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New application of sesquiterpenoids

A compound and solvate technology, applied in the field of pharmaceutical use, can solve the problems of unrecorded inflammation treatment effects, etc., and achieve good inflammation inhibition, good inflammation, and the effect of inhibiting nuclear translocation

Pending Publication Date: 2020-02-07
UNIVERSITY OF MACAU
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no record in the prior art which single compound it contains has a good therapeutic effect on inflammation

Method used

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  • New application of sesquiterpenoids
  • New application of sesquiterpenoids
  • New application of sesquiterpenoids

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] This embodiment provides a compound shown in formula (1), coded as LB, that is, hereinafter LB all represent compounds shown in formula (1)

[0040]

[0041] Its preparation method is as follows:

[0042] (1) Weigh 700g of Herba chinensis medicinal material powder, add 7L of ethanol with 50% concentration, heat to a slight boil, reflux for extraction for 1 hour, filter after cooling, collect the filtrate, and use 50% ethanol for reflux to extract the filter residue according to the above method 2 Second-rate. Combine the three extracts and concentrate under reduced pressure to 700mL;

[0043] (2) Weigh 700 g of activated D101 macroporous resin, add it to the above concentrated solution, let it stand for adsorption for 24 hours, and then load it into a separation column. Elute with pure water until the eluent is nearly colorless, then elute with appropriate amount of 50% and 95% ethanol in turn until the eluent is nearly colorless, combine the eluents, concentrate u...

experiment example 1

[0047] To detect the toxicity of LB to RAW264.7 cells

[0048] Specific detection method: RAW264.7 was treated with LB (0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM, 20 μM and 40 μM) without adding lipopolysaccharide (LPS) and adding LPS (1 μg / mL), respectively Cells were left for 24 hours before cell viability was measured by MTT assay. For test results, see figure 1 A and B in,figure 1 A in A is the MTT detection result of different concentrations of LB when no LPS is added; figure 1 B in B is the MTT detection results of different concentrations of LB when the LPS is 1 μg / mL; the data are the mean ± SD of the smallest three independent experiments.

[0049] RAW264.7 cells were treated with LB (5 μM, 10 μM, and 20 μM) for 24 hours without adding lipopolysaccharide (LPS) and adding LPS (1 μg / mL), and then measured by LDH assay kit Lactate dehydrogenase (LDH) content. For test results, see figure 1 In C, data are mean ± SD of a minimum of three independent experiments.

[005...

experiment example 2

[0052] Detection of LB on NO, PGE in RAW264.7 cells 2 and pro-inflammatory proteins

[0053] Specific detection method: RAW264.7 cells were pretreated with LB (5 μM, 10 μM, 20 μM) for 1 hour, and then stimulated with LPS (1 μg / mL) for 12 hours, collected supernatant, and detected NO with Griess reagent, ELISA kit Detection of IL-6, MCP-1, TNF-α and PGE 2 . For test results, see figure 2 (A)-(E) in, where figure 2 A in is the test result of No, figure 2 B in is the detection result of IL-6, figure 2 C in is the detection result of MCP-1, figure 2 D in is the detection result of TNF-α, figure 2 E in is PGE 2 test results. Data are means ± SD of a minimum of three independent experiments.

[0054] according to figure 2 It can be seen that compared with the control, ***p2 and production of proinflammatory proteins.

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Abstract

The invention relates to the field of drug application, in particular to new application of sesquiterpenoids. Specifically, application of an inhibitor to preparation of an anti-inflammatory drug is provided, the inhibitor includes at least one of a compound shown in a formula (1) (please see the specifications for the formula), a pharmaceutically acceptable salt of the compound, a solvate of thecompound, a polymorphic substance of the compound, and a tautomer of the compound. The inhibitor can effectively inhibit releasing of nitric oxide (NO) and phenyl glycidyl ether (PGE2) due to LPS induction, secretion of cell factors IL-6, TNF-alpha and MCP-1 and generation of reactive oxygen species (ROS) are inhibited. Meanwhile, expression of an NF-kappa B signal pathway and downstream proteinsiNOS and COX-2 can also be inhibited, nuclear translocation of an activator protein AP-1 (p-c-Jun) is inhibited, and thus the sesquiterpenoids have a good inflammation inhibiting effect and play a good role in inflammation inhibiting.

Description

technical field [0001] The present invention relates to the field of medicine application, in particular to a new application of sesquiterpene compounds. Background technique [0002] Inflammation is a self-defense reaction process produced by the body against the damage caused by inflammatory factors. Prostaglandins (PGs) and leukotrienes (LTs) are the most important inflammatory mediators produced by the metabolism of arachidonic acid (AA) in inflammation-related processes, and are involved in rheumatism, rheumatoid arthritis, colitis, pain, asthma, Occurrence and treatment of atherosclerosis, stroke, Alzheimer's disease, cancer and other indications. In the metabolic network of AA, cyclooxygenase (COX) is the key enzyme for the release of prostaglandin PG, among which cyclooxygenase-1 (COX-1) is closely related to the synthesis of physiological PGs, and COX-2 is mostly induced , is associated with the generation of inflammatory PGs, so COX-2 is a key target in the treat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61K36/28A61P29/00A61P19/04A61P19/02A61P1/00A61P9/10
CPCA61K31/365A61K36/28A61P29/00A61P19/04A61P19/02A61P1/00A61P9/10
Inventor 余华王一涛令狐克刚赵冠丁
Owner UNIVERSITY OF MACAU
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