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Dibenzofuran derivative as well as preparation method and application thereof

A compound and solvate technology, applied in the field of dibenzofuran derivatives and their preparation, can solve the problems of insufficient research and development and utilization, and achieve good anti-rheumatoid arthritis effect

Active Publication Date: 2018-04-20
FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although the Asparagus vine plant has a good curative effect, it has not been fully researched and developed.

Method used

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  • Dibenzofuran derivative as well as preparation method and application thereof
  • Dibenzofuran derivative as well as preparation method and application thereof
  • Dibenzofuran derivative as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0097] The preparation of embodiment 1 compound of the present invention

[0098] 1. Extraction

[0099] (1) Take 63 kg of rhizomes of Tengsu chinensis, crush them into coarse powder, soak them in 120 L of 90% ethanol solution, and extract them by cold soaking for 3 times, each time for 3 days. The extracts were combined and concentrated under reduced pressure to obtain 2650 g of the ethanol extract of Suteng.

[0100] (2) Disperse and mix 2650 g of the ethanol extract extract with 8 L of water, extract with petroleum ether and ethyl acetate in turn, concentrate under reduced pressure and dry in vacuo to obtain the extract of ethyl acetate (435.0 g).

[0101] 2. Separation and purification of compounds

[0102] Take 435.0 g of the extract from the ethyl acetate fraction, separate and purify it by silica gel column chromatography (100-200 mesh), mix and mix the sample, and elute with chloroform. The gradient elution procedure is shown in Table 1.

[0103] Table 1 Gradient el...

experiment example 1

[0120] Experimental Example 1 Anti-rheumatoid arthritis activity

[0121] The proliferation inhibitory activity of compounds on synoviocytes was detected by MTT assay. Synoviocytes were cultured in RPMI 1640 medium (containing 10% fetal bovine serum, penicillin and streptomycin at a concentration of 100 μg / mL, and L-glutamine at a concentration of 1 mmol / L), at 37°C and 5% CO 2 Incubate in a saturated humidity incubator until logarithmic growth phase. The synoviocytes in the logarithmic growth phase were inoculated into 96-well plates (the cell concentration was 1x105 / mL). After the cells adhered to the wall for 13 hours, 100 μL of each of the nine test samples with different concentration gradients and the positive control drug methotrexate were added, and an equal volume of the administration medium was added to the negative control group. After co-incubating for 48 h, 10 μL of MTT solution (5 mg / mL) was added to each well, and the supernatant was aspirated after continuin...

Embodiment 2

[0123] Example 2 Pharmacodynamic Research on Anti-rheumatoid Arthritis

[0124] Animals: SPF grade healthy rats, Wistar, male, six weeks old, weighing 180-200 g, purchased from Shanghai Slack Experimental Animal Co., Ltd. [certificate number: SCXK (Shanghai) 2012-0002]. The experimental animal center of Fujian University of Traditional Chinese Medicine was fed in an SPF-level laboratory with a light / dark cycle of 12 / 12h, a temperature of 25.0±0.5°C, and a relative humidity of 50%-70%.

[0125] 1. Establishment of bovine type II collagen-induced arthritis rat (CIA) model

[0126] Specific modeling method: Bovine type II collagen (2 mg / mL) and complete Freund's adjuvant (CFA) were mixed in equal volumes, and ground to make collagen emulsion. Subcutaneously inject collagen emulsion 0.2mL / rat at the base of the tail at 2cm, and inject at the base of the rat tail at 3cm on the 7th day (mixed emulsion of bovine type II collagen and incomplete Freund's adjuvant (IFA) in equal volume...

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Abstract

The invention discloses a compound of formula i as shown in the specification, or a stereisomer, a pharmaceutically acceptable salt, a solvate, a prodrug or a metabolite of the compound. In the formula, R1, R2, R3 and R4 are respectively independently hydroxyl, sulfydryl, carboxyl, amino, C1-C4 alkyl or C1-C4 alkoxy. The invention provides a completely novel compound of the formula i as shown in the specification. The compound has a relatively good anti-rheumatoid arthritis function, and a novel option is provided for clinical screening and / or preparation of anti-rheumatoid arthritis medicines.

Description

technical field [0001] The invention relates to a dibenzofuran derivative, a preparation method and application thereof. Background technique [0002] Bauhinia championi (Benth.) Benth is a woody vine of the genus Bauhinia championi (Benth.) Benth. etc., distributed in Zhejiang, Jiangxi, Fujian, Guangdong, Guangxi, Hunan, Hubei, Guizhou and other provinces and regions, its nature is flat, bitter, non-toxic, has the effect of expelling wind and dampness, promoting qi and blood circulation, and is clinically used to treat rheumatic joints It is mainly used to treat epigastric pain, rheumatic joint pain, acute and chronic lumbago and leg pain among the people. [0003] Although the Asparagus vine plant has a good curative effect, it has not been fully researched and developed. Further clarification of the components of Asparagus chinensis will lay a certain theoretical foundation for the further use of Asparagus genus plant resources in the future to develop drugs with clear ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/91A61K31/343A61P19/02
CPCC07D307/91
Inventor 徐伟张玉琴林羽褚克丹
Owner FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE
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