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Iridoid compound and application of metabolite of iridoids compound in preparing drug-resistance bacterium infection resisting drug

A technology of iridoids and metabolites, which is applied to the active ingredients of hydroxyl compounds, antibacterial drugs, drug combinations, etc., and can solve the problems of antibiotics being difficult to work and adverse reactions

Inactive Publication Date: 2016-06-22
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The emergence of bacterial drug resistance and the infection of drug-resistant bacteria often make empiric treatment difficult to be effective, and bring great challenges to clinical anti-infective treatment
The emergence of methicillin-resistant Staphylococcus aureus (MRSA) is an increasingly serious problem after the widespread use of antibiotics in clinic: common antibiotics are difficult to work, although vancomycin is the most effective antibiotic for MRSA infection, but clinically Widespread use can lead to serious adverse reactions, and bacteria resistant to vancomycin have been reported

Method used

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  • Iridoid compound and application of metabolite of iridoids compound in preparing drug-resistance bacterium infection resisting drug
  • Iridoid compound and application of metabolite of iridoids compound in preparing drug-resistance bacterium infection resisting drug
  • Iridoid compound and application of metabolite of iridoids compound in preparing drug-resistance bacterium infection resisting drug

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0026] Experimental Example 1: Separation and structure identification of in vivo metabolites of syringpicroside A

[0027] Syringin A was ultrasonically dissolved in drinking water, administered orally to 20 male SD rats at a dose of 100 mg / kg, and the urine was collected for a total of 20 days. A total of 2.4 L of urine was collected and stored in a freezer. The collected urine was extracted four times with ethyl acetate and n-butanol respectively. The ethyl acetate layer extract and the n-butanol layer extract were concentrated respectively, and the endogenous substances were tracked in parallel with blank urine through various column chromatography methods, and the in vivo metabolites of syringpicroside A in urine were analyzed. Separation and purification, a total of 9 metabolites were isolated, the metabolic pathway is as follows.

[0028]

Embodiment 2

[0029] Embodiment 2: The determination of the minimum inhibitory concentration (MIC) of iridoids and metabolites to 4 kinds of bacteria

[0030] Tested strains: Staphylococcus aureus (MSSA)

[0031] Methicillin-resistant Staphylococcus aureus (MRSA)

[0032] Penicillin-resistant Streptococcus pneumoniae (PRSP)

[0033] Vancomycin-resistant enterococci (VRE) were clinically isolated from the Laboratory Department of the 463rd Hospital of the People's Liberation Army.

[0034] Drugs and reagents: vancomycin hydrochloride for injection (VH, Eli Lilly Japan K.K); normal saline (Shandong Yuwang Industrial Co., Ltd.). Beef extract; peptone; NaCl; NaOH (Tianjin Bodi Chemical Co., Ltd.); water (sterile water).

[0035] Medium: Mueller-Hinton (MH) Broth Medium (g / L):

[0036]

[0037] Accurately weigh various components, stir and mix well, then add NaOH to adjust the pH to 7.2-7.4. Sterilize under high pressure steam at 0.1MPa for 30min.

[0038] Test compounds: Syringopicrosi...

experiment example 3

[0046] Experimental example 3: Determination of in vivo anti-Staphylococcus aureus infection activity of syringpicroside A (compound 1)

[0047]Select 72 Kunming mice, randomly divide them into 9 groups, 8 in each group, and mark them as blank group (K), positive group (VH), syringpicroside A high-dose group (Sy-H), syringpicroside A Medium dose group (Sy-M), syringpicroside A low dose group (Sy-L) and clove leaf group (DXY). After intragastric administration, methicillin-resistant Staphylococcus aureus (10 9 CFU / ml) 2 times, 0.1ml / 10g for the first time, 0.15ml / 10g for the second time. The administration was continued, and the number of deaths in each group was observed after 7 days.

[0048] Grouping and dosing are as follows:

[0049] Blank group: normal saline

[0050] VH group (positive group): vancomycin hydrochloride (300mg / kg, clinical dose)

[0051] DXY group (clove leaf group): clove leaf (82.2mg / kg, calculated as tablet core)

[0052] Sy-L group (low dose grou...

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Abstract

The invention relates to an iridoid compound with the general formula I-III and application of the in-vivo metabolite of the iridoid compound in preparing a drug-resistance bacterium infection resisting drug. It is found through in-vivo and in-vitro MRBS resisting experiments that the iridoid compound and the metabolite of the iridoid compound have remarkable drug-resistance bacterium resisting activity and can be used for being developed into the drug-resistance bacterium resisting drug.

Description

technical field [0001] The invention relates to a class of iridoid compounds and uses thereof, in particular to the use of the iridoid compounds in inhibiting methicillin-resistant Staphylococcus aureus. The present invention also relates to the main in vivo metabolites of the iridoid compounds used as drugs for anti-drug-resistant bacterial infections, pharmaceutical compositions containing them, their in vivo and in vitro anti-drug-resistant bacterial activities, and methods of use. Background technique [0002] The emergence of bacterial resistance and the infection of drug-resistant bacteria often make empiric treatment difficult to be effective, which brings great challenges to clinical anti-infective treatment. The emergence of methicillin-resistant Staphylococcus aureus (MRSA) is an increasingly serious problem after the widespread use of antibiotics in clinic: common antibiotics are difficult to work, although vancomycin is the most effective antibiotic for MRSA infe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K31/352A61K31/05A61K31/192A61K31/12A61P31/04A61P11/00A61P1/12A61P1/00A61P13/12A61P13/10A61P31/02A61P11/04
CPCA61K31/05A61K31/12A61K31/192A61K31/352A61K31/7048Y02A50/30
Inventor 殷军周正圆韩娜刘志惠
Owner SHENYANG PHARMA UNIVERSITY
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