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Pentacyclic triterpene enterovirus EV71 inhibitors, and medicinal compositions and medicinal use thereof

A kind of pentacyclic triterpenoids, the technology of use, is applied in the field of pentacyclic triterpenoid enterovirus EV71 inhibitor, its pharmaceutical composition and medical use field

Inactive Publication Date: 2015-08-19
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Pleconaril is still in clinical trials as a broad-spectrum anti-picornavirus drug

Method used

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  • Pentacyclic triterpene enterovirus EV71 inhibitors, and medicinal compositions and medicinal use thereof
  • Pentacyclic triterpene enterovirus EV71 inhibitors, and medicinal compositions and medicinal use thereof
  • Pentacyclic triterpene enterovirus EV71 inhibitors, and medicinal compositions and medicinal use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Antiviral activity test of compounds against EV71 enterovirus

[0042] 1. Objective: To use human foreskin fibroblasts as virus host cells, and use XTT method to determine the antiviral activity of samples against EV71 enterovirus.

[0043] 2. Reagents, cells and viruses: sodium XTT(3,3′-[1-(phenylaminoyl)-3,4-tetrazolium]-bis(4-methoxy-6-nitro)benzenesulfonate ) kit was purchased from Roche Diagnostics Co., Ltd., Germany. Broad-spectrum antiviral drug ribavirin (Sigma, USA) was used as a positive control, and 0.1% DMSO was used as a negative control. Reagents and media for cell culture were purchased from Gibco BRL, USA. Human foreskin fibroblasts (CCFS-1 / KMC) were used to culture clinically isolated EV71 virus (BrCr type, GenBank accession number: U22521). Add 10% fetal bovine serum, 100 U / ml penicillin G sodium salt, 100 μg / ml streptomycin sulfate and 0.25 μg / ml amphotericin B to the minimum essential medium (MEM), in 5% CO 2 , Cells were expanded at 37°C. Add 2...

Embodiment 2

[0062] Preparation of pharmaceutical compositions: tablets

[0063] The pentacyclic triterpene compound of the present invention or a pharmaceutically acceptable salt or ester thereof (1 g), lactose (23 g) and microcrystalline cellulose (5.7 g) were mixed with a mixer. The resulting mixture is pressed into shape with a roller compactor, and it is worth flake-like pressed material. The flake pressed material was ground into powder with a hammer mill, and the obtained powder material was sieved through a 20-mesh sieve. A portion of light silica (0.3g) and magnesium stearate (0.3g) was added to the sieved mass and mixed. The resulting mixed product is compressed with a tablet machine to prepare tablets.

Embodiment 3

[0065] Preparation of pharmaceutical compositions: gelatin capsules

[0066] Pentacyclic triterpene compound of the present invention or its pharmaceutically acceptable salt or ester (1g) and microcrystalline cellulose (0.35g) and lactose (0.15g) are granulated with water, then this granule is combined with hinge carboxymethyl Sodium cellulose (0.04g) and magnesium stearate (0.01g) were mixed. The resulting mixed product is filled with gelatin capsules to prepare gelatin capsules. (the gelatin capsule used in the present invention is produced by China Suzhou Capsule Co., Ltd., and this gelatin capsule meets the medicinal standard)

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PUM

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Abstract

The invention relates to the pharmacy field, concretely relates to a use of a series of pentacyclic triterpene compounds as enterovirus EV71 inhibitors, and especially relates to an application in the preparation of medicines for preventing and treating EV71 infection induced hand-foot-and-mouth diseases and complications thereof, such as synanche, myocarditis, pulmonary edema, encephalitis, herpes, septicemia, hypertension, hyperglycemia, cognitive function disorder, poliomyelitis-like paralysis and many nerve system associated diseases. The invention also discloses medicinal compositions of the series of the pentacyclic triterpene compounds as enterovirus EV71 inhibitors.

Description

technical field [0001] The present invention relates to the pharmaceutical field, in particular to the use of a series of pentacyclic triterpene compounds as enterovirus EV71 inhibitors, especially in the preparation of hand, foot and mouth disease caused by EV71 infection and its complications such as angina, myocarditis, pulmonary edema, Encephalitis, herpes, sepsis, hypertension, hyperglycemia, cognitive dysfunction, poliomyelitis-like paralytic diseases and other diseases related to the nervous system are used in the prevention and treatment of drugs. The invention also discloses a series of pentacyclic triterpene compounds as pharmaceutical composition of anti-EV71 medicine. Background technique [0002] Hand, foot and mouth disease mostly occurs in children under 5 years of age. The clinical manifestations are fever, rashes or herpes on the hands, feet, mouth and other parts. Symptoms such as paralysis, the disease progresses rapidly in individual severe patients, lea...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61K31/704A61K31/58A61K31/7024A61K31/7056A61K31/585A61K31/7028A61P31/14A61P9/00A61P7/10A61P25/00A61P9/12A61P3/10A61P25/28A61P7/00
CPCY02A50/30
Inventor 温小安孙宏斌蔣連財程克光张丽颖郝佳张璞
Owner CHINA PHARM UNIV
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