Preparation method of 3(alpha)-hydroxyl-30-olive-12,20(29)-diene-28-acid and application in preparing anti-tumor drug

An anti-tumor drug and olean fruit technology is applied in the field of biomedicine to achieve the effects of rich material sources, good application development potential and good environmental benefits

Active Publication Date: 2014-03-05
SOUTH CHINA BOTANICAL GARDEN CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there are no reports of its antitumor activity

Method used

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  • Preparation method of 3(alpha)-hydroxyl-30-olive-12,20(29)-diene-28-acid and application in preparing anti-tumor drug
  • Preparation method of 3(alpha)-hydroxyl-30-olive-12,20(29)-diene-28-acid and application in preparing anti-tumor drug
  • Preparation method of 3(alpha)-hydroxyl-30-olive-12,20(29)-diene-28-acid and application in preparing anti-tumor drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: Preparation of 3α-hydroxy-30-olean-12,20(29)-diene-28-acid in Akebia clover fruit

[0025] 1.1 Plant source and identification

[0026] The fruit samples of Akebia trifolia (Thumb.) Koidz., a plant material for extraction, were collected from Hunan Province in September 2009 and identified by Xing Fuwu, a researcher at South China Botanical Garden, Chinese Academy of Sciences.

[0027] 1.2 Extraction and separation

[0028] The sample (dried fruit of Akebia trifoliata, weighing 1.0 kg) was crushed and extracted three times with 95% ethanol at room temperature, the combined filtrate was concentrated under reduced pressure to remove the organic solvent ethanol, and the crude extract of the total extract was obtained. The total extract was suspended in 500ml of water, extracted three times with an equal volume of petroleum ether, and the extract was concentrated under reduced pressure to obtain total petroleum ether extract (16g). Dissolve the petroleum ether ...

Embodiment 2

[0033] Example 2: Preparation of 3α-hydroxy-30-olean-12,20(29)-diene-28-acid in the stems and leaves of Akebia trifoliata

[0034] 2.1 Plant source and identification: same as Example 1

[0035] 2.2 Extraction and separation:

[0036] The sample (Akebia trifoliate stems and leaves, dry weight 1.0 kg) was crushed and extracted three times with 95% ethanol at room temperature, and the combined filtrate was concentrated under reduced pressure to remove the organic solvent ethanol to obtain the crude extract of the total extract. Suspend the total extract in 500ml of water, extract three times with an equal volume of petroleum ether, and concentrate the extract under reduced pressure to obtain total petroleum ether extract (13g). Dissolve the petroleum ether total extract with acetone (150mL), add normal phase silica gel (80-100 mesh) to mix the sample at a weight ratio of 1:1.5, evaporate to dryness, and dry the column (200-300 mesh, 300g) to dry Samples were loaded using petro...

Embodiment 3

[0038] Take the stems, leaves or fruits of Akebia, Akebia changxu, Akebia basilicate and Akebia trilobata as samples, and finally purify according to the extraction and separation methods described in Example 2 to obtain the pure compound 3α-hydroxyl of formula (I) -30-Olean-12,20(29)-dien-28-oic acid.

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Abstract

The invention provides a preparation method of 3(alpha)-hydroxyl-30-olive-12,20(29)-diene-28-acid and an application in preparing an anti-tumor drug. The method provided by the invention extracts and separates strong-effect and low-toxicity anti-tumor active substances from the akebia quinata plant, the sources of the plant material are abundant, and the extraction preparation method is easy to operate; the plant body is not damaged to ensure long-time use when in extraction from plant fruits, thereby increasing economic benefits and being environment-friendly; moreover, the monomer compound is stable and easy to store. The pharmacological experiment indicates that the compound 3(alpha)-hydroxyl-30-olive-12,20(29)-diene-28-acid has remarkable activity in inhibiting the growth of tumor cells, and has a development potential in preparing an anti-tumor drug, or can be used as a pilot compound for developing an anti-tumor drug with effect and low toxicity, and has good prospects in application and development.

Description

Technical field: [0001] The invention belongs to the field of biomedicine, and in particular relates to a preparation method of a nortriterpene compound 3α-hydroxy-30-olean-12,20(29)-diene-28-acid or a pharmaceutically acceptable salt thereof in the preparation of antitumor drugs in the application. Background technique: [0002] Tumor is the second health killer of human after cerebrovascular disease. With the development of economy and society, the incidence of tumors is increasing worldwide, and the number of tumors in my country is also increasing year by year. Tumor diseases are causing more and more serious losses to the health of our people and the national economy. [0003] Chemosynthetic antineoplastic drugs with cytotoxic activity occupy an important position in the treatment of tumors, but the significant side effects of existing antineoplastic drugs have always been a difficult problem in the treatment of tumors. The current clinical drug therapy for tumors has...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P35/00C07J63/00
Inventor 谭建文王晶郑梦斐周忠玉董丽梅
Owner SOUTH CHINA BOTANICAL GARDEN CHINESE ACADEMY OF SCI
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