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Withanolide compound and application thereof

A kind of ester compound and compound technology, applied in the field of medicine

Active Publication Date: 2020-09-29
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The withanide components were extracted and separated from Physalis Physalis, and the application and specific mechanism of action of these components in the preparation of antitumor drugs have not been reported.

Method used

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  • Withanolide compound and application thereof
  • Withanolide compound and application thereof
  • Withanolide compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Extraction, separation and structure identification of withanide compounds:

[0031] The aerial part (9.0 kg) of P. minima L. was heated and refluxed twice with 75% ethanol aqueous solution with a volume concentration of 10 mass times, each time for 2 hours. The extracts were combined and concentrated to obtain 840 g of crude extract. The crude extract was dispersed in 5 L of water, extracted three times with equal volumes of petroleum ether and ethyl acetate, and the solvent was recovered to obtain the ethyl acetate extract (200.0 g).

[0032] The ethyl acetate extract was separated by silica gel column chromatography, and dichloromethane with a volume ratio of 100:1, 50:1, 30:1, 20:1, 15:1, 10:1, 8:1 and 5:1 - Gradient elution with methanol as the eluent to obtain 8 fractions (E1-E8).

[0033] Fraction E3 was separated by silica gel column chromatography and eluted with dichloromethane-methanol gradient with volume ratios of 100:1, 30:1, 15:1 and 10:1 to obtain 4 fra...

Embodiment 2

[0071] Example 2: Detection of antitumor activity of withanolide compounds

[0072] Using the MTT method, human melanoma cells A375 (ATCC) in the logarithmic growth phase were taken, 3×10 per well 3 seeded in a 96-well plate and placed in CO 2 Incubator (37°C, 5% CO 2, saturated humidity) for cultivation. After 24 hours, DMEM medium (Gibco) containing different drug concentrations was added, 10 μL / well, the final concentrations were 10, 5, 2.5, 1.25, 0.625, 0.3125, 0.15625 μM, and 3 samples were set for the sample addition group and the blank control group. Duplicate wells, and set a blank control group and a positive control group (5-fluorouracil). After continuing to cultivate for 48 hours, add MTT working solution (5 mg / mL), 20 μL / well, after 2.5 hours, discard the medium, add DMSO 150 μL / well, shake on a plate shaker at 500 rpm for 5 minutes, and measure each The OD value of hole, measuring wavelength is 490nm, calculates cell proliferation inhibition rate: cell prolif...

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Abstract

The invention discloses a withanolide compound and application thereof. The withanolides compound is characterized in that the withanolides compound has a structure as shown in a formula (I) or an optical isomer thereof, activity evaluation is carried out by using an in-vitro activity screening evaluation system, the compound disclosed by the invention is found to be capable of effectively inhibiting the growth of human malignant melanoma cells, and the withanolides compound disclosed by the invention is prompted to be capable of being used as a medicine for treating tumor diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to withanolide compounds and their extraction methods and uses, and also includes the pharmaceutical composition thereof, that is, the use of the withanolide compound composition in the preparation of antitumor drugs. Background technique [0002] Physalis minima L. is an annual herbaceous plant of Physalis minima L. in Solanaceae. It is mainly distributed in Yunnan, Guangdong, Guangxi and Sichuan in my country. "Chinese Materia Medica" records that it has the effects of clearing heat and promoting dampness, eliminating phlegm and relieving cough, softening hard masses and resolving stagnation. According to literature reports, the main component of Physalis is withanide compound, which is a type of ergosterane compound with a skeleton of 28 carbon atoms, and its C-22 and C-26 form a side chain of a δ lactone ring . Modern pharmacological experiments show that these co...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00C07J17/00A61K31/585A61P35/00
CPCC07J71/001C07J17/00A61P35/00
Inventor 邱峰陈丽霞张萌康宁丁丽琴
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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