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Melittin and use thereof

A technology of melittin and endotoxin, applied in the fields of peptides, antibacterial drugs, drug combinations, etc., can solve problems such as inaccurate curative effect

Inactive Publication Date: 2005-12-07
THE FIRST AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIVERSITY OF PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In animal experiments, the above preparations have a certain protective effect on organ damage caused by sepsis, but in clinical trials, they have not been approved by the US FDA due to inaccurate efficacy.

Method used

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  • Melittin and use thereof
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  • Melittin and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1: the synthesis of melittin

[0037]1.1 Synthesis of melittin resin peptide resin: Weigh 0.05mmol of Fmoc-L-Lys-PEG-PS resin (or other polypeptide synthetic resin) and pour it into a synthesis column, add about 15ml of refined dimethylformamide (DMF) to swell 30min, take another 50ml of 1.0mmol diisopropylethylamine (DIPEA) (8.7ml DIPEA+41.3ml DMF), 0.5mmol of azabenzotriazole methyluronium hexafluorophosphate (HATM) 50ml (9.5g HATM+40.5 ml DMF) and an appropriate amount of DMF (Deblock solution) containing 20% ​​hexahydropyridine were added to the reagent bottle respectively, and 2 mmol of Fmoc-amino acids were successively weighed in a suitable container according to the melittin amino acid sequence of the present invention. According to the solid-phase chemical synthesis method invented by merrifield, the amino acid sequence of melittin is sequentially carried out from the C-terminus. Add the Deblock liquid depeptidation resin Fmoc protecting group to the...

Embodiment 2

[0047] Example 2: Protective effect of melittin on Escherichia coli ATCC25922 live bacteria / LPS challenged mice

[0048] 2.1 Experimental method: Kunming mice were randomly divided into 5 groups, 20 in each group, melittin control group, live bacteria control group and LPS control group were injected with melittin (3 mg / kg), E. ATCC25922 (2×10 9 CFU / 20g body weight) and LPS 20mg / kg; 9 CFU / 20g body weight) were injected with melittin (3mg / kg) within 20s, and the melittin / LPS treatment group was injected with LPS 20mg / kg 10 seconds after the injection of melittin 3mg / kg. The total volume injected was 200 μl / 20 g body weight. The mice were observed for death within 3 days.

[0049] 2.2 Experimental results: The mental state of the mice in the melittin treatment group was sluggish but recovered quickly, and their appetite, activity and responsiveness to external stimuli were improved in a short period of time, which were better than those in the live bacteria / LPS control group....

Embodiment 3

[0050] Embodiment 3: the antibacterial action of melittin

[0051] 3.1 Experimental method: The antibacterial activity of melittin against 18 strains of bacteria was detected by microdilution method and compared with other antibiotics. ① Take Escherichia coli ATCC25922 and inoculate it in LB culture medium, incubate at 37°C for 18 hours, then transfer to fresh culture medium and cultivate it for 4 hours, and use LB culture medium to adjust the bacterial concentration to 1×10 5 CFU / ml. ②Take a 96-well culture plate, with 8 wells as a column, a total of 12 columns. Add 200 μl of bacterial solution to the first column, add 100 μl of bacterial solution to the second to eleventh columns, and add 100 μl of LB culture solution to the last column as a negative control. ③Take melittin and 6 kinds of other antibiotics, each diluted with normal saline to 10.24mg / ml. ④ The first line is for doubling dilution of melittin. Add 10 μl of melittin to the first well, mix well, aspirate 100 μ...

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Abstract

The invention discloses Melittin, a micro-molecular polypeptide of amino acid type antibacterial / mAb with the formula of INLKAIAALAKKLL-NH2. The invention can be applied for the preparation of medicaments for eradicating bacteria and treating pyaemia.

Description

technical field [0001] The present invention relates to small molecule polypeptides of amino acid type and applications thereof, more specifically a kind of melittin and its use in the preparation of medicaments for treating sepsis through sterilization, neutralization of endotoxin (lipopolysaccharide, LPS) and inhibition of respiratory burst in the application. Background technique [0002] Sepsis is the leading cause of death in clinically critically ill patients, especially Gram-negative (G - ) Bacillus infection. G - The fatality rate of bacteremia is 20-30%, while the fatality rate of septic shock developed from bacteremia can be as high as 50-80%. At present, there is no effective clinical treatment for sepsis, which makes the treatment of infectious diseases more difficult. Researching its pathogenesis and finding effective treatment measures have always been the focus of clinical medicine. [0003] In recent years, with the in-depth research on sepsis, the G - T...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08
Inventor 郑江郭毅斌周红吕根法卫国
Owner THE FIRST AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIVERSITY OF PLA
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