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Compound with anti-Candida albicans activity, preparation method and application thereof

A technology of Candida albicans and compounds, applied in the field of compounds with anti-Candida albicans activity and its preparation, can solve the problems of application limitation, high price, high toxicity and side effects, etc., and achieve the effect of extensive development and application prospects

Active Publication Date: 2016-08-10
SHANGHAI LAIYI BIOMEDICAL RES & DEV CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, Candida albicans antibiotics and chemically synthesized drugs used for clinical treatment are extremely limited, and their toxic and side effects are relatively high, and they are expensive, so their clinical application is limited

Method used

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  • Compound with anti-Candida albicans activity, preparation method and application thereof
  • Compound with anti-Candida albicans activity, preparation method and application thereof
  • Compound with anti-Candida albicans activity, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Example 1 , Preparation of compounds

[0045] 1.1. Fermentation

[0046] Streptomyces lavenduligriseus CGMCC No.10249 was inoculated in the seed medium, and cultured on a shaking table at 28°C and 220r / min for 2 days, and then the cultured seeds were inoculated at an inoculation amount of 8%. In the fermentation medium in the 5L fermenter, cultivate at 26-28°C for 5-7 days.

[0047] 1.2. Separation and purification

[0048] The fermentation product obtained in Example 1.1 was extracted with methanol, and the extract was obtained by distillation under reduced pressure. Extract the obtained extract with n-butanol, and distill under reduced pressure to obtain the extract. The obtained extract was separated by silica gel column chromatography with a 200-300 mesh silica gel column, and gradient elution was carried out using chloroform and methanol as the elution solvent, wherein the percentages of methanol were 0%, 10%, 20%, respectively. 30%, 40%, 50% and 100%, respec...

Embodiment 2

[0049] Embodiment 2, the structural identification of compound 1

[0050] Compound 1 obtained in Example 1.2 is detected by positive ion electrospray mass spectrometry, and its spectrum is as follows figure 1 As shown, the quasi-molecular ion peak is shown as: m / z 671.4010[M+H] + , the molecular formula is C35 h 58 o 12 , adopt Bruker Avance II-400 type superconducting nuclear magnetic resonance instrument to measure the hydrogen spectrum of sample ( figure 2 ), carbon spectrum ( image 3 ) and related two-dimensional spectra (HMQC spectrum, H-H COZY spectrum, HMBC spectrum, Figure 4~6 ), and its NMR data are shown in Table 1.

[0051] Table 1, the NMR data table of compound 1 (CD 3 OD , , 400MHz)

[0052] position

δ H

δ C

HMBC

1

173.0

2

2.44,t(11.9)

59.6

2’,4

3

4.23,t(13.1)

72.7

2,4

4a

1.46-1.50,m

42.5

4b

1.37-1.40,m

5

4.06-4.10,m

72.3

6

...

Embodiment 3

[0057] Embodiment 3, the structural identification of compound 2

[0058] Compound 2 obtained in Example 1.2 is detected by positive ion electrospray mass spectrometry, and its collection of spectra is as follows: Figure 7 As shown, the quasi-molecular ion peak is shown as: m / z 751.4241[M+Na] + , the molecular formula is C 38 h 64 o 13 , adopt Bruker Avance II-400 type superconducting nuclear magnetic resonance instrument to measure the hydrogen spectrum of sample ( Figure 8 ), carbon spectrum ( Figure 9 ) and related two-dimensional spectra (HMQC spectrum, H-H COZY spectrum, HMBC spectrum, Figure 10-12 ), and its NMR data are shown in Table 2.

[0059] The NMR data table of table 2, compound 2 (CD 3 OD , , 400MHz)

[0060] position

δ H

δ C

HMBC

1

173.0

2

2.73

60.4

2’,4

3

4.36

73.2

2,4

4

1.68

41.3

5

4.18

73.9

6a

1.73

45.3

6b

1.80

...

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Abstract

The invention discloses a compound with anti-Candida albicans activity, a preparation method and application thereof. The compound has a structural formula shown as formula (I) or (II) in the specification. The invention not only provides a new compound, and also the compound can be used for preparation of anti-Candida albicans infection drugs, therefore the development and application prospects are broad.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and specifically relates to a compound with anti-candida albicans activity and a preparation method and application thereof. Background technique [0002] Candida albicans is a common deep infection opportunistic pathogenic fungus. In recent years, with the wide application of radiotherapy, chemotherapy, immunosuppressants and broad-spectrum antibiotics, it is very easy to cause the imbalance of the internal environment and the imbalance of flora in the immunocompromised patients, and the Candida albicans infection is on the rise, which has become the main disease. One of fungal infection diseases. At present, Candida albicans antibiotics and chemically synthesized drugs for clinical treatment are extremely limited, and their toxic and side effects are relatively high, and they are expensive, so their clinical application is limited. Microorganisms are one of the important sources of many i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/04C07D313/00C12P17/18C12P17/08C12N1/20A61K31/365A61P31/10C12R1/465
Inventor 杨甲月杨志钧罗敏玉殷瑜杨天戈梅
Owner SHANGHAI LAIYI BIOMEDICAL RES & DEV CENT
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