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Coumarin ether compounds and new use of composition

A technology of coumarin and compounds, applied in the field of pharmacy, can solve the problems of mitochondrial toxicity, easy drug resistance, and too expensive interferon

Active Publication Date: 2009-07-29
XIANGBEI WELMAN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the price of interferon is too expensive, which brings a heavy economic burden to most patients
Nucleoside drugs are prone to drug resistance, and the drug resistance rate of virus mutations in the third year after oral administration of Heptin is as high as 49%, and most patients rebound after stopping the drug
Therefore, it is difficult to determine the course of treatment of nucleoside antiviral drugs, and only about 15% of patients can completely stop the drug at the end
Among many nucleoside antiviral drugs, adefovir has a lower incidence of mutant strains and drug resistance, but the drug has nephrotoxicity, and animal experiments have shown that it is toxic to the mitochondria of renal epithelial cells (Yao Guangbi. Outlook for Chronic Viral Virus Treatment of Hepatitis. Liver, 2002, 7(1): 62)

Method used

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  • Coumarin ether compounds and new use of composition
  • Coumarin ether compounds and new use of composition
  • Coumarin ether compounds and new use of composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] The compound wedelolide extracted from Eclipta alba

[0074] (1) soaking and filtering

[0075] Eclipta whole grass 300kg, fully immersed in 0.75 tons of ethanol (concentration 95%)→soak overnight (10 hours)→coarse filtration, thereby removing the whole grass residue (retention)→net filtration (suction filtration) or high-speed centrifugation (10000rpm, 10 minutes), thereby removing dust and fine residue → green clarified filtrate.

[0076] (2) Ethanol recovery

[0077] Recover ethanol by distillation, the temperature does not exceed 60°C → distill for 2 hours each time, remove the extract in the reaction kettle to the collection bucket (the extract is dark dark green, slightly viscous) → repeat the above steps until all ethanol is recovered .

[0078] (3) Second soaking and back distillation

[0079] Recover 0.75 tons of ethanol, re-soak the whole herb residue → soak overnight, the requirements for coarse filtration, net filtration and distillation recovery are the...

Embodiment 2

[0092] Inhibitory effect of wedelolide on virus in vitro

[0093] Cells and viruses: herpes simplex virus type 1 (HSV-I), respiratory syncytial virus (RSV), poliovirus type 1 (Poliovirus-1), coxsackievirus type A-7 (CVA-7), ECHO-11 and Vero cells were purchased from the National Institute for the Control of Pharmaceutical and Biological Products, Ministry of Health.

[0094] Experimental drug: APL-1 (prepared in Example 1).

[0095] Experimental method: Vero cells were inoculated in 96-well cell culture plates, the number of cells was 25,000 / well, conventionally cultured with PRMI1640 medium for 24 hours, and 100TCID were added 50 For HSV-I, RSV, Poliovirus-1, CVA-7, ECHO-11, set 6 replicate wells for each virus, discard the virus solution after 2 hours and wash with Hanks solution for 3 times, then add the concentration of 1 μg / ml, 5 μg / ml, 10 μg / ml of APL-1, incubated at 37°C for 96 hours, and observed the degree of cytopathic changes in the cells of each group.

[0096]...

Embodiment 3

[0107] Antiviral effect of wedelolide in mice

[0108] Experimental animals: 70 male SPF grade BALB / C mice, purchased from Shanghai Slack Experimental Animal Co., Ltd., weighing 18-20 g. Raised in SPF grade animal room, 12h light / 12h dark, free intake of feed and water.

[0109] Virus strain: herpes simplex virus type I (HSV-1) Sm44 strain, purchased from National Institute for the Control of Pharmaceutical and Biological Products, Ministry of Health.

[0110] Experimental drugs: APL-1 (prepared in Example 1), ribavirin (ribavirin, purchased from Jiaozuo Kangli Pharmaceutical Co., Ltd., 0.1 g / ml).

[0111] Experimental method: Using different dilutions of the virus liquid, the experimental mice were inoculated intracranially with HSV-1 (TCID 50 =10 -7 ·ml -1 ), observed for 14 days. According to the number of mouse deaths, calculate the LD of the virus 50 , to determine the amount of virus inoculum. According to the probability unit method of half number effect, measure...

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PUM

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Abstract

The invention belongs to the pharmacology field and discloses a tonka-bean grass ether compound or pharmaceutically acceptable salt or ester, or the function of extractives of the compound in preparing antiviral drugs. Compositions containing the tonka-bean grass ether compound or the pharmaceutically acceptable salt or ester or the extractives of the compound are also disclosed.

Description

technical field [0001] The invention belongs to the field of pharmacy, and more specifically, the invention relates to a new application of a coumarin compound or a composition containing the compound. Background technique [0002] Currently, antiviral drugs on the market are mainly divided into interferon and nucleoside drugs. As an antiviral drug, interferon has been widely used clinically. But its toxic and side effects are ubiquitous. The most common is fever and flu-like syndrome. The patient loses weight, hair loss, emotional agitation, bone marrow suppression causes blood cells, thrombocytopenia, and mild anemia. Occasionally, nervous system damage can occur, affecting the function of the endocrine system. Some patients also produce interferon Antibody (Lu Libiao, Bao Xiangying, He Fuqiang. Side effects of interferon in clinical application. Guangxi Medicine, 2003, 25(4): 572-574). In addition, the price of interferon is too expensive, which brings a heavy economic...

Claims

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Application Information

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IPC IPC(8): C07D493/04A61K31/37A61P31/12
CPCY02A50/30
Inventor 俞强
Owner XIANGBEI WELMAN PHARMA CO LTD
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