Dendropanax dentiger coumarin compound and application thereof to drug

A technology of ginseng and coumarins and compounds, applied in the field of medicine, can solve problems such as expensive and adverse drug reactions

Active Publication Date: 2020-10-23
JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The western medicines currently used to treat RA are very expensive, and most of them will have many adverse reactions

Method used

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  • Dendropanax dentiger coumarin compound and application thereof to drug
  • Dendropanax dentiger coumarin compound and application thereof to drug
  • Dendropanax dentiger coumarin compound and application thereof to drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Extraction and purification of three coumarin compounds in ginseng root

[0040] Take 10.0 kg of tree ginseng roots, heat and reflux three times with 100 kg of 70% ethanol for 3 hours each time, and concentrate the extract under reduced pressure to obtain 1.3 kg of extract. The extract was suspended in 1L of water, extracted successively with equal volumes of petroleum ether, ethyl acetate and n-butanol, and concentrated to dryness respectively. Take 216 g of n-butanol extract, mix the sample with silica gel (weight ratio 1:1), put it on a silica gel column (column size: 11*120cm), and mix it with dichloromethane-methanol (100:0→0:100, v / v) Gradient elution to obtain 9 fractions Frs. C1-C9. (1st to 9th fractions)

[0041] Dichloromethane-methanol 5:1 eluted fraction Fr.C7 (the seventh fraction 70.0 g) was subjected to octadecylsilane column chromatography (column specification: 4.2*40 cm), methanol-water (5%→30 %) gradient elution to obtain 3 fractions Fr...

Embodiment 2

[0043] Example 2: Structural identification of three coumarin compounds in ginseng

[0044]The compound of formula I, compound of formula II and compound of formula III separated in Example 1 were identified as three kinds of ginseng Soybean compounds. Wherein, the formula I structural compound is a new coumarin derivative that has not been reported in the literature, and the formula II structural compound and the formula III structural compound are known compounds (but the activity of treating rheumatoid arthritis and rheumatoid arthritis disease has not been see report).

[0045] Wherein, the compound of formula I is light yellow powder. HR-ESI-MS gives the quasi-molecular ion peak m / z 531.17083 ([M+H] + , Calculated value: 531.17066), determine its molecular formula as C 23 h 31 o 14 . The hydrogen spectrum of formula I structure compound is as figure 1 As shown, (DMSO- d 6 , 600MHZ) there are 2 methoxy hydrogen signals δ H 3.90 and 3.82 (each, 3H, s, 8 / 6-CH 3 ...

Embodiment 3

[0053] Embodiment 3: Cytotoxicity evaluation experiment of coumarin compounds in ginseng to MH7A

[0054] Cell culture: MH7A cells (Guangdong Geneo Biotechnology Co., Ltd.) were subcultured for 5-10 passages, and the culture conditions were penicillin (final concentration: 100 U / mL), streptomycin (final concentration: 100 μg / mL), 10 High-glucose DMEM medium with % FBS, when the cells are confluent to 90%, discard the old medium, wash the cells twice with 2 ml PBS, add 2 mL of 0.25% (w / v) Trypsin-0.53 after discarding the PBS Mix the digestion solution with mM EDTA and observe it under a microscope for about 30 s. When the cells become round, quickly add 2 ml of complete medium to stop the digestion, and gently pipette to collect the cells. Centrifuge at 800 rpm at 4°C for 5 min, discard the supernatant, resuspend the cells with complete medium, culture in separate bottles, and change the medium every other day.

[0055] Cell viability assay: adjust MH7A cell density to 5 × 10...

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Abstract

The present invention relates to the technical field of development of drugs for treating inflammatory diseases and in particular to an application of a dendropanax dentiger coumarin compound to the preparation of a drug for treating rheumatoid arthritis or rheumatic arthritis. The dendropanax dentiger coumarin compound has one of chemical structural formulae shown as follows. Proven by activity screening experiments, three coumarin compounds in dendropanax dentiger has an obvious effect on inhibiting nitric oxide released by MH7A cells induced by tumor necrosis factor alpha (TNF-alpha), and median inhibitory concentration (IC50) values are respectively 7.87+ / -0.7 mu M (formula I), 13.82+ / -1.1 mu M (formula II) and 39.88+ / -2.3 mu M (formula III). The application provides a new research direction for the development of a drug for clinically treating rheumatoid arthritis and rheumatic arthritis.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of coumarin compounds in tree ginseng in the preparation of medicines for treating rheumatoid arthritis or rheumatoid arthritis. Background technique [0002] Rheumatoid arthritis (RA) is a common chronic, systemic autoimmune disease that can cause joint destruction, joint deformity, and even disability. The western medicines currently used to treat RA are very expensive, and most of them have many adverse reactions. Therefore, it has broad prospects to find drugs for the treatment of RA from natural medicines, especially traditional ones. [0003] MH7A cells are a kind of human rheumatoid arthritis fibroblast-like synoviocytes, which are closely related to rheumatoid arthritis and rheumatoid arthritis. MH7A cells have the activity of releasing nitric oxide, which will aggravate inflammation. Therefore, if it is found that the natural product can inhibit the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/075C07H1/08A61K31/37A61K31/7048A61P19/02A61P29/00
CPCA61K31/37A61K31/7048A61P19/02A61P29/00C07H1/08C07H17/075
Inventor 杨丽何军伟刘荣华
Owner JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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