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Preparation method for physalin B and application thereof in anti-lung tumor drug

A technology of Physalis bitterin and tumor drugs, which is applied in the field of traditional Chinese medicine, can solve the problems of lack of drugs and difficulty in large-scale production, and achieve the effects of simplified preparation process, simple operation and high purity

Inactive Publication Date: 2017-08-04
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The object of the present invention aims at the deficiency that the existing technology is not easy to realize industrialized large-scale production, and provides a preparation method of Physalis B and its application in anti-lung tumor pharmacy, which solves the lack of related problems in the current treatment of lung tumor diseases. drug problem

Method used

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  • Preparation method for physalin B and application thereof in anti-lung tumor drug
  • Preparation method for physalin B and application thereof in anti-lung tumor drug
  • Preparation method for physalin B and application thereof in anti-lung tumor drug

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The preparation of embodiment 1 Physalin B:

[0021] (1) Extraction:

[0022] Take 5 kg of dried calyx of Physalis alkekengi, add it to 15 L of 60vol% ethanol and carry out hot reflux extraction twice, each time for 2 hours, combine the two extracts, then concentrate under reduced pressure to no alcohol, add 1 times the volume of ethyl acetate was extracted twice, and then the two extracts were combined, and the ethyl acetate layer was evaporated to dryness under reduced pressure to obtain 560 g of extract.

[0023] (2) Purification:

[0024] The medicinal extract that step (1) is obtained is dissolved completely with ethyl acetate, after D101 macroporous adsorption resin adsorption, successively with the water of 10 times of column volumes, 20vol% ethanol, 40vol% ethanol, 50vol% ethanol, 60vol% ethanol and 70vol% ethanol was eluted, and the 70vol% ethanol eluted fraction was collected, concentrated under reduced pressure, and evaporated to dryness to obtain 375kg of ...

Embodiment 2

[0025] The preparation of embodiment 2 Physalin B:

[0026] (1) Extraction:

[0027] Take 5kg of dried calyx of Physalis alkekengi, add it to 25L of 60vol% ethanol and carry out hot reflux extraction twice, each time reflux for 2 hours, combine the two extracts, then concentrate under reduced pressure to no alcohol, add Three times the volume of ethyl acetate was extracted twice, and then the two extracts were combined, and the ethyl acetate layer was evaporated to dryness under reduced pressure to obtain 582 g of extract.

[0028] (2) Purification:

[0029] The extract was dissolved in ethyl acetate, adsorbed with D101 macroporous adsorption resin, and then eluted with 20 times column volume of water, 20vol% ethanol, 40vol% ethanol, 50vol% ethanol, 60vol% ethanol and 70vol% ethanol, and collected 70vol% The fraction eluted with % ethanol was concentrated under reduced pressure and evaporated to dryness to obtain 381 kg of powder. Load the sample at a ratio of 3:1 (weight o...

Embodiment 3

[0030] Embodiment 3 structure identification:

[0031] The molecular weight of the compound was analyzed by ESI-TOFMS as m / z: 510.1897, and the corresponding molecular formula was C 28 h 30 o 9 , and its MS / MS spectrum shows ( figure 2 Shown) the main product ions are 493, 475, 451 and 171 etc. 13 C-NMR spectrum (100MHz, DMSO-d 6 ) gives 28 carbon signals, δ CThere are 4 carbon signals above 160, suggesting that there may be 4 carbonyl groups: δ C 202.4 is the carbonyl carbon signal (C-1) of α and β unsaturated ketones on the six-membered ring, δ C 171.8, 167.3 are ester carbonyl carbon signals (C-18, C-26), δ C 209.4 is the carbon signal of ketone. δ C 106.3 is the ketal carbon, and this signal is a characteristic signal in the carbon spectrum of physalis compounds, which is preliminarily considered to be consistent with the spectral characteristics of physalis compounds. δ C 126.7, 146.1 are △ conjugated with carbonyl 2,3 ;δ C 135.5, 123.4 is △ 5,6 ; 1 ...

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Abstract

The invention discloses a preparation method of physalicin B and its application in anti-lung tumor pharmacy, belonging to the technical field of medicine. After process optimization, the extraction and purification yield of Physalisin B is about 0.07%, and the purity of the obtained monomer is above 97%. Physalisin B can be well enriched in the lungs after intravenous administration, and it has a significant inhibitory effect on lung cancer cells, which is significantly stronger than cisplatin (positive drug), and it is concentration-dependent; The physin B cannot be effectively absorbed into the body by the body, so an effective amount of physin B and pharmaceutically acceptable adjuvant components can be prepared into a solid or liquid preparation for parenteral administration Drug pathway for the treatment of lung tumor diseases.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine, and relates to a preparation method of Physalin B (Physalin B), an antitumor active ingredient in plants of the genus Physalis, and its application in anti-lung tumor pharmacy. Background technique [0002] Cancer is currently second only to cardiovascular disease as a major disease that seriously threatens human health. As a major group of diseases, cancer includes more than 200 different tumors. Various tumors have different characteristics in the occurrence and response to treatment, and the mechanism is very complicated. Lung cancer is the most common malignant tumor in the world. With the complexity of the atmospheric environment in recent years, its incidence has been increasing year by year. Among them, non-small cell lung cancer accounts for 80% of the incidence of lung cancer (NSCLC), and has become the leading cause of cancer death. Primary cause [Clin Cancer Res.2009,15(6)...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/22A61K31/366A61P35/00
CPCC07D493/22
Inventor 郑运亮王洁曹聪朱羚
Owner ZHEJIANG UNIV
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