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Application of berberine ion pair compound to preparation of anti-breast-cancer drug

A technology of compound and ion pair, which is applied in the field of medicine, can solve the problems of toxic side effects, low oral availability, high price, etc., and achieve the effects of small toxic side effects, obvious curative effect, and simple preparation

Inactive Publication Date: 2018-01-09
FUJIAN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Drug therapy is mainly limited to cytotoxic chemotherapy such as anthracycline doxorubicin and paclitaxel, and there are problems such as toxic side effects and drug resistance, and existing endocrine therapy and Herceptin-based molecular targeted therapy cannot be used
Compared with non-triple-negative breast cancer, the current research has not found that one or several chemotherapy regimens have a higher complete pathological response rate and less drug resistance in the treatment of triple-negative breast cancer
Triple-negative breast cancer has a high recurrence rate, metastasis rate, and mortality rate. At present, there is a lack of effective treatment methods. The targeted drugs for triple-negative breast cancer that are currently on the market have unsatisfactory efficacy, side effects and drug resistance, and are expensive. , patients can hardly afford it, and it is urgent to develop targeted drugs against triple-negative breast cancer with high efficiency and low toxicity (Xia Xianghou et al. International Journal of Surgery, 2014, 41 (11): 766-769)
[0008] Studies at home and abroad have shown that berberine has the effects of inhibiting proliferation, inducing apoptosis, anti-metastasis, anti-invasion and inhibiting angiogenesis on breast cancer cells, but the overall efficacy is not strong
The physical and chemical properties of berberine hydrochloride have defects, the oral availability is low, and it is difficult to exert clinical therapeutic effect

Method used

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  • Application of berberine ion pair compound to preparation of anti-breast-cancer drug
  • Application of berberine ion pair compound to preparation of anti-breast-cancer drug
  • Application of berberine ion pair compound to preparation of anti-breast-cancer drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Example 1 The in vitro inhibitory effect of braidin on triple-negative breast cancer MDA-MB-231 cells

[0045] 1.1 Cell culture MCF-7 and MDA-MB-231 cells were respectively used in DMEM and L-15 medium, containing fetal bovine serum with a volume fraction of 0.1, 100 K U·L -1 Penicillin and 100 mg·L -1 Streptomycin, set at 37°C, volume fraction 0.05 and CO 2 , Routine culture in an incubator with saturated humidity, digested and passaged with 0.25% trypsin. Cells in the exponential proliferation phase 3 days after subculture were used in the experiment;

[0046] 1.2 Method to detect the effect of huanggui on the proliferation of breast cancer cells Collect tumor cells in logarithmic growth phase, prepare single cell suspension with complete culture medium, inoculate in 96-well plate, MCF-7 cells per well 8×10 3 1.2×10 MDA-MB-231 cells per well 4 set CO 2 incubator overnight. Set up vehicle control group and different concentrations of bradycardin treatment groups...

Embodiment 2

[0052] Example 2 The effect of huanggui on the MDA-MB-231 cell cycle

[0053] 2.1 Detection of cell cycle by flow cytometry Take the cells in the logarithmic growth phase, digest with trypsin, resuspend into a single cell suspension, and inoculate in a 6-well plate (the number of cells is 5×10 5 / hole). Cells were collected after 24 h of exposure to different concentrations of huanggui, and washed twice with PBS. Fix with 75% ethanol overnight at 4°C. PI was added to each sample (final mass concentration was 10 mg L -1 ) 10 µL, RNaseA (final mass concentration is 50 mg·L -1 ) 50 µL and PBS 340 µL, mix well, incubate at 37°C in the dark for 30 min, and measure the fluorescence intensity by flow cytometry.

[0054] Results After the cells were treated with huanggui for 24 h, most of the cells were arrested in the S phase, while the cells in the G phase decreased or even lost. Huanggui 0.6, 1.2, 2.4 mg·L -1 The S phase cells in the treatment group increased from 19.97% in t...

Embodiment 3

[0055] Example 3 Effect of Huangguisu on the Apoptosis Rate of MDA-MB-231 Cells

[0056] 3.1 TUNEL method for detection of apoptosis in tumor tissue The tumor tissue specimens were embedded in paraffin, and the slice thickness was 6 μm. The TUNEL test was carried out according to the instructions of the kit. In the TUNEL-stained sections, the nuclei had yellow-brown granules or patches were apoptotic cells. Five slices were made in each group, and five high-power fields (×400) were randomly selected for each slice, and the percentage of positive cells in 1000 cells was calculated, that is, the apoptosis index.

[0057] Data processing and results The median inhibitory concentration (IC) of cells was calculated by medium-effect linear regression 50 ); for other measurement data ±S means, SPSS 13.0 statistical analysis, comparing the significance of the difference between the two groups. The result is as image 3 As shown, after the cells were treated with huanggui for 24 h...

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Abstract

The invention discloses the application of a berberine ion-pair compound in the preparation of anti-breast cancer drugs. The compound has dual mother nuclear pharmacological effects and lipophilicity. The present invention shows that triple-negative breast cancer cells are highly sensitive through in vitro tumor cell tests and in-vivo animal tests, and the compound has obvious inhibitory effects on breast cancer cells, especially triple-negative breast cancer cells. Proliferation, inducing apoptosis, and inhibiting the growth of nude mouse transplanted tumors in vivo, the potency in vitro is significantly higher than that of its lead berberine hydrochloride. It is a safe, effective, abundant drug source, low price, convenient to take, and excellent Potential drugs with promising clinical applications.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the application of a class of berberine ion-pair compounds in the preparation of anti-breast cancer. Background technique [0002] The berberine ion-pair compound is an ion-pair compound formed by combining the berberine cation and the adduct of alkanoyl acetaldehyde sodium bisulfite, commonly known as the anion of houttuydine sodium. The tentative common name of Huangguisu (referred to as HB), the molecular formula is: C 32 h 41 SNO 9 , Molecular weight: 615.73, the general structural formula is as follows: [0003] [0004] where R is C 8 -C 12 of alkyl. [0005] The compound has been disclosed by Chinese invention patent (ZL2005101366552). In addition, the anti-hepatic cancer application of this compound has been disclosed by a Chinese invention patent (ZL201010213692X). [0006] The inventors have conducted extensive research on the anticancer effect o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4375A61K31/513A61K33/24A61K31/7048A61K31/282A61K31/555A61P35/00
Inventor 林菁贾本真唐建武王希
Owner FUJIAN MEDICAL UNIV
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