Biomedical use of chloranthus japonicus sied lactone D serving as indoleamine 2, 3-dioxygenase 1 inhibitor

A kind of technology of dioxygenase and silver thread grass, which is applied in the field of medicine

Inactive Publication Date: 2018-09-21
覃明疆
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[0006] So far, there are no reports that agaride A, agaride C...

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  • Biomedical use of chloranthus japonicus sied lactone D serving as indoleamine 2, 3-dioxygenase 1 inhibitor
  • Biomedical use of chloranthus japonicus sied lactone D serving as indoleamine 2, 3-dioxygenase 1 inhibitor
  • Biomedical use of chloranthus japonicus sied lactone D serving as indoleamine 2, 3-dioxygenase 1 inhibitor

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Embodiment Construction

[0028] The following describes the substantive content of the present invention in detail in conjunction with the drawings and embodiments, but does not limit the protection scope of the present invention.

[0029] Aggrestolide A, Aggrestolide C, Aggrestolide D, Aggrestolide E, Aggrestolide F and Agurolide Alcohol are self-made or purchased, purity ≥ 98, chemical Structural formula such as figure 1 shown.

[0030] Activity test method The method disclosed in the reference literature (Zhang Man et al., Synthesis and Activity Research of Novel Indoleamine 2,3-Dioxygenase 1 Inhibitor, Chinese Journal of Medicinal Chemistry, February 2018, Volume 28, Issue 1 ). Specifically:

[0031] The recombinant human IDO1 protein is expressed in Escherichia coli and purified by nickel affinity chromatography. The IDO1 inhibitory activity of the target compound was determined using L-tryptophan as a substrate. Dissolve the compound to be tested in DMSO solution with a volume fraction of 1...

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Abstract

The invention discloses biomedical use of chloranthus japonicus sied lactone D serving as an indoleamine 2, 3-dioxygenase 1 inhibitor. Chloranthus japonicus sied lactone A, chloranthus japonicus siedlactone C, chloranthus japonicus sied lactone D, chloranthus japonicus sied lactone E and chloranthus japonicus sied lactone F are discovered to be effective inhibitors of indoleamine 2, 3-dioxygenase1 (IDO1). Many investigations indicate that abnormal expression of IDO1 is related to a tumor cell fleeing immune system, and therefore, IDO1 is expected to be a new tumor treatment strategy. Currently, indoximod, epacadostat and NLG 919 are IDO1 inhibitors in the clinical phase, and multiple inhibitors are at the biological activity testing stage; the IDO1 inhibitor is promising.

Description

technical field [0001] The present invention belongs to the field of medicine, and in particular relates to the use of silverwortide A, silverwort C, silverwort D, silverwort E and silverwort F as indoleamines 2,3 - Biomedical use of dioxygenase 1 inhibitors. Background technique [0002] Silver thread grass Chloranthus japonicus Sieb. is a plant of the genus Chloranthus japonicus, which was first recorded in "Shen Nong's Materia Medica". The whole herb is used as medicine, distributed in northern China, and also found in the Far East, Korean Peninsula, and Japan. It mainly grows on hillsides at an altitude of 500-2,500m, in the shade of miscellaneous trees in valleys, or in the grass on the edge of ditch. The plant has a strong effect of promoting blood circulation and removing blood stasis, reducing swelling and relieving pain, and expelling wind and dampness. "Shaanxi Chinese Herbal Medicine" records that it "dispels dampness and cold, regulates qi and activates blood, d...

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Application Information

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IPC IPC(8): C07D493/10A61K31/365A61P35/00
CPCC07D493/10A61K31/365A61P35/00C07B2200/07
Inventor 刘新平
Owner 覃明疆
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