid in the preparation of drugs for curing and preventing atherosclerotic lesions, acute or chronic inflammation, ischemia reperfusion injury and neurodegenerative diseases caused by peroxynitrite. The invention selects rosmarinius officinalis, which is Chinese herbal medicine having medicinal value, as the research object, and the effective active component of rosmarinius officinalis is separated and purified to obtain the rosmarinic acid. The rosmarinic acid can effectively inhibit the bio-macromolecule damage induced by peroxynitrite, particularly, the rosmarinic acid can effectively inhibit the DNA chain breakage induced by peroxynitrite with the inhibition ratio reaching 40% under low concentration and the rosmarinic acid can further inhibit the protein tyrosine nitration and the low-density lipoprotein lipid peroxidation induced by peroxynitrite with the inhibition ratio reaching higher than 50% under low concentration.

Description

technical field [0001] The invention relates to the application of single component rosmarinic acid in rosemary extract to effectively inhibit the toxicity of endogenous oxidant peroxynitrite. Background technique [0002] Rosmarinic acid (cichoric acid) is a polyphenolic hydroxy acid, which is a condensation product of a molecule of caffeic acid and a molecule of 3,4-dihydroxyphenyl lactic acid (that is, danshensu). It was first obtained from the rosemary plant in 1958. (Rosmarinius officinalis) and its structure is as follows. Rosmarinic acid is widely distributed, mainly in Labiatae, Boraginaceae, Cucurbitaceae, Basswood and Umbelliferae. Studies have found that rosmarinic acid has a strong antioxidant effect. Studies have shown that its mechanism of action is: rosmarinic acid competes with unsaturated fatty acids to combine with lipid peroxyl to terminate the chain reaction of lipid peroxidation and reduce the rate of lipid peroxidation, while rosmarinic acid is oxidiz...

Claims

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Application Information

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IPC IPC(8): A61K31/216A61P43/00A61P9/10A61P29/00A61P25/28
Inventor 罗云敬钟儒刚潘竟林韩治国
Owner BEIJING UNIV OF TECH
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