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Low toxicity pimamycin derivatives and preparation method and application thereof

A pimamycin and derivative technology, which is applied in the field of low-toxic pimamycin derivatives and their preparation, can solve the problems of hemolytic toxicity, limiting the application value of polyene antibiotics and the like

Active Publication Date: 2016-08-24
上海览通生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, while polyene antibiotics exhibit high antifungal activity, they also have severe hemolytic toxicity, which severely limits the clinical application value of polyene antibiotics.

Method used

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  • Low toxicity pimamycin derivatives and preparation method and application thereof
  • Low toxicity pimamycin derivatives and preparation method and application thereof
  • Low toxicity pimamycin derivatives and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Prepare 500ml of seed medium and 5L of fermentation medium according to the seed medium and fermentation culture formula, respectively, pack them in 250ml triangular bottles, fill each bottle with 50ml, sterilize at 115°C for 30min, insert the spores of the mutant strain QZ02 into the above seeds In the culture medium, at 220 rpm, at 30° C., on a shaker for 24 hours to obtain a seed culture solution. The seed culture solution was added to the fermentation medium according to 10% inoculum amount, and cultured on a shaker at 220 rpm at 30° C. for 5 days to obtain a fermentation culture of the mutant strain QZ02. Centrifuge the 5L fermentation culture obtained from the fermentation culture, collect the fermented cells, wash the cells with water for 3 times, remove the washing liquid, and freeze-dry the cells overnight; Centrifuge to obtain the extract, repeat the ultrasonic extraction 3 times, combine the extracts, filter the extracts, concentrate under reduced pressure to...

Embodiment 2

[0033]According to the seed medium and fermentation culture formula, prepare 1L seed medium and 10L fermentation medium respectively, pack them into 250ml triangular bottles, fill each bottle with 50ml, and sterilize at 115°C for 30min, insert the spores of the mutant strain QZ02 into the above seeds In the culture medium, at 220 rpm, at 30° C., on a shaker for 24 hours to obtain a seed culture solution. The seed culture solution was added to the fermentation medium according to 10% inoculum amount, and cultured on a shaker at 220 rpm at 30° C. for 5 days to obtain a fermentation culture of the mutant strain QZ02. Centrifuge the 10L fermentation culture obtained from the fermentation culture, collect the fermented cells, wash the cells with water for 3 times, remove the washing liquid, and freeze-dry the cells overnight; Centrifuge to obtain the extract, repeat the ultrasonic extraction 3 times, combine the extracts, filter the extracts, concentrate under reduced pressure to o...

Embodiment 3

[0035] Determination of Antifungal Activity and Hemolytic Toxicity of Pimaricin Derivatives in Vitro

[0036] The determination of antifungal activity in vitro is based on Candida albicans as the indicator bacteria. By measuring the growth of Candida albicans at different concentrations of antibiotics, the MIC of the corresponding antibiotics can be obtained. 50 and MIC 90 value. First, the overnight culture solution of Candida albicans was inoculated in LB medium at a ratio of 1 / 10000, and distributed in 96-well plates at 200 μl / well. The DMSO solutions of the Pimaricin derivatives and Pimaricin at different concentrations (0-800 μg / ml) were prepared, and added to the above LB medium at a ratio of 2%. Place the 96-well plate in a 34°C incubator, culture it statically for 12 hours, and use a microplate reader to measure the OD under different concentrations of antibiotics 660 . MIC can be obtained by drawing the inhibition curve of the measured data against the concentrati...

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Abstract

The invention discloses a low-toxicity pimaricin derivate. A molecular formula of the low-toxicity pimaricin derivative is C33H49NO10 and the chemical structural formula is shown in the specification. The low-toxicity pimaricin derivative is obtained by performing production strain (Streptomyces chattanoogensis QZ02) construction, fermentation and culture of mutant strain QZ02, thallus treatment, organic reagent extraction, reversed phase column chromatography and high performance liquid chromatography separation. The compound has the advantages of stable structure, high activity and extremely low toxicity, and can be used as an antifungal drug and a food antiseptic; therefore, the low-toxicity pimaricin derivative has good application prospect.

Description

technical field [0001] The invention relates to a technology for separating secondary metabolites of microorganisms, in particular to a low-toxicity pitamamycin derivative and its preparation method and application. technical background [0002] With the increasing number of patients with immune system deficiency, the incidence and harm of systemic fungal infection are also increasing. Fungal pathogens have the characteristics of high transmission rate, high proliferation rate, and high lethality rate, and they are highly resistant to many drugs. At present, the antifungal drugs that can be used clinically to treat systemic fungal infections are very limited, and all of them have different degrees of side effects and toxicity. Among them, polyene antibiotics have extremely efficient antibacterial and antibacterial activities against a variety of fungal pathogens, and the development of pathogen resistance to them is very slow, and are currently recognized as the most effect...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H17/08C12P19/62A61P31/10A23L3/3562C12R1/465
Inventor 白林泉齐震康前进姜春艳
Owner 上海览通生物科技有限公司
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