HIV latency-resistant effective part of euphorbia and use thereof

An effective part, Euphorbia technology, applied in the field of medicine, can solve the problems of large toxic and side effects, unsatisfactory and other problems

Active Publication Date: 2012-10-17
SHANGHAI XINHAO BIOLOGICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this strategy has several treatment options in clinical practice, the results are still unsatisfactory. Either the activator is ineffective, or it is effective but has severe side effects.

Method used

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  • HIV latency-resistant effective part of euphorbia and use thereof
  • HIV latency-resistant effective part of euphorbia and use thereof
  • HIV latency-resistant effective part of euphorbia and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Preparation of Effective Fraction of Euphorbia for Anti-HIV Latency

[0076] Euphorbia (1kg, powder or chopped medicinal material) was extracted with 95% ethanol and refluxed (8L x 3), and the ethanol was recovered to obtain ethanol extract (0.26kg).

[0077] The ethanol extract was dissolved in 300 mL of hot water, and extracted with ethyl acetate (300 mL x 3) after cooling to obtain an ethyl acetate extract (47 g).

[0078] The ethyl acetate extract was subjected to silica gel column chromatography (2kg, column diameter: 10.0cm), eluted with petroleum ether: ethyl acetate (100:1) (20L) to remove the oily part, and then dichloromethane: methanol (1: 2) (20L) was eluted to obtain the effective fraction (43.4g).

[0079] Carry out LC-MS to the obtained effective part, the method is as follows:

[0080] Analytical chromatographic conditions:

[0081] The chromatographic column was Zorbax SB-C18column (5 μm, 250mm×4.6mm; Agilent Technologies, USA); the mobile phase was ...

Embodiment 2

[0086] Preparation of effective fraction of Kansui anti-HIV latent effect

[0087] Gansui (1kg, powdered or chopped medicinal material) was extracted with water (10L x 2) and concentrated to obtain a water extract (0.33kg).

[0088] The water extract was dissolved in 300mL hot water (90°C), cooled and subjected to macroporous adsorption resin chromatography (1L), followed by 60% ethanol-water (4L) and 90% ethanol-water (4L) to obtain 90% ethanol-water The water eluate (49g) is the active part.

[0089] Carry out LC-MS to the obtained effective part, the method is as follows:

[0090] Analytical chromatographic conditions:

[0091] The chromatographic column was Zorbax SB-C18column (5 μm, 250mm×4.6mm; Agilent Technologies, USA); the mobile phase was A phase 0.5% acetic acid water, and B phase was 0.5% acetic acid acetonitrile. The gradient is as follows: from 25% Phase B to 40% Phase B in 30min, from 40% Phase B to 50% Phase B in 30min-45min, from 50% Phase B to 70% Phase B ...

Embodiment 3

[0096] Effects of effective fractions on HIV latency-induced activation

[0097] 3.1. Method

[0098] C11 cell is a latently infected cell model of HIV, which is obtained by infecting the human T lymphocyte cell line Jurkat with HIV-1 lentivirus carrying the EGFP reporter gene, through cell sorting and HIV integration detection, and has HIV integration but no expression EGFP T lymphocyte line. C11 cells are Jurkat stable strains that are infected by the HIV lentivirus carrying the reporter gene GFP and do not express at the same time, so they are used for screening and activating HIV-1 drugs for latent infection (see application number 200810038851.X, invention title "a screening for activating latent infection HIV-1 compound T lymphocytes and its preparation method" Chinese patent application), the preservation number is CCTCC NO.C200821.

[0099] In this example, 2×10 per well 4 C11 cells were planted in a 96-well plate, and 100 μl of 1640 medium (Gibco) containing 10% FB...

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Abstract

The invention provides a HIV latency-resistant effective part of euphorbia and a use thereof. Through an ingenious activity screening method, it is found that a traditional Chinese medicine euphorbia has effects of resisting AIDS. Through solvent extraction, extraction and column chromatography processes and the combination with activity screening, the HIV latency-resistant effective part of euphorbia is determined and is prepared; and the HIV latency-resistant effective part of euphorbia can be used as an active ingredient having effects of resisting AIDS. The HIV latency-resistant effective part of euphorbia has effects of HIV latency intervention, can be combined with antiretroviral drugs thereby promoting removal of latent virus reservoirs, and provides a novel approach for thorough curing of AIDS.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to the discovery of an effective part of an active traditional Chinese medicine and its preparation method, as well as its application in anti-HIV latent treatment. Background technique [0002] Acquired Immunodeficiency Syndrome (AIDS) is an infectious disease caused by HIV infection that seriously endangers people's life and health. According to WHO statistics, there are more than 40 million AIDS patients in the world, with 5 million new patients and 3 million deaths each year. [0003] At present, the clinical treatment of AIDS is mainly Highly active antiretroviral therapy (HAART), which not only effectively controls HIV replication, but also can rebuild the immune function of AIDS patients, opening the door of hope for the treatment of AIDS . [0004] People once hoped to completely eliminate HIV in the body by virtue of HAART, so as to achieve the goal of completely curing AIDS. Howev...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/47A61P31/18A61K125/00A61K127/00A61K135/00
CPCA61K36/47A61P31/18
Inventor 朱焕章马忠俊
Owner SHANGHAI XINHAO BIOLOGICAL TECH
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