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Compound with antitumor activity and preparation method and application thereof

An anti-tumor activity and compound technology, which is applied in the field of compounds with anti-tumor activity and their preparation, can solve the problems of no anti-tumor active compounds and no WITHANOLIDE compounds obtained by separation, and achieves strong elution ability and improved separation efficiency. Effect

Active Publication Date: 2012-06-27
ZHEJIANG UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] The literature "Studies on the chemical constituents of the persistent calyx of Physalis trichotilloides" (Zhang Hui; Research on the chemical constituents of the persistent calyx of Physalis trichophyllum; Chinese herbal medicine; 2010 No. 11) discloses the research on the chemical constituents of the dried persistent calyx of Physalis trichophyllum, including the chemical composition of the compound Extraction and separation, biological activity screening of monomeric compounds, although the chemical components were separated to obtain 4 sterol compounds and 11 flavonoid compounds, but no WITHHANOLIDE type compounds were obtained, and no highly effective anti-tumor compounds were found. Active compound with technical defects

Method used

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  • Compound with antitumor activity and preparation method and application thereof
  • Compound with antitumor activity and preparation method and application thereof
  • Compound with antitumor activity and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0055] 1) Put 1Kg of Physalis pilosus into an extraction tank, add 8 times the weight of the medicinal material in an ethanol aqueous solution containing 95% ethanol volume percentage (i.e. 8Kg of ethanol aqueous solution), and extract under reflux at 90°C. The time is 2 hours, a total of 2 extractions (a total of 16Kg in ethanol aqueous solution), and the combined extracts;

[0056] 2) Concentrate the extract obtained in step 1) (recover ethanol) to nearly dryness to obtain 12 g of thick extract, dilute with 1 L of water, extract with 1 L of dichloromethane each time, extract 3 times in total, and combine dichloromethane for extraction liquid;

[0057] 3) 5 g of the extract obtained by concentrating the dichloromethane extract obtained in step 2) is subjected to silica gel column chromatography (wet packing, dry loading), wherein the packing used in the chromatographic column is a 100-mesh column layer Analysis of silica gel, the weight ratio of extract and column chromatogr...

Embodiment 2

[0060] 1) Put 1Kg of Physalis pilosus into an extraction tank, add 8 times the weight of the medicinal material in an ethanol aqueous solution containing 95% ethanol volume percentage (i.e. 8Kg of ethanol aqueous solution), and extract under reflux at 90°C. The time is 2 hours, a total of 2 extractions (a total of 16Kg in ethanol aqueous solution), and the combined extracts;

[0061] 2) Concentrate the extract obtained in step 1) (recover ethanol) to nearly dryness to obtain 12 g of thick extract, after diluting with 1 L of water, use petroleum ether, dichloromethane and ethyl acetate in sequence according to the polarity of a single Organic solvent is extracted, and each organic solvent is used 1L each time, and each organic solvent is extracted 3 times, and petroleum ether extract, dichloromethane extract, ethyl acetate extract are respectively obtained, and are detected by thin layer chromatography (TLC). The purplish red spots of the compound with anti-tumor activity in Ph...

Embodiment 3

[0065] 1) Put 1Kg of Physalis pilosus into an extraction tank, add 95% ethanol aqueous solution (i.e. ethanol aqueous solution 10Kg) containing 10 times of the weight of the medicinal material each time, and extract under reflux at 100°C. The time is 3 hours, a total of 3 extractions (a total of 30Kg in ethanol aqueous solution), and the combined extracts;

[0066] 2) Concentrate the extract obtained in step 1) (recover ethanol) to nearly dryness to obtain 16 g of thick extract, dilute with 800 mL of water, extract with 800 mL of dichloromethane each time, extract 3 times in total, and combine dichloromethane for extraction liquid;

[0067] 3) 8 g of the extract obtained by concentrating the dichloromethane extract obtained in step 2) is subjected to silica gel column chromatography (wet column loading, dry loading), wherein the filler used in the chromatographic column is a 200-mesh column layer Analysis of silica gel, the weight ratio of extract and column chromatography si...

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Abstract

The invention discloses a compound with antitumor activity, which is a compound shown as a formula I, and can be applied to preparation of an antitumor medicament and preparation of a medicament for preventing tumors. The invention further discloses a preparation method of the compound with antitumor activity. The method comprises the following steps of: performing reflux extraction on physalis pubescens L. with an extraction solvent to obtain an extracting solution; concentrating the extracting solution, diluting with water, and extracting with an organic solvent to obtain a dichloromethane extracting solution, wherein the organic solvent at least comprises dichloromethane; and concentrating the dichloromethane extracting solution, passing through a chromatographic column, eluting with an eluting system, and recrystallizing to obtain the compound with antitumor activity. The preparation method is simple and reliable, high operability and high efficiency are achieved, industrial mass production can be performed, popularization and application are facilitated, and a good application prospect is achieved.

Description

technical field [0001] The invention belongs to the field of biochemistry and medicine, and in particular relates to a compound with antitumor activity extracted from Physicum edulis and its preparation method and application. Background technique [0002] Withanolide-type compounds are a class of ergostane-type steroidal compounds with 28 carbon atoms, and their main structure is shown in the structure of formula II, wherein the T part in the structure of formula II may be a, b, c, d , one of e, f, g, h. WITHHANOLIDE-type compounds are divided into classic and non-classical. The classic WITHHANOLIDE type compounds occupy the absolute majority in nature, and these compounds are mainly distributed in several genera of Solanaceae (Solanaceae), and several genera include Physalis. The biological activities of WITHANOLIDE compounds are mainly reflected in anti-tumor, anti-inflammatory, anti-bacterial and as insect repellent for plants. Due to the complex structure of these co...

Claims

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Application Information

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IPC IPC(8): C07J21/00A61K31/58A61K9/20A61P35/00
Inventor 马忠俊季龙袁永雷
Owner ZHEJIANG UNIV
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