Novel use of niclosamide and pharmaceutically acceptable salt thereof

A kind of niclosamide and pharmaceutical technology, applied in the direction of medical preparations containing active ingredients, drug combinations, antineoplastic drugs, etc., to achieve the effect of improving prognosis and improving curative effect

Inactive Publication Date: 2008-09-03
GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0012] At present, there is no literature report about the drug being used in clinical treatment of cancer

Method used

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  • Novel use of niclosamide and pharmaceutically acceptable salt thereof
  • Novel use of niclosamide and pharmaceutically acceptable salt thereof
  • Novel use of niclosamide and pharmaceutically acceptable salt thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] With different concentrations of the compound niclosamide (1×10 -8 ~1×10 -5 M) Treat A549 (lung adenocarcinoma), L-78 (lung squamous cell carcinoma), Du145 (prostate cancer), KB (oral epithelial cell carcinoma), OS-RC-2 (kidney cancer), colon cancer (HT-29 ) six kinds of cells, MTT after 72 hours, incubated for another 4 hours, and then measured their absorbance at 570nm with a microplate reader. The results showed that niclosamide treatment can significantly reduce the absorption of MTT by various cells, indicating that niclosamide can significantly inhibit the proliferation of these five types of cells, and the inhibition rate is positively correlated with the drug concentration. According to the growth inhibitory effect of niclosamide on these five kinds of cells, we calculated the half inhibitory concentration (IC50) of niclosamide to these five kinds of cells as 1×10 -8 ~1×10 -5 M. see Figure 1-Figure 5 .

Embodiment 2

[0040] With different concentrations of niclosamide (1×10 -8 ~1×10 -5 M) Du145 (prostate cancer) cells were treated, and the cells were treated with PI (propidium iodide) in 12, 24, 36, and 48 hours after the treatment, and then detected by flow cytometry, it was found that niclosamide could significantly Prolong the G1 phase of Du145 cells, and the G1 phase becomes longer with the increase of drug concentration. See Figure 6.

[0041] Table 1

[0042]

Embodiment 3

[0044] With different concentrations of niclosamide (1×10 -8 ~1×10 -5 M) Du145 (prostate cancer) cells were treated, and the cells were taken 12, 24, 36, and 48 hours after the treatment and treated with AnnexinV (Annexin V) / 7AAD (7-amino-actinomycin D), and then treated with flow Annexin V-positive cells were detected by a cytometer, and it was found that the positive rate of Du145 cells could be significantly increased by niclosamide treatment, indicating that niclosamide can induce apoptosis of Du145 cells, and the apoptotic cells increased with the concentration of niclosamide. Larger and longer processing time. Figure 7a is the expression of AnnexinV in cells after treatment with low-concentration drugs, Figure 7b It is the expression of AnnexinV in the cells after high-concentration drug treatment. See Figure 7.

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Abstract

The invention discloses an application of niclosamide or pharmaceutically-acceptable salts thereof in preparing anti-tumor drugs, which provides a candidate drug for tumor patients and may further improve the therapeutic effect and the prognosis to patients. The effectiveness of niclosamide or pharmaceutically-acceptable salts thereof on various tumor cells indicates that the composition may be used for treating various cancers such as cerebroma, genitourinary tumor, lymphatic system, stomach cancer, cancer of larynx, nasopharyngeal cancer, skin cancer, bone cancer, leukaemia, leukaemia, breast cancer, histiocytic lymphoma, non-small-cell lung cancer, small-cell lung cancer, lung adenocarcinoma, epidermoid cancer, pancreatic cancer, prostatic cancer, liver cancer and epithelial cell cancer.

Description

technical field [0001] The invention relates to a new application of the compound niclosamide or a pharmaceutically acceptable salt thereof. technical background [0002] Tumor is currently the number one killer of human health and life, and its incidence rate is second only to cardiovascular diseases. And with the impact of environmental pollution or other factors, the incidence of malignant tumors is rapidly increasing. According to the data released by the World Health Organization in 2003, there were 10 million malignant tumor patients in the world in 2000, and 6.2 million deaths due to malignant tumors, accounting for 12% to 25% of the total deaths. It is expected that by 2020, there will be 15 million new cases worldwide each year. In recent years, although some novel tyrosine protein inhibitors and other targeted new drugs have been developed and marketed, they are still far from meeting the growing needs of clinical cancer patients. The research and development of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/167A61P35/00
Inventor 丁克裴端卿段磊任小梅吕满万晓祯何嫱张章
Owner GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI
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