Chalcomoracin, a biologically active monomer component in mulberry leaves based on ultraviolet induction, and its preparation method and use

A biologically active and mulberry leaf technology, which is applied in the field of preparation of the monomer component chalcomoracin, can solve problems such as the preparation process is not clear, and achieve the effect of reasonable technical route, reasonable economy, and anti-radiotherapy sensitization of malignant tumors

Inactive Publication Date: 2020-05-22
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to solve the technical problem in the prior art that the preparation process of UV-induced CMR is not yet clear, and to provide a preparation method based on UV-induced bioactive monomer component chalcomoracin (CMR) in mulberry leaves

Method used

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  • Chalcomoracin, a biologically active monomer component in mulberry leaves based on ultraviolet induction, and its preparation method and use
  • Chalcomoracin, a biologically active monomer component in mulberry leaves based on ultraviolet induction, and its preparation method and use
  • Chalcomoracin, a biologically active monomer component in mulberry leaves based on ultraviolet induction, and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: Preparation of Ultraviolet Induced Mulberry Leaf Extract Chalcomoracin

[0025] Freshly picked mulberry leaves were washed and irradiated with ultraviolet light (UV-B band) for 15 minutes, and the irradiated mulberry leaves were dried at 60°C. After the dried mulberry leaves are crushed, add 20 times the volume of petroleum ether, soak for 24 hours, filter, soak the filter residue with 5 times the volume of ethyl acetate for 24 hours, extract twice, filter, combine the extracts, and recover ethyl acetate ester to obtain the total extract extract. Take the total extract extract, add ethanol to dissolve, then add 200 mesh silica gel 2 times the weight of the total extract extract, evaporate the solvent to obtain a mixed sample, take 20 times the 200 mesh silica gel of the mixed sample weight, pack into the chromatographic column, keeping the diameter-to-height ratio at 1:10, performing gradient elution with a dichloromethane-methanol mixed solvent system (99:1...

Embodiment 2

[0029] Embodiment 2: the antitumor effect of UV-induced mulberry leaf extract chalcomoracin (CMR)

[0030] 2.1 In vitro antitumor effect of CMR

[0031] Human prostate cancer cells (PC-3) and breast cancer cells (MDA-MB-231) were inoculated in 96-well plates at 5000 cells / well, and the experiment was divided into control group and different concentrations of UV-induced mulberry leaf extract (CMR) 24 hours after inoculation, the administration group added 100 μL / well of serum-free medium containing different concentrations of CMR, so that the final concentration of CMR was 0, 2.5, 5, 7.5, 10 μM, and incubated for 48 hours, MTT method Check cell viability. The experiment was repeated three times, and the results are shown in Table 1 and Table 2.

[0032] Table 1 The effect of UV-induced mulberry leaf extract on the activity rate of PC-3 (mean ± standard deviation)

[0033]

[0034] Table 2 The effect of ultraviolet-induced mulberry leaf extract on the activity rate of MDA-...

Embodiment 3

[0040] Embodiment 3: The radiotherapy sensitization effect of CMR

[0041] The lung cancer PC-9 cell suspension was inoculated into 500 cells / well of 6-well culture plate, and the cells were divided into control group and irradiation group (IR group, irradiation doses were 0, 1, 2, 4, 6, 8G, respectively). , CMR group (with concentrations of 0, 2.5, 5, 7.5, 10 μM) and IR+CMR group. After irradiation and drug treatment, the culture was continued for two weeks, and the supernatant was discarded and stained with crystal violet to count the number of colonies. Calculated according to the following formula: Cell Survival Fraction (SF)=clonal formation rate of the experimental group / clonal formation rate of the control group, clone formation rate=number of clones / number of inoculated cells×100%. The average lethal dose (D0), quasi-localized dose (Dq), cell survival fraction (SF2) after 2Gy irradiation was calculated by software fitting, the cell survival curve was drawn, and the ex...

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Abstract

The invention discloses a biological activity monomer ingredient chalcomoracin inside mulberry leaves based on ultraviolet induction and a preparation method and application thereof. The preparation method comprises the following steps: (1) selecting freshly picked mulberry leaves, drying and smashing through ultraviolet induction; (2) carrying out degreasing, extraction and concentration steps onthe smashed dry mulberry leaves to obtain a total extract; and (3) carrying out silicagel column separation and Sephadex LH-20 gel column purification on the total extract to obtain a chalcomoracin pure product, and adopting an HPLC analytical method for measurement, wherein the purity of the pure product is greater than 85%. The method for preparing chalcomoracin from the mulberry leaves after ultraviolet induction provided by the invention is economical and reasonable in technical route, and the obtained product is controllable in quality; and the chalcomoracin has obvious malignant tumor resistance and radiation oncology sensibilization, is novel and unique in mechanism of action, and can be applied to preparing novel anti-tumor medicine.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a preparation method and application of chalcomoracin (CMR), a monomer component in mulberry leaves, based on ultraviolet induction. Background technique [0002] Mulberry (Morus alba L.) is a deciduous tree or shrub of the genus Moraceae, and its leaves, twigs, root bark, and fruit ears can be used as medicine. Mulberry leaves are frost-dried leaves of the Moraceae plant mulberry. Mulberry leaves are bitter, cold, and return to the lung and liver meridians. They have the effects of dispelling wind and heat, clearing the liver and improving eyesight. , hot cough, conjunctival congestion, swelling and pain, dark eyes embolism. In addition, mulberry leaves are also the main food source for silkworms because of their large leaves and thick and juicy flesh. Mulberry likes a warm and humid climate, is resistant to cold and drought, and is planted all over the country, mostly i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D307/80A61P35/00C12P17/04
CPCC07D307/80C12P17/04
Inventor 朱玮韩昊特张琳胡瑾虞娇娇杨丙贤管祺杰田景奎
Owner ZHEJIANG UNIV
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