Antiatherosclerotic sparstolenin B compound and preparation method thereof

A technology of black trilobide and compound, which is applied in the field of preparation of trilobide B and the compound, and can solve the problems of trilobide anti-atherosclerosis active ingredients and activities that have not been reported.

Inactive Publication Date: 2010-12-01
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Acta Pharmaceutica Sinica, 2008, 43(1), 63), but there is no report on the activity of xanthene compounds in Trigon, and there is no report on the anti-atherosclerotic active ingredient of Trigon

Method used

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  • Antiatherosclerotic sparstolenin B compound and preparation method thereof
  • Antiatherosclerotic sparstolenin B compound and preparation method thereof
  • Antiatherosclerotic sparstolenin B compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] The extraction separation method of embodiment 1 black trigonal lactone B (sparstolenin B) compound

[0025] Take 18Kg of dried tubers of Sparganium stoleniferum purchased from Zhejiang, crush them, soak them in 85% ethanol aqueous solution for 2 days, heat and reflux with 85% ethanol aqueous solution to extract three times, combine the three extracts, and concentrate under reduced pressure until there is no alcohol smell , the concentrated solution is diluted with 1 times of water to become a suspension, then extracted with sherwood oil, ethyl acetate, and n-butanol respectively, and the ethyl acetate extract is combined and concentrated to obtain 60.5 grams of extract, and the extract is subjected to a silica gel column (200~ 300 mesh) chromatography, eluted with petroleum ether: ethyl acetate gradient (100:0, 99:1, 98:2, 96:4..., 70:30), and checked by thin layer chromatography, the collection containing black triangular The fractions of lactone B (sparstolenin B) we...

Embodiment 2

[0026] Example 2 Inhibitory effect of trigolide B on arterial smooth muscle cell migration (scratch assay (Chun-ChiLiang, Ann Y Park & ​​Jun-Lin Guan.Nature Protocols, 2007, 2(2), 329))

[0027] Will 1×10 6 Rat arterial smooth muscle cells were seeded in a culture dish, cultured in DMEM medium containing 10% FBS for 24 hours, removed the medium, and then cultured in serum-free DMEM for 24 hours. Scrape a straight line across the cells with a 200 μL pipette tip to create a scratch between the cells and wash the cells twice with DMEM. Add fresh DMEM medium containing 0.5% FBS, and at the same time add different concentrations of trigonolactone B so that the final concentrations are 10, 20 and 50 μg / ml, and set up a blank control. 37°C, 5% CO 2 After continuing to culture under the conditions for 48 hours, take pictures, measure the migration distance of the cells, calculate the average migration distance and perform t test on the data with Prism software. ± 0.035, the blank c...

Embodiment 3

[0028] Example 3 Inhibition of macrophage-mediated LDL oxidation by black trigolide B

[0029] Will 1×10 6 THP-1 cells were seeded in 24-well culture dishes, added RPMI-1640 medium containing 20ng / ml TPA (12-O-tetradecanoylphorbol-13-acetate), at 37°C, 5% CO2 conditions for 72 hours. Discard the culture medium, wash twice with RPMI-1640, add 100 μg / ml human low-density lipoprotein (LDL) and 1 μM CuSO 4 500 μl of fresh culture medium was added, and different concentrations of trigolide B were added at the same time so that the final concentrations were 10, 20 and 50 μg / ml respectively. A blank control group was set up, and 6 replicate wells were set up in each group, and the culture was continued for 4 hours. The cell culture fluid was collected and centrifuged, and 100 μl of the supernatant was taken, analyzed by TBA colorimetry, the OD value was measured at a wavelength of 535 nm by a microplate reader, and the concentration of MDA (malondialdehyde) was calculated to show th...

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Abstract

The invention discloses a new xanthene compound-sparstolenin B of which the chemical structural formula is as follows. The sparstolenin B is obtained by extracting and separating the dried tuber of Sparganium stoleniferum Buch-Ham. The sparstolenin B has the functions of inhibiting migration of arterial smooth muscle cells, inhibiting macrophage-mediated low-density lipoprotein oxidation and inhibiting platelet aggregation activity, and can be used as a medicament for curing and preventing atherosclerosis diseases.

Description

technical field [0001] The invention relates to the technical field of traditional Chinese medicine, in particular to a novel compound sparstolenin B (sparstolenin B) with anti-atherosclerosis activity isolated from the traditional Chinese medicine Sanleng and a preparation method of the compound. Background technique [0002] Atherosclerosis (AS) is the pathological and pathophysiological basis of ischemic cardiovascular and cerebrovascular diseases. It is one of the most common diseases of middle-aged and elderly people with serious consequences of disability or death. Drug prevention and treatment of atherosclerosis has always been a hot spot in the medical field. The dry tuber of Sparganium stoleniferum Buch-Ham (Sparganium stoleniferum Buch-Ham), a traditional Chinese medicine, has the functions of breaking blood and promoting Qi, eliminating stagnation and relieving pain. It is commonly used clinically to treat stroke, coronary heart disease, angina pectoris, tumor, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/06A61K31/352A61P9/10
Inventor 梁侨丽吴启南樊大平段金廒高羽
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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