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Valinomycin B, preparation method and medical purpose thereof

A technology of valinomycin and drugs, which is applied in the field of preparation of drugs for the treatment of glioma, and can solve the problems of severe drug resistance, hindering drug efficacy, and limited curative effect

Active Publication Date: 2016-09-28
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is a serious shortage of anti-glioma drugs at present, and temozolomide is the only option for the treatment of glioma alone
Moreover, the curative effect of the existing drugs for treating glioma including temozolomide is limited, and most of them have serious deficiencies, and the outstanding performances are: (1) most of them are chemicals, with large toxic and side effects; (2) severe drug resistance of tumor cells (3) The blood-brain barrier prevents the drug from reaching the brain and exerting its curative effect

Method used

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  • Valinomycin B, preparation method and medical purpose thereof
  • Valinomycin B, preparation method and medical purpose thereof
  • Valinomycin B, preparation method and medical purpose thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1. Isolation and cultivation of Streptomyces parvulus P11-23B (Streptomyces parvulus P11-23B)

[0038] Take 1 gram of air-dried sea mud and dilute it with seawater to a concentration of 1×10 -6 g / mL sample diluent, take 200 μL of sample diluent and evenly disperse it in a petri dish containing Gause’s agar solid medium, and after culturing at 28°C for 7 days, transfer different colonies separately Transfer to another Petri dish containing Gore's agar solid medium, and continue culturing at 28°C for 7 days. Finally, a well-grown single colony (P11-23B) was inoculated on the slant medium of Gowell's agar for culture, and then stored in a 4°C refrigerator for later use.

Embodiment 2

[0039] Example 2. Identification of Streptomyces parvulus P11-23B (Streptomyces parvulus P11-23B)

[0040] The species of the obtained strain P11-23B was identified by 16S rDNA sequence analysis.

[0041] 2.1 Experimental reagents and instruments

[0042] PCR reagent: EX Taq enzyme (TaKaRa), dNTP (TaKaRa), primer (Invitrogen synthesis), primer sequence is: TACGGYTACCTTGTTACGACTT and AGAGTTTGATCMTGGCTCAG;

[0043] Marker: DL500

[0044] Experimental equipment: centrifuge, electrophoresis instrument, PCR instrument, ABI 3730XL sequencer.

[0045] 2.2 Experimental steps

[0046] Bacterial genomic DNA extraction;

[0047] Electrophoresis detection

[0048] PCR amplification

[0049] a. PCR reaction system

[0050]

[0051] b. PCR reaction conditions

[0052]

[0053] 10°C∞,

[0054] c. Electrophoresis detection,

[0055] d. Sequencing: Gel cutting, purification and sequencing,

[0056] e. Analysis results: spliced ​​sequences.

[0057] 2.3 Experimental results

...

Embodiment 3

[0061] Embodiment 3. Preparation of Streptomyces parvulus P11-23B (Streptomyces parvulus P11-23B) fermentation broth

[0062] Take the colony of Streptomyces parvulus P11-23B and inoculate it into a 500mL Erlenmeyer flask containing 200mL of liquid Gowell medium, and culture the culture solution containing the P11-23B strain at 28°C for 7 days with rotation (180rpm) to obtain Inoculum solution. Transfer 5mL of the strain solution into a 500mL Erlenmeyer flask containing 200mL of liquid Gowell medium, and culture it with rotation (180rpm) shaking at 28°C for 7 days to obtain a fermentation broth of P11-23B with antitumor activity.

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Abstract

The invention provides a compound valinomycin B having glioma activity resistance, provides an active substance producing strain streptomyces parvus separated and cultured from sea mud, and the active substance valinomycin B can be prepared. The streptomyces parvus is preserved in the China Center for Type Culture Collection and named as P11-23B (Streptomyces parvus P11-23B) with a preservation number of CCTCC NO: M 2015675 on Nov, 12th, 2015. The valinomycin B has features of obviously inhibiting multiplication of various kinds of glioma cells, obviously inhibiting glioma cell cycle at G0 / G1 phase, and reducing the protein level expression of several key enzymes with different metabolism approaches of glioma cells, and has unique anti-tumor effect. The valinomycin B can be used for preparing medicines for treating glioma. The chemical structural formula of the valinomycin B is as shown in the specification.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a method for preparing an antitumor active compound Valinomycin B from marine actinomycete Streptomyces parvulus P11-23B and the compound used in the preparation of a medicament for treating glioma. aspect applications. Background technique [0002] Glioma is the most common and malignant brain tumor in the brain, accounting for 70% of all malignant brain tumors. According to the statistics of the World Health Organization, malignant glioma is the second cause of death for tumor patients under the age of 34, and the third cause of death for patients aged 35 to 54, which seriously endangers human health and life. Due to the special location of glioma, the operation is difficult and it is not easy to completely remove the tumor. Therefore, radiotherapy and drugs are particularly important for the treatment of glioma. However, there is currently a serious lack of anti-glioma drugs, and temoz...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D273/00C12N1/20C12P17/14A61P35/00C12R1/465
CPCC07D273/00C12P17/14C12N1/205C12R2001/465
Inventor 张治针叶雪威连晓媛
Owner ZHEJIANG UNIV
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