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Procyanidin A2, and preparation method and application thereof

A technology of proanthocyanidins and methanol, applied in pharmaceutical formulations, medical preparations containing active ingredients, digestive system, etc., can solve problems such as limited identification and utilization of active substances, and achieve sustainable development, wide application prospects, and inhibition of proliferation. Effect

Active Publication Date: 2013-12-25
SOUTH CHINA BOTANICAL GARDEN CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Litchi leaves are the branches and leaves of litchi fruit trees, which can be harvested throughout the year. They are rich in resources and have good medicinal effects, but the identification and utilization of their active substances are still very limited.

Method used

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  • Procyanidin A2, and preparation method and application thereof
  • Procyanidin A2, and preparation method and application thereof
  • Procyanidin A2, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1: Proanthocyanidin A 2 Preparative isolation and structural elucidation.

[0025] 1. Proanthocyanidin A 2 Preparation and separation

[0026] 1) Material selection: choose fresh lychee leaves;

[0027] 2) Drying and crushing: drying or drying the lychee leaves, using a pulverizer to crush them into powder, passing through a 20-mesh sieve, collecting the sieved powder, and obtaining the lychee leaf powder;

[0028] 3) Leaching: Add 5 times the volume (5mL / g litchi leaf powder) of 40% methanol aqueous solution to the lychee leaf powder, extract at 60°C for 4 hours, filter, and collect the filtrate;

[0029] 4) Organic solvent classification: Concentrate the above filtrate at 40°C to remove methanol, add 1 times its volume of water, and successively extract three times with equal volumes of petroleum ether, ethyl acetate, and n-butanol; select ethyl acetate The extract of the ester phase was concentrated to obtain an extract for subsequent purification.

...

Embodiment 2

[0040] 1) Material selection: choose fresh lychee leaves;

[0041] 2) Drying and pulverizing: drying or drying the lychee leaves, using a pulverizer to pulverize them into powder, and passing through a 120-mesh sieve to obtain the lychee leaf powder;

[0042] 3) Extraction: add lychee leaf powder to 20 times the volume (20mL / g lychee leaf powder) of 100% methanol solution, extract at room temperature (25°C) for 30 hours, filter, and collect the filtrate;

[0043] 4) Organic solvent classification: Concentrate the above-mentioned filtrate at 60°C to remove methanol, add 3 times its volume of water, successively extract 12 times with equal volumes of petroleum ether, ethyl acetate, and n-butanol; select ethyl acetate After the ester phase extract was concentrated, the extract was obtained for subsequent purification.

[0044] Subsequent purification steps are the same as in Example 1, thus obtaining and identifying proanthocyanidin A 2 .

[0045] Proanthocyanidin A obtained b...

Embodiment 3

[0047] 1) Material selection: choose fresh lychee leaves;

[0048]2) drying and crushing: dry or dry the lychee leaves, use a pulverizer to pulverize them into powder, and pass through a 60-mesh sieve to obtain the lychee leaf powder;

[0049] 3) Extraction: Add 10 times the volume of litchi leaf powder (10mL / g litchi leaf powder) to a 40% ethanol aqueous solution, extract at 40°C for 15 hours, filter, and collect the filtrate;

[0050] 4) Organic solvent classification: Concentrate the above-mentioned filtrate at 60°C to remove ethanol, add 2 times the volume of water, and successively extract 6 times with equal volumes of petroleum ether, ethyl acetate, and n-butanol; After the ester phase extract was concentrated, the extract was obtained for subsequent purification.

[0051] Subsequent purification steps are the same as in Example 1, and are obtained and identified as proanthocyanidin A 2 .

[0052] Proanthocyanidin A obtained by this method 2 The yield is 2.25 ~ 3.58g...

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Abstract

The invention discloses procyanidin A2 and a preparation method and application thereof. Procyanidin A2 has a structural formula as represented by formula (I). According to the invention, a procyanidin compound--procyanidin A2 is prepared and separated from litchi liquid, and yield of procyanidin A2 is as high as 1.26 to 5.26 g / kg (while purity is 80 to 90%); results of activity experiments show that the compound has good antioxidant activity which is substantially better than that of a synthesized anti-oxidant BHT frequently used in the food industry and the compound can be used for preparation of an anti-oxidant or free-radical scavenger; moreover, the compound has good antineoplastic activity, can effectively inhibit propagation of human liver cancer Hep-G2 cells and human cervical carcinoma Hela cells, is used for preparation of antitumor drugs and has wide application prospects. The invention is of critical significance to promotion of deep processing of litchi, increase of added values of litchi products and promotion of sustainable development of the processing industry of litchi.

Description

Technical field: [0001] The invention belongs to the field of natural products, and in particular relates to proanthocyanidin A with strong antioxidant activity and antitumor activity prepared and isolated from litchi leaves 2 And its preparation method and application. Background technique: [0002] Procyanidin is a general term for a class of flavonoids widely present in the plant kingdom, and is a polymer of flavan-3-ol or flavan-3,4-diol. In edible plants, proanthocyanidins are composed of (+)-catechin and (-)-epicatechin, mainly through B-type bonding (C4-C8 or C4-C6) and A-type bonding ( C4-C8 and C2-O-C7) are connected and polymerized, and the degree of polymerization ranges from 2 to 10. In addition, according to the degree of polymerization, two, three and tetramers are usually called oligomer proanthocyanidins. Those above pentamers are called high polymers. Relevant studies have shown that proanthocyanidins have various biological functions, such as anti-oxida...

Claims

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Application Information

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IPC IPC(8): C07D493/18A61K31/353A61P39/06A61P35/00A61P15/00A61P1/16
Inventor 杨宝蒋跃明温玲蓉
Owner SOUTH CHINA BOTANICAL GARDEN CHINESE ACADEMY OF SCI
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