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New application of geraniol and derivative thereof in preparing drugs for MRSA infectious diseases

A technology of geraniol and its derivatives, applied in the field of new applications of geraniol and its derivatives in the preparation of MRSA infectious disease drugs, can solve the problem of linezolid, daptomycin, ceftaroline, Rivancin, dalbavancin, tedizolid phosphate and other problems, to achieve the effect of alleviating oxidative stress and inflammatory response, enhancing activity, and good synergistic effect

Active Publication Date: 2018-06-22
CHENGDU MEDICAL COLLEGE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although new drugs such as linezolid, daptomycin, ceftaroline, oritavancin, dalbavancin, and tedizolid phosphate have been approved by the FDA for the treatment of MRSA in succession, the clinical effects of these drugs have been found in recent years. Drug-resistant strains, and the probability of getting them is gradually increasing, so the research and development of new anti-MRSA = infection drugs is particularly urgent

Method used

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  • New application of geraniol and derivative thereof in preparing drugs for MRSA infectious diseases
  • New application of geraniol and derivative thereof in preparing drugs for MRSA infectious diseases
  • New application of geraniol and derivative thereof in preparing drugs for MRSA infectious diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Geraniol and its in vitro anti-MRSA activity in combination with β-lactam antibiotics

[0031] 1 Experimental materials

[0032] 1.1 Experimental strains

[0033] Standard strains: methicillin-resistant Staphylococcus aureus MRSA standard strains ATCC43300 and ATCC33591, purchased from the American Type Culture Collection.

[0034] Clinical isolates: 30 clinical isolates of MRSA, sourced from Sichuan Provincial Maternal and Child Health Hospital, identified as Staphylococcus aureus by VITEK32 and 16srRNA, identified as MRSA by cefoxitin antibacterial drug susceptibility test and mecA gene, see the strain source and serial number Table 1.

[0035] Table 1: Numbers and origins of tested strains

[0036]

[0037] 1.2 Drugs

[0038] Experimental drug: the invented drug Geraniol, Sigma-aldrich, batch number MKBQ1662V.

[0039] Antibiotics: Amoxicillin hydrochloride trihydrate, batch number B326BA3634, Sangon Bioengineering (Shanghai) Co., Ltd.; Cephalexin m...

Embodiment 2

[0076] Example 2 Geraniol anti-MRSA infection curative effect research in vivo

[0077] 1 Experimental materials

[0078] 1.1 Experimental strains

[0079] Standard strain: methicillin-resistant Staphylococcus aureus MRSA standard strain ATCC43300, purchased from the American Type Culture Collection.

[0080] 1.2 Drugs

[0081] Experimental drug: the invented drug Geraniol, Sigma-aldrich, batch number MKBQ1662V.

[0082] Positive drug: Vancomycin, Sigma.

[0083] 1.3 Experimental animals

[0084] KM mice, SPF grade, half male and half female, body weight (20±2) g, provided by Chengdu Institute of Biological Products Co., Ltd., Sichuan Province, animal production license number SCXK (Sichuan) 2016-08.

[0085] 1.4 Medium

[0086] MUELLER-HINTON BROTH (MHB), batch number 583507, British OXOID company; MUELLER-HINTONAGAR (MHA), batch number 1376993, British OXOID company; nutrient agar, batch number 20150810, Beijing Aoboxing Biotechnology Co., Ltd.

[0087] 2 Experimental...

Embodiment 3

[0107] Example 3 Mechanism of action of geraniol against MRSA

[0108] 1 Experimental materials

[0109] 1.1 Experimental strains

[0110] Standard strain: methicillin-resistant Staphylococcus aureus MRSA standard strain ATCC43300, purchased from the American Type Culture Collection.

[0111] 1.2 Drugs

[0112] Experimental drugs: invented drug Geraniol, Sigma-aldrich, lot number MKBQ1662V; Vancomycin, Sigma company. .

[0113] 1.3 Experimental animals

[0114] KM mice, SPF grade, half male and half female, body weight (20±2) g, provided by Chengdu Institute of Biological Products Co., Ltd., Sichuan Province, animal production license number SCXK (Sichuan) 2016-08.

[0115] 1.4 Medium

[0116] MUELLER-HINTON BROTH (MHB), batch number 583507, British OXOID company; MUELLER-HINTONAGAR (MHA), batch number 1376993, British OXOID company; nutrient agar, batch number 20150810, Beijing Aoboxing Biotechnology Co., Ltd.

[0117] 1.5 Main reagents

[0118] Mouse TNF-α (Tumor Nec...

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Abstract

The invention provides application of geraniol and a derivative thereof in preparing drugs for MRSA infectious diseases. The invention further provides a pharmaceutical composition for treating drug-resistant staphylococcus infectious diseases. The invention finally provides combination drugs for treating the drug-resistant staphylococcus infectious diseases. The combination drugs comprise the geraniol which has unit preparations of the same or different specifications and is used for dosing simultaneously or separately and drugs for treating the drug-resistant staphylococcus infectious diseases. The geraniol and the derivative thereof are natural drugs, for sing use, growth of MRSA can be effectively inhibited or MRSA is killed, an oxidative stress and inflammatory reaction caused by MRSAinfection can be relieved, and the geraniol and the derivative thereof can be used for treating the staphylococcus infectious diseases; meanwhile by combining beta-lactam antibiotics, the activity ofthe MRSA can be significantly enhanced, and the good synergistic effect is achieved; the drugs are prepared to be drugs for treating MRSA infection, and the clinical application prospect is good.

Description

technical field [0001] The invention relates to the new application of geraniol and its derivatives, in particular, the application in the preparation of medicines for treating staphylococcal infectious diseases. Background technique [0002] Methicillin-resistant Staphylococcus aureus (MRSA) is known as a "super bug". Since it was first discovered in the UK in 1961, it has spread around the world at an alarming rate. Currently, MRSA infections have exceeded AIDS, tuberculosis and viral hepatitis have become the first cause of death among patients, seriously threatening public health security. Although new drugs such as linezolid, daptomycin, ceftaroline, oritavancin, dalbavancin, and tedizolid phosphate have successively been approved by the FDA for the treatment of MRSA, in recent years, the clinical efficacy of these drugs has been found. Drug-resistant strains, and the probability of getting them increases gradually, so the research and development of new anti-MRSA = in...

Claims

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Application Information

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IPC IPC(8): A61K31/045A61K45/06A61P31/04
CPCA61K31/045A61K45/06A61K2300/00
Inventor 代敏彭成孙丰慧龙娜娜唐华侨林琳李建龙
Owner CHENGDU MEDICAL COLLEGE
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