New application of hydroquinone compound

Abstract

The invention relates to new application of a hydroquinone compound, particularly application of a hydroquinone compound (shikonin) in preparing medicines for resisting hepatitis C virus (HCV). The hydroquinone compound (shikonin) has obvious activity for resisting HCV, and the selection index is up to 43.56; and thus, the hydroquinone compound (shikonin) can be used as a lead compound for treating hepatitis C. The molecular formula of the hydroquinone compound (shikonin) is C16H16O5, and the chemical structural formula is disclosed in the specification.

Description

technical field

[0001] The invention relates to an application of a compound, in particular to a new application of a hydroquinone compound shikonin, and belongs to the technical field of medicines. Background technique

[0002] Hepatitis C virus (HCV), the leading cause of liver cancer and cirrhosis, infects more than 3% of the world's population and is considered one of the leading causes of chronic liver disease. The current standard treatment, including PEG-IFN / RBV combination, is only effective for more than half of the patients infected with hepatitis C virus (HCV), and has significant side effects. The treatment effect is not ideal. Therefore, it is of great practical significance to search for new anti-HCV drugs or lead compounds from traditional Chinese medicine, plants and fungi resources. However, the screening platform for anti-HCV compounds is not yet perfect compared with other viral screening platforms. There are few reports about anti-HCV natural products....

Examples

Embodiment 1

[0020] A. Dried 20 kg Xinjiang comfrey ( A. euchroma ) After the stem bark is crushed, according to the mass / volume ratio (kg / L) of comfrey powder: ethanol aqueous solution = 1:2, fully mix 40 L of ethanol aqueous solution with a volume concentration of 95% and 20 kg of Xinjiang comfrey powder, Soak at room temperature for 24 hours to obtain an extract, repeat the extraction for 3 times, and combine the extracts;

[0021] B. Concentrate the extract in step A under reduced pressure as usual, recover ethanol until there is no ethanol smell, and then use petroleum ether to repeatedly extract the extract at room temperature according to the volume ratio of extract:petroleum ether=1:1 Second, after recovering the petroleum ether, the extract was obtained;

[0022] C. According to the volume ratio of extract: ethyl acetate=1:1, the extract of step B was repeatedly extracted 3 times with ethyl acetate at room temperature, and concentrated under reduced pressure to recover ethyl ace...

Embodiment 2

[0027] In this example, Huh 7.5.1 cells were infected with type 2a chimeric virus J6 / JFH1 to produce infectious virus particles, an HCV cell culture system (HCV cell culture, HCVcc), with interferon and ribavirin as positive controls , MTT cytotoxicity test and in vitro anti-HCV efficacy evaluation of anti-HCV drugs.

[0028] The compound shikonin was dissolved in DMSO, 0.22 mu M membrane filter sterilization, the concentration of the original drug solution was 10 mg / mL.

[0029] Human liver cancer cell line Huh 7.5.1 was treated with DMEM (Dulbecco’s modified Eagle’s medium, DMEM) containing 15% newborn bovine serum at 37°C and 5% CO 2 cultured in an incubator. Virus J6 / JFH1 was cultured from Huh 1 cells and stored at -80°C.

[0030] 1) MTT method to detect the cytotoxicity of samples

[0031] Huh 7.5.1 cells in the logarithmic growth phase were taken, and 9×10 3 cells / well cells were spread in 96-well plate, after 5 hours of attachment, add 2 mu L DMSO gradient dilu...

technical field

[0001] The invention relates to an application of a compound, in particular to a new application of a hydroquinone compound shikonin, and belongs to the technical field of medicines. Background technique

[0002] Hepatitis C virus (HCV), the leading cause of liver cancer and cirrhosis, infects more than 3% of the world's population and is considered one of the leading causes of chronic liver disease. The current standard treatment, including PEG-IFN / RBV combination, is only effective for more than half of the patients infected with hepatitis C virus (HCV), and has significant side effects. The treatment effect is not ideal. Therefore, it is of great practical significance to search for new anti-HCV drugs or lead compounds from traditional Chinese medicine, plants and fungi resources. However, the screening platform for anti-HCV compounds is not yet perfect compared with other viral screening platforms. There are few reports about anti-HCV natural products....

Examples

Embodiment 1

[0020] A. Dried 20 kg Xinjiang comfrey ( A. euchroma ) After the stem bark is crushed, according to the mass / volume ratio (kg / L) of comfrey powder: ethanol aqueous solution = 1:2, fully mix 40 L of ethanol aqueous solution with a volume concentration of 95% and 20 kg of Xinjiang comfrey powder, Soak at room temperature for 24 hours to obtain an extract, repeat the extraction for 3 times, and combine the extracts;

[0021] B. Concentrate the extract in step A under reduced pressure as usual, recover ethanol until there is no ethanol smell, and then use petroleum ether to repeatedly extract the extract at room temperature according to the volume ratio of extract:petroleum ether=1:1 Second, after recovering the petroleum ether, the extract was obtained;

[0022] C. According to the volume ratio of extract: ethyl acetate=1:1, the extract of step B was repeatedly extracted 3 times with ethyl acetate at room temperature, and concentrated under reduced pressure to recover ethyl ace...

Embodiment 2

[0027] In this example, Huh 7.5.1 cells were infected with type 2a chimeric virus J6 / JFH1 to produce infectious virus particles, an HCV cell culture system (HCV cell culture, HCVcc), with interferon and ribavirin as positive controls , MTT cytotoxicity test and in vitro anti-HCV efficacy evaluation of anti-HCV drugs.

[0028] The compound shikonin was dissolved in DMSO, 0.22 mu M membrane filter sterilization, the concentration of the original drug solution was 10 mg / mL.

[0029] Human liver cancer cell line Huh 7.5.1 was treated with DMEM (Dulbecco’s modified Eagle’s medium, DMEM) containing 15% newborn bovine serum at 37°C and 5% CO 2 cultured in an incubator. Virus J6 / JFH1 was cultured from Huh 1 cells and stored at -80°C.

[0030] 1) MTT method to detect the cytotoxicity of samples

[0031] Huh 7.5.1 cells in the logarithmic growth phase were taken, and 9×10 3 cells / well cells were spread in 96-well plate, after 5 hours of attachment, add 2 mu L DMSO gradient dilu...

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