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Compound with antibacterial activity and antitumor activity and preparation method and applications thereof

A technology of anti-tumor drugs and compounds, applied in the field of microorganisms, can solve problems such as unoptimistic curative effects

Inactive Publication Date: 2011-03-09
SICHUAN INDAL INST OF ANTIBIOTICS CHINA NAT PHARMA GROUP CORP +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At the same time, the incidence of malignant tumors is increasing year by year, and has become the number one killer of Chinese people's health. However, the curative effect of existing tumor treatment drugs is not optimistic. Therefore, the current urgency of the demand for new anti-tumor drugs is self-evident of

Method used

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  • Compound with antibacterial activity and antitumor activity and preparation method and applications thereof
  • Compound with antibacterial activity and antitumor activity and preparation method and applications thereof
  • Compound with antibacterial activity and antitumor activity and preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Bacteriological properties of strain SIIA-H8968

[0028] The inventors isolated many microbial strains from the soil in Sichuan Province, my country, and conducted a series of studies on the metabolites of these strains, and found that the secondary metabolites of strain SIIA-H8968 had obvious antibacterial and antitumor activities.

[0029] The taxonomic characteristics of strain SIIA-H8968 are as follows:

[0030] 1. Morphological properties

[0031] The basal hyphae developed well, with irregular branches, but no partitions were seen. There are few aerial hyphae that form spores, and the front end of the spore chain is cord-shaped or densely helical (10-20 spores) with 1-3 turns. Spore size: 0.6-0.7 μm wide, 1.0-0.5 μm long, cylindrical, smooth surface. No sporulation was observed in the agar medium. Also, the formation of sporangia and sclerotia and the motility of spores were not observed.

[0032] 2. The nature of cultivation

[0033] Table 1 show...

Embodiment 2

[0048] Embodiment 2: the preparation of compound WSS2277

[0049] 1. The liquid containing 1.0% glucose, 2.5% soluble starch, 0.3% cottonseed meal, 0.5% fish meal, 0.3% NZ CASE (purchased from Japan Wako Pure Pharmaceutical Co., Ltd.), 0.2% yeast extract and 0.2% calcium carbonate The incubation was based on moist heat sterilization at 121°C for 20 minutes. Then inoculate an appropriate amount of strain CGMCC No.3629 under aseptic operation, shake culture at 28° C. and 200 rpm for 4 days, and use it as a seed culture solution.

[0050] Then will contain 2.0% glycerol, 2.0% dextrin, 1.0% soytone, 0.2% (NH 4 ) 2 SO 4 30 L of liquid culture medium composed of 0.2% calcium carbonate was adjusted to pH 7.0, then loaded into a 50 L fermenter, and steam sterilized at 121° C. for 20 minutes. Then, under aseptic operation, the aforementioned seed culture solution was added thereto at a 4% inoculum amount, and cultured at 28° C. and 200 rpm for 4 days.

[0051] After the cultivatio...

Embodiment 3

[0055] Embodiment 3: identification and analysis of the compound of the present invention

[0056] The chemical structure of the compound WSS2277 obtained by the above method was analyzed and confirmed by ultraviolet absorption spectrum, 1H-NMR nuclear magnetic resonance spectrum, 13C-NMR nuclear magnetic resonance spectrum and the like.

[0057] The physical and chemical properties of compound WSS2277 are as follows:

[0058] 1. Appearance: yellow amorphous powder

[0059] 2. Molecular weight: 1092

[0060] 3. Molecular formula: C 60 h 84 o 18 , the structural formula is as follows:

[0061]

[0062] 4. Ultraviolet absorption spectrum λMAX (nm): 360nm

[0063] 5.1H-NMR nuclear magnetic resonance spectrum: the sample is dissolved in deuterated dimethyl sulfoxide (DMSO-d6), and measured at 500MHz, the results are shown in figure 1 , the specific data is:

[0064] chemical shift

[0065] 6.25

[0066] Description: s singlet, d doublet, dd doublet ...

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Abstract

The invention relates to the microbial field and discloses a compound generated by a microorganism and a preparation method and applications thereof. The structural formula of the compound is shown in the formula I. The invention also provides the microorganism used for producing the compound, wherein the microorganism is preserved in the China General Microbiological Culture Collection Center and has the preservation number of CGMCCNo.3629. The compound of the invention has antibacterial activity and antitumor activity, and can be used to prepare medicines for curing bacterial infection and tumor and have wide clinical application prospect.

Description

technical field [0001] The invention relates to the field of microorganisms, in particular to a compound produced by microorganisms with antibacterial activity and antitumor activity, as well as its preparation method and application. Background technique [0002] In recent years, bacterial infection has become one of the major threats to human health. With the widespread use of antibiotics, pathogenic bacteria continue to mutate under natural selective pressure to produce drug resistance. For example, the drug resistance of Staphylococcus aureus, which seriously threatens human health, has increased from less than 10% in the 1940s to penicillin G. It has grown to 50% over the course of several years. Since the emergence of methicillin multidrug-resistant Staphylococcus aureus (MRSA) in 1961, along with the widespread use of the second and third generation cephalosporins, the incidence of MRSA has been increasing, from less than 3% before 1992 to an increase nearly 40 perc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D321/00A61K31/365C12P17/08A61P35/00A61P31/04C12N1/20
Inventor 褚以文照井祐一赵子翰野泽修王辂
Owner SICHUAN INDAL INST OF ANTIBIOTICS CHINA NAT PHARMA GROUP CORP