Applications of rotundic acid in preparation of anti-influenza virus drugs

Abstract

The present invention discloses applications of rotundic acid in preparation of anti-influenza virus drugs, further applications of rotundic acid in preparation of drugs for treatment of pneumonia caused by influenza viruses, wherein the influenza virus is preferably influenza A H1N1 virus. According to the present invention, the in vitro cell experiment results prove that the IC50 value of the rotundic acid on H1N1 influenza virus is 5.8 [mu]g / mL, and is comparable to the IC50 value of the positive drug ribavirin; and the mouse influenza model pharmacological experiment results prove that the rotundic acid can significantly reduce the lung index of influenza-infected mice, and shows a certain dose-effect characteristic on H1N1.

Description

technical field

[0001] The invention discloses a new application of biscin, specifically the application of biscin in the preparation of anti-influenza virus drugs. Background technique

[0002] Influenza virus (abbreviated as influenza virus) can cause acute respiratory infection and pose a threat to human health. Among them, influenza A virus is easy to mutate due to its antigenicity, and the influenza A H1N1 influenza caused by it has the characteristics of wide epidemic range, strong infectivity, and high incidence rate. At present, the response to influenza virus is mainly through vaccines and drug treatment. Among them, M2 ion channel inhibitors amantadine and neuraminidase inhibitors are commonly used anti-influenza virus drugs clinically in many countries, but these two types of anti-viral drugs are now showing varying degrees of drug resistance, and some Certain toxic side effects. Therefore, it is very important and urgent to find new anti-influenza drugs with h...

Examples

Embodiment 1

[0012] The preparation of embodiment 1 rescue must be medicinal material extract

[0013] Get an appropriate amount of Bing medicinal materials, crush them, pass through a No. 1 sieve, add 8 times the amount of 70% (volume fraction) ethanol to the medicinal materials, heat and reflux for extraction twice, each time for 1 hour, filter, combine the extracts, put them in a rotary evaporator, Concentrate under reduced pressure at 80°C to a thick paste. Transfer the concentrated liquid to a decompression drying oven, continue drying and crushing at 80°C, and obtain the extract of the rescued Bing medicinal material.

Embodiment 2

[0014] Example 2 In vitro Influenza Virus Inhibition Experiment

[0015] 1. Experimental materials

[0016] 1.1 The drug under test: basic acid (extracted from basic acid, purity > 98%).

[0017] 1.2 Control drug: ribavirin, oleanolic acid, extract of the medicinal material of Qubing (see Example 1)

[0018] 1.3 Virus strain: Influenza A H1N1 influenza virus murine lung adaptation strain (FM / 1 / 47 strain). Passage chicken embryos, test in BSL-3 (Biosafety Laboratory Level 3), subpackage, and store at -80°C.

[0019] 1.4 Cell model: dog kidney cell MDCK cell

[0020] The above drugs were fully dissolved in dimethyl sulfoxide (DMSO) and stored at -20°C for later use.

[0021] 2. Experimental method

[0022] 2.1 Determination of virus virulence

[0023] MDCK cells were divided into 5 × 10 4 Inoculate a 96-well culture plate at a concentration of / mL, 100 μl per well, 37°C, 5% CO 2 Culture to form a confluent monolayer of cells. 100 μl of 10-fold serial dilution of the vir...

Embodiment 3

[0032] Example 3 In vivo Influenza Suppression Experiment

[0033] 1. Experimental materials

[0034] 1.1 The drug under test: basic acid (extracted from basic acid, purity > 98%).

[0035] 1.2 Control drug: Tamiflu, oleanolic acid, extract of the medicinal material of Qubing (see Example 1)

[0036] 1.3 Virus: Mouse lung-adapted strain of influenza A H1N1 virus (FM / 1 / 47 strain). Passage chicken embryos, test in BSL-3 (Biosafety Laboratory Level 3), subpackage, and store at -80°C.

[0037] 2. Experimental animals

[0038] 80 BALB / c mice weighing 18g-22g were purchased from Guangdong Experimental Animal Center.

