Ursolic acid saponin, preparation method thereof and application in resisting highly pathogenic H5N1 influenza virus
A technology of ursolic acid saponin and ursolic acid ester, which is applied in the preparation of antiviral agents, steroids, sugar derivatives, etc., can solve the problems of high variability of influenza virus and no vaccine for influenza virus once and for all.
Inactive Publication Date: 2011-01-12
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI +1
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At the same time, due to the high variability of influenza virus, there is no vaccine against influenza virus once and for all.
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Abstract
The invention discloses ursolic acid saponin, a preparation method thereof and application in resisting highly pathogenic H5N1 influenza virus, and specifically relates to ursolic acid saponin compounds shown in general formula (I). A series of ursolic acid saponin is prepared from natural product ursolic acid serving as raw material by introducing an ester group into the C-28 site through structural modification at first, then introducing beta-glucosyl into the C-3 site, selectively protecting 3,6-OHs of the glucose by using BBTZ and introducing glycosyl into 2,4-OHs of the glucose. Pharmacological test shows that the ursolic acid saponin compounds have obvious inhibition effect on the invasion process of the H5N1 highly pathogenic influenza viruses on host cells and can be used as a medicament for preventing or treating the influenza viruses. The invention also discloses a pharmaceutical composition containing the ursolic acid saponin compounds and the combination of the compounds of the invention and other anti-virus medicines.
Description
technical field The present invention relates to a new class of ursolic acid saponins, a method for preparing such ursolic acid saponins, a pharmaceutical composition containing such ursolic acid saponins, and the use of such ursolic acid saponins in the preparation of anti-influenza virus drugs, especially The invention relates to an application in medicines against highly pathogenic H5N1 influenza viruses; it belongs to the technical field of chemical medicines. Background technique Influenza A virus belongs to the Orthomyxoviridae family, and its genome consists of 8 single-stranded segmented negative-strand RNAs, encoding at least 10 proteins: hemagglutinin (HA), neuraminidase (NA) , polymerase (Polymerase basic protein 1, PB1; Polymerase basic protein 1, PB2; Polymerase acidic protein, PA), nucleoprotein (Nucleoprotein, NP), matrix protein (Matrix protein 1, M1; Matrixprotein 2, M2), non-structural Protein (Non-structural protein 1, NS1; Non-structural protein 2, NS2)....
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IPC IPC(8): C07H15/256C07J63/00C07H1/00C07J75/00A61K31/704A61P31/16
CPCY02P20/55
Inventor 郭颖李英霞曹颖莉
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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