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A new n-benzylacridone type alkaloid and its preparation method and application

A benzylacridone type, alkaloid technology, applied in the field of medicine, can solve the problems such as no research reports on fungus, achieves the effects of facilitating pharmacological and clinical research, the preparation method is simple and feasible, and the structure is novel

Active Publication Date: 2020-09-22
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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  • A new n-benzylacridone type alkaloid and its preparation method and application
  • A new n-benzylacridone type alkaloid and its preparation method and application
  • A new n-benzylacridone type alkaloid and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 Preparation of N-benzylacridone-type alkaloids

[0029] Step (1), take the dried fungus (9 kg) and place it in 95% ethanol, immerse the medicinal material for 2-4 cm, and soak it at room temperature for 18 hours; then heat under reflux for 3 hours, stand for filtration, and concentrate the obtained filtrate to alcohol-free taste, to obtain the total thick paste of fungus and vegetables (850 grams);

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

[0031] Step (3), adjust pH=11 of the supernatant with ammonia water, extract with chloroform, ethyl acetate and n-butanol successively, and concentrate and dry each extract to obtain chloroform thick paste (36.8 g), ethyl acetate thick paste (258.5 g) g), n-butanol thick paste (364.0 g); the above-mentioned thick paste was screened for lipid-lowering activity by DiI-LDL cell ...

Embodiment 2

[0041]The hypolipidemic activity of Example 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 15 mg / mL DiI mother solution. The DiI stock 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 1.063 g / mL with sodium bromide and ultracentrifuged for 24 h. In the uppermost layer of the gradient is labeled LDL, which is separated from free DiI. The upper layer of DiI-LDL was collected, dialyzed for 24 h and then transferred to PBS buffer (3 L) for 24 h. The dialyzed DiI-LDL was filtered and sterilized with a 0.22 μm filter, and its protein content was measured before use.

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

[0046] HepG2 cells (Shanghai Jining Industrial Co., Ltd.) were seeded on a 24-well plate, cultured in DMEM ...

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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 in particular relates to a new N-benzylacridone type alkaloid, a preparation method thereof, and use in the preparation of blood lipid-lowering drugs. Background technique [0002] The fungus dish (scientific name: Gynura cusimbua), whose leaves are similar to fungus, is popular among the people as a medicinal and edible vegetable. Fungus vegetables are widely distributed in most parts of my country, with very rich resources and high nutritional value. Ancient books record that fungus has the functions of connecting tendons and bones, reducing swelling and dissipating blood stasis, and is mainly used for fractures, bruises, rheumatoid arthritis and other diseases. Modern pharmacological studies have found that fungus has various pharmacological activities such as antioxidant, antiviral, and antibacterial and anti-inflammatory. At the same time, it was found that the fungus contains a varie...

Claims

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Application Information

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Patent Type & Authority Patents(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