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Application of lithocholic acid compound in preparation of antibacterial product

An antibacterial product, technology of lithocholic acid, applied in the direction of cosmetic preparations, cosmetics, antibacterial drugs, etc., can solve the problems such as the report of the application of antibacterial products of lithocholic acid and its derivatives.

Active Publication Date: 2021-10-29
南充市中心医院 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But there is no report on the application of lithocholic acid and its derivatives in the preparation of antibacterial products

Method used

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  • Application of lithocholic acid compound in preparation of antibacterial product
  • Application of lithocholic acid compound in preparation of antibacterial product
  • Application of lithocholic acid compound in preparation of antibacterial product

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] In this case, a series of lithocholic acid compounds (abbreviated as LA series compounds) were tested for MIC by using the agar double dilution method to investigate the effect of lithocholic acid compounds on methicillin-resistant Staphylococcus aureus (MRSA), methicillin Sensitive Staphylococcus aureus (MSSA), Escherichia coli Esbls+, Escherichia coli Esbls-, the in vitro antibacterial activity (MIC value) of Pseudomonas aeruginosa, and compare with positive control levofloxacin; Wherein, MIC 50 and MIC 90 Respectively refer to the MIC (MIC: Minimum Inhibitory Concentration) required to inhibit 50% or 90% of the tested bacteria.

[0028] 1.1 Test product

[0029] Table 1 Information about the test product

[0030]

[0031] The structural formula of above-mentioned LA series compound is as follows:

[0032]

[0033] The information of the test items is shown in Table 1. The above test items were all prepared with DMSO to a maximum concentration of 3.84 mg / ml b...

Embodiment 2

[0087] On the basis of Example 1, this example further carried out the MIC test of compound LA-1 and compound LA-9 to methicillin-resistant Staphylococcus aureus (MRSA), methicillin-sensitive Staphylococcus aureus (MSSA) ( Expand the number of strains to 20).

[0088] 1 Test product and reference product

[0089] 1.1 Test product

[0090] Table 5 information on the test product

[0091]

[0092] The information of the test products is shown in Table 5. The above test products were all prepared with DMSO to a maximum concentration of 3.84mg / ml before use, and then double-diluted sequentially.

[0093] 1.2 Reference substance

[0094] Name: Levofloxacin Lactate Sodium Chloride Injection, commercially available.

[0095] Batch number: 118190906 Manufacturer: Zhejiang Pharmaceutical Co., Ltd.

[0096] Properties: Pale yellow liquid Specification: 500mg / 250ml

[0097] Storage Conditions: Sealed in a cool, dry place shading.

[0098] 2 Test instruments and reagents

[009...

Embodiment 3

[0142] In this example, on the basis of Example 1 and Example 2, the inhibitory effect of compound LA-1 and compound LA-9 on methicillin-resistant Staphylococcus aureus (MRSA) biofilm formation was further investigated.

[0143] 1 Test product and reference product

[0144] 1.1 Test product

[0145] Table 9 information on the test product

[0146]

[0147] The information of the test products is shown in Table 9. Before use, the above test products were prepared with sterilized deionized water to a maximum concentration of 128ug / ml, and then double-diluted sequentially.

[0148] 1.2 Reference substance

[0149] Name: Norvancomycin

[0150] Batch number: 130338-201704 Manufacturer: China National Institutes for Food and Drug Control

[0151] Appearance: white powder Specification: 150mg / bottle

[0152] Storage Conditions: Sealed in a cool, dry place shading.

[0153] 2 Test instruments and reagents

[0154] DensiCHEK TM Plus electronic turbidimeter (Merieux Diagnosti...

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Abstract

The invention discloses application of a lithocholic acid compound in preparation of an antibacterial product, belongs to the technical field of biological pharmacy, and discovers the application of a series of lithocholic acid compounds in the preparation of the antibacterial product for the first time. Experiments show that a compound LA-1, a compound LA-5 and a compound LA-9 have a good bacteriostatic activity, the bacteriostatic effects of the three compounds on MRSA and MSSA are superior to those of other tested bacteria, and the bacteriostatic activity of the compound LA-9 on MRSA and MSSA is better than that of the compound LA-1 and the compound LA-5. Meanwhile, further experiments show that the two compounds LA-1 and LA-9 perform the bacteriostatic activity on MRSA and MSSA through the effect of resisting the growth of a staphylococcus aureus biofilm.

Description

technical field [0001] The invention relates to the technical field of biopharmaceuticals, in particular to the application of lithocholic acid compounds in the preparation of antibacterial products. Background technique [0002] The World Health Organization issued a report stating that the current development of new antibiotics is seriously insufficient to combat the growing threat of antimicrobial resistance. The report also identified 12 priority pathogens, including drug-resistant bacteria such as Staphylococcus aureus. In recent years, due to the abuse of traditional antibiotics and the accelerated evolution of multidrug-resistant bacteria, many bacteria have developed drug resistance. In addition, due to commercial interests and other reasons, compared with the speed of research and development of antibacterial drugs, bacterial resistance is developing at an alarming rate. At the same time, drug-resistant bacteria such as Staphylococcus aureus are widely distributed...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/63A61Q17/00A61K31/575A61K31/58A61P31/04
CPCA61K8/63A61Q17/005A61K31/575A61K31/58A61P31/04Y02A50/30
Inventor 张仕瑾周明月王娅俐兰杨苏强孙文武吴滨
Owner 南充市中心医院
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