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Application of schisanlactone E extracted from kadsura heteroclita in preparation of drug for resisting rheumatoid arthritis

A rheumatoid and arthritis technology, applied in the field of botanical medicine, can solve the problems of strong adverse reactions, large side effects, incurable rheumatoid arthritis, etc., and achieve the effect of inhibiting vitality, improving symptoms, and using safety.

Active Publication Date: 2020-10-16
HUNAN UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Rheumatoid arthritis is currently incurable. The main purpose of current treatment is to reduce joint inflammation, inhibit the development of lesions and irreversible bone destruction, protect the function of joints and muscles as much as possible, and finally achieve the goal of complete remission or reduction of disease activity.
At present, the commonly used drugs for the treatment of rheumatoid arthritis are non-steroidal anti-inflammatory drugs such as indomethacin and antineoplastic drugs such as methotrexate, but these drugs have relatively large side effects, and long-term use will produce strong adverse effects. reaction

Method used

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  • Application of schisanlactone E extracted from kadsura heteroclita in preparation of drug for resisting rheumatoid arthritis
  • Application of schisanlactone E extracted from kadsura heteroclita in preparation of drug for resisting rheumatoid arthritis
  • Application of schisanlactone E extracted from kadsura heteroclita in preparation of drug for resisting rheumatoid arthritis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Hemocytin extraction:

[0057] Take the blood tube (Schisandra chinensis) 20kg dry cane, dry it in the shade and then pulverize it, extract it 3 times with 95% ethanol under reflux, each time for 2 hours, combine the filtrates, recover the solvent under reduced pressure to obtain 475g of alcohol extract, take 385g of blood Add 4000 mL of water to the ethanol extract to dissolve it, and then extract with petroleum ether, chloroform, ethyl acetate, and n-butanol in sequence, and obtain 145 g of the chloroform layer extract. Take 145g of the extract from the chloroform layer, mix the sample with silica gel, pack the column with silica gel wet method (80-100 mesh silica gel 3.4kg, 10×120cm chromatography column), load the sample with dry method, and elute with petroleum ether-ethyl acetate gradient (5 :1 to 0:1), resulting in 8 fractions (fractions 1-8). Among them, Fraction 4 was recrystallized to obtain 1200.0 mg of Schisanlactone (Schisanlactone E, SE).

Embodiment 2

[0059] Effect of hemocytin on the proliferation of rheumatoid arthritis fibroblast-like synoviocytes (RAFLS):

[0060] 1. RAFLS cell culture: RAFLS cells were placed in a 6cm cell culture dish using 100 U / ml of penicillin, 100 μg / ml of streptomycin as a double antibody, and 10% fetal bovine serum (FBS) high-sugar DMEM medium. at 37°C, 5% CO 2 Cultured in an incubator, after the cells adhered to the wall and grew well, they were passaged once every 2-3 days.

[0061] 2. Compare the effects of SE, methotrexate, indomethacin, and sinomenine on the viability of RAFLS cells:

[0062] Take the RAFLS cells in the logarithmic growth phase in a 6cm cell culture dish, wash them twice with 1×PBS, take 500μL of 0.25% trypsin cell digestion solution and place them in a 37°C incubator for 4min, and then wash them with 1mL of 10%FBS The DMEM medium was digested, and the cells were collected, placed in a 1.5mL EP tube, centrifuged at 900rpm for 5min, the supernatant was removed, and then 1m...

Embodiment 3

[0072] The inhibitory effect of hemocytin on the production of inflammatory factors:

[0073] 1. RAFLS cell culture: RAFLS cells were placed in a 6cm cell culture dish using 100 U / ml of penicillin, 100 μg / ml of streptomycin as a double antibody, and 10% fetal bovine serum (FBS) high-sugar DMEM medium. at 37°C, 5% CO 2 Cultured in an incubator, after the cells adhered to the wall and grew well, they were passaged once every 2-3 days.

[0074] 2. The effect of SE on the inflammatory factors produced by LPS-induced RAFLS was detected by Elisa method:

[0075] Take the RAFLS cells in the logarithmic growth phase of a 6cm cell culture dish, wash them twice with 1×PBS, take 500 μL of 0.25% trypsin cell digestion solution, place them in a 37°C incubator for 4 minutes, and then use 1mL of 10% FBS DMEM medium Stop digestion, collect cells, place in 1.5mL EP tube, centrifuge at 900rpm for 5min, remove supernatant, then add 1mL 10% FBS DMEM medium to prepare single cell suspension, and...

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Abstract

The invention relates to a botanical drug, and discloses an application of schisanlactone E extracted from kadsura heteroclita in preparation of a drug for resisting rheumatoid arthritis. The schisanlactone E extracted from the kadsura heteroclita can effectively inhibit the proliferation of rheumatoid arthritis fibroblast-like synoviocytes (RAFLS), effectively inhibit the generation of lipopolysaccharide-induced inflammatory factors TNF-alpha, IL-1[beta] and IL-6 of the RAFLS and increase the expression level of IL-10, and has a relatively good anti-inflammatory effect. The occurrence rate ofAIA-induced rat arthritis can be effectively inhibited, the swelling degree of the rat toes is reduced, and the changes of pathology and radiology images of the rat toes are improved. The invention further discloses a drug with the schisanlactone E extracted from the kadsura heteroclita as an active ingredient, and the drug can be prepared into various dosage forms such as tablets, capsules or injections and is used for inhibiting the pathological changes caused by the rheumatoid arthritis and preventing bone joints from being damaged.

Description

technical field [0001] The invention relates to herbal medicine, in particular to the application of hemocytin in the preparation of anti-rheumatoid arthritis medicine. Background technique [0002] Blood tube is a commonly used medicinal plant of the Tujia family. It is a heterogeneous plant of the genus Schisandra in the family Schisandraceae, Kadsuraheteroclita (Roxb) Craib, and its cane is often used as medicine. Blood tube nature and flavor are sweet, slightly pungent, warm. It has the effects of nourishing blood and activating blood, expelling wind and dampness, promoting qi and relieving pain. Tujia people often use it to treat rheumatic arthralgia, epigastric pain, menstrual pain, bone pain, rheumatoid arthritis, lumbar muscle strain, cold, postpartum wind paralysis and other diseases. The 2005 edition of the Chinese Pharmacopoeia included "Heterogeneous Schisandra cane", which is one of the main components of Zhonghua Dieda Pills and is used to treat bruises. [0...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/366A61P19/02A61P29/00
CPCA61K31/366A61P19/02A61P29/00
Inventor 王炜余黄合刘斌蔡雄李斌彭彩云江星明
Owner HUNAN UNIV OF CHINESE MEDICINE
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