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Application of iridoid in preparation of anti-SARS (severe acute respiratory syndromes) medicines

A technology of iridoids and compounds, applied in the field of medicinal chemistry, can solve the problem of no relevant reports on inhibitory effects

Inactive Publication Date: 2013-05-29
TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there is no relevant report on the inhibitory effect of natural iridoids on the main protease of SARS coronavirus

Method used

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  • Application of iridoid in preparation of anti-SARS (severe acute respiratory syndromes) medicines
  • Application of iridoid in preparation of anti-SARS (severe acute respiratory syndromes) medicines
  • Application of iridoid in preparation of anti-SARS (severe acute respiratory syndromes) medicines

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Expression, purification and crystal growth of embodiment 1SARS coronavirus main protease

[0042] According to the literature (Yang H. et al., Proc Natl Acad Sci, 2003 Nov; 100 (23): 13190-13915), the expression, purification and crystal growth of the main protease of SARS coronavirus are carried out, and the diffraction resolution is higher (higher than ) crystals of the SARS coronavirus main protease. The specific method is as follows:

[0043] 1) the construction of the expression vector of SARS coronavirus main protease, concrete steps comprise:

[0044] a. Use the cDNA library of the SARS virus strain numbered BJ01 provided by Beijing Huada Gene Center, and use PCR technology to amplify in vitro;

[0045] Forward primer: 5′-CGGGATCCAGTGGTTTTAGGAAAATG-3′

[0046] Reverse primer: 5′-CCGCTCGAGTCATTGGAAGGTAACACCAGA-3′

[0047] b. After the gene fragment amplified by PCR is digested with BamHI and XhoI double enzymes, a fragment of about 1 kb in size is recovered ...

Embodiment 2

[0060] The screening method of embodiment 2SARS coronavirus main protease inhibitors

[0061] The method for the screening SARS coronavirus main protease inhibitor that the present invention adopts is the screening method disclosed in CN101418334A such as Rao Zihe, and concrete method is as follows:

[0062] The assay of the activity of the main protease of SARS coronavirus is done using the fluorescent substrate MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2 (purity greater than 95%, Shanghai Gil Biochemical Co., Ltd.). The amino acid sequence of the fluorescent substrate is derived from the N-terminal self-cleaving sequence of the SARS coronavirus main protease.

[0063] The instrument used for the determination of fluorescence intensity was a Fluoraskan Ascent fluorimeter (ThermoLabsystems, Helsinki, Finland), and the wavelengths of excitation light and emission light were 320 nm and 405 nm, respectively.

[0064] In buffer solution (50mM Tris-HCl (pH 7.3), 1mM EDTA (containing or not cont...

Embodiment 3

[0066] The preparation of the alternative sample of embodiment 3 Gentiana chinensis

[0067] 2 kg of dried and pulverized Gentiana medicinal materials were extracted 3 times with 7.5 liters of 95% ethanol under reflux, each time for 2 hours, 18 kg of Gentiana medicinal materials were extracted 9 times respectively, and the extracts obtained by reflux extraction with 9 times of 95% ethanol were combined and concentrated Obtain 4.5 kilograms of extractum.

[0068]The obtained 4.5 kg extract was divided into 4 parts with 1.5 liters of double distilled water to suspend and ultrasonically dissolve for 2 hours, then pour it into a 5 liter separatory funnel, and use sherwood oil, dichloromethane, Extract with ethyl acetate and n-butanol each time with 2.5 liters of organic solvent, shake fully, stand for 6 hours, extract each solvent 3 times, separate the organic solvent phase and the water phase, and combine the extracts of various solvent layers Concentrate with an EYELA N1001 typ...

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Abstract

The invention provides application of iridoid with a general formula (I) in preparation of medicines for treating or preventing SARS (severe acute respiratory syndromes). R1 is selected from H, CH3, COOH or COOCH3; R2 is selected from H or OH; R3 is selected from H, OH, and OCOCH3; R4 is selected from H, OH or CH3; R5 is selected from H, CH3, OCOCH3, OH or CH2OH; R6 is selected from H, OH or CH3; and R7 is selected from H or OH. The IC50 (half maximal inhibitory concentration) value of compound 6 beta-hydroxyipolamiide is 138.8 muM, the IC50 value of compound shanzhiside methyl ester is 104.1 muM, and the IC50 value of compound 8-o-acetyl shanzhiside methyl ester is 125 muM.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, in particular the invention relates to the use of iridoid compounds. Background technique [0002] Severe acute respiratory syndrome (severe acute respiratory syndrome, SARS) is a severe acute respiratory infectious disease, also known as infectious atypical pneumonia. The pathogen of SARS is a virus belonging to the genus Coronaviridae (Peiris J. et al., Lancet, 2003, 361: 1319-1325). Coronaviruses belong to the family Coronaviridae, and coronaviruses are the currently known positive-strand RNA viruses with the largest genome (Siddell S.G. et al., Coronaviruses, toroviruses, and arteriviruses.in Topley & Wilson's Microbiology and Microbia Infections, 10th edition, Vol.Virology (eds.Mahy, B.W.J.&ter Meulen, V.) 823-856 (Hodder Arnold.London, 2005). The genus Coronavirus contains about 26 species, according to their natural host, gene sequence and serotype relationship It can be divi...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P31/14
Inventor 饶子和娄智勇郭宇陈卫强王波牛国君冯金磊李金楠
Owner TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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