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Mixed-source terpenoid and application thereof in preparing anti-inflammatory drug thereof

A technology of mixed-source terpenoids and compounds, which is applied in the field of mixed-source terpenoids and their preparation of anti-inflammatory drugs, and can solve the problems of unreported anti-inflammatory activities of terretonin and its analogs

Active Publication Date: 2018-10-12
ZHOUKOU NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, so far, there are very few reports on the activity of terretonins, and there is no report that terretonin and its analogs have anti-inflammatory activity

Method used

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  • Mixed-source terpenoid and application thereof in preparing anti-inflammatory drug thereof
  • Mixed-source terpenoid and application thereof in preparing anti-inflammatory drug thereof
  • Mixed-source terpenoid and application thereof in preparing anti-inflammatory drug thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1: Microbial fermentation culture and preparation of compounds

[0054] 1. Fermentation culture and extraction of fermented product

[0055] 1) Production strains

[0056] In this example, the bacteria used to ferment and produce compound I-IV were Aspergillus terreus isolated from the digestive tract of Pacific oyster ( Aspergillus terreus ) ML-44 strain, which is preserved in China General Microorganism Culture Collection Center (CGMCC), and the preservation number is CGMCC No. 15664.

[0057] 2) Fermentation culture

[0058] According to the routine method of microbial culture, take out Aspergillus from the refrigerator at 4°C ( Aspergillus terreus ) ML-44 test tube slant, scrape appropriate amount of spores with an inoculation loop under sterile conditions, and inoculate them in 5 newly prepared PDA solid medium (composition: glucose 2%, agar 2%, NaCl 1.5%, with 20 % potato boiled liquid) on the plate, activated and cultured in an incubator at 28°C for...

Embodiment 2

[0076] Embodiment 2: Anti-inflammatory activity test of compound I-IV

[0077] 1. Experimental materials

[0078] 1) Preparation of the tested sample solution

[0079] The test samples were pure compounds I-IV isolated and refined in Example 1 above. Precisely weigh an appropriate amount of sample, and use methanol to make a solution of the required concentration for testing the activity.

[0080] 2) Subculture of cell lines and cells

[0081] The activity test adopts mouse macrophage RAW 264.7 cell line. RAW 264.7 cells were routinely passaged in DMEM medium containing 10% fetal bovine serum and 100 μg / ml of penicillin and streptomycin, and maintained at 37°C in a cell culture incubator with 5% carbon dioxide.

[0082] 2. Activity test method

[0083] 1) Inhibitory effect of compounds on LPS-induced NO release from RAW 264.7 cells

[0084] The inhibitory effect of compounds I-IV on LPS-induced NO release from RAW 264.7 cells was tested by Griess method. Take the RAW 26...

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Abstract

The invention relates to a mixed-source terpenoid and application thereof in preparing an anti-inflammatory drug. The structure of the mixed-source terpenoid is as shown in the formula I, a preparation method of the mixed-source terpenoid comprises the steps that marine-derived aspergillus terreus ML-44 ferment is subjected to extraction, separation and purification to obtain the mixed-source terpenoid. The mixed-source terpenoid has the effect of restraining LPS from inducing RAW 264.7 cell NO production, and the effect is not achieved by restraining cell proliferation or toxicity, so that the mixed-source terpenoid has anti-inflammatory activity, therefore, the mixed-source terpenoid can be used for curing inflammatory diseases as the anti-inflammatory drug, and a lead compound is provided for developing a novel anti-inflammatory drug. The formula I is shown in the description.

Description

technical field [0001] The invention relates to a mixed-source terpenoid compound and its use in the preparation of anti-inflammatory drugs. Background technique [0002] Mixed terpenes are used to describe natural products formed by hybridizing other biosynthetic pathways through the isopentenyl pathway. They have complex and variable structural diversity, and thus show a variety of biological activities. Some of these compounds have been used clinically as therapeutic drugs, such as the antineoplastic drug vinblastine, the immunosuppressant mycophenolate mofetil, and the acetylcholinesterase inhibitor Doshkinin B, etc. Terretonins are a class of fungal-derived mixed terpenoids with 3,5-demethylorsellinic acid (DMOA) and arnesylpyrophosphate (FPP) as synthetic precursors, mainly isolated from Aspergillus fermentation products (Guo et al., Molecular genetic characterization of a cluster in A. terreus for biosynthesis of the meroterpenoid terretonin. Org Lett. 2012, 14:5...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J73/00A61K31/585A61P29/00C12N1/14C12P33/00C12R1/66
CPCA61P29/00C07B2200/07C07J73/003C12N1/14C12P33/00C12N1/145C12R2001/66
Inventor 吴长景刘晓萌崔香杨明生李博宋亚杰
Owner ZHOUKOU NORMAL UNIV
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