Preparation method and application of macrocyclic spermine compound incasine B

A macrospermine and compound technology, applied in the field of natural medicinal chemistry, can solve problems such as unreported treatment of breast cancer, and achieve the effects of low cost, good industrialization prospects and little pollution

Active Publication Date: 2021-11-16
强德深圳生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Prior art There is no report that it has the effect of treating breast cancer

Method used

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  • Preparation method and application of macrocyclic spermine compound incasine B
  • Preparation method and application of macrocyclic spermine compound incasine B
  • Preparation method and application of macrocyclic spermine compound incasine B

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Compound incasine B extracted from Artemisia annua

[0035]50.5kg of dried Artemisia annua was extracted by percolating with 95% ethanol in batches, and concentrated under reduced pressure to obtain a crude extract. Suspend the crude extract with water, adjust the pH to 3 with 1% HCl, stir, stand still, extract and remove impurities with chloroform, then adjust the pH of the acidic aqueous layer after removal of impurities to 10 with 2% ammonia water, stir, and stand still Placed, extracted several times with chloroform, and concentrated the chloroform extract under reduced pressure to obtain 285.6 g of total alkali. The total alkali is suspended in 30% ethanol, and eluted with 30%, 50%, 70% and 95% ethanol in sequence through D101 macroporous resin column chromatography, and the 70% and 95% parts are detected by HPLC and combined Obtained sample 50g. Dissolve the Artemisia macroporous resin mixture in dichloromethane, mix the sample with 50g of silica gel ...

Embodiment 2

[0036] Example 2: Incasine B compounds can significantly inhibit the proliferation of breast cancer cells MDA-MB-231, BT549

[0037] 1. Breast cancer cells MDA-MB-231, BT549 were mixed with 5×10 3 One / well was inoculated in a 96-well cell culture plate, and the medium volume in each well was 200 μL, cultured for 24 hours, and then starved overnight;

[0038] 2. Add compounds with different concentration gradients (100 μM, 50 μM, 25 μM, 12.5 μM, 6.25 μM, 3.125 μM) and incubate for 24 hours, 48 ​​hours, and 72 hours, respectively;

[0039] 3. Add 20 μL of MTT working solution to each well, and continue to culture in a carbon dioxide incubator for 4 hours;

[0040] 4. Discard the supernatant in the culture plate, add 150 μL DMSO (dimethyl sulfoxide), shake for 10 minutes, select a wavelength of 490 nm on a microplate reader for detection, and draw the growth curve of the cells.

[0041] Such as figure 2 As shown, different concentrations of incasine B compounds can significan...

Embodiment 3

[0042] Embodiment 3: incasine B compound can promote the apoptosis of breast cancer cell MDA-MB-231

[0043] 1. The breast cancer cell MDA-MB-231 was mixed with 5×10 5 Individuals / well were inoculated in a 6-well cell culture plate, and the medium volume in each well was 1 mL, cultured for 24 hours, and then starved overnight;

[0044] 2. Add compounds with different concentration gradients (25 μM, 50 μM) and incubate for 48 hours;

[0045] 3. First collect the supernatant into a centrifuge tube, then carefully digest with EDTA-free trypsin to collect the cell culture medium into a centrifuge tube. Centrifuge at about 500g for 5 minutes to pellet the cells;

[0046] 4. Wash the cells twice with pre-cooled PBS, and centrifuge at about 500g for 5 minutes to collect the cells;

[0047] 5. Add 100 μL pre-cooled 1×AnnexinV Binding Buffer to resuspend the cells;

[0048] 6. Add 5 μL AnnexinV-FITC and 5 μL PI, mix gently, and react for 15 minutes at room temperature in the dark; ...

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Abstract

The invention discloses a preparation method and application of a macrocyclic spermine compound incasine B, and belongs to the technical field of natural pharmaceutical chemistry. On one hand, the invention provides application of the macrocyclic spermine compound incasine B in preparation of a medicine for resisting breast cancer diseases, and a medicinal preparation for preventing or treating breast cancer. On the other hand, the invention provides a preparation method of the macrocyclic spermine compound incasine B. The macrocyclic spermine compound separated from the traditional Chinese medicinal material incarvillea sinensis has a very good inhibition effect on breast cancer cells, and can remarkably inhibit proliferation of the breast cancer cells MDA-MB-231 and BT549. The invention can provide a material basis for the development of novel anti-breast cancer drugs, and is beneficial to the further development of the medicinal value of the traditional Chinese medicinal material incarvillea sinensis. An effective small molecular drug is provided for treating breast cancer and the like, and can be widely applied to the fields of medicine and biology.

Description

technical field [0001] The invention belongs to the technical field of natural medicine chemistry, and in particular relates to a preparation method and application of a macrocyclic spermine compound incasineB. Background technique [0002] Breast cancer refers to malignant tumors that occur in the glandular epithelial tissue of the breast. However, traditional treatment methods such as surgery, radiotherapy, and chemotherapy have poor specificity and specificity, and will inevitably have a lethal effect on normal cells and tissues, bringing great side effects to patients. Therefore, finding efficient and specific targeted drugs will greatly improve the therapeutic effect of breast cancer. [0003] Artemisia sinensis (Incarvillae sinensis), also known as Artemisia curcuma, Artemisia annua, Speranium, etc., is a plant of the genus Incarvillae in the family Bignoniaceae. The whole herb is used as medicine, and it is mainly distributed in the southwest, northwest, northeast, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/529A61P35/00A61P35/04C07D487/08
CPCA61K31/529A61P35/00A61P35/04C07D487/08
Inventor 代小勇张玉波
Owner 强德深圳生物医药科技有限公司
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