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Application of benzopyran alkaloid

A benzopyran alkaloid, benzopyran biological technology, applied in the field of medicine to achieve the effect of weakening the shrinkage ability

Active Publication Date: 2012-11-07
上海盛通康维药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] At present, there are some literature reports about benzopyran alkaloid benzopyran compounds, such as Japanese patents [Kawamura, N.; Tsuji, E.; Watanabe, Y.; Tsuchihashi, K.; Takako, T.Benzopyran derivatives, their manufacture with Streptomyces species, and their use for treatment of asthma and rheumatoid arthritis. Daiichi Seiyaku Co., Ltd.; Mercian Corp.: Kyoto, Japan, 7 March 2000.] and literature [Min-Juan Xu, Xiao-Jin Liu, Yi- Lei Zhao, Dong Liu, Zhen-Hao Xu, Xiao-Meng Lang, Ping Ao, Wen-Han Lin, Song-Lin Yang, Zhi-Gang Zhang and Jun Xu, Identification and Characterization of an Anti-Fibrotic Benzopyran Compound Isolated from Mangrove -Derived Streptomyces xiamenensis, Marine Drugs10:639-654, 2012.], the extraction, isolation and structural identification of benzopyran alkaloids were reported, and it was reported that they have anti-inflammatory and anti-fibrosis activities, but this has not yet been seen The report of anti-hypertrophic scar activity of similar compounds

Method used

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  • Application of benzopyran alkaloid
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  • Application of benzopyran alkaloid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1 Separation and purification of benzopyran alkaloid (compound 1)

[0022] Take the S.xiamenisis strain for plate culture (30 liters) for 7 days. After collecting and chopping the plate agar, extract it with a mixed solvent of equal volume ethyl acetate:methanol:formic acid=80:15:5 (volume ratio) 3 times, 12 hours each time. The extracts were combined and concentrated to obtain 12 grams of the total extract. Take the total extract (6 grams), dissolve it with an appropriate amount of chloroform-methanol mixed solvent, add 10 grams of 200-300 mesh silica gel G (product of Qingdao Ocean Chemical Group Co., Ltd.) On the column, chloroform-methanol [100:1, 50:1, 20:1, 10:1, 5:1, (volume ratio) to methanol] gradient elution, the polarity of the elution solvent can be increased by increasing the methanol in chloroform Gradient increase in the amount of each eluted fraction received 200 ml respectively, and the combined fractions were detected according to thin layer ...

Embodiment 2

[0027] Example 2 Benzopyran alkaloids inhibit the proliferation and viability of normal human skin fibroblasts

[0028] The materials are as follows:

[0029] Cells: normal human skin fibroblasts (NHSF cells); drug: compound 1 obtained from the above examples.

[0030] Method: NHSF cells grown to 70-80% confluence were digested with 0.25% trypsin and seeded in 96-well plate, 1×10 per well 3 cells. After 24 hours, the medium was changed and the drug was added. The final concentration of compound 1 in the drug treatment group was 30 μg / ml, and the solvent DMSO concentration was 1 / 10000. The control group was DMSO, and the final concentration was 1 / 10000. The culture medium and drugs were changed every two days. Cell viability was measured on 0d, 2d, 4d, and 6d after adding the drug. The measurement method is aspirating out the medium, adding 100 μl of complete medium and 10 μl of CCK-8 reagent to each well, and incubating in the incubator for 60 minutes to measure the light ...

Embodiment 3

[0032] Example 3 Benzopyran alkaloids block the adhesion experiment of human normal skin dermis-derived fibroblasts and human monocytes / macrophages

[0033] The materials are as follows:

[0034] Cells: normal human skin fibroblasts (NHSF cells); human monocyte / macrophage (Human acute monocytic leukemia cell line, THP-1); drug: compound 1 obtained from the above examples.

[0035] Method: NHSF cells were inoculated into 24-well plates, and 500 μl of cell suspension was inoculated in each well at a density of 1×10 5 / ml, fully confluent after 3 days of culture. Centrifuge THP-1 cells 24 hours before co-cultivation and resuspend with DMEM plus 10% FBS and 1% double antibody. Suspended to make THP-1 cell density 5×10 4 / ml. Aspirate the supernatant of NHSF cells, wash once with PBS, add 500 μl of THP-1 suspension to each well, add 318 to each well of the drug treatment group to make the final concentration 30 μg / ml, the solvent DMSO concentration is 1 / 10000, and the control gro...

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PUM

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Abstract

The invention relates to the technical field of medicines, in particular to application of a benzopyran alkaloid. The application of the benzopyran alkaloid to the preparation of medicines for restraining formation of hypertrophic scars is involved; the benzopyran alkaloid has the structural formula which is shown in specifications; and the benzopyran alkaloid can restrain proliferation and viability of normal human skin fibroblast, block the adhesion of normal human skin fibroblast (NHSF) and human mononuclear / macrophage (THP-1), and weaken contractility of the normal human skin fibroblast (NHSF).

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of a benzopyran alkaloid. Background technique [0002] At present, there are some literature reports about benzopyran alkaloid benzopyran compounds, such as Japanese patents [Kawamura, N.; Tsuji, E.; Watanabe, Y.; Tsuchihashi, K.; Takako, T.Benzopyran derivatives, their manufacture with Streptomyces species, and their use for treatment of asthma and rheumatoid arthritis. Daiichi Seiyaku Co., Ltd.; Mercian Corp.: Kyoto, Japan, 7 March 2000.] and literature [Min-Juan Xu, Xiao-Jin Liu, Yi- Lei Zhao, Dong Liu, Zhen-Hao Xu, Xiao-Meng Lang, Ping Ao, Wen-Han Lin, Song-Lin Yang, Zhi-Gang Zhang and Jun Xu, Identification and Characterization of an Anti-Fibrotic Benzopyran Compound Isolated from Mangrove -Derived Streptomyces xiamenensis, Marine Drugs10:639-654, 2012.], the extraction, isolation and structural identification of benzopyran alkaloids were reported, and it ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/353A61P17/02
Inventor 徐岷涓张志刚刘晓瑾徐俊
Owner 上海盛通康维药业有限公司
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