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New N-benzyl acridone alkaloid as well as preparation method and use thereof

A technology of benzylacridone type and alkaloids, which is applied in the field of medicine, can solve the problems such as no research reports on fungus, and achieve the effects of being convenient for pharmacological and clinical research, simple and easy to prepare, and novel in structure

Active Publication Date: 2018-11-13
中食安泓(广东)健康产业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the inventor consulted the literature and found that there is no relevant research report on the effect of fungus on reducing blood lipids.

Method used

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  • New N-benzyl acridone alkaloid as well as preparation method and use thereof
  • New N-benzyl acridone alkaloid as well as preparation method and use thereof
  • New N-benzyl acridone alkaloid as well as preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The preparation of embodiment 1N-benzylacridone type alkaloids

[0029] Step (1), take the dried fungus (9 kg) and put it in 95% ethanol, immerse the medicinal material for 2-4 cm, soak at room temperature for 18 hours; then heat and reflux for 3 hours, stand and filter, and concentrate the obtained filtrate to no alcohol taste, to obtain the total thick paste of fungus (850 grams);

[0030] Step (2), according to the volume ratio of 1:1.5, uniformly suspend the total thick paste of fungus in 1.3% HCl solution, let it stand for 22 hours, and filter to obtain the supernatant;

[0031] Step (3), adjust supernatant liquid pH=11 with ammoniacal liquor, extract with chloroform, ethyl acetate, n-butanol successively, each extract is concentrated and dried to obtain chloroform thick paste (36.8 grams), ethyl acetate thick paste (258.5 gram), n-butanol thick ointment (364.0 gram); Adopt DiI-LDL cell phagocytosis test to carry out lipid-lowering activity screening to above-ment...

Embodiment 2

[0041]The hypolipidemic activity of embodiment 2 compound I

[0042] experimental method

[0043] (1) Preparation of DiI-LDL

[0044] DiI (Beijing Zhongsheng Ruitai Technology Co., Ltd.) was dissolved in DMSO to prepare a DiI mother solution of 15 mg / mL. The DiI mother solution was added to the LDL / LPDS (V / V=1:2) mixture, so that the final concentration of DiI was 300 μg / mg LDL. Water bath at 37°C for 18h. The density of the mixture was adjusted to 1.063g / mL with sodium bromide, and ultracentrifuged for 24h. At the top of the gradient solution is labeled LDL, which is separated from free DiI. The upper layer of DiI-LDL was collected, dialyzed for 24 hours, then transferred to PBS buffer (3 L) and dialyzed for another 24 hours. The dialyzed DiI-LDL was filtered and sterilized with a 0.22 μm filter, and its protein content was measured before use.

[0045] (2) Mark HepG2 cells with DiI-LDL

[0046] HepG2 cells (Shanghai Ji Ning Industrial Co., Ltd.) were inoculated on a 2...

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Abstract

The invention discloses new N-benzyl acridone alkaloid separated from malabar spinach; the new N-benzyl acridone alkaloid is shown in a formula I. The N-benzyl acridone alkaloid has a remarkable bloodlipid reduction activity; therefore, the invention also discloses use of the N-benzyl acridone alkaloid in preparation of blood lipid-lowering drugs. The formula I is described in the description.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a novel N-benzylacridone alkaloid, a preparation method thereof and an application in the preparation of blood lipid-lowering medicines. Background technique [0002] Fungus (scientific name: Gynura cusimbua), whose leaves are similar to fungus, is a kind of vegetable with both medicine and food, and is very popular among the people. Fungus vegetables are widely distributed in most parts of our country, with very rich resources and high nutritional value. According to ancient books, fungus has the functions of connecting tendons and bones, reducing swelling and dissipating blood stasis, and is mainly used to treat fractures, bruises, rheumatoid arthritis and other diseases. Modern pharmacological research has found that fungus has various pharmacological activities such as anti-oxidation, anti-virus, anti-bacterial and anti-inflammatory. At the same time, it was fou...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/153A61P3/06
CPCA61P3/06C07D491/153
Inventor 魏荣锐马勤阁钟国跃杨明
Owner 中食安泓(广东)健康产业有限公司
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