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Large ring lactone antibiotic and preparing method thereof

A technology for macrolides and antibiotics, which is applied in the field of new macrolide antibiotics and their preparation, and can solve problems such as unsatisfactory absorption, distribution, metabolism, and unstable structure of macrolides

Inactive Publication Date: 2004-04-14
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

One of the reasons is that due to years of clinical application, many pathogenic bacteria have developed drug resistance to existing macrolides, such as Staphylococcus aureus, Streptococcus, pneumococcus, etc., making macrolides The clinical application of antibiotics is limited, coupled with the unstable structure of many macrolides, the absorption, distribution, and metabolism in the body are not satisfactory, so it is necessary to conduct in-depth research on macrolide antibiotics

Method used

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  • Large ring lactone antibiotic and preparing method thereof
  • Large ring lactone antibiotic and preparing method thereof
  • Large ring lactone antibiotic and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Preparation of compound (I)

[0030] (1) Strain cultivation and fermentation:

[0031] ①Preparation of culture medium (g / l): Take 5.0g of glucose, 40.0g of soluble starch, 4.0g of peptone, 2.0ml of corn steep liquor, K 2 HPO 4 0.5g, MgSO 4 ·7H 2 O 0.5g, NaCl 0.5g, add water to 1000ml at pH 6.0, sterilize at 121°C for 15min; ②Fermentation: add Streptomyces luteogriseus via. In the sterilized medium, the amount of bacteria added is 10% of the weight of the fermentation medium, and the shake flask is fermented at 160 rpm, 28°C, and fermented for 4 days;

[0032] (2) Fermentation broth treatment: ①The fermentation broth was centrifuged at 4800 rpm for 20 minutes; ②Extracted 5 times with an equal volume of ethyl acetate, and the ethyl acetate part was back-extracted with 2:1 volume of water to remove pigment impurities; ③Recover ethyl acetate to obtain a brown oil with an active site; ④Carry out silica gel column chromatography, use dichloromethane:methanol 1:0 to 0:1 ...

Embodiment 2

[0049] Determination of antibacterial activity of the compound prepared in Example 1 against Bacillus subtilis. Bacillus subtilis was used as the test bacteria, and the following positive control drugs were selected:

[0050] Erythromycin (Tianjin Jinshi Pharmaceutical Co., Ltd., batch number: 020302);

[0051] Acetylspiramycin (Tianjin Zhongxin Pharmaceutical Group Co., Ltd. Xinxin Pharmaceutical Factory, batch number: 030104);

[0052] Lijunsha (erythromycin ethylsuccinate, Xi'an Lijun Pharmaceutical Co., Ltd., batch number: 0303075-14);

[0053] According to the Oxford cup and saucer method, the agar gel was spread on a plane, and after 24 hours, the diameter of the inhibition zone was measured.

[0054] Adopt the concentration that same wants to compare sample (2 mg / ml) and the compound (2 mg / ml) prepared by the embodiment of the present invention 1, survey its bacteriostatic zone, the bacteriostatic zone of compound of the present invention is far greater than that of p...

Embodiment 3

[0056] The compound prepared in Example 1 is also effective against drug-resistant Staphylococcus aureus.

[0057] The minimum inhibitory concentration (MIC) for Staphylcoccus aureus (Staphylcoccus aureusATCC29213) is 12 μg / ml.

[0058] The minimum inhibitory concentration (MIC) for Roxithromycin-resistant Streptococcus pneumoniae (RRSP) is 0.5 μg / ml.

[0059] The above strains were all preserved by the Institute of Pharmaceutical Biotechnology, Chinese Academy of Medical Sciences.

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Abstract

The invention discloses a kind of macrolide antibiotic and the manufacturing method, the method includes following steps: (1) culture yeasting: óƒ the producing of incubation media: blends glucose, soluble starch, peptone, corn pulp, K2HPO4, MgSO4.H2O, NaCl and water, carries on sterilization; ó yeasts: the garcinia grey chain mycete strain into the sterilized incubation media, shakes the bottle and carries on yeasting; (2) processes the yeasted liquid: óƒ centrifugates yeasted liquid; ó isochoric extract acetic ester, partial acetic ester is inversely extracted by water and the pigment impurities are eliminated; ó� reclaims acetic ester and gets brown oil which has active part; óœ carries on silica pole chromatography and gets the coarse product; ó¦ purifies the coarse product.

Description

technical field [0001] The invention relates to a novel macrolide antibiotic and a preparation method thereof. Background technique [0002] Macrolide antibiotics are a class of antibiotics commonly used in clinical practice. They are widely used for their broad antibacterial spectrum, obvious antibacterial effect and definite curative effect. At present, the main research directions of macrolide antibiotics are as follows: ① Find new structure, to discover antibiotics with higher antibacterial potency, better antitumor efficacy, and broader spectrum; ②Explore physiologically active substances other than antibacterial activity, and open up new uses such as motilin-like effects, immunosuppressants, etc.; ③Continue Modify the structure of existing macrolide antibiotics such as erythromycin, so that the drug can be used for infection of drug-resistant bacteria. One of the reasons is that due to years of clinical application, many pathogenic bacte...

Claims

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Application Information

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IPC IPC(8): A61P31/04C07D519/00C12P17/18
Inventor 元英进王志平王蕾李霞范晋勇
Owner TIANJIN UNIV
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