[0039] 3. Experimental method

[0040] The BALB / c mice were randomly divided into 8 groups, namely, the blank control group, the model control group, the Tamiflu control group, the oleanolic acid group, the medicinal material extract group of BALB, and the high, medium and low levels of BALB. 3 dosage groups, 10 rats in each group. Except for the blank control g...

technical field

[0001] The invention discloses a new application of biscin, specifically the application of biscin in the preparation of anti-influenza virus drugs. Background technique

[0002] Influenza virus (abbreviated as influenza virus) can cause acute respiratory infection and pose a threat to human health. Among them, influenza A virus is easy to mutate due to its antigenicity, and the influenza A H1N1 influenza caused by it has the characteristics of wide epidemic range, strong infectivity, and high incidence rate. At present, the response to influenza virus is mainly through vaccines and drug treatment. Among them, M2 ion channel inhibitors amantadine and neuraminidase inhibitors are commonly used anti-influenza virus drugs clinically in many countries, but these two types of anti-viral drugs are now showing varying degrees of drug resistance, and some Certain toxic side effects. Therefore, it is very important and urgent to find new anti-influenza drugs with h...

Examples

Embodiment 1

[0012] The preparation of embodiment 1 rescue must be medicinal material extract

[0013] Get an appropriate amount of Bing medicinal materials, crush them, pass through a No. 1 sieve, add 8 times the amount of 70% (volume fraction) ethanol to the medicinal materials, heat and reflux for extraction twice, each time for 1 hour, filter, combine the extracts, put them in a rotary evaporator, Concentrate under reduced pressure at 80°C to a thick paste. Transfer the concentrated liquid to a decompression drying oven, continue drying and crushing at 80°C, and obtain the extract of the rescued Bing medicinal material.

Embodiment 2

[0014] Example 2 In vitro Influenza Virus Inhibition Experiment

[0015] 1. Experimental materials

[0016] 1.1 The drug under test: basic acid (extracted from basic acid, purity > 98%).

[0017] 1.2 Control drug: ribavirin, oleanolic acid, extract of the medicinal material of Qubing (see Example 1)

[0018] 1.3 Virus strain: Influenza A H1N1 influenza virus murine lung adaptation strain (FM / 1 / 47 strain). Passage chicken embryos, test in BSL-3 (Biosafety Laboratory Level 3), subpackage, and store at -80°C.

[0019] 1.4 Cell model: dog kidney cell MDCK cell

[0020] The above drugs were fully dissolved in dimethyl sulfoxide (DMSO) and stored at -20°C for later use.

[0021] 2. Experimental method

[0022] 2.1 Determination of virus virulence

[0023] MDCK cells were divided into 5 × 10 4 Inoculate a 96-well culture plate at a concentration of / mL, 100 μl per well, 37°C, 5% CO 2 Culture to form a confluent monolayer of cells. 100 μl of 10-fold serial dilution of the vir...

Embodiment 3

[0032] Example 3 In vivo Influenza Suppression Experiment

[0033] 1. Experimental materials

[0034] 1.1 The drug under test: basic acid (extracted from basic acid, purity > 98%).

[0035] 1.2 Control drug: Tamiflu, oleanolic acid, extract of the medicinal material of Qubing (see Example 1)

[0036] 1.3 Virus: Mouse lung-adapted strain of influenza A H1N1 virus (FM / 1 / 47 strain). Passage chicken embryos, test in BSL-3 (Biosafety Laboratory Level 3), subpackage, and store at -80°C.

[0037] 2. Experimental animals

[0038] 80 BALB / c mice weighing 18g-22g were purchased from Guangdong Experimental Animal Center.

[0039] 3. Experimental method

[0040] The BALB / c mice were randomly divided into 8 groups, namely, the blank control group, the model control group, the Tamiflu control group, the oleanolic acid group, the medicinal material extract group of BALB, and the high, medium and low levels of BALB. 3 dosage groups, 10 rats in each group. Except for the blank control g...

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