Application of sesquiterpene lactone compound in preparation of drugs for treating optic neuritis

An ester compound, optic neuritis technology, applied in the medical field of autoimmune diseases, can solve the problems of treatment failure, large systemic side effects, hormone tolerance of treatment methods, etc.

Pending Publication Date: 2020-10-09
ACCENDATECH LUOYANG CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current existing treatment methods are all widely suppressing the immune system of the whole body and reducing the systemic autoimmune reaction. The patients have relatively large systemic side effects and the risk of serious infection, and the treatment methods are likely to cause hormone resistance and lead to treatment failure.
[0006] Therefore, NMO is seriously short of safe and effective drugs, and the clinical needs have not been met. The development of new drugs for the treatment of this disease is very urgent.

Method used

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  • Application of sesquiterpene lactone compound in preparation of drugs for treating optic neuritis
  • Application of sesquiterpene lactone compound in preparation of drugs for treating optic neuritis
  • Application of sesquiterpene lactone compound in preparation of drugs for treating optic neuritis

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] The molecular formula of the sesquiterpene lactone compound used to prepare the medicine for treating neuromyelitis optica studied in this embodiment is as follows: figure 1 As shown, also known as ACT001, the chemical name of ACT001 is: (3R, 3aS, 9R, 9aS, 9bS)-3-((dimethylamino)methyl)-9-hydroxyl-6,9-dimethyl -3,3a,4,5,7,8,9,9a-octahydroazulene[4,5-b]furan-2(9bH)-one fumarate is a michelactone derivative. Molecular formula such as figure 1 shown. In this example, ACT001 was used to study the treatment of patients with AQP4 autoimmune antibody-positive neuromyelitis optica.

[0026] Pharmacological and drug efficacy experiments are as follows:

[0027] 1. We first conducted an in vitro test on the active ingredients. According to the in vitro test results, ACT001 can inhibit the proliferation of BV-2 cells in vitro, and its IC50 value is 23.6 μM. And it can significantly reduce the release of microglial inflammatory factors (TNF-α, IL-6, NO) activated by LPS at 10 μ...

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Abstract

The invention relates to optic neuritis drug research, in particular to an application of sesquiterpene lactone compounds in preparation of optic neuritis treatment drugs, and the sesquiterpene lactone compounds and pharmaceutically acceptable auxiliary materials are prepared into a medicament. The research finds that ACT001 can effectively inhibit the inflammatory response of microglia, and can significantly reduce the release of inflammatory factors including NO, TNF-alpha and IL-6. The effect of inhibiting BV2 cell proliferation is achieved. The compound has a good curative effect on opticneuritis, especially optic neuromyelitis.

Description

technical field [0001] The invention belongs to the medical field of autoimmune diseases, and in particular relates to the application of sesquiterpene lactone compounds in the preparation of medicaments for treating optic neuritis. Background technique [0002] Neuromyelitis optica (NMO) is a demyelinating disease involving the optic nerve and spinal cord. The disease was first reported in 1872 and was initially considered to be a single-course central nervous system lesion. In Asian countries, there are many reports on NMO. In my country alone, there are currently more than 300,000 NMO patients. In the neuro-ophthalmology clinic, classic NMO-associated optic neuritis (C-NMO-ON) mainly manifests as simultaneous or sequential onset in both eyes, rapid vision loss, with or without eye pain; poor recovery of visual function, usually left behind Severe visual impairment in both eyes or at least one. Recurrent NMO-associated optic neuritis (R-NMO-ON) usually occurs in one eye...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P27/02A61P25/00
CPCA61K31/365A61P27/02A61P25/00
Inventor 李洪恩李秋影龚建苗鲍世琦张雪梅孙同花
Owner ACCENDATECH LUOYANG CO LTD
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