Application of phenylethanoid glycoside compound and composition thereof in preparation of medicine for preventing and treating new coronal pneumonia

A composition and drug technology, applied in the field of medicine, can solve the problems of vaccines and antiviral drugs without specific effects for severe pneumonia

Pending Publication Date: 2021-10-12
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Currently, there is no effective vaccine or antiviral drug for severe pneumonia caused by SARS-CoV-2 coronavirus

Method used

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  • Application of phenylethanoid glycoside compound and composition thereof in preparation of medicine for preventing and treating new coronal pneumonia
  • Application of phenylethanoid glycoside compound and composition thereof in preparation of medicine for preventing and treating new coronal pneumonia
  • Application of phenylethanoid glycoside compound and composition thereof in preparation of medicine for preventing and treating new coronal pneumonia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0156] Example 1: Isolation and structural identification of phenylethanol glycosides in Forsythia

[0157] 1.1. Method

[0158] Forsythia fruit (5Kg) purchased from Shanghai Tongrentang was crushed and soaked in 70% industrial ethanol (50L) at room temperature for 3 times, each time for 7 days. After the ethanol extracts were combined and concentrated, the obtained fluid extract (about 1Kg) was suspended in 15L of distilled water and then extracted 3 times with ethyl acetate (10L) to remove the middle and low polar components; the water layer was concentrated to 3L and then applied to a macroporous resin column Chromatography (AB-8, 3Kg) was sequentially eluted with 25 L of water, 10% ethanol, 40% ethanol, 70% ethanol and 95% ethanol. According to HPLC-MS analysis, forsythiaside components were mainly concentrated in the elution site of 40% ethanol. 40% of the eluate was concentrated and the obtained extract was taken 10 g, mixed with OSD, and then subjected to ODS (RP-C18,...

Embodiment 2

[0168] Example 2: Inhibitory effect of forsythiaside compounds on 2019-nCoV-3CLpro

[0169]The inhibitory activity of phenylethanol glycosides in Forsythia glycosides on 2019-nCoV3CLpro enzyme activity was evaluated by fluorescence resonance energy transfer method. The volume of the entire enzymatic reaction system is 120 μL, the final concentration of protease is 30 nM, and the final concentration of substrate is 20 μM. The buffer of the reaction system includes 50mM Tris pH7.3, 1mM EDTA. Add samples such as 2019-nCoV 3CLpro protease and different concentrations of compounds or mixtures to the 96-well plate, incubate at 30°C for 10 minutes, add the substrate and quickly put it into a microplate reader for reading. Excitation light and emission light were 340 nM and 405 nM, respectively. The test time is 10min, and the fluorescence value is read every 30s. In the final result, the reading value of the first 2 minutes was used to fit the reaction rate, and compared with the ...

Embodiment 3

[0178] Example 3: Isolation and structural identification of other phenylethanol glycosides

[0179] With reference to the literature and the above-mentioned preparation method, salidroside (Salidroside), pyloroside A1 (Jionoside A1) and B1 (Jionoside B1), isergoside (Isoacteoside), echinacoside (Echinacoside) and cistanche glycoside A (Cistanoside A), Poliumoside, Angoroside C (Angoroside C), Calceolarioside B (calceolarioside B), Desrhamnosylmartynoside (Desrhamnosylmartynoside) were obtained from Rhodiola rosea (Rhodiola rosea), Radix Rehmanniae Praeparata, Cistanche tubulosa, Callicarpa kwangtungensis, Scrophularia ningpoensis, Akebia quinata, Scutellaria prostrata. The structures of the compounds were identified by 1H NMR, 13C NMR and mass spectrometry.

[0180] Salidroside: white powder, ESI-MS m / z 299.3[M-H]+; 1H NMR (400 MHz, MeOH-d4) phenylethyl alcohol fragment: δ7.06 (2H, d, J = 8.6Hz, H-2,6),6.69(2H,d, J=8.6Hz,H-3,5),2.83(2H,m,H-7),3.70 and 4.03(each 1H,m,H-8a,8b...

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Abstract

The invention relates to application of a phenylethanoid glycoside compound and a composition thereof in preparation of a medicine for preventing and treating new coronal pneumonia. Specifically, the invention relates to application of a phenylethanoid glycoside compound and a pharmaceutical composition thereof as a 2019 novel coronavirus (SARS-CoV-2) 3CL protease inhibitor in preparation of drugs for treating and/or preventing and relieving respiratory tract infection, pneumonia and other related diseases caused by 2019 novel coronavirus infection.

Description

technical field [0001] The present invention relates to the field of medicine, in particular to the new application of phenylethanol glycoside compounds and compositions thereof, especially the use of phenylethanol glucoside compounds and compositions thereof in anti-coronavirus (SARS-CoV-2 or 2019-nCoV) use. Background technique [0002] Among the acute infectious diseases, most of them are viral infectious diseases, the incidence rate of viral infectious diseases is high, and the mortality rate is also high. Due to the limited means of detection and diagnosis, outbreaks of new outbreaks caused by new viruses are often characterized by suddenness, randomness, and unpredictability. Health and life safety. [0003] Novel coronavirus (SARS-CoV-2) infection can cause severe pneumonia. The transmission route of the SARS-CoV-2 virus is not fully understood. It is known that it can be transmitted through droplets and contact, and there is human-to-human transmission and infecti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7032A61K45/06A61K31/513A61K31/4706A61K31/675A61K31/427A61K31/4965A61P31/14A61P11/00
CPCA61K31/7032A61K45/06A61K31/513A61K31/4706A61K31/675A61K31/427A61K31/4965A61P31/14A61P11/00A61K2300/00
Inventor 叶阳许叶春姚胜赵文峰柯昌强苏海霞
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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