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Benzopyran compounds with anti-complement activity and application of benzopyran compounds

A technology of benzopyran and compounds, applied in the field of benzopyran compounds, to achieve the effect of broad market prospects

Active Publication Date: 2019-12-13
YANBIAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, the research on the anti-complement activity of Rhododendron xing'an leaves has not been reported yet, and its extraction, purification and application in health care products, food, medicine and other fields are in the exploratory stage

Method used

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  • Benzopyran compounds with anti-complement activity and application of benzopyran compounds
  • Benzopyran compounds with anti-complement activity and application of benzopyran compounds
  • Benzopyran compounds with anti-complement activity and application of benzopyran compounds

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Experimental program
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Effect test

Embodiment 1

[0030]

[0031] The monomer compounds, i.e. compound 1 and compound 2, were isolated according to the following steps:

[0032] (1) Soak 17.0kg dry rhododendron leaves with 95% ethanol, extract at room temperature 3 times, each time for 7 days, to obtain 3.8kg ethanol extract;

[0033] (2) The Rhododendron 95% ethanol extract obtained in step (1) is suspended with distilled water, and extracted 3 times with sherwood oil, ethyl acetate, and n-butanol successively to obtain 915 g of sherwood oil extract, ethyl acetate Ester extract 569.0g, n-butanol extract 597g;

[0034] (3) Take 569.0 g of the ethyl acetate extract obtained in step (2), put it in a normal phase silica gel column, and mix it with dichloromethane-methanol (25:1, 20:1, 15:1, 10:1, 5 :1) The solvent system is subjected to gradient elution, and a total of 11 components (Fr.E1-E11) are obtained;

[0035] (4) Take Fr.E1 (154.0g) and install it in a normal phase silica gel column, and perform gradient elution wit...

Embodiment 2

[0040] Example 2. Anti-complement classical pathway test in vitro

[0041] Compound 1 and Compound 2 act on the classical pathway of complement (the classical pathway) to evaluate the anti-complement activity of the compound, and the specific steps are as follows:

[0042] By adding sheep red blood cells (2.0×10 9 individual / mL) and hemolysin (Hemolysin 1:30) (Nanjing Senbega Biotechnology Co., Ltd., item number: SBJ-RXS10) in GVB-Ca 2+ / Mg 2+ (Beijing Kulaibo Technology Co., Ltd., article number: DZSL0356-500ML) to prepare sensitized red blood cells (Eshe), the cell concentration of sensitized Eshe is 1.0×10 9 individual / mL. Dissolve the test sample (compound 1 or compound 2) in DMSO, glucose (negative control) and heparin (positive control) in GVB-Ca 2+ / Mg 2+ middle. A pool of normal human serum (NHSP 1:40) was chosen for maximal lysis in the absence of complement inhibitors. Various dilutions of the test samples were pre-incubated with 150 μL of NHSP for 90 min at 3...

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Abstract

The invention discloses benzopyran compounds with anti-complement activity and application of the benzopyran compounds in preparation of anti-complement medicines. According to the invention, researchmethods in the natural medicinal chemistry and the modern pharmacology are utilized to research the anti-complement active substances of the rhododendron plant Rhododendron dauricum L. of Ericaceae,and two benzopyran compounds are separated from an ethyl acetate extract of a 95% ethanol extract. The benzopyran compounds have inhibition effect on the classical pathway of immune complement, and the CH50 value of the inhibition effect of the benzopyran compounds is 0.90-1.87 mM, and the benzopyran compounds can be used for preparing complement inhibitors.

Description

technical field [0001] The invention belongs to the pharmaceutical field of traditional Chinese medicine and natural medicine, and relates to a benzopyran compound with anti-complement effect and its application. Background technique [0002] The complement system is part of the body's innate immune system and plays an important role in homeostasis, inflammation and innate defense against foreign pathogens. Overactivation of the complement system in cells can be detrimental and is associated with a range of diseases, including inflammatory diseases, viral and bacterial infections and gastrointestinal disorders. Thus, modulation of complement activity can be beneficial in the treatment of various complement-associated diseases. Activation of the complement system mainly consists of three distinct pathways. The classical pathway (CP) is activated by the formation of immune complexes on the surface of pathogens and calreticulin expressed on apoptotic cells, which leads to the...

Claims

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Application Information

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IPC IPC(8): C07D311/58A61P37/06
CPCC07D311/58A61P37/06
Inventor 周微叶超孙金凤李镐马英杰王荣申
Owner YANBIAN UNIV
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