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Ephedra sinica/ephedra intermedia/ephedra equisetina stem extract and active components and application thereof

A technology of ephedra and ethanol extract, which is applied in the field of pharmacy, can solve the problem of no specific medicine for new coronavirus infection

Inactive Publication Date: 2021-01-15
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no specific drug for the prevention and treatment of new coronavirus infection

Method used

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  • Ephedra sinica/ephedra intermedia/ephedra equisetina stem extract and active components and application thereof
  • Ephedra sinica/ephedra intermedia/ephedra equisetina stem extract and active components and application thereof
  • Ephedra sinica/ephedra intermedia/ephedra equisetina stem extract and active components and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] The preparation of embodiment one ephedra water extract

[0026] 1. Materials

[0027] Dried ephedra herbaceous stems; Milli-Q Direct 8 pure water / ultrapure water integrated system (Bedford, the United States); rotary evaporator (Tokyo Physical and Chemical Company); decoction machine and spray dryer (Shanghai Yaoshi Instruments and Equipment).

[0028] 2. Method

[0029] Take 1kg of ephedra, chop it into a 20L decoction machine, add 10L of pure water, soak for 30 minutes, heat to boil, decoct for 20 minutes, collect the medicinal liquid; add 8L of pure water, heat to boil, decoct for 15 minutes Minutes, combined decoction, filtered, decoction concentrated in a 20L rotary evaporator at a temperature of 50 ° C and a vacuum of -0.095 MPa to 2 L under reduced pressure, and the concentrate was placed in a spray dryer at an air inlet temperature of 130 ° C, Spray drying is carried out under the conditions of air outlet temperature above 75°C and atomizer pressure of 0.2 MP...

Embodiment 2

[0030] The preparation of embodiment diephedrine ethanol extract

[0031] 1. Materials

[0032] Dried ephedra herbaceous stems; methanol and formic acid are chromatographically pure, and other reagents are analytically pure. Milli-Q Direct 8 pure water / ultrapure water integrated system (Bedford, USA); KQ-800DE digital ultrasonic instrument (Kunshan Ultrasonic Instrument Co., Ltd.); EYELA rotary evaporator (Tokyo Physical and Chemical Company); low-temperature high-speed centrifuge (Thermo), YHG-9245A type electric heating constant temperature blast drying oven (Shanghai Yao's Instrument and Equipment).

[0033] 2. Method

[0034]Crush the ephedra, soak it in 85% ethanol according to the ratio of solid to liquid 1:5, reflux and extract three times at 80°C, filter to obtain the extract, repeat the extraction three times, combine the extract, add methanol to fully dissolve, and then extract three times with n-heptane , recover the solvent to obtain methanol layer extract and n...

Embodiment 3

[0035] The identification of the main component of ephedrine ephedrine ethanol extract

[0036] 1. Materials and methods

[0037] 1.1 Materials

[0038] Ephedrine alcohol extract powder (prepared by Example 2), UHPLC-Q-Exactive Orbitrap HRMS liquid mass spectrometry system: Dionex Ultimate 3000 high pressure liquid chromatography series Q Exactive quadrupole / electrostatic field orbitrap high resolution mass spectrometer (U.S. Thermo Fisher Scientific); Acquity BEH C18 chromatographic column (100mm×2.1mm, 1.7μm, American Waters Company);

[0039] 1.1 Method

[0040] Chromatographic conditions are using Dionex Ultimate 3000 high pressure liquid phase system, Acquity BEH C 18 Chromatographic column (100mm×2.1mm, 1.7μm); mobile phase is 0.1% formic acid water and methanol, gradient elution, elution program is 0-2min, 4% methanol; 2-6min, 4%-12% methanol; 6 ~38min, 12%-70% methanol; 38~38.5min, 70% methanol; 38.5~39min, 70%~95% methanol; 39~43min, 95% methanol; 43~45min, 4%...

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Abstract

The invention relates to the field of pharmacy, in particular to ephedra sinica / ephedra intermedia / ephedra equisetina stem extract capable of inhibiting novel coronavirus 3CL proteolytic enzymes as well as active components and application of the ephedra sinica / ephedra intermedia / ephedra equisetina stem extract. The ephedra sinica / ephedra intermedia / ephedra equisetina stem extract is ephedra sinica / ephedra intermedia / ephedra equisetina stem water extract and ephedra sinica / ephedra intermedia / ephedra equisetina stem alcohol extract; and the active components comprise herbacetin, gallic acid, quercetin and apigenin. The ephedra sinica / ephedra intermedia / ephedra equisetina stem extract and the active components thereof can be used for treating patients infected with novel coronaviruses.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to an extract of ephedra and its active ingredient and its medical application. Background technique [0002] Viral pneumonia (COVID-19) caused by the novel coronavirus (SARS-CoV-2) has become a public health emergency of international concern. The virus is generally excreted through respiratory secretions, can be transmitted through droplets, and can also be transmitted through contact. During the process of virus infecting the host, the 3CL proteolytic enzyme (also known as M pro ) is a class of cysteine ​​hydrolases that can cleave polyproteins during viral replication to generate multiple active functional proteins, which play an important role in viral transcription and replication. Therefore, 3CL proteolytic enzyme can be used as a key and safe therapeutic target against 2019-nCoV. At present, there is no specific drug for the prevention and treatment of new coronavirus ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/17A61P31/14A01N65/00A01P1/00A01N25/04C11D3/382C11D3/48
CPCA61K36/17A61P31/14A01N65/00A01N25/04C11D3/382C11D3/48A61K2236/331A61K2236/39A61K2236/51A61K2236/333A61K2236/55C11D2111/12
Inventor 葛广波胡情熊媛朱广灏
Owner SHANGHAI UNIV OF T C M
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