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A new compound and its application in the preparation of bacterial inhibitor

A technology of bacterial inhibitors and compounds, applied in the field of new compounds and their application in the preparation of bacterial inhibitors, can solve the problems of high myocardial toxicity, affecting applications, and low water solubility

Active Publication Date: 2020-05-19
NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although CSL has significant pharmacological activity, its low water solubility, high myocardial toxicity and strong killing effect on normal cells have seriously affected its clinical application.

Method used

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  • A new compound and its application in the preparation of bacterial inhibitor
  • A new compound and its application in the preparation of bacterial inhibitor
  • A new compound and its application in the preparation of bacterial inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1, acquisition, identification and preservation of bacterial strains

[0031] 1. Acquisition of strains

[0032] 1. Get the disease-free fresh leaves of Tripterygium wilfordii plant in Yao County, Dali, Yunnan Province, and carry out surface disinfection. Surface disinfection method: rinse with clean water, rinse 4 times with clean water, rinse with 75% alcohol for 30s, then soak in 5% sodium hypochlorite for 2s, rinse with sterile water 10 times.

[0033] 2. Sterile filter paper absorbs the moisture on the surface, cuts off the liquid-contact side with a sterilized blade, then cuts the inside into small pieces and transplants it into the modified Martin solid medium containing 150mg / L penicillin and 120mg / L streptomycin , and then pick the growing single colonies for culture.

[0034] 3. Further carry out continuous purification to obtain a purely cultured strain, which is named LGT-5 strain.

[0035] 2. Identification of strains

[0036] 1. Colony morph...

Embodiment 2

[0051] Embodiment 2, application Phomopsis LGT-5 prepares 16-OH-Celastrol

[0052] 1. Application of Phomopsis LGT-5 for tripterine transformation

[0053]1. Inoculate Phomopsis LGT-5 into a Erlenmeyer flask containing 150mL of modified Martin liquid medium, and cultivate it with shaking at 28°C and 180rpm until the logarithmic growth phase (usually the culture time is 1 day), at this time Phomopsis The concentration of mold LGT-5 was 5 g dry weight / L culture system. Dry weight measurement method: sample the culture system, collect the bacteria by centrifugation, wash thoroughly with sterile water, and then dry to dry weight.

[0054] 2. After completing step 1, add 2 mL of tripterine solution (containing 50 mg of tripterine, the solvent is DMSO) to the culture system, and culture with shaking at 28° C. and 180 rpm for 5 days. That is, the ratio of Phomopsis LGT-5 and tripterine is: 0.75 g dry weight of Phomopsis LGT-5: 50 mg tripterine.

[0055] 3. After completing step 2,...

Embodiment 3、1

[0066] Example 3, Functional Verification of 16-OH-Celastrol

[0067] Test compound: Celastrol or 16-OH-Celastrol prepared in Example 2.

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PUM

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Abstract

The invention discloses a new compound and its application in the preparation of bacterial inhibitors. The compound provided by the invention is a compound as shown in the formula (III). The application of the compound as shown in the formula (III) in the preparation of a bacterial inhibitor is also within the protective range of the invention. In comparison with tripterine, there is no significant difference in the antibacterial activity of 16-OH-Celastrol, but its cytotoxicity is greatly reduced. The product can be used as a novel bacteriostatic drug.

Description

technical field [0001] The invention belongs to the field of biotechnology, and in particular relates to a new compound and its application in the preparation of bacterial inhibitors. Background technique [0002] Tripterygium wilfordii has antibacterial, anti-inflammatory, and anti-tumor effects. The active ingredient in Tripterygium wilfordii is Celastrol (CSL). The structural formula of tripterine is as follows: [0003] [0004] Although CSL has significant pharmacological activity, its low water solubility, high myocardial toxicity and strong killing effect on normal cells have seriously affected its clinical application. What needs to be solved at present is to improve or retain pharmacological activity while reducing toxicity so as to improve the therapeutic index. [0005] Biotransformation of natural active lead compounds is a method of using biological systems (such as: enzymes, microorganisms, plant cells) to modify the specific molecular structure of natura...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J63/00A61K31/56A61P31/04A01N37/42A01P1/00C12P33/02C12R1/645
CPCA01N37/42A61P31/04C07J63/008C12P33/02
Inventor 吴秀丽刘成张彩芳周丽刘河涛王洒
Owner NINGXIA MEDICAL UNIV
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