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A class of ergostane steroid compound, its preparation method and use

A technology of steroidal compounds and ergosteranes, which is applied in the field of anti-AIDS drugs and can solve problems such as drug resistance

Active Publication Date: 2021-03-23
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in long-term medical practice, these drugs have begun to develop drug resistance, and their defects in toxicity, tolerance, and ease of use have gradually been exposed. It is necessary to continue to in-depth discover new anti-AIDS drugs

Method used

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  • A class of ergostane steroid compound, its preparation method and use
  • A class of ergostane steroid compound, its preparation method and use
  • A class of ergostane steroid compound, its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] The preparation of compound 1-4 in the present invention in embodiment 1

[0079] Dry the whole herb powder (5Kg) with 95% ethanol at room temperature to extract 3 times, concentrate the extract under reduced pressure to obtain 300g extract, dilute with an appropriate amount of distilled water and extract 4 times with ethyl acetate, and concentrate the ethyl acetate part under reduced pressure Obtain 120g crude extract afterward, this crude extract is through MCI column gradient elution, and eluent is that the volume ratio is successively 4:6,5:5,6:4,7:3,8:2,9:1 The mixed solution of methanol and water, collect the eluate eluted by the mixed solution of methanol and water with a volume ratio of 6:4 and 7:3 to obtain component A (40g), collect the mixed solution of methanol and water with a volume ratio of 8:2 The solution eluted eluate afforded Fraction B (30 g).

[0080] Component A (40g) is subjected to silica gel column chromatography (200-300 mesh) and the volume r...

Embodiment 2

[0088] Anti-AIDS activity test of embodiment 2 compounds of the present invention

[0089] The anti-AIDS activity of compounds 1, 2, 3 and 4 prepared in Example 1 was tested.

[0090] 3-(4,5-dimethylthiazole-2)-2,5-diphenyltetrazolium bromide was purchased from Thermo Fisher Scientific; nevirapine, human acute lymphoblastic leukemia cells MT-4 cells , HIV NL4-3 virus was purchased from the National Institutes of Health AIDS Research and Reference Reagent Program https: / / www.aidsreagent.org; phosphate buffered saline, 10% v / v polyethylene glycol octylphenyl ether acid Isopropanol solution and formazan were purchased from Bioshop, Canada.

[0091] Anti-AIDS experiment: The anti-AIDS activity and the toxicity test in MT-4 cells induced by the compound were carried out with reference to the prior art method reported in Antiviral Chem.Chemother.2015, 24, 28-38, with nevirapine (NVP, nevirapine) as a positive control. MT-4 cells were added to 96-well plates containing compounds o...

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Abstract

The invention relates to the technical field of anti-aids drugs and an ergostane-type steroid compound and a preparation method and application thereof, in particular to an ergostane-type steroid compound selected from a following compound which is shown in the description and a preparation method and application thereof in preparation of anti-aids drugs. The ergostane-type steroid compound has aremarkable anti-aids effect. At the same time, it is found in a research that there is a certain structure-function relationship between the compound and activity, and a basis is provided for furtherstructural optimization. The compound has a novel chemical structure, remarkable biological activity and a great development prospect and is expected to be developed into a new anti-aids drug withoutdrug resistance.

Description

technical field [0001] The invention belongs to the technical field of anti-AIDS drugs, and relates to a class of ergostane-type steroid compounds, a preparation method thereof and an application in preparing anti-AIDS drugs. Background technique [0002] AIDS (acquired immunodeficiency syndrome, AIDS), also known as acquired immunodeficiency syndrome, is a chronic infectious disease caused by human immunodeficiency virus (Human Immunodeficiency Virus, HIV), mainly through sexual contact, blood and mother-to-child transmission. In 1981, HIV was first discovered in the United States; then the Pasteur Institute in France isolated the virus in 1983; in 1986, the World Health Organization (WHO) officially named HIV as Human Immunodeficiency Virus (Human Immunodeficiency Virus, HIV). HIV mainly invades and destroys CD4 + T lymphocytes lead to impairment or even deficiency of the body's cellular immune function, and eventually complicated with various serious opportunistic infect...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J9/00A61K31/575A61P31/18
CPCC07J9/00
Inventor 岳建民韩迎山周彬戈樱子马克·温伯格
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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