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Preparation method and application of cucurbitacin c and its analogs

A technology of cucurbitacin and its analogues, which is applied in the field of natural medicinal chemistry and can solve the problems of not introducing the preparation method

Active Publication Date: 2016-08-17
INST OF VEGETABLE & FLOWERS CHINESE ACAD OF AGRI SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Only in 1968, Indian researchers introduced the extraction and separation of cucurbitacin C from melon, but did not introduce its preparation method
However, the method for extracting and preparing cucurbitacin C and its analogs from cucumber fruit and cucumber leaves and its medicinal use have never been reported.

Method used

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  • Preparation method and application of cucurbitacin c and its analogs
  • Preparation method and application of cucurbitacin c and its analogs
  • Preparation method and application of cucurbitacin c and its analogs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 Extraction of Cucurbitacin C, Deacetylcucurbitacin C, Dihydrocucurbitacin C, and Dihydrodeacetylcucurbitacin C

[0037] 1. Extraction and separation

[0038] 70kg of cucumber leaves were chopped and extracted for 1 hour with 95% ethanol under reflux, and extracted 3 times in total. The solvent was concentrated under reduced pressure at 90°C to obtain 780 g of solid extract. Suspend 700 g of the solid extract in water, extract 8 times with petroleum ether, remove the petroleum ether layer, and collect the water layer. Centrifuge the water layer, collect the filtrate, and use D101 macroporous resin column for chromatographic separation. The length of the column bed is 150cm, and the inner diameter of the column is 20cm. According to the flow rate of 40ml / min, water and ethanol of different concentrations are eluted in sequence: the water elution is Site 1, 30% ethanol eluted as site 2, 80% ethanol eluted as site 3, 95% ethanol eluted as site 4, each site was e...

Embodiment 2

[0069] Example 2 Anticancer Activity Cell Experiment of Cucurbitacin C and Its Analogs

[0070] 1. Experimental cells

[0071] Human lung cancer cell line A549, human prostate cancer cell line Du145, and human colon cancer cell line HCT116.

[0072] The above cell lines were respectively cultured in RPMI1640 complete culture medium supplemented with 10% inactivated newborn calf serum. Add 100IU / mL penicillin, 100μg / mL streptomycin and 10mM HEPES to the culture medium, and place at 37°C, 5% CO 2 cultured in an incubator. The cells used in the experiment were all in the logarithmic growth phase.

[0073] 2. Experimental drugs

[0074] Four kinds of cucurbitacins prepared in Example 1: cucurbitacin C, deacetylcucurbitacin C, dihydrocucurbitacin C, and dihydrodeacetylcucurbitacin C; 201102) as a positive control drug. The drug concentration of 0.1 μM-80 μM is prepared in the culture medium.

[0075] 3. Determination of anticancer activity

[0076] Determination by MTT meth...

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Abstract

The present invention relates to the field of natural medicine chemistry, and specifically provides a preparation method and applications of cucurbitacin C in cucumber and analogs thereof, wherein the cucurbitacin C analogs are deacetylation cucurbitacin C, dihydro cucurbitacin C and dihydro deacetylation cucurbitacin C. According to the present invention, experiment results prove that the cucurbitacin C and the analogs thereof have anti-cancer cell cytotoxic activity and can be used for cancer treatment.

Description

technical field [0001] The invention relates to the field of natural medicinal chemistry, in particular to a preparation method and application of cucurbitacin C in cucumber and its analogues. Background technique [0002] Many plants contain compounds with anticancer activity, such as paclitaxel extracted from the bark of the Pacific yew (Taxus brevifolia), and hydroxyhippin extracted from the bark and fruit of the camptotheca acuminata. Phytidine is a widely used anticancer drug. Therefore, finding natural sources of anticancer drugs from plants is currently a research hotspot in cancer treatment. [0003] Cucumber (Latin name Cucumis sativus Linn, English name Cucumber), Cucurbitaceae Cucumber plant, also known as cucumber, cucumber, is a common vegetable in my country. At the same time, cucumber is also a traditional Chinese herbal medicine, and its fruits and leaves can be used as medicine. "Compendium of Materia Medica" records cucumber: main clearing heat and quenc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J9/00A61K31/575A61P35/00
CPCC07J9/00
Inventor 黄三文周渊曾建国尚轶马永硕
Owner INST OF VEGETABLE & FLOWERS CHINESE ACAD OF AGRI SCI
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