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A kind of antitumor compound, its extraction method and its application

A technology for anti-tumor drugs and compounds, which is applied in the field of compounds to achieve the effect of good research and development prospects

Active Publication Date: 2018-11-23
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] But so far, there are very few reports on the active ingredients of Physalis edulis at home and abroad. The active ingredients were studied

Method used

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  • A kind of antitumor compound, its extraction method and its application
  • A kind of antitumor compound, its extraction method and its application
  • A kind of antitumor compound, its extraction method and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Extraction and isolation of active compounds from physalis stems and leaves

[0028] Solanaceae Physalis Physalis Physalis pubescens L., an annual herbaceous plant, Physalis pubescens L. dried stems and leaves (9.3kg), extracted twice with 75% ethanol water reflux, 2 hours each time, combined the extracts, recovered the solvent under reduced pressure, and obtained after concentration The total extract (1170.0g). The total extract was dispersed into 4 times the amount of water, extracted three times with equal volumes of petroleum ether, ethyl acetate, and n-butanol, and the solvent was recovered under reduced pressure to obtain 15.0 g of petroleum ether layer extract and 99.0 g of ethyl acetate layer extract. And 200.0g of n-butanol layer extract, 850.0g of remaining water layer.

[0029] The ethyl acetate layer extract was subjected to silica gel column chromatography and dichloromethane-methanol (100:1 to 0:100) gradient elution to obtain 9 sub-fractions (Fr.1 ...

Embodiment 2

[0031] Example 2: Extraction and separation of active compounds from berries

[0032] The fruit (17.5kg) of Physalis pubescens L., an annual herbaceous plant of Solanaceae Physalis, was extracted twice with 75% ethanol water reflux for 2 hours each time. The extracts were combined, the solvent was recovered under reduced pressure, and the total was obtained after concentration. Extract (1420.0g). The total extract was dispersed in 4 times the amount of water, extracted three times with equal volumes of petroleum ether, ethyl acetate, and n-butanol, and the solvent was recovered under reduced pressure to obtain 49.0 g of petroleum ether layer extract and 46.0 g of ethyl acetate layer extract. And 70.0g n-butanol layer extract, the remaining water layer is 1246.0g.

[0033] The ethyl acetate layer extract was subjected to silica gel column chromatography and dichloromethane-methanol (100:1 to 0:100) gradient elution to obtain 10 sub-fractions (E1 to E10). Subfraction E3 was chromat...

Embodiment 3

[0056] Example 3: Detection of compound anti-tumor activity

[0057] The MTT method was used to detect the activity of the compounds disclosed in the present invention, using human prostate cancer cells (C4-2B and 22Rvl), human kidney cancer cells (786-0, A-498, Caki-2, ACHN), and human melanoma Take cells (A375 and A375-S2) as an example.

[0058] Take 100μL of the above cells in the logarithmic growth phase, 2×10 per well 4 Inoculate in 96-well plate, set CO 2 Incubator (37℃, 5% CO 2 , Saturated humidity) culture. After 12 hours, add 10μL / well, and dilute the working solution of the sample with the culture medium to the final concentration of 10, 5, 2.5, 1.25, 0.625, 0.3125, 0.15625μM, respectively. There are 3 multiple wells for the sample group and the blank group. After culturing for 72 hours, add MTT working solution, 20μL / well, 3 hours later, discard the medium, add DMSO 150μL / well, shake at 500rpm on a plate shaker for 3 minutes, measure the OD value of each well with a mi...

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Abstract

The embodiments of the invention disclose an antitumor compound, an extraction method therefor and an application of the antitumor compound. The compound has a structure represented by a general formula (I) shown in the description or a general formula (II) shown in the description and an optical isomer of the general formula (I) or general formula (II). The compound disclosed by the invention and compositions thereof can be used for effectively inhibiting the growth of hormone-independent prostatic carcinoma cells, heterogeneous renal carcinoma cells and human malignant melanoma cells, so that the compound disclosed by the invention and the compositions thereof can serve as drugs for treating tumors and have a good research and development prospect.

Description

Technical field [0001] The present invention relates to a compound, in particular to a natural compound extracted from physalis, a method for extracting the compound, a pharmaceutical composition containing the compound, and the use of the compound and the pharmaceutical composition in the preparation of antineoplastic drugs. Background technique [0002] Physalis pubescens L. is an annual herbaceous plant belonging to the physalis of the Solanaceae family. It is recorded in "Chinese Medicinal Materials" edited by Xu Guojun that the calyx fruits of Physalis pubescens are used as lantern herbs. Physalis physalis has a sour and sour taste, enters the lung meridian, has the effects of clearing heat and detoxification, clearing the throat, diuresis and hemostasis. The folk used to treat acute pharyngitis is effective. (Xu Guojun. Chinese Medicinal Materials Science. Volume 2 [M]. Beijing: China Medical Science and Technology Press. 1996: 1161-1162.) Its traditional efficacy is in li...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J17/00C07J21/00A61K31/7048A61K31/58A61K31/585A61K31/7004A61K31/7028A61P35/00
CPCC07J17/005C07J21/00
Inventor 邱峰陈丽霞夏桂阳康宁丁丽琴
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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