Triterpene saponin compound of cycro jackfruit alkyl, and effect for anti tumor

A technology of cyclopine and triterpene saponins, which is applied in the fields of antineoplastic drugs, steroids, organic chemistry, etc., to achieve the effect of inhibiting proliferation

Inactive Publication Date: 2007-05-09
肖培根 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

There is no report similar to the chemical structure of the compounds of the present invention and derivatives thereof

Method used

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  • Triterpene saponin compound of cycro jackfruit alkyl, and effect for anti tumor
  • Triterpene saponin compound of cycro jackfruit alkyl, and effect for anti tumor
  • Triterpene saponin compound of cycro jackfruit alkyl, and effect for anti tumor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Embodiment 1: the preparation of compound 1

[0045] Take 4.0Kg of the rhizome of Actaea asiatica Hara, and extract it three times with 20L of 70% ethanol under reflux, each time for three hours; after combining the three extracts, recover the solvent to obtain the extract. Dissolve the extract in 1L of water, extract with 1L of petroleum ether, 4L of ethyl acetate, and 4L of n-butanol in sequence to obtain 300 g of ethyl acetate extract. The ethyl acetate extract was subjected to low-pressure column chromatography on silica gel (200-300 mesh), and eluted with petroleum ether-acetone-methanol system gradient (1:0:0-9:1:0-8:2:0.2-7: 2.5:0.5-6:3:1-4:4:2), 5000ml each, collected and combined into 5 fractions, of which the first fraction (102g) was subjected to silica gel (200-300 mesh) low-pressure column chromatography again, Gradient elution with chloroform-methanol system (10:0-9:1-8:2-7:3-6:4-5:5), 5000ml each, collected 9 fractions in total. Among them, the seventh ...

Embodiment 2

[0047] Tablet preparation

[0048] Formula I compound 20g

[0049] Lactose 80g

[0050] Magnesium Stearate 1.0%

[0051] 3% povidone ethanol solution appropriate amount

[0052] A total of 1000 capsules were made

[0053] Take the prescription amount of compound 1 and mix the prescription amount of lactose evenly, add 3% povidone ethanol solution to make soft material, pass through 18 mesh sieve to make granules, dry at 50°C for 30-45 minutes, granulate, add magnesium stearate, mix well , Tablets. Each tablet contains 20mg of the compound.

Embodiment 3

[0055] Preparation of capsules

[0056] Formula I compound 20g

[0057] Lactose 80g

[0058] Magnesium Stearate 1.0%

[0059] 3% povidone ethanol solution appropriate amount

[0060] A total of 1000 capsules were made

[0061] Take prescription amount of compound of formula I and the prescription amount of lactose, mix evenly, add 3% povidone ethanol solution to make soft material, pass through 18 mesh sieve to make granules, dry at 50°C for 30-45 minutes, granulate, add magnesium stearate, mix Evenly, fill in No. 1 capsule. Each capsule contains 20mg of the compound.

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Abstract

This invention relates to a cycloartane triterpenoid compound and its anti-tumor applications. The compound, with a general chemical formula shown in formula I, has in vitro anti-tumor activity. The compound and its derivatives can be used to manufacture anti-tumor drugs.

Description

Technical field: [0001] The present invention relates to the extraction and separation of a new compound and its derivatives from the whole herb or rhizome of Cimicifuga foliage, the skeleton of which belongs to cyclopine-type triterpene saponins; the present invention also relates to the use of the compound in the preparation of medicines, especially In the field of preparation of antitumor drugs. Background technique: [0002] Cimicifuga (Tribe Cimicifuga) belongs to Ranunculaceae, including 5 genera of Cimicifuga genus, Cimicifuga genus, Cimicifuga genus, Cimicifuga genus, and Cimicifuga genus. Among them, Actaea asiatica Hara is a plant of the genus Actaea; it is a commonly used folk herbal medicine. Its rhizome or whole herb is used in medicine, and has the effects of expelling rash, clearing away heat and detoxifying, and promoting Yang Qi; folks are used to treat wind-heat headache, measles impervious, and Yang poisoning; anal prolapse and uterine shedding. The main...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J53/00C07J75/00A61K31/704A61K9/00A61P35/00
Inventor 肖培根杨梦苏高璟春张金超黄峰
Owner 肖培根
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