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Physalin A extracting process and medical application thereof

A technology of physostigmine and extraction process, applied in the field of medicine, can solve the problem that the pharmacological action mechanism of physostigmine A is rarely studied and the like

Active Publication Date: 2013-07-24
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Physalin A (Physalin A) is one of the main components in the persistent calyx of Physalis, a white crystal with a molecular weight of 526. At present, there are many studies on the pharmacological effects of Physalis, but the research on the pharmacological mechanism of Physalin A Rarely, there is only one literature report that it induces apoptosis in prostate cancer cells (Biol Pharm Bull, 2011, 34: 1584-1588), while the application and specific mechanism of Physalisin A in other tumors are unknown. No report
There is no literature report on the extraction and preparation process of Physalin A, the main medicinal component in Physalis

Method used

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  • Physalin A extracting process and medical application thereof
  • Physalin A extracting process and medical application thereof
  • Physalin A extracting process and medical application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1: Optimization of Physalis A extracting process

[0038] 1 Experimental method

[0039] Physalis bitterin A is derived from Physalis ( Physalis alkekengi L. var. franchetii (Mast.) Makino) extracted and isolated. The extraction conditions of Physalis A were optimized, and the best process combination was determined through single factor investigation (extraction method, solvent, time, concentration, liquid-solid ratio) and orthogonal design experiments.

[0040] 2 Experimental results

[0041] Selection of extraction method (extraction time is 60 min):

[0042]

[0043]

[0044] According to the extraction method and solvent selection, it is finally determined to use 70% ethanol for reflux extraction.

[0045] Single factor experiments mainly investigated the effects of extraction time, liquid-to-solid ratio, and ethanol concentration on the extraction rate.

[0046] Factors and levels determined:

[0047]

[0048] Orthogonal experiment...

Embodiment 2

[0053] Embodiment 2: the refining process of Physalis A crude extract

[0054] 1 Experimental method

[0055] According to the results obtained from the above orthogonal experiments, the optimal combination process is used for extraction, specifically: using vegetable physalis ( Physalis alkekengi L. var. franchetii (Mast.) Makino) 1 kg of commercially available finished medicinal materials was used as a raw material, and reflux extraction was carried out by 70% ethanol, the ratio of liquid to material was 60:1, reflux extraction was carried out for 40 minutes, and a total of three extractions were carried out; the obtained extract was concentrated to obtain an extract of about 160 g, dispersed into 10 times the amount of water, extracted three times with the same volume of ethyl acetate; the ethyl acetate layer extract was evaporated to dryness to obtain about 34 g of extract, and an appropriate amount of acetone was slowly added to make it just completely dissolved. After...

Embodiment 3

[0060] Example 3: The growth inhibitory effect of physalicin A on ten kinds of tumor cells in vitro

[0061] 1 Experimental method

[0062]Eight out of ten types of tumor cells (HT1080, A375-S2, HepG2, HeLa, A549, HCT116, A431, MCF7) adhered to the wall, and two types (U937, HL60) were grown in suspension with 10% fetal bovine serum, 100 U / ml Penicillin, 100 μg / ml streptomycin in RPMI-1640 culture medium, placed in 5% CO 2 , cultured in a 37°C incubator.

[0063] For adherent cells, cells in the logarithmic growth phase were prepared to make 6×10 4 1 / ml concentration of cell suspension, 100 μl per well was inoculated in a 96-well plate and cultured overnight. After the cells were fully adhered to the wall, the original culture medium was removed and different concentrations of Physicine A or DMSO were added (final concentration less than 0.1 %, negative control), 100 μl per well. Incubate at 37°C for 24 hours. After the culture, add 10 μl of 5 mg / ml MTT to each well and c...

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Abstract

The invention belongs to the technical field of medicines, in particular relates to a physalin A extracting process and medical application thereof, in particular relates to a novel application of physalin A in preparation of an anti-tumor dug and in particular relates to the use of physalin A in treatment of human fibrosarcoma and human malignant melanoma. After process optimization, the extracting rate of physalin A is 0.2133%. Physalin A can be used for inhibiting the growth of various tumor cells, particularly has obvious inhibiting action on the growth of the human fibrosarcoma and human malignant melanoma, but does not inhibit the activities of the human normal cells obviously. The mechanism is that the downstream caspase family-associated protein is activated by activating Fas death receptors, so that the tumor cells are induced to generate apoptosis. Meanwhile, the physalin A can be used for inducing the tumor cells to generate autophagy for achieving autophagy antagonism apoptosis in the HT1080 and the A375-S2 cells; and the p53 protein and the MAPK (Mitogen-Activated Protein Kinase)-familty p38 protein have a key regulation effect. The physalin A can be used for preparing a digestive tract dosage form or a non-digestive tract dosage form, which can be used for treating tumors including the human fibrosarcoma and human malignant melanoma.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to an extraction process of Physalis A and its medical use, in particular to its new use in preparing medicines for treating tumors. [0002] Background technique [0003] Malignant tumor (commonly known as cancer) is one of the important diseases that endanger human life and health. In the past 20 years, the morbidity and mortality of tumors have shown an upward trend both in the world and in China. According to WHO statistics, there were about 12.7 million new cancer patients and 7.6 million deaths in the world in 2008. In 2000, the incidence of cancer in my country was 1.8-2 million, and the death rate was 1.4-1.5 million. [0004] Fibrosarcoma (fibrosarcoma) is a malignant soft tissue sarcoma formed by fibroblasts and collagen fibers. The latest data show that fibrosarcoma accounts for only 10% of soft tissue sarcomas (Am J Surg Pathol, 2010, 34: 1504-1513). Alth...

Claims

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Application Information

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IPC IPC(8): C07D493/22A61K31/366A61P35/00A61P35/02
Inventor 邱峰何昊池岛乔陈丽霞康宁
Owner SHENYANG PHARMA UNIVERSITY
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