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Iridoid glycoside compound and preparation method and application thereof

A technology of iridoid glycosides and compounds, applied in the field of medicine, can solve the problems of inconvenient storage and use, high price, etc., and achieve the effects of excellent anti-inflammatory effect, easy preparation, and easy control of process parameters

Active Publication Date: 2021-02-02
JIANGSU KANION PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as an antibody drug, tocilizumab has disadvantages such as high price, inconvenient storage and use, etc.

Method used

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  • Iridoid glycoside compound and preparation method and application thereof
  • Iridoid glycoside compound and preparation method and application thereof
  • Iridoid glycoside compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065]Example 1 Preparation and structure identification of iridoid glycosides

[0066]1. Instrument:

[0067]Nuclear magnetic resonance experiment: Swiss Bruker Avance 2600 fully digital superconducting nuclear magnetic resonance instrument; UV spectrum: JASCOV-550 ultraviolet-visible spectrometer; Infrared spectrum: JASCO FT / IR-480 plus infrared spectrometer, KBr tablet; ESI- MS: FINIGAN LCQ Advantage MAX mass spectrometer; HR-ESI-MS and UPLC-Q-TOF-MS: Waters Synapt G2 Q-TOF-MS; analytical high performance liquid chromatography (Waters): Waters e2695+DAD 2998; preparative High performance liquid chromatograph (Waters): Waters 1515+2489 UV / Visible; Column: C18 column (Phenomenex Gemini, 5μm, 4.6×250mm); C18column (Phenomenex Gemini, 5μm, 10×250mm); C18column (Waters, Aquity , BEH, 1.7μm, 3.0×150mm); Multifunctional microplate reader: Synergy HT (Bio-Tek Instruments Inc., Burleigh, USA); Thermo Scientific BB15 CO2 cell incubator, American Thermoelectric; Nikon TS100 inverted microscope; U...

Embodiment 2

[0084]Example 2 Test method for inhibitory activity of inflammatory factor IL-6:

[0085]1. Experimental process:

[0086]Compounds I-IV were prepared with DMSO to prepare a mother solution (100mM) of the required concentration, and 1.2 μL was added to 1199 μL of serum-free DMEM. After mixing, 495 μL was added to each well in a 24-well plate.

[0087]The Raw264.7 cells were digested with 0.25% trypsin (containing 0.02% EDTA), and the cell density was adjusted to 1×10 in DMEM medium containing 10% FBS.5Pieces / ml, evenly inoculated to a 24-well plate, 400μl per well. After planting the plate, put it in the incubator for 24 hours. After culturing for 24 hours, remove the 24-well plate, aspirate the supernatant, and add the drug-containing medium prepared by serum-free DMEM medium: ①Solvent control group: add 495μl of serum-free DMEM containing 1 / 1000 DMSO to each well ②Model group: Add 495μl of serum-free DMEM medium containing 1 / 1000 of DMSO to each well; ③Dosing sample group: Add 495μl of med...

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PUM

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Abstract

The invention provides an iridoid glycoside compound or pharmaceutically acceptable salt, a solvate, tautomer, a stereoisomer, prodrug molecules and a metabolite thereof. A cell experiment verifies that the nitrogen-containing iridoid glycoside compound prepared by the invention shows an excellent anti-inflammatory effect, and can be used as a lead compound for developing novel anti-inflammatory drugs.

Description

Technical field[0001]The present invention relates to the technical field of medicine, in particular to an iridoid glycoside compound and a preparation method and application thereof.Background technique[0002]Inflammation is a very common and important basic pathological process, and most of the common diseases and frequently-occurring diseases of various organs are inflammatory diseases, such as furuncle, carbuncle, pneumonia, hepatitis, nephritis, etc.[0003]IL-6 (Interleukin-6) is a kind of inflammatory mediator, mainly produced by monocytes, macrophages, Th2 cells, vascular endothelial cells and fibroblasts. It stimulates the proliferation of B cells and secretes antibodies to stimulate T cell proliferation and CTL Activation and stimulation of hepatocytes to synthesize acute-phase proteins and other parametric pathways are involved in inflammation.[0004]IL-6 inhibitors (IL-6i) inhibit the immune inflammatory cascade by targeting IL-6 and play a therapeutic role in chronic inflam...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H1/08C07H17/04A61K31/7048A61P29/00
CPCC07H1/08C07H17/04A61P29/00
Inventor 肖伟李海波梅玉丹于洋邓奕刘文君王振中杨彪曹亮胡晗绯
Owner JIANGSU KANION PHARMA CO LTD
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