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Spirocyclosporine x and its application in the preparation of medicaments for the treatment of influenza A

A type of influenza virus and drug technology, applied in the field of medicine, can solve the problems of increased drug resistance, drug side effects, and no scientific and comprehensive elaboration of antiviral mechanism

Active Publication Date: 2020-06-19
广州南方医大科技园有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, the anti-influenza drugs in global clinical application mainly include neuraminidase inhibitors and M2 ion channel inhibitors, but the development and application of these drugs have been plagued by the increase of drug resistance and drug side effects.
However, its antiviral mechanism has not been scientifically and comprehensively elucidated

Method used

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  • Spirocyclosporine x and its application in the preparation of medicaments for the treatment of influenza A
  • Spirocyclosporine x and its application in the preparation of medicaments for the treatment of influenza A
  • Spirocyclosporine x and its application in the preparation of medicaments for the treatment of influenza A

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 Separation, Preparation and Structure Identification of Compound SSX

[0037]The fungus Cochliobolus lunatus SCSIO41401 is a symbiotic fungus of seaweed, collected from the waters near Yongxing Island in the South China Sea (Journal of Natural Products, Cytotoxic and Antibacterial Eremophilane Sesquiterpenes from the Marine-Derived Fungus Cochliobolus lunatus SCSIO41401, WEI Fang et al., 2018, 81-41405). The strain can be provided by the School of Pharmacy, Southern Medical University. The strain is stored in MB medium, which consists of: agar 15g, malt extract powder 15g, coarse sea salt 24.4g, water 1000mL, pH 7.2-7.4.

[0038] Take a small amount of slant bacteria for seed fermentation culture (medium: 6.25g maltose, 6.25g malt extract powder, 1g yeast extract powder, 6.25g peptone, 1.25g potassium dihydrogen phosphate, 20g sea salt, 1000mL distilled water, pH 7.0), 500 100 ml in an Erlenmeyer flask, culture conditions: 25°C, 180 rpm. After 3 days of cultu...

Embodiment 2

[0046] The cytotoxicity detection of embodiment 2 compound SSX

[0047] The cytotoxicity of compound SSX was detected by MTT method. The specific method is as follows:

[0048] MDCK cells by 1 x 10 4 / well seeded in 96-well plate at 37°C, 5% CO 2 Cultured in a constant temperature cell culture incubator until monolayer, the compound SSX diluted serially was added to a 96-well plate, 200 μl per well, and cultured for 48 hours. The culture supernatant was discarded, and 100 μL of DMEM medium containing 0.5 mg / ml MTT was added to each well, and incubated at 37 °C for 4 h. The absorbance at 570 nm was detected by a multifunctional microplate reader (GeniosPro, Tecan, US). The survival rate of the cells was used as an indicator of the toxicity of the compound SSX to MDCK cells.

[0049] Cell viability (%)=E / N×100

[0050] E is the absorbance of the drug group, and N is the absorbance of the cell control group.

[0051] Test results: Compound SSX has less cytotoxicity, CC 50...

Embodiment 3

[0053] The inhibitory activity of embodiment 3 compound SSX to various subtype influenza viruses

[0054] In vitro antiviral experiments of the present invention involve multiple subtypes of influenza A viruses, including A / Aichi / 2 / 68 (H3N2), A / FM-1 / 1 / 47 (H1N1), A / Puerto Rico / 8 / 34(H1N1), H274Y and A 690(H3), the specific method is as follows:

[0055] MDCK cells by 2 x 10 4 / well seeded in 96-well plate at 37°C, 5% CO 2 cultured to a monolayer in a constant temperature cell incubator. Use 100TCID 50 Infect the cells with influenza A virus, 100 μl per well, incubate at 37°C for 1 hour, discard the virus solution, add 200 μl of compound SSX serially diluted in DMEM (containing 1 μg / ml TPCK), and continue to incubate for 48 hours. Combining the MTT method and the plaque experiment, reflecting the antiviral activity of the compound SSX is determined by the protective effect of the compound SSX on cells, including observing the cell virus phenomenon (CPE) caused by the compoun...

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Abstract

The invention discloses application of spirocyclosporin X to the preparation of a drug for treating influenza A. Influenza viruses are influenza A viruses and are preferably selected from H1N1, H3N2,H5N1 or H7N9. An action mechanism of the spirocyclosporin X in the anti-influenza A viruses is to inhibit the ribonucleoprotein complex vRNP activity by binding to PB2cap proteins; and the drug for preventing and treating the influenza is prepared. Sites at which the spirocyclosporin X binding to the influenza virus PB2cap proteins are arginine 355 (Arg355), asparagine 429 (Asn429), lysine 339 (Lys 339), methionine 431 (Met431) and phenylalanine 325 (Phe325).

Description

technical field [0001] The invention relates to the application of spirocycline X in anti-influenza A virus drugs, and belongs to the technical field of medicine. Background technique [0002] Influenza virus infection is an infectious disease that seriously endangers human health. Prevention and treatment of influenza, especially drug treatment, is imminent. So far, the anti-influenza drugs in global clinical application mainly include neuraminidase inhibitors and M2 ion channel inhibitors, but the development and application of these drugs have been plagued by the increase of drug resistance and drug side effects. . For this reason, people are eager to find and develop new anti-influenza drugs. It is particularly important to find low-toxic and effective anti-influenza drugs from natural products. [0003] Studies have shown that the ocean is an important resource for finding drug leads. From a large number of marine natural products, not only some anticancer and anti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D209/54A61K31/403C12P17/10A61P31/16C12R1/645
CPCA61P31/16C07D209/54C12P17/10
Inventor 杨洁唐斓周雪峰刘叔文陈飞敏
Owner 广州南方医大科技园有限公司
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