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Compounds, compositions and use for anticancer therapy

A compound and drug technology, applied in the field of tumor and chemotherapy, can solve the problems of electron transfer process without tPMET and coupling of oxidative phosphorylation

Inactive Publication Date: 2012-05-02
天津药和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

However, most research efforts on tPMET have focused on the development of tumor-specific nitrogen oxide (tNOX) inhibitors, without directly targeting the tPMET electron transfer process and the coupling of oxidative phosphorylation.

Method used

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  • Compounds, compositions and use for anticancer therapy
  • Compounds, compositions and use for anticancer therapy
  • Compounds, compositions and use for anticancer therapy

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0165] Example 1 mPMS dose-response relationship

[0166] Methods: A and B: HT1080 (Fig. 2A) and UM-SCC6 (Fig. 2B) cells were given different concentrations of mPMS shown in the figure, combined with 1 mMWST-1c and 10, 30 or 100 M apigenin for 4 hours, and then, changed to Normal growth medium for 24 hours. CCK8 kit was used to measure cell viability. Parallel controls were 0.12 mM mPMS, or 10% WST-1c. AP0: no apigenin control, AP10: 10M apigenin, AP30: 30M apigenin, AP100: 10M apigenin. Results: The data showed that mPMS and apigenin dose-dependently killed HT1080 and UM-SCC6 cells (Fig. 2A and B). HT1080 cells were applied with mPMS, and mPMS+WST-1, and the IC50 of mPMS combined with apigenin 100M was 5M, while the IC50 of the untreated control mPMS was 60M. SCC6 cells were applied with mPMS, and mPMS+WST-1, and the IC50 of mPMS combined with apigenin 100M was 30M, while the IC50 of the untreated control mPMS was 80M.

example 2

[0167] Example 2 Dose-response relationship of different cells to mPNS

[0168] Non-cancerous human keratinocytes (HEKA), human malonoma cell line SK-MEL-5 (SK5), human head and neck tumor cell line Cal27 (Cal27), and UM-SCC6 (SCC6) cells, and human soft tissue sarcoma cell line HT1080 (HT1080) were cultured with mPMS 30, 40 or 50M for 4 hours and then in normal growth medium for an additional 24 hours. CCK8 kit was used to measure cell viability. The data showed dose-dependent cell death and sensitivity differences to mPMS among different cell lines to mPMS treatment from each cell line (Figure 3). Among them, non-tumor-derived primary cultured HEKA cells were the least sensitive to mPMS, with an IC50 of 50M mPMS, while its IC50 was 20 and 30M from the IC50 of Cal27, UM-SCC6 and HT1080 cell mPMS, respectively.

example 3

[0169] Example 3 The effect of combined treatment of apigenin and WST-3 in inducing cancer cell death,

[0170] Methods: UM-SCC6, HT1080, Cal27, SK-MEL-5, and HEKA cells were administered alone or in combination with 50 or 100M WST-3 or 10 or 30M apigenin, or in combination with different concentrations of WST-3 and apigenin 4 hours, untreated cells were used as controls, and then changed to normal growth medium for 24 hours. The cell viability was measured using CCK8 kit. Data corrected as % of untreated control cells.

[0171] Results: A: Response of different cells to treatment with WST-3, apigenin, and combination. Application of 50M WST-3 (WST-3) or 30M apigenin (Apigenin) alone to each tested cell line showed no or less cell death effect compared to untreated cells (CTRL). Combination of WST-3 and apigenin (celery + WST-3) leads to synergistic cell death in all four tested human cancer cell lines of SK-MEL-5, Cal27, UM's SCC6 and HT1080, but not tumor human cells Onl...

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Abstract

Cell plasma membrane impermeable compounds and compositions thereof used for anticancer treatment are provided. The compounds contain functional groups capable of blocking and / or inhibiting trans-plasma membrane electron transport (tPMET), cell surface respiration and uncoupling cell surface oxidative-phosphorylation. The compositions comprise at least one of the cell plasma membrane impermeable compounds in combination with compounds of multi-function inhibitor capable of inhibiting cancer cell hypoxia responses.

Description

[0001] Related application: This application claims to incorporate US Provisional Application No. 61156,507, whose filing date is March 1, 2009 as the priority date, and PCT / CN2010 / 070813. [0002] technical field of invention [0003] The invention relates to the fields of tumor and chemotherapy. Specifically, the present invention provides new drug ingredients, targets for drug development, and medical applications to achieve more effective and non-toxic cancer treatment. Background technique [0004] Cancer is a deadly disease and one of the leading causes of death worldwide. In 2004, 740 million people died of cancer worldwide (accounting for about 13% of the total death toll). This number is already expected to continue to increase, with an estimated 12 million deaths from cancer worldwide by 2030. Even though cancer mortality rates in the United States have remained stable over the past decade, cancer incidence, prevalence, and mortality are still on the rise in devel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/41A61K31/352A61K31/498A61P35/00
CPCC07D257/04A61K31/353A61K31/41A61P35/00A61K2300/00
Inventor 于明
Owner 天津药和生物医药科技有限公司
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