Application of A-ring trihydroxyl substituted pentacyclic triterpene compound to pharmacy

A technology of pentacyclic triterpenes and trihydroxyl groups is applied in the application field of preparing antibacterial or anti-tobacco mosaic virus medicines, and can solve the problems that the research on anti-phytopathogenic bacteria and anti-tobacco mosaic virus has not been reported before.

Active Publication Date: 2014-07-16
THE KEY LAB OF CHEM FOR NATURAL PROD OF GUIZHOU PROVINCE & CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the research on the anti-phytopathogenic bacteria and anti-tobacco mosaic virus of this type of compound has never been reported.

Method used

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  • Application of A-ring trihydroxyl substituted pentacyclic triterpene compound to pharmacy
  • Application of A-ring trihydroxyl substituted pentacyclic triterpene compound to pharmacy
  • Application of A-ring trihydroxyl substituted pentacyclic triterpene compound to pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0161] Embodiment 1 of the present invention: take any one of compound I17, U2, U4, A2, A3, add appropriate amount of starch and microcrystalline cellulose according to the pharmaceutical method and mix well, mix the hydroxymethyl cellulose solution with the above-mentioned Mix the powder, pass through 80-mesh sieve to obtain wet granules, dry at 50-60°C, pre-screen carboxymethyl starch salt, magnesium stearate and talcum powder, then add to the above granules and press into tablets to obtain tablets . The preparation is taken orally, twice a day, and the dose of each dose is 5-30 mg based on the crude drug. For the treatment of infectious diseases caused by Staphylococcus aureus such as suppurative infection, pneumonia, pseudomembranous enteritis, pericarditis, etc.

Embodiment 2

[0162] Example 2: Take any one of the compounds I3, I15, I18, I23, U1, U3, U5, and A4, add an appropriate amount of sodium citrate, polyethylene glycol, and distilled water according to the pharmaceutical method, mix well and fully dissolve, adjust The pH of the solution is 7.5-8.5, filtered, the concentration of the crude drug is 1 mg / ml, divided into 2 ml per ampoule, and sterilized to obtain the injection. The preparation is used for injection, twice a day, and the amount of each injection is 5-30 mg based on the raw drug. For the treatment of infectious diseases caused by Staphylococcus aureus.

Embodiment 3

[0163] Embodiment 3: Take any one of the compounds Ia, Ic, Ij, Io, Ip, I13, A1, A5, A7, pulverize through an 80 mesh sieve, add an appropriate amount of vegetable oil containing 10% beeswax according to the pharmaceutical method, and mix well ; Prepare capsule material with gelatin: glycerin: distilled water: preservative = 1: 0.4: 0.8: 0.003, add the mixture of the aforementioned compounds and vegetable oil, and compress to obtain soft capsules. The preparation is taken orally, twice a day, and the dose of each dose is 5-30 mg based on the crude drug. For the treatment of infectious diseases caused by Staphylococcus aureus.

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Abstract

The invention discloses an application of an A-ring trihydroxyl substituted pentacyclic triterpene compound to preparation of an antibacterial or anti-tobacco mosaic virus drug. The general formula of the compound is as shown in the specification, wherein hydroxyls of C1, C2 and C3 are respectively in alpha configuration or beta configuration; R1 and R2 are selected from hydrogen or methyl and are different from each other; R3 is selected from -COOH, -CH2OH, -CHO, -COOR1, -CONH2, -CONHR1 and -CONR1R2; R1 and R2 are selected from alkyl containing 1-15 carbon atoms, substituted or unsubstituted phenyl and substituted or unsubstituted phenyl alkyl; and the substituent group is selected from halogen, hydroxyl, cyan, amino, nitryl, sulfydryl or phenyl, acyl, aryl, alkoxy and alkyl containing 1-15 carbon atoms. The compounds have antibacterial or anti-tobacco mosaic virus activity, have extremely high bacteriostatic activity especially to gram positive bacteria, phytophthora nicotiana and tobacco mosaic virus, and have a good application prospect in fields of medicines and pesticides.

Description

technical field [0001] The invention relates to the application of A-ring trihydroxyl-substituted pentacyclic triterpene compounds in pharmacy, especially the application in the preparation of antibacterial or anti-tobacco mosaic virus medicines, which belongs to the technical field of pharmaceutical use of compounds. Background technique [0002] Pentacyclic triterpenoids are widely distributed in nature, and they have various biological activities, including antitumor, antibacterial, antiviral, antihypertensive, hypoglycemic, etc. (Dzubak Petr, Hajduch Marian, Vydra David.et al.Pharmacological activities of natural triterpenoids and their therapeutic implications. Nat. Prod. Rep., 2006, 23, 394–411.). In recent years, due to the wide antibacterial spectrum of pentacyclic triterpenes, they have strong inhibitory effects on some bacteria or fungi (Wolska KI., Grudniak AM, Fiecek B, Kraczkiewicz-Dowjat A, Kurek A. Antibacterial activity of oleanolic and ursolic acids and the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P31/04A61P31/10A01N45/00A01P1/00A01P3/00
CPCA01N31/04A01N35/02A01N37/36
Inventor 杨小生黄丽荣骆衡史亚男郝小江
Owner THE KEY LAB OF CHEM FOR NATURAL PROD OF GUIZHOU PROVINCE & CHINESE ACADEMY OF SCI
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