Medicinal application of A type proanthocyanidin trimer polyphenol

A procyanidin and application technology, applied in the direction of drug combination, medical preparations containing active ingredients, antipyretics, etc., can solve the problem of less polyphenols in oligomeric procyanidins and no A-type trimeric procyanidins Issues such as the report on the immunosuppressive effect of polyphenols, to achieve the effect of inhibiting arthritis

Active Publication Date: 2015-01-14
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 procyanidin polyphenols, and there are few reports on the differences in the effects between type A and type B
At the same time, there is no report on the immunosuppressive effect of A-type trimeric procyanidin polyphenols

Method used

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  • Medicinal application of A type proanthocyanidin trimer polyphenol
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  • Medicinal application of A type proanthocyanidin trimer polyphenol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1: Preparation of Compound Cinnamtannin B-1 (CAS No.: 88082-60-4)

[0017] 1.0 kg of Chaigui medicinal material was reflux extracted with 5L of 95vol% ethanol aqueous solution, refluxed for 2 hours each time, refluxed and extracted 3 times in total, the extracts were combined, concentrated under reduced pressure to obtain an extract (about 800 mL); After adding 1 times the amount of water to suspend, sequentially extract with petroleum ether (1000mL×3) and ethyl acetate (1000mL×3), collect the ethyl acetate extract; recover ethyl acetate under reduced pressure and perform silica gel column chromatography, Gradient elution was carried out with petroleum ether and ethyl acetate in sequence, received in sections, and combined to obtain 17 fractions; each fraction was separated by silica gel column chromatography and reverse phase silica gel column chromatography, and finally purified by Sephadex LH-20 , the compound Cinnamtannin B-1 was obtained as a white powder. ...

Embodiment 2

[0025] Example 2: Preparation of Compound Cinnamtannin D-1 (CAS No.97233-60-2)

[0026] Use 5L of 95vol% ethanol aqueous solution to reflux extract 10.0kg of Chaigui medicinal material, reflux for 2 hours each time, reflux extract for 3 times in total, combine the extracts, concentrate under reduced pressure to obtain extract (about 800mL); After adding 1 times the amount of water to suspend, sequentially extract with petroleum ether (1000mL×3) and ethyl acetate (1000mL×3), collect the ethyl acetate extract; recover ethyl acetate under reduced pressure and perform silica gel column chromatography, Gradient elution was carried out with petroleum ether and ethyl acetate in sequence, received in sections, and combined to obtain 17 fractions; each fraction was separated by silica gel column chromatography and reverse phase silica gel column chromatography, and finally purified by Sephadex LH-20 , the compound Cinnamtannin D-1 was obtained as a white powder.

[0027] After analysi...

Embodiment 3

[0035] Detect the cytotoxicity of compound of the present invention with MTT method:

[0036] Sample group: DMSO solvent was used to prepare the compounds prepared in Examples 1 and 2 into solutions with concentrations of 12.5 μg / mL, 25 μg / mL and 50 μg / mL, respectively;

[0037] Control group: RPMI-1640 culture medium;

[0038] BALB / c mouse spleen lymphocytes (4 × 10 5 pc / well) were co-cultured with the samples of each experimental group for 48 h, and MTT solution (5 mg / mL) was added 4 h before the end of the culture. After the culture, 150 μL of the culture supernatant was aspirated, and 150 μL of DMSO was added to dissolve the formazan particles, shaken at a low speed for 10 min, and the OD value was read at 570 nm with a microplate reader.

[0039] The cell viability value (OD value) of each experimental group was detected, and the detailed detection results are shown in Table 1.

[0040] Table 1 The measured cell OD value of each experimental group after 48h of action ...

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Abstract

The invention discloses medicinal application of A type proanthocyanidin trimer polyphenol. The medicinal application is that the A type proanthocyanidin trimer polyphenol is taken as one of active compositions or the only one active composition to prepare medicine preparations for treating immunologic diseases. Experiments show that the half cell lethal concentration of the A type proanthocyanidin trimer polyphenol is larger than 50 mu g/mL, and the A type proanthocyanidin trimer polyphenol has inhibiting effect on propagation of lymphocyte induced by mitogen ConA and secretion of cytokines IL-6 and IFN-gamma important for immunoloregulation and inflammation reactions, is expected to be taken as one of active compositions or the only one active composition for preparing medicine preparations for treating immunologic diseases, especially is expected to be taken as one of active compositions or the only one active composition for preparing medicine preparations for treating rheumatoid arthritis, and has medicinal value.

Description

technical field [0001] The invention relates to a medicinal use of A-type trimeric procyanidin polyphenols, belonging to the technical field of medicines. Background technique [0002] Rheumatoid arthritis (RA) is one of the most important diseases that endanger human health at present, and is called "the cancer that never dies". RA is a chronic systemic autoimmune inflammatory disease characterized by multi-joint involvement, synovial inflammation, and bone and cartilage destruction. Its pathogenesis has not yet been fully elucidated. disorders are closely related. The prevalence of RA in my country is about 0.3%-0.4%, and there are about 4 million patients. The disability rate is 60% within 5-10 years of the disease course, and 90% of patients in the late stage lose their social labor force and self-care ability, which is the main reason for the loss of adult labor force. One, thus causing many family problems as well as a huge social burden. The current treatment method...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/35A61P37/02A61P19/02A61P29/00
CPCA61K31/353
Inventor 李医明杨以阜贾琦陈亮杨扬
Owner SHANGHAI UNIV OF T C M
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