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Application of cortex magnolia officinal extract in preparing medicine for healing and preventing acquired immune deficiency syndrome

An extract, AIDS technology, applied in the field of medicinal chemistry

Inactive Publication Date: 2013-06-05
TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But except magnolol and honokiol, other active ingredients in magnolia bark that have inhibitory effect on HIV-1 protease have not been reported yet.

Method used

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  • Application of cortex magnolia officinal extract in preparing medicine for healing and preventing acquired immune deficiency syndrome
  • Application of cortex magnolia officinal extract in preparing medicine for healing and preventing acquired immune deficiency syndrome
  • Application of cortex magnolia officinal extract in preparing medicine for healing and preventing acquired immune deficiency syndrome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 HIV-1 protease inhibitor activity detection method

[0023] Fluorescence resonance energy transfer (FRET) technology was used to measure the activity of inhibitors against HIV-1 protease, and the substrate was designed according to the recognition site of HIV-1 protease: MCA-gama-abu-Ser-Gln-Asn- Tyr-Pro-Ile-Val-Gln-Glu-Lys-Dnp, when the inhibitor has no effect on HIV-1 protease, HIV-1 protease can cleave the substrate, and the quencher (Dnp) is away from the fluorescent group (MCA ), the fluorophore absorbs a wavelength of 320nm and excites a wavelength of 405nm, and the fluorescence intensity is detected by a detector. If the inhibitor has an effect on HIV-1 protease, the quenching group will not be cut off, and the fluorophore absorbs a wave of 320nm The latter part of the energy will be transferred to the quenching group, and the intensity of the excitation wave at 405nm will be weakened, so as to detect the inhibitory effect of the inhibitor on HIV-1 prot...

Embodiment 2

[0024] Example 2 IC 50 Value determination method

[0025]Prepare a high-concentration solution (generally 200uM) of the compound to be tested, and then perform a 1 / 2 concentration gradient dilution to form a series of concentration solutions. Generally, the activity at 12 concentrations is determined, and then the remaining activity corresponding to each compound concentration is calculated. Use the software GraphPad Prism 5 software analysis, make the curve of residual activity value and the logarithmic value of compound concentration, calculate IC 50 value.

Embodiment 3

[0026] Example 3 The method for separating and purifying HIV-1 protease inhibitors from Magnolia officinalis

[0027] 1) Extraction and extraction of Magnolia officinalis medicinal materials

[0028] Take 15 kg of Magnolia officinalis as raw material, extract with 95% ethanol at 60°C, add 5 liters of 95% ethanol to each kg of Magnolia officinalis, and extract three times, and the obtained extract is filtered through gauze and then concentrated to obtain the extract. paste, the extract was dissolved into a suspension with a small amount of water, and three times the volume of ethyl acetate was added to extract three times to obtain the ethyl acetate extract, and the n-butanol extract was obtained in the same way, and the remaining components were concentrated to dryness into the water phase.

[0029] 2) Test the inhibitory activity of ethyl acetate and n-butanol extract to HIV-1 protease

[0030] Test the inhibitory effect of ethyl acetate extract and n-butanol extract to HIV-...

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PUM

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Abstract

The invention provides application of lignin-class chemical compounds in preparing medicine for healing and preventing acquired immune deficiency syndrome, wherein the lignin-class chemical compounds are 6'-O-methyl honokiol, Randaiol, Magnolignan C and Strebluslignanol. The Strebluslignanol has good human immunodeficiency virus-1 (HIV-1) protease inhibitory activity, and the half maximal inhibitory concentration (IC50) of the Strebluslignanol reaches 35 %mM. The lignin-class chemical compounds are made from cortex magnolia officinal extract.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, in particular, the invention relates to the application of the compound, especially the application of the compound extracted from Magnolia officinalis in the treatment and prevention of AIDS. Background technique [0002] Acquired immunodeficiency syndrome (Acquired Immune Deficiency Syndrome, abbreviated as AIDS), also known as AIDS, is an infectious disease caused by the human immunodeficiency virus (HIV). HIV virus is a virus that can attack the human immune system. It targets the most important T4 lymphocytes in the human immune system, engulfs and destroys T4 lymphocytes in large quantities, thereby destroying the human immune system and eventually causing the immune system to collapse. It makes the human body fall ill due to the loss of resistance to various diseases, resulting in various infections or tumors, and finally leads to death. [0003] The harm of AIDS has swept the...

Claims

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Application Information

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IPC IPC(8): A61K31/05A61K31/065A61K31/085A61P31/18
Inventor 饶子和杨诚娄智勇郭宇周红刚陈卫强张坛杰唐延婷李金楠冯金磊
Owner TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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