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Application of jasminum grandiflorum extract or active ingredients thereof in preparation of elastase inhibitor

A technology of elastase and active ingredients, applied in the direction of active ingredients of hydroxyl compounds, medical preparations containing active ingredients, organic active ingredients, etc., can solve problems such as loss of elasticity, loss of skin elasticity, and wrinkles

Active Publication Date: 2021-09-14
WUYI UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Elastase is an endopeptidase that can hydrolyze elastin and collagen, and the hydrolysis of elastin and collagen can lead to aging manifestations such as skin loss of elasticity, sagging, and wrinkles, although this process is under healthy skin aging conditions Normal process, but environmental factors and oxidative stress in internal cells such as fibroblasts in the dermis, not only overexpress elastase, but also promote the hydrolysis of elastin and collagen, which in turn exacerbates the mechanical structure of the skin. loss of skin elasticity, sagging, and wrinkles. It also reduces the number of fibroblasts in the dermis and changes the shape of fibroblasts, thereby accelerating skin aging; in addition, under normal physiological conditions, elastase can assist phagocytic cells to eliminate harmful substances. Bacteria can promote wound healing and tissue regeneration, but its overexpression can cause the body's inflammatory response, promote the proliferation and metastasis of cancer cells, and induce various diseases including emphysema

Method used

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  • Application of jasminum grandiflorum extract or active ingredients thereof in preparation of elastase inhibitor
  • Application of jasminum grandiflorum extract or active ingredients thereof in preparation of elastase inhibitor
  • Application of jasminum grandiflorum extract or active ingredients thereof in preparation of elastase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Extraction and Purification of Jasmine Extract and Active Components thereof

[0036] Dry the jasmine needles in the air and pulverize them into powder. Take 8 kg of jasmine needles powder and extract them with 10 L of 80% ethanol aqueous solution at normal temperature and pressure for three times for 3 days each time to obtain the jasmine needles alcohol extract. Concentrate under reduced pressure to obtain the ethanol extract; then add 2L distilled water to the ethanol extract to dissolve it, and then extract three times with 1L petroleum ether (1L×3), and then extract the residue three times with 1L ethyl acetate (1L×3). 3) extracted three times with 1L n-butanol (1L×3), combined and collected the ethyl acetate extract, and concentrated to obtain the ethyl acetate layer extract of jasmine needles.

[0037] The active ingredients in the ethyl acetate layer extract of jasmine needles include OLE and HT, and the method for separating and purifying HT from the ...

Embodiment 2

[0041] Example 2 The inhibitory effect test of jasmine needle extract and its active ingredients on elastase

[0042] This embodiment is to investigate the inhibitory effect test of OLE and HT to elastase, and concrete test method is as follows:

[0043] 1. Preparation of test solution:

[0044] Use dimethyl sulfoxide (Dimethyl sulfoxide, DMSO) to prepare the stock solution with a concentration of 100 mg / mL from the extract of the jasmine needle ethyl acetate layer prepared in Example 1, and dilute successively to a final concentration of 1000 μg / mL, 500 μg / mL mL, 250μg / mL, 125μg / mL, 62.5μg / mL.

[0045] The HT prepared in Example 1 was prepared into a stock solution with a concentration of 100 mM with DMSO, and diluted successively, and the final concentrations were 1000 μM, 500 μM, 250 μM, 125 μM, and 62.5 μM. .

[0046] The OLE prepared in Example 1 was prepared into a stock solution with a concentration of 100 mM with DMSO, and diluted successively, and the final concent...

Embodiment 3

[0054] Example 3 Synergistic inhibitory effect test of oleuropein and hydroxytyrosol on elastase

[0055] In this embodiment, to explore whether oleuropein (OLE) and hydroxytyrosol (HT) have a synergistic inhibitory effect on elastase, the specific test method is as follows:

[0056] 1. Elastase activity inhibition test

[0057] (1) Sample preparation:

[0058] The samples with a concentration of 100 mM were diluted in turn so that the final concentrations of OLE and HT were 62.5 μM, 125 μM, 250 μM, 500 μM, and 1000 μM as the samples to be tested; at the same time, the mixture of OLE and HT with equal volume and equimolar concentration (OLE+HT ) is the sample to be tested.

[0059] (2) Test method and test result

[0060] Take 10 μL of samples to be tested at different concentrations and add them to a 96-well plate, then add 120 μL of Tris-HCl buffer solution (concentration: 2 mM, pH=8) into the 96-well plate, and then add 20 μL of Tris-HCl buffer solution with a concentrat...

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to application of a jasminum grandiflorum extract or active ingredients thereof in preparation of an elastase inhibitor, and the jasminum grandiflorum extract is an ethyl acetate layer extract of jasminum grandiflorum; and the effective ingredients of the jasminum jasminoides extract comprise oleuropein and hydroxytyrosol. The oleuropein, the hydroxytyrosol or the jasminum grandiflorum extract all have an effect of inhibiting activity of elastase, skin aging, emphysema and other diseases caused by overexpression of the elastase are avoided, and when the oleuropein and the hydroxytyrosol which are equal in molar concentration are mixed in an isovolumetric mode, an inhibiting effect on elastase is higher. Therefore, the oleuropein, hydroxytyrosol or jasminum grandiflorum extract provides a new choice for improving skin aging or treating chronic complications of emphysema.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to the application of jasmine needle extract or its active ingredients in the preparation of elastase inhibitors. Background technique [0002] Elastase is an endopeptidase that can hydrolyze elastin and collagen, and the hydrolysis of elastin and collagen can lead to aging manifestations such as loss of elasticity, sagging, and wrinkles in the skin, although this process is under healthy skin aging conditions Normal process, but environmental factors and oxidative stress in internal cells such as fibroblasts in the dermis, not only overexpress elastase, but also promote the hydrolysis of elastin and collagen, which in turn exacerbates the mechanical structure of the skin. loss of skin elasticity, sagging, and wrinkles. It also reduces the number of fibroblasts in the dermis and changes the shape of fibroblasts, thereby accelerating skin aging; in addition, under norma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K31/05A61P11/00A61K8/34A61K8/60A61K8/9789A61K36/63A61Q19/08
CPCA61K31/7048A61K31/05A61P11/00A61K8/9789A61K8/602A61K8/347A61Q19/08A61K36/63A61K2800/782A61K2800/592A61K2300/00
Inventor 李冬利李慧芳马航周致言彭兴家张奕孜谢寅正吴盼盼刘文锋徐学涛张焜
Owner WUYI UNIV
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