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Heptaene macrolide polyketone antibiotic FR-008 compound

A FR-008, macrolide technology, applied in the field of biomedicine, can solve problems such as limitations, and achieve the effect of strong antifungal activity

Inactive Publication Date: 2004-11-10
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the application of polyene macrolides is still mainly limited to the treatment of fungal diseases.

Method used

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  • Heptaene macrolide polyketone antibiotic FR-008 compound
  • Heptaene macrolide polyketone antibiotic FR-008 compound
  • Heptaene macrolide polyketone antibiotic FR-008 compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1: the fermentation medium of Streptomyces FR-008

[0035] Soybean cake flour medium:

[0036] Starch 4%,

[0037] Soy bean cake powder 5%,

[0038] NaCl 0.3%

[0039] PH value: 7.2

Embodiment 2

[0040] Embodiment 2: the fermentation culture of Streptomyces FR-008

[0041] Use an inoculation loop to pick a small amount of spores from the slant where Streptomyces FR-008 grows, inoculate in 10 250ml Erlenmeyer flasks containing 30ml soybean meal medium, and cultivate at 28°C for 48 hours. About 300 ml of the culture solution was inoculated as a seed into a fermenter containing 10 L of medium. The culture temperature is 28° C., and the rotation speed is 500 rpm. Under the condition of aeration rate of 10L / min, cultivate for 72 hours.

Embodiment 3

[0042] Embodiment 3: FR-008 extraction and separation

[0043] Use a high-speed centrifuge to centrifuge 10 liters of FR-008 fermentation broth at a speed of 6000rpm at 4°C, and extract the sediment three times with 5 times of n-butanol; the supernatant is concentrated under reduced pressure at about 40°C with a rotary evaporator to 1 / 10 volume, and then extracted three times with n-butanol. The extracts were combined and concentrated with a rotary evaporator at a temperature lower than 55 °C to a thick substance. Wash the thick matter with ether, centrifuge, discard the supernatant, and wash twice with ether to obtain about 20 g of yellow powder.

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PUM

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Abstract

A heptaene large ring lactone polyketone antibiotic FR-008 compound has the chemical structural formulas I and II, wherein the FR-008 polyketone antibiotic has antimycotic activity and high toxity to mosquito larvae, and can be applied in search and development for medical, indultrial and agricultural compounds.

Description

technical field [0001] The invention relates to a polyketide antibiotic, in particular to a heptacene macrolide polyketide antibiotic FR-008 compound, which belongs to the technical field of biomedicine. technical background [0002] Streptomyces is one of the main microbial groups in soil. Polyketides are a class of natural products. Many polyketide antibiotics have been used in medical, veterinary and agricultural applications, including erythromycin (antibacterial), nystatin (antifungal), abamectin (antiparasitic), sodium Bamycin (immunosuppressant) and daunorubicin (antineoplastic). For example, the immunosuppressant FK506 blocks the immune response by inhibiting the signaling pathways required for T cell activation and growth. FK506 is used to prevent graft rejection. And is used in the treatment of certain autoimmune diseases. Structurally, FK506 is also a macrolide, which can be produced by some Streptomyces species. [0003] After searching the literature, it wa...

Claims

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Application Information

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IPC IPC(8): A61P31/10C07H17/08
Inventor 邓子新陈实周秀芬黄曦
Owner SHANGHAI JIAO TONG UNIV
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