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Pharmaceutical composition for treating systemic lupus erythematosus

A lupus erythematosus and drug technology, applied in directions such as drug combinations, pharmaceutical formulations, allergic diseases, etc., can solve problems such as no reports on the treatment of lupus erythematosus with no reported compounds, few reports on the activity of oligomeric proanthocyanidins, etc.

Active Publication Date: 2020-02-07
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are few reports on the activity of oligomeric proanthocyanidins, and there is no report on the treatment of lupus erythematosus with compounds CinnamtanninB-1 and CinnamtanninD-1, and there is no report that compounds CinnamtanninB-1 and CinnamtanninD-1 have aromatic hydrocarbon receptor inhibition effect

Method used

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  • Pharmaceutical composition for treating systemic lupus erythematosus
  • Pharmaceutical composition for treating systemic lupus erythematosus
  • Pharmaceutical composition for treating systemic lupus erythematosus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: Preparation of compound CinnamtanninB-1 (CAS No. 88082-60-4)

[0029] 1.0 kg of cinnamon medicinal materials were refluxed and extracted with 5L of 95 vol% ethanol aqueous solution for 2 hours each time for a total of 3 reflux extractions. The extracts were combined and concentrated under reduced pressure to obtain an extract (about 800 mL); into the extract After suspending in 1 times amount of water, it was extracted with petroleum ether (1000mL×3) and ethyl acetate (1000mL×3) successively, and the ethyl acetate extract was collected; the ethyl acetate was recovered under reduced pressure and then subjected to silica gel column chromatography. Gradient elution was performed with petroleum ether and ethyl acetate, received in sections, and combined to obtain 17 fractions; the 14th fraction was separated by reversed-phase silica gel column chromatography, eluted with methanol-water, received in sections, and combined to obtain 5 fractions; the third fraction was...

Embodiment 2

[0037] Example 2: Preparation of compound CinnamtanninD-1 (CAS No. 97233-60-2)

[0038] 10.0 kg of cinnamon medicinal materials were refluxed and extracted with 5L of 95 vol% ethanol aqueous solution for 2 hours each time for a total of 3 reflux extractions. The extracts were combined and concentrated under reduced pressure to obtain an extract (about 800 mL); into the extract After suspending in 1 times the amount of water, it was extracted with petroleum ether (1000mL×3) and ethyl acetate (1000mL×3) successively, and the ethyl acetate extract was collected; the ethyl acetate was recovered under reduced pressure and then subjected to silica gel column chromatography. Gradient elution was performed with petroleum ether and ethyl acetate, received in sections, and combined to obtain 17 fractions; the 14th fraction was separated by reversed-phase silica gel column chromatography, eluted with methanol-water, received in sections, and combined to obtain 5 fractions; the fourth fracti...

Embodiment 3

[0046] Example 3: Detecting the cytotoxicity of the compound of the present invention by MTT method

[0047] MTT experiment process:

[0048] Sample group: The compounds prepared in Examples 1 and 2 were formulated into solutions with concentrations of 12.5 μg / mL, 25 μg / mL and 50 μg / mL with DMSO solvent;

[0049] Control group: RPMI-1640 culture medium;

[0050] 6-week-old Balb / c mice were sacrificed and sterilized with 75% ethanol. The spleen was aseptically removed, and the spleen was ground with a glass slide, passed through a 200-mesh filter, centrifuged at 4°C, 1200 rpm for 5 minutes, discarded the supernatant, and added 0.6 to each spleen ml of erythrocyte lysate, mix well, let stand for 30s, wait for flocculent precipitation, add PBS to 10ml, 4℃1200rpm, centrifuge for 5 minutes, discard the supernatant, add 2ml PBS, pass 200 mesh filter membrane, add PBS to 10ml, Centrifuge at 1200rpm at 4℃ for 5 minutes, add 1640 culture medium, take 10μl cell suspension and add 190μl trypan ...

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Abstract

The invention discloses medicinal application of Cinnamtanin B-1 and Cinnamtanin D-1. The medicinal application refers to taking a Cinnamtanin B-1 and / or Cinnamtanin D-1 compound as one of active ingredients or the only one active ingredient for preparing a medicinal preparation for treating the disease of lupus erythematosus. Experiments show that A-type trimeric procyanidin compounds have a half-cell lethal concentration of less than 50mu g / mL, and can effectively inhibit the lupoid acne lesion of NZB / W mice, thus being expected to be used as one of the active ingredients or the only one active ingredient for preparing the medicinal preparation for treating the lupus erythematosus. The medicinal value of the compounds is highly anticipated.

Description

Technical field [0001] The invention relates to a pharmaceutical composition for the treatment of systemic lupus erythematosus, in particular to a pharmaceutical composition for the treatment of systemic lupus erythematosus containing compounds CinnamtanninB-1 and / or CinnamtanninD-1. Background technique [0002] Systemic lupus erythematosus (SLE) is an autoimmune disease involving multiple systems and multiple organs. The incidence of males and females ranges from 1:7 to 10. The prevalence in my country is about 70 per 100,000 , And is increasing year by year. It is known that the onset of SLE is closely related to sex hormones, but which sex hormone or its content is related to it is still a big controversy. The cause of SLE is unknown, and there is still a lack of specific therapeutic drugs. Before hormone treatment, the 5-year mortality rate of patients with lupus erythematosus was almost 100%. After treatment with hormones and immunosuppressants, the current 5-year mortalit...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/353C07D493/18A61P37/02
CPCA61K31/353C07D493/18
Inventor 李医明杨以阜贾琦张皓月陈亮施晨晨杨扬
Owner SHANGHAI UNIV OF T C M
